CN1254230C - Method of enhancing delivery of oil-soluble skin care actives - Google Patents

Abstract

A water-in-silicone emulsion composition comprising silicone oil, silicone elastomer, and an oil-soluble skin care active agent, wherein the oil-soluble active agent is such as terpene alcohols, phytosterols, anti-acne active agents, beta-hydroxy acids, Vitamin _B3 compounds, retinoids, antioxidants/radical scavengers, chelating agents, flavonoids, anti-inflammatory agents, anti-cellulite agents, local anesthetics and mixtures thereof. A method of enhancing the delivery of oil-soluble skin care actives using silicone elastomers.

Description

Methods of enhancing delivery of oil-soluble skin care actives

Cross References to Related Applications

This application is a continuation-in-part of co-pending US Patent No. 09/613,266, filed July 10, 2000, which is hereby incorporated by reference, and to which this application claims the benefit of priority.

                      

The present invention relates to water-in-oil emulsion compositions comprising silicone elastomers. More particularly, the present invention relates to methods of enhancing the delivery of oil-soluble skin care actives to the skin using water-in-silicone emulsion compositions comprising silicone elastomers.

Background technique

Many skin care actives are known in the art comprising oil-soluble actives such as terpene alcohols, phytosterols, anti-acne actives, beta-hydroxy acids, vitamin _B3 compounds, retinoids, antioxidants/radical scavengers, chelating agents, flavonoids, anti-inflammatory agents, anti-cellulite agents, and local anesthetics, which are known to provide skin benefits. Very commonly used are oil-in-water and water-in-oil emulsion compositions, which may contain various oil-soluble skin care actives in the oil phase of the emulsion. In general, the oily phase consists of organic oils, such as mineral oil. However, water-in-oil emulsion compositions tend to give the skin an oily feel and are thus undesirable from a consumer standpoint.

Additionally, when an oil-soluble skin care active is present in the oil phase of oil-in-water and water-in-oil emulsions, it is often difficult to formulate such compositions so that the active is released when it is applied to the skin. (separated from) the oily phase. Therefore, the effectiveness of such oil-soluble active agents is limited in practice in which the active agent in the composition is delivered to the skin very little.

Accordingly, there is a need to improve the efficacy of compositions containing oil-soluble skin care actives. It is generally believed that the amount of active agent delivered to the skin (i.e., the active agent that penetrates the skin) is primarily controlled by two factors: 1) the concentration of the active agent in the oil; 2) the solubility of the active agent in the oil relative to the active agent in the oil. Solubility in skin. The second factor results in a kinetic equilibrium at the skin surface.

One way to enhance the delivery of skin care actives to the skin is to increase the amount of oil-soluble skin care actives present in the composition. However, this increases cost, increases the potential for adverse reactions with other ingredients, and increases the potential for skin irritation

An alternative approach is to reduce the solubility of oil-soluble skin care actives in the oil phase, which can lead to increased amounts of actives that separate from the oil phase and enter the skin. Unfortunately, oil-soluble skin care actives are inherently soluble in oil, making it difficult to reduce solubility sufficiently to achieve this effect. Additionally, changing the solubility of an oil-soluble active in the oil will negatively affect the concentration of the active in the oil phase; that is, the amount of active will be lower. As discussed above, the concentration of the active agent in the composition is also a factor in skin penetration.

One way to improve the oily feel of water-in-oil emulsions is to replace the organic oil discontinuous phase with silicone oil. Silicones give the skin a smooth, oil-free feel. A variety of silicone elastomers, including emulsifying and non-emulsifying silicone elastomers, are known in the art for formulating stable skin care compositions with various benefits. See, for example, US Patents 5,412,004, 5,654,362, 5,889,108 and 5,811,487.

Specific combinations of silicone elastomers are also known, such as that taught in US Pat. No. 6,221,979, to dissolve water-soluble and oil-soluble skin care actives to obtain a uniform composition. However, oil-soluble skin care actives are poorly soluble in silicones.

Therefore, there is a need for skin care compositions that improve the delivery of oil-soluble skin care actives to the skin and that also impart good aesthetic benefits.

Invention overview

The present invention relates to topical water-in-oil compositions for enhanced delivery of oil-soluble skin care actives comprising silicone oil, silicone elastomer and oil-soluble skin care actives. Preferably, the oil-soluble skin care active is selected from the group consisting of terpene alcohols, phytosterols, anti-acne actives, beta-hydroxy acids, vitamin _B3 compounds, retinoids, antioxidants/radical scavengers, chelating agents, Flavonoids, anti-inflammatory agents, anti-cellulite agents, local anesthetics and mixtures thereof.

The present invention also relates to methods of enhancing the delivery of oil-soluble skin care actives to the skin.

                    Invention Details

While the contents of the specification are concluded in the claims which particularly point out and distinctly claim the invention, it is believed that the invention will be better understood from the following description.

All percentages and ratios herein are by weight of the total composition and all measurements made are at 25°C unless otherwise indicated.

As used herein, "skin care product" means a product intended to treat or care for or moisturize, condition or cleanse the skin in some way. Products expressed by the phrase "skin care product" include, but are not limited to, moisturizers, personal cleansing products, occlusive drug delivery plasters, nail polishes, face powders, wipes, hair conditioners, skin lotions, shaving creams etc.

As used herein, unless otherwise stated, the term "ambient conditions" refers to ambient conditions of about one atmosphere of pressure, about 50% relative humidity, and about 25°C.

The compositions of the present invention may comprise, consist of, or consist essentially of the ingredients of the present invention as well as other ingredients described herein. Here, "consisting essentially of these ingredients" means that the composition or component may contain other ingredients, as long as the other ingredients do not significantly change the basic and novel characteristics of the claimed composition or method.

All percentages, parts and ratios are based on the total weight of the skin care compositions of the present invention, unless otherwise specified. All such weights as they pertain to listed ingredients are based on the active level and, therefore, do not include carriers or by-products that may be included in commercially available products, unless otherwise specified.

The publications cited herein are hereby incorporated by reference in their entirety.

In some embodiments of the invention, the skin care actives used herein can be categorized according to the benefit provided or postulated mode of action. It should be understood, however, that the actives used herein can sometimes provide more than one benefit or work through multiple modes of action. Thus, classifications are made here for convenience, but are not intended to limit the actives to the particular application or applications listed.

The term "keratinous tissue" as used herein refers to the outermost protective covering of mammals (such as humans, dogs, cats, etc.) containing keratin, which includes, but is not limited to, skin, lips, hair, toes, fingers , epidermis, hooves and other parts.

The term "dermatologically acceptable" herein means that the composition or component is suitable for contact with human keratinous tissue without undue toxicity, incompatibility, instability, allergic reaction, and the like.

The term "safe and effective amount" herein refers to an amount of a compound or composition which significantly produces a beneficial effect, preferably a beneficial keratinous tissue appearance or feel effect, or a beneficial hair appearance or feel effect, independently or in combination included herein Said various benefits, but can avoid serious side effects, such as producing a reasonable benefit-harm ratio, the dosage is within the reasonable judgment range of the skilled person.

"Signs of skin aging" include, but are not limited to, all externally visible and/or tactile manifestations as well as any other macroscopic or microscopic effects attributable to skin aging. These signals can be caused by intrinsic and extrinsic factors, such as chronic aging and/or environmental aggression. These signals can arise from processes including, but not limited to: development of textural discontinuities such as wrinkles and rough deep lines, skin lines, fissures, bumps, coarse pores (e.g. associated with accessory structures such as sweat glands, sebaceous glands, and hair follicles) ), or rough or uneven skin, loss of skin elasticity (loss and/or inactivation of functional skin elastin), sagging (including loss and/or damage of functional subcutaneous musculature and puffiness of eye bags and lower cheeks), skin firmness Loss, loss of skin firmness, loss of skin resilience due to deformation, discoloration (including the under-eye area), blemishes, sallowness, dark areas such as age spots, freckles, horniness, abnormal coloration, hyperkeratosis, elastosis, collagen Destruction, and other organizational changes in the stratum corneum, epidermis, dermis, skin vasculature (eg, telangiectasias and spider vessels), and subcutaneous tissue, especially in areas adjacent to the skin.

The presence of one or more oil-soluble skin care actives in skin care compositions such as moisturizing creams or lotions is desirable to provide skin care benefits such as regulating skin condition. However, it is also desirable to increase the delivery potential of a given active. The use of silicone elastomers increases the delivery potential of oil-soluble skin care actives, thereby increasing the potency of specific actives.

The present invention is useful for therapeutically modulating visible and/or tactile discontinuities in mammalian skin, including discontinuities in skin texture and skin tone. For example, a decrease in the apparent diameter of the pore, the apparent height of the tissue immediately adjacent to the pore approaching that of interadnexal skin, more even skin tone, and/or the length of fine lines and/or wrinkles , depth and/or other dimension reduction.

The compositions of the invention are also suitable for regulating the condition of the skin and especially for regulating the condition of keratinous tissue. Regulating the condition of the skin, ie the condition of the skin of mammals, especially humans, is often desired because various external and/or internal factors contribute to these conditions. Examples include environmental damage, radiation (including ultraviolet radiation), chronic aging, menopausal conditions (eg, postmenopausal skin changes), stress, disease, and the like. For example, "regulating skin condition" includes prophylactic and/or therapeutic regulation of skin condition and may involve one or more of the following benefits: skin densification (i.e. structuring of the epidermis and/or dermis and/or subcutaneous (i.e. subcutaneous fat) or muscle) layer, and when applicable toe/nail and hair shaft cuticle) to reduce skin atrophy, increase tangles at the dermal junction (also known as the ridge network), and prevent loss of skin elasticity (functional skin elasticity Loss, damage, and/or inactivation of proteins) such as elastosis, sagging, loss of skin elasticity due to deformation; discoloration of non-melanotic skin such as dark circles, spots (eg, uneven reddening due to rosacea) (hereinafter referred to as "erythema"), sallow (pale), discoloration due to capillaries or their dilation.

As used herein, prophylactically regulating skin condition includes delaying, minimizing and/or preventing visible and/or tactile discontinuities in the skin (eg, macroscopic or palpable irregularities in skin texture).

As used herein, therapeutically regulating skin condition includes improving, eg reducing, minimizing and/or eliminating skin discontinuities.

The compositions of the present invention provide additional benefits including stability, absence of significant (consumer unacceptable) skin irritation and good aesthetics.

It has now surprisingly been found that the addition of silicone elastomers to water-in-silicone compositions enhances the delivery of oil-soluble skin care actives compared to conventional oil-in-water and/or water-in-oil compositions up. Such compositions also have good aesthetic properties and are popular with consumers. The present invention has discovered that water-in-silicone compositions having silicone elastomers in the oil phase enhance the delivery of oil-soluble skin care actives such as terpene alcohols, phytosterols, anti-acne actives, beta- Hydroxy acids, vitamin _B3 compounds, retinoids, antioxidants/radical scavengers, chelating agents, flavonoids, anti-inflammatory agents, anti-cellulite agents, and local anesthetics.

Without being limited by theory, it is generally believed that although oil-soluble skin care actives can be stably formulated in the silicone oil phase with the aid of silicone elastomers, the presence of silicone oil and silicone elastomers can create A non-preferred environment. Thus, when the composition is applied to the skin, the oil-soluble skin care actives are separated from the silicone elastomer and delivered into the skin. The separation effect results in better delivery of oil-soluble skin care actives into the skin than if they were present in the conventional oil phase.

The present invention also relates to a method of enhancing the penetration of oil-soluble skin care actives into the skin by applying to the skin a composition comprising a silicone elastomer.

The compositions of the present invention comprise a silicone oil, a silicone elastomer, and an oil-soluble skin care active. Preferred compositions of the present invention are water-in-silicone oil emulsion compositions comprising a silicone elastomer and an oil-soluble skin care active in a continuous oil phase.

The composition also includes various other components. The composition of the present invention is described in detail below.

I. Oil-soluble skin care active agent

The compositions of the present invention contain a safe and effective amount of an oil-soluble skin care active. "Oil-soluble active agent" may be defined as any active material that is immiscible with water. Preferably, the composition comprises from about 0.001% to about 40%, by weight of the formed composition, of an oil-soluble skin care active, more preferably from about 0.01% to about 40%, especially preferably from about 0.05% % to about 30%, and still more preferably from about 0.1% to about 20%, more preferably from about 0.1% to about 10%.

Non-limiting examples of oil soluble actives that may be used in the present invention include oil soluble terpene alcohols, phytosterols, anti-acne actives, beta-hydroxy acids, vitamin _B3 compounds, retinoids, antioxidants/radical scavengers agents, chelating agents, flavonoids, anti-inflammatory agents, anti-cellulite agents, local anesthetics and mixtures thereof. A preferred oil-soluble skin care active for use herein is farnesol.

a) Oil-soluble terpene alcohols

"Terpene alcohol" as used herein refers to an organic compound composed of two or more 5-carbon atom isoprene units [CH ₂ =C(CH ₃ )-CH=CH ₂ ] and a terminal hydroxyl group group composition.

Examples of oil-soluble terpene alcohols useful herein include farnesol, farnesol derivatives, farnesol isomers, geraniol, geraniol derivatives, geraniol isomers, phytantriol, Phytantriol derivatives, phytantriol isomers and mixtures thereof. The preferred substance for use here is farnesol.

i) Farnesol and its derivatives

Farnesol is a naturally occurring substance that is thought to serve as a precursor and/or intermediate in the biosynthesis of squalene and sterols, especially cholesterol. Farnesol is also involved in protein modification and regulation (eg farnesylation of proteins) and there are nuclear receptors responsive to farnesol.

Chemically farnesol is [2E,6E]-3,7,11-trimethyl-2,6,10-dodecatrien-1-ol, where farnesol includes isomers and tautomers body. Farnesol is available as farnesol (mixture of isomers, available from Dragoco, 10 Gordon Drive, Totowa, New Jersey) and trans-trans-farnesol (available from Sigma Chemical Company, P.O. Box 14508, St. Louis , Missouri) is commercially available. A suitable farnesol derivative is farnesol acetate, which is commercially available from Aldrich Chemical Company (P.O. Box 2060, Milwaukee, WI).

ii) Geraniol and its derivatives

Geraniol is the common name and its chemical name is 3,7-dimethyl-2,6-octadien-1-ol. As used herein, geraniol includes its isomers and tautomers. Geraniol is commercially available from Aldrich Chemical Company (P.O. Box 2060, Milwaukee, WI). Suitable derivatives of geraniol include geraniol acetate, geranylgeraniol, geranyl pyrophosphate and geranylgeraniol pyrophosphate. All of the above materials are commercially available from Sigma Chemical Company, P.O. Box 14508, St. Louis, MO. For example, geraniol can be used as a spider vein/red spot repair agent, dark circle/swollen eye repair agent, sallow complexion repair agent, sagging repair agent, anti-itch agent, skin tightening agent, pore shrinker, oil/shine Reducer, post-inflammatory hyperpigmentation repair agent, wound treatment agent, anti-cellulite agent and regulator of skin texture, including wrinkles and fine lines.

iii) Phytantriol and its derivatives

Phytantriol is the common name for the compound 3,7,11,15-tetramethylhexadecane-1,2,3-triol. Phytantriol is commercially available from BASF (1609 Biddle Avenue, Whyandotte, MI). For example, phytantriol is used as a capillary/erythema repair agent, dark circle/puffy eye bubble repair agent, sallow complexion repair agent, sagging repair agent, anti-itch agent, skin tightening agent, pore reducer, oil/shine reducer agent, post-inflammatory hyperpigmentation repair agent, wound treatment agent, anti-cellulite agent (anti-cellulite agent), and regulates skin texture, including wrinkles and fine lines.

b) Phytosterols

Phytosterols and their derivatives are known to help brighten and brighten the skin. Non-limiting examples of oil-soluble phytosterol derivatives include β-sitosterol, campesterol, lupenol, lupenol, α-spinasterol, stigmasterol, derivatives thereof, and combinations thereof. More preferably, the phytosterol derivatives are selected from the group consisting of β-sitosterol, campesterol, brassicasterol, stigmasterol, their derivatives and combinations thereof.

Phytosterols are generally obtained from the unsaponifiable fraction of vegetable oils and fats, in the form of free sterols, acetylated derivatives, sterol esters, ethoxylates or glycoside derivatives. More preferably, the phytosterols are free sterols. As used herein, "phytosterols" include isomers and tautomers thereof, and are commercially available from Aldrich Chemical Company (Milwaukee, WI), Sigma Chemical Company (St. Louis, MO) and Dragoco (Totowa, New Jersey).

c) Oil-soluble vitamin compounds

Many vitamins known in the art to provide various skin benefits are oil soluble, as are some or all of their derivatives. As such, these oil-soluble vitamins are useful herein as oil-soluble skin care actives. Non-limiting examples of such oil-soluble vitamins include retinoids, vitamin _B3 compounds, vitamin C (eg, vitamin C palmitate), vitamin D, vitamin K, vitamin E, and mixtures thereof. Preferred for use herein are retinoids, vitamin _B3 compounds, which are discussed in detail below.

i) Retinoids

As used herein, "retinoids" include all natural and/or synthetic congeners of vitamin A or retinol-like compounds that possess the biological activity of vitamin A in the skin, as well as geometric isomers of these compounds and stereoisomers. Non-limiting examples of retinoids employed herein include retinol, retinol esters (such as _C2 - _C22 alkyl esters of retinol, including retinyl palmitate, retinyl acetate, retinoic acid), retinal, and/or retinoic acid (including all-trans retinoic acid and/or 13-cis retinoic acid), preferably retinoids other than retinoic acid. These compounds are well known in the art and are commercially available from various sources such as Sigma Chemical Company (St. Louis, MO), and Boerhinger Mannheim (Indianapolis, IN). Other suitable retinoids are tocopheryl retinoate [(cis or trans) tocopheryl retinoate, adapalene {6-[3-(1-adamantyl)-4-methoxyphenyl]- 2-naphthoic acid} and tazarotene (ethyl 6-[2-(4,4-dimethylthiochroman-6-yl)-ethynyl]nicotinate). Preferred retinoids are retinol, retinyl palmitate, retinyl acetate, retinyl propionate, retinal and combinations thereof, but any oil soluble retinoid may be used herein.

ii) Oil-soluble vitamin _B3 compound

Oil-soluble vitamin _B3 compounds are especially useful in regulating skin condition. Non-limiting examples of oil-soluble vitamin _B3 compounds include niacin esters, including non-vasodilating esters of niacin (eg, tocopheryl niacin). Examples of suitable vitamin _B3 compounds are well known in the art and are available from various commercial sources such as Sigma Chemical Company (St. Louis, MO), ICNBiomedicals Inc. (Irvin, CA) and Aldrich Chemical Company (Milwaukee, CA). WI).

iii) Oil-soluble vitamin E compound

Vitamin E and several of its derivatives are known to be particularly useful as antioxidant/radical scavengers. Such antioxidants/radical scavengers are particularly useful against UV radiation, which can cause exfoliation or texture changes of the stratum corneum, and against other environmental factors that can cause skin damage.

Non-limiting examples of oil-soluble vitamin E compounds include tocopherol (vitamin E), tocopheryl sorbate, tocopheryl acetate, and other tocopherol esters. Preferred antioxidants/radical scavengers are tocopheryl sorbate, tocopheryl acetate and mixtures thereof. A class of materials also useful here are tocotrienols, which are related to vitamin E.

d) Anti-acne actives

Non-limiting examples of oil-soluble anti-acne actives include resorcinol and erythromycin.

e) Beta-Hydroxy Acids

Non-limiting examples of oil-soluble beta-hydroxy acids include salicylic acid and its derivatives, such as octanoyl derivatives. Beta-hydroxy acids are known to be useful in anti-acne and anti-aging.

f) Chelating agent

As used herein, "chelating agent" or "chelating agent" means an active agent capable of removing metal ions from a system by forming complexes so that the metal ions cannot readily participate in or catalyze chemical reactions. The addition of chelating agents is particularly effective in preventing skin damage from UV rays and other environmental factors that can cause excessive scaling or changes in skin tissue.

Typical oil-soluble chelating agents useful herein are disclosed in US Patent No. 5,487,884, issued 1/30/96, to Bissett et al; International Application Publication 91/16035, published 10/31/95, to Bush et al; and Bush et al. International Application Published 91/16034, Publication Date 10/31/95. The oil-soluble chelating agents used in the compositions of the present invention are preferably furildioxime, furilmonoxime and derivatives thereof.

g) flavonoids

Flavonoid compounds are broadly disclosed in US Patents 5686082 and 5686367, which are incorporated herein by reference. Non-limiting examples of flavonoids suitable for use in the present invention include isoflavones, flavanones selected from unsubstituted flavanones, monosubstituted flavanones, and mixtures thereof; chalcones selected from unsubstituted chalcones Ketones, monosubstituted, disubstituted, and trisubstituted chalcones and mixtures thereof; flavones selected from unsubstituted flavones, monosubstituted, and disubstituted flavones, and mixtures thereof; one or more iso Flavones; coumarins selected from unsubstituted coumarins, monosubstituted, and disubstituted coumarins, and mixtures thereof; chromones selected from unsubstituted chromones, monosubstituted, and disubstituted Chromotones, and mixtures thereof; one or more serotonins; one or more chroman-4-ones; one or more chromanols; isomers (eg cis/trans isomers); and mixtures thereof. The term "substituted" herein refers to a flavonoid in which one or more hydrogen atoms of the flavonoid have been independently replaced by a hydroxyl group, a C1-C8 alkyl group, or a C1-C4 alkoxy group.

Examples of suitable flavonoids include, but are not limited to, unsubstituted flavanones, monohydroxyflavanones (such as 2'-hydroxyflavanones, 6-hydroxyflavanones, 7-hydroxyflavanones, etc.), Oxyflavanone (such as 5-methoxyflavanone, 6-methoxyflavanone, 7-methoxyflavanone, 4'-methoxyflavanone, etc.), unsubstituted chalco Chalcone (especially unsubstituted trans-chalcone), monohydroxychalcone (such as 2'-hydroxychalcone, 4'-hydroxychalcone, etc.), dihydroxychalcone (such as 2', 4-Dihydroxychalcone, 2',4'-Dihydroxychalcone, 2,2'-Dihydroxychalcone, 2',3-Dihydroxychalcone, 2',5'-Dihydroxychalcone Chalcone, etc.), and trihydroxychalcone (such as 2', 3', 4'-trihydroxychalcone, 4,2', 4'-trihydroxychalcone, 2,2', 4' -trihydroxychalcone, etc.), unsubstituted flavones, 7,2'-dihydroxyflavones, 3',4'-dihydroxynaphthoflavones, 4'-hydroxyflavones, 5,6-benzoflavones, and 7 , 8-benzoflavone, unsubstituted isoflavone, daidzein (7,4'-dihydroxyisoflavone), 5,7-dihydroxy-4'-methoxyisoflavone, soybean isoflavone (soybean Extract mixture), unsubstituted coumarin, 4-hydroxycoumarin, 7-hydroxycoumarin, 6-hydroxy-4-methylcoumarin, unsubstituted chromone, 3-formylchromone, 3-formyl-6-isopropyl chromone, unsubstituted romansin, unsubstituted chroman-4-one, unsubstituted chroman-4-ol, and mixture.

Preferred here are unsubstituted flavanones, methoxyflavanones, unsubstituted chalcones, 2'-4 dihydroxychalcones, isoflavones, and mixtures thereof. More preferred are unsubstituted flavanones, unsubstituted chalcones (especially the trans isomer), isoflavones, and mixtures thereof.

The flavonoid compounds used herein are commercially available from a variety of sources such as Indofine Chemical Company (Somerville, New Jersey), Steraloids Company (Wilton, New Hampshire), NovaSoy from Archer Daniels Midland Co. (Decatur, Illinois) and Aldrich Chemical Company (Milwaukee, Wisconsin).

Mixtures of the above flavonoid compounds may also be used.

h) Anti-inflammatory agents

Non-limiting examples of oil-soluble anti-inflammatory agents employed herein include steroidal anti-inflammatory agents such as corticosteroids (e.g. hydrocortisone), and oil-soluble non-steroidal anti-inflammatory agents such as propionic acid derivatives (e.g. profen, naproxen, and/or ketopropionate).

Mixtures of these oil-soluble anti-inflammatory agents as well as their cosmetically and/or pharmaceutically acceptable salts and esters of these agents may also be used. For example etofenamate (a derivative of flufenamic acid) is particularly suitable for topical application.

Non-limiting examples of so-called "natural" anti-inflammatory agents that can be used in the present invention include those that can be obtained in the form of extracts or synthetically prepared from natural sources (such as plants, fungi, microbial by-products) by appropriate physical and/or chemical isolation methods. obtained reagents. For example, candelilla wax, bisabolol (eg, alpha-bisabolol), and/or phytosterols (eg, phytosterol) may be employed.

i) Anti-cellular agent

Non-limiting examples of oil-soluble anti-cellulant skin care actives useful herein include oil-soluble xanthine compounds, such as caffeine.

j) Local anesthetic

Non-limiting examples of oil-soluble local anesthetics include benzocaine, lidocaine, and pharmaceutically acceptable salts thereof.

II. Polysiloxane Elastomer

The compositions of the present invention also comprise from about 0.1% to about 30% by weight of the composition of a silicone elastomer component. Preferably, the compositions comprise from about 0.1% to about 30%, more preferably from about 0.5% to about 10%, by weight of the composition, of the silicone elastomer component. All these percentages for silicone elastomers are based on the amount of elastomer and therefore do not include carriers or by-products contained in commercially available forms. Typically commercially available silicone elastomers are incorporated into the overall composition in the form of a solution with silicone oil. This amount of silicone oil is considered to be the total percentage of silicone oil present in the composition of the invention.

Suitable for use herein are silicone elastomers which may be emulsifying or non-emulsifying crosslinked silicone elastomers or mixtures thereof. There is no specific limitation on the kind of curable organopolysiloxane composition that can be used as a starting material for the crosslinked organopolysiloxane elastomer. An example of this is an addition reaction-curing organopolysiloxane composition in which, under platinum metal catalysis, an Addition reaction curing; condensation curing organopolysiloxane composition which cures by a dehydrogenation reaction between a hydroxyl-terminated diorganopolysiloxane and a SiH-containing diorganopolysiloxane in the presence of an organotin compound Condensation curing organopolysiloxane composition, wherein in the presence of organotin compounds or titanates by condensation reaction between hydroxyl-terminated diorganopolysiloxane and hydrolyzable organosilane (the condensation reaction can be Dehydration, dealcoholization, deoxime, deamination, deamidation, decarboxylation and deketation reactions are examples) curing; peroxide curing organopolysiloxane compositions, wherein heat curing is carried out in the presence of an organic peroxide catalyst; As well as organopolysiloxane compositions curable by high-energy radiation such as gamma-rays, ultraviolet rays or electron beams.

Addition reaction curing organopolysiloxane compositions are preferred for their rapid cure rate and good uniformity in cure. Particularly preferred addition reaction curing organopolysiloxane compositions are prepared from:

(A) an organopolysiloxane having at least 2 lower alkenyl groups in each molecule;

(B) organopolysiloxanes having at least 2 silicon-bonded hydrogen atoms in each molecule; and

(C) Platinum type catalyst.

Regarding the above, component (A) is an essential component of an organopolysiloxane forming a polysiloxane elastomer, and is cured by an addition reaction between this component and component (B) catalyzed by component (C). The component (A) must contain at least 2 silicon-bonded lower alkenyl groups per molecule; less than 2 lower alkenyl groups will not give a well-cured product because a network structure will not be formed. Examples of the lower alkenyl group are vinyl, allyl and propenyl. Although the lower alkenyl group may be present anywhere in the molecule, its presence at the terminal end of the molecule is preferred. The molecular structure of this component may be linear, branched linear, cyclic or network, although slightly branched linear chains may be preferred. The molecular weight of this ingredient is not specifically limited, so its viscosity can vary from a low viscosity liquid to a very high viscosity gum. In order for the resulting cured product to be in the form of a rubber elastomer, a viscosity of at least 100 centistokes at 25 degrees Celsius is preferred. Examples of these organopolysiloxanes are methylvinylsiloxane, methylvinylsiloxane-dimethylsiloxane copolymer, dimethylvinylsiloxy-terminated dimethylpolysiloxane Oxane, Dimethylvinylsiloxy-blocked Dimethicone-Methylphenylsiloxane Copolymer, Dimethylvinylsiloxy-blocked Dimethicone-Dimethicone Phenylsiloxane-methylvinylsiloxane copolymer, trimethylsiloxy-terminated dimethylsiloxane-methylvinylsiloxane copolymer, trimethylsiloxy-terminated Terminated dimethylsiloxane-methylphenylsiloxane-methylvinylsiloxane copolymer, dimethylvinylsiloxy-terminated methyl (3,3,3-trifluoropropyl ) polysiloxane and dimethylvinylsiloxy terminated dimethylsiloxane-methyl(3,3,-trifluoropropyl)siloxane copolymer.

Ingredient (B) is an organopolysiloxane having at least 2 silicon-bonded hydrogen atoms per molecule and is a crosslinker for ingredient (A). Curing occurs by an addition reaction of silicon-bonded hydrogen atoms in the component with lower alkenyl groups in the component (A), catalyzed by component (C). This component (B) must contain at least 2 silicon-bonded hydrogen atoms per molecule to function as a crosslinker. In addition, the sum of the number of alkenyl groups per molecule of ingredient (A) and the number of silicon-bonded hydrogen atoms per molecule of ingredient (B) is at least 5. Values lower than 5 should be avoided because network structures are essentially not formed.

There is no specific limitation on the molecular structure of this component, and it may be any of straight chain, straight chain including branched chain, cyclic and the like. The molecular weight of this ingredient is not specifically limited, but a viscosity at 25 degrees Celsius of 1 to 50,000 centistokes is preferred to obtain good miscibility with ingredient (A). Preferably this ingredient is added in such an amount that the molar ratio between the total amount of silicon-bonded hydrogen atoms in the ingredient and the total amount of all lower alkenyl groups in ingredient (A) is in the range (1.5:1) to (20: 1) within the range. When the molar ratio is lower than 0.5:1, it is difficult to obtain excellent curing properties. When the ratio (20:1) is exceeded, the hardness tends to increase to a high level when the cured product is heated. Furthermore, when an organopolysiloxane containing a large number of alkenyl groups is supplementally added for eg strengthening purposes, it is preferred that the SiH-containing component is supplementally added in such an amount as to offset the alkenyl groups. Specific examples of this ingredient are trimethylsiloxy-terminated methylhydrogenpolysiloxane, trimethylsiloxy-terminated dimethylsiloxane-methylhydrogensiloxane copolymer, and dimethylsiloxane Cyclosiloxane-methylhydrogen-siloxane cyclic copolymer.

Ingredient (C) is a catalyst for the addition reaction of silicon-bonded hydrogen atoms and alkenyl groups, specific examples are chloroplatinic acid, possibly soluble in alcohols or ketones and this solution is optionally aged, chloroplatinic acid-alkene complexes , chloroplatinic acid-alkenyl siloxane complex, chloroplatinic acid-diketone complex, platinum black and supported platinum.

Component C is added preferably at 0.1 to 1,000 parts by weight, more preferably at 1 to 100 parts by weight per 1,000,000 parts by weight of the total amount of components (A) plus (B) as the platinum type metal. Other organic groups which may be bonded to the silicon in the organopolysiloxane forming the basis of the curable organopolysiloxane composition described above are, for example, alkyl groups such as methyl, ethyl, propyl, butyl and octyl substituted alkyl groups such as 2-phenylethyl, 2-phenylpropyl and 3,3,3-trifluoropropyl; aryl groups such as phenyl, tolyl and xylyl; substituted aryl groups such as benzene ethyl; and monovalent hydrocarbon groups substituted by, for example, epoxy groups, carboxylate groups, mercapto groups, and the like.

An example of preparing an organopolysiloxane elastomer powder is as follows: the above-mentioned organopolysiloxane composition (addition curing, condensation curing or Oxide solidification) mixed with water, after uniform mixing in a homomixer, colloid mill, homogenizer, propeller mixer, etc., cured by draining into hot water (at a temperature of at least 50 degrees Celsius), and then dried; by Cures organopolysiloxane compositions (addition-curable, condensation-curable or peroxide-curable) by spraying them directly into a hot gas stream; radiation-curable organopolysiloxanes cure by spraying them under high-energy radiation Oxane compositions to obtain powders; organopolysiloxane compositions (addition-curable, condensation-curable, peroxide-curable) or highly energy-curable organopolysiloxane compositions cured by high-energy radiation After solidification, the product is pulverized using known pulverizers such as ball mills, ultra-mist pulverizers, kneaders, rolling mills, etc., thereby forming powders.

The compositions of the present invention may comprise an emulsifying crosslinked organopolysiloxane elastomer, a non-emulsifying crosslinked organopolysiloxane elastomer, or mixtures thereof. The term "non-emulsifying" as used herein defines a crosslinked organopolysiloxane elastomer that does not contain polyoxyalkylene units. As used herein, the term "emulsified" refers to a crosslinked organopolysiloxane elastomer having at least one polyoxyalkylene (eg, polyoxyethylene or polyoxypropylene) unit. Preferred emulsifying elastomers herein include polyoxyalkylene-modified elastomers formed by reacting divinyl compounds, especially siloxane polymers with at least two free vinyl groups, with Si-H bonds on the polysiloxane backbone. body. Preferably, the elastomer is dimethyl polysiloxane cross-linked at Si-H sites on the molecular spherical MQ resin. Emulsified crosslinked organopolysiloxane elastomers are described, inter alia, in U.S. Patents 5,412,004 (issued 5/2/95), 5,837,793 (issued 11/17/98) and 5,811,487 (issued 9/22/98) A selection of cross-linked polymers for which all patents are incorporated herein by reference in their entirety. Additionally, emulsifying elastomers composed of dimethicone copolyol crosspolymer (and) dimethicone are commercially available from Shin Etsu under the tradename KSG-21.

The silicone elastomers of the present invention can be tested by subjecting them to high shear (approximately 5,000 psi) in the presence of a solvent for the silicone elastomer in a sonicator with or without circulation. Treatment and further processing, treatment 1 to 60 passes, in order to obtain a specific average particle size of polysiloxane elastomer. Less than 10 passes will result in an average particle size of about 20 to 200 microns. 10 to 60 passes will result in an average particle size of less than 20 microns as measured by Horiba LA-910. The term "particle size" of an elastomer as used herein means the particle size of the elastomer in its expanded state. As used herein, "swelling" means the extension of an elastomer particle beyond its normal size and shape as a result of its absorption of solvent compounds.

Preferably, the non-emulsifying elastomer is a dimethicone/vinyl dimethicone crosspolymer. These dimethicone/vinyl dimethicone crosspolymers are manufactured by manufacturers including Dow Corning (DC 9040 and DC 9041), General Electric (SFE839), Shin Etsu (KSG-15, 16, 18 [Dimethicone/Phenylvinyl Dimethicone Crosspolymer]) and Grant Industries (GRANSIL ^™ class of elastomers) are available from many suppliers. U.S. Patent No. 4,970,252 issued November 13, 1990 to Sakuta et al., U.S. Patent No. 5,760,116 issued June 2, 1998 to Kilgour et al., and U.S. Patent 5,654,362 issued August 5, 1997 to Schulz, Jr. et al. Crosslinked organopolysiloxane elastomers suitable for use in the present invention and methods of making them are further described in No., all of which are hereby incorporated by reference. Additional crosslinked organopolysiloxane elastomers suitable for use in the present invention are described in Japanese Patent Application JP 61-18708 assigned to Pola Kasei Kogyo KK.

Preferred commercially available elastomers for use herein are Dow Corning's 9040 Silicone Elastomer Blend, Shin Etsu's KSG-21, and mixtures thereof.

III. Silicone oil

The composition of the present invention contains a safe and effective amount of silicone oil. Preferably, the composition comprises from about 5% to about 99% silicone oil, preferably from about 15% to about 95%, more preferably from about 20% to about 90%, by weight of the formed composition , and particularly preferably from about 25% to about 85%.

Non-limiting examples of common silicone oils that may be used in the present invention include cyclomethicone, dimethicone, and mixtures thereof.

The compositions of the present invention may be anhydrous. "Anhydrous" means that the composition contains less than 5%, preferably less than 1%, water. In such anhydrous systems, the composition may be a combination comprising a silicone oil, a silicone elastomer, and an oil-soluble active agent.

The compositions of the present invention may also contain an aqueous phase, for example in the form of a water-in-oil emulsion. Emulsions according to the invention generally contain an aqueous phase and a lipid or oil. Lipids or oils can be obtained from animal, vegetable or petroleum sources, and they can be natural or synthetic (ie, man-made). Such fats or oils are preferably silicone oils. Preferably, the emulsion also contains an emulsifier at a level of from about 1% to about 10%, more preferably from about 2% to about 5%, by weight of the carrier. Emulsifiers are used to emulsify silicone elastomers, silicone emulsifiers, nonionics, anionics and cationics. For example, McCutcheon's Detergents and Emulsifiers , North American Edition (1986), pages 317-324, disclose suitable emulsifiers. The emulsifier is preferably an emulsifying silicone elastomer, silicone emulsifier or a combination thereof.

Suitable emulsions have a wide range of viscosities depending on their intended product form. Viscosities ranging from about 5,000 centipoise to about 100,000 centipoise are preferred.

Lotions may contain a variety of optional ingredients. Based on the water solubility and dispersibility of a given component in the composition, one skilled in the art will determine whether a given component will pass primarily into the water phase or into the oil/silicone phase.

Preferably, the compositions of the present invention contain an aqueous phase and are in the form of a water-in-silicone emulsion. More preferably, the composition is a water-in-silicone emulsion, the oil phase of the composition comprising at least 51% silicone oil by weight of the oil phase. The water-in-silicone emulsions are fully described below.

Water-in-silicone emulsion

Water-in-silicone emulsions contain a continuous silicone phase and a dispersed aqueous phase.

(a) Continuous polysiloxane phase

Preferred water-in-silicone emulsions herein comprise from about 25 to about 90%, preferably from about 27% to about 80%, more preferably from about 30% to about 70%, by weight of the formed composition, of continuous silicone Mutually. The continuous polysiloxane phase exists as an external phase which contains or surrounds the discontinuous aqueous phase described below.

The continuous silicone phase comprises the polyorganosiloxane oil used in the composition. The organopolysiloxane oil can be volatile, nonvolatile, or a mixture of volatile and nonvolatile silicones. The term "nonvolatile" refers herein to those polysiloxanes which are liquid at room temperature and have a flash point (at one atmosphere) of 100°C or higher. The term "volatile" refers herein to all other silicone oils. Suitable organopolysiloxanes can be selected from a wide variety of polysiloxanes spanning a wide range of volatility and viscosity. Suitable polyorganosiloxane oils include polyalkylsiloxanes, cyclic polyalkylsiloxanes and polyalkylarylsiloxanes.

The polyalkylsiloxanes in the composition include polyalkylsiloxanes having a viscosity of from about 0.5 to about 1,000,000 centistokes at 25°C. This type of polyalkylsiloxane can be represented by the general formula R ₃ SiO[R ₂ SiO] _x SiR ₃ , wherein R is a C1-C30 alkyl group (preferably R is methyl or ethyl, more preferably methyl; in the same There may also be different alkyl groups in the molecule), x is an integer from 0 to about 10,000, x can be selected to obtain the desired molecular weight up to about 10,000,000 or more. Commercially available polyalkylsiloxanes include polydimethylsiloxanes, also known as dimethicones, examples of which include the Vicasil ^(R) series sold by General Electric Company, and the Dow Corning( ^R) 200 series sold by Dow Corning Corporation. Specific examples of suitable polydimethylsiloxanes include Dow ^Corning® 200 fluid, which has a viscosity of 0.65 centistokes and a boiling point of 100°C, Dow ^Corning® 225 fluid, which has a viscosity of 10 centistokes and a boiling point of greater than 200°C, and Dow Corning® ²⁰⁰ Fluids with viscosities of 50, 350 and 12,500 centistokes and boiling points greater than 200°C. Suitable dimethicones include those represented by the formula (CH ₃ ) ₃ SiO[(CH ₃ ) ₂ SiO] _x [CH ₃ RSiO] _y Si(CH ₃ ) ₃ wherein R is 2 to 30 carbon atoms The linear or branched chain, x and y are each an integer of 1 or more, and x and y can be selected to obtain a desired molecular weight up to about 10,000,000 or more. Examples of these alkyl-substituted dimethicones include cetyl dimethicone and lauryl dimethicone.

Cyclic polyalkylsiloxanes suitable for use in the composition include those represented by the formula [ _SiR2 -O] _n , wherein R is an alkyl group (preferably R is methyl or ethyl, more preferably methyl), and n is An integer of about 3 to about 8, more preferably an integer of about 3 to about 7, and most preferably an integer of about 4 to about 6. When R is methyl, these materials are generally known as cyclomethicones. Commercially available cyclomethicones include Dow ^Corning® 244 fluid, viscosity 2.5 centistokes, boiling point 172°C, which mainly contains cyclomethicone (i.e., n=4), Dow ^Corning® 344 fluid, viscosity 2.5 centistokes Stokes, boiling point 178°C, it mainly contains cyclomethicone (i.e. n=5), Dow Corning ^® 245 fluid, viscosity 4.2 centistokes, boiling point 205°C, it mainly contains cyclomethicone and cyclomethicone A mixture of methylpentasiloxane (i.e. n = 4 and 5), and Dow ^Corning® 345 fluid, viscosity 4.5 centistokes, boiling point 217 ° C, it mainly contains cyclomethicone, cyclomethicone A mixture of alkanes and cyclomethicone (ie n = 4, 5 and 6).

Also suitable are materials such as trimethylsiloxysilicate, which is a polymer corresponding to the general formula [(CH ₂ ) ₃ SiO _1/2 ] _x [SiO ₂ ] _y , where x is from about 1 to about 500 is an integer, y is an integer from about 1 to about 500. Commercially available trimethylsiloxysilicate is sold as a mixture with the dimethicone Dow Corning ^(R) 593 Fluid.

Dimethiconol is also suitable for use in the composition. Such compounds can be represented by chemical formulas R ₃ SiO[R ₂ SiO] _x SiR ₂ OH and HOR ₂ SiO[R ₂ SiO] _x SiR ₂ OH, wherein R is an alkyl group (preferably R is methyl or ethyl, more preferably methyl base) and x is an integer from 0 to about 500, x is selected to obtain the desired molecular weight. Commercially available dimethicones are generally sold as mixtures with dimethicone or cyclomethicone (eg Dow Corning ^(R) 1401, 1402 and 1403 fluids).

Polyalkylaryl siloxanes are also suitable for use in the composition. Especially polymethylphenylsiloxanes having a viscosity of from about 15 to about 65 centistokes (25°C).

Preferred polyorganosiloxanes herein are selected from the group consisting of polyalkylsiloxanes, alkyl substituted dimethicones, cyclomethicones, trimethicone silicates, dimethicone Silicone alcohols, polyalkylaryl siloxanes and mixtures thereof. More preference is given here to polyalkylsiloxanes and cyclomethicones. Preferred among the polyalkylsiloxanes are dimethicones.

As noted above, the continuous silicone phase may contain one or more non-silicone oils. The concentration of non-silicone oils in the continuous silicone phase is preferably minimized or avoided together to further enhance the delivery of oil-soluble skin care actives. Suitable non-silicone oils have a melting point of about 25°C or less at about 1 atmosphere. Examples of non-silicone oils for the continuous silicone phase are those well known in the chemical art of topical personal care products, where the product is in the form of a water-in-oil emulsion, such as mineral oils, vegetable oils, synthetic oils, Semi-synthetic oil etc.

(b) Dispersed aqueous phase

The topical compositions of the present invention may also comprise a dispersed aqueous phase forming from about 10% to about 75% by weight of the composition. In emulsion technology, the term "dispersed phase" is a term well known to those skilled in the art and refers to small particles or droplets suspended or surrounded in a continuous phase. The dispersed phase is also called the internal or discontinuous phase. The dispersed aqueous phase is a dispersion of water droplets or particles suspended or surrounded in the above-mentioned continuous polysiloxane phase.

The aqueous phase can be water, or a combination of water and one or more water-soluble or water-dispersible ingredients. Preferably the aqueous phase comprises greater than about 50% water by weight of the aqueous phase. Non-limiting examples of such optional ingredients include thickeners, acids, bases, salts, chelating agents, gums, water-soluble or water-dispersible alcohols and polyols, buffers, preservatives, water-soluble skin care actives, water-dispersible Sexual skin care actives, sunscreens, pigments, etc. Water-soluble and water-dispersible skin care actives are described in detail below under Optional Ingredients.

(c) Emulsifier for dispersing the aqueous phase

The water-in-silicone emulsions of the present invention preferably include an emulsifier. In a preferred embodiment, the composition contains from about 0.1% to about 10% emulsifier, more preferably from about 0.5% to about 7.5%, most preferably from about 1% to about 5%, by weight of the formed composition count. Emulsifiers help to disperse and suspend the aqueous phase in the continuous silicone phase.

A variety of emulsifiers can be employed herein to form the preferred water-in-silicone emulsions. Known or conventional emulsifiers can be used in the composition provided that the emulsifier selected is chemically and physically compatible with the essential ingredients of the compositions of the present invention and produces the desired dispersing properties. Suitable emulsifiers include silicone emulsifiers, silicone-free emulsifiers and mixtures thereof, which are known to those skilled in the topical personal care product art. Preferably, these emulsifiers have an HLB value of less than about 14, more preferably from about 2 to about 14, still more preferably from about 4 to about 14. Emulsifiers with HLB values outside this range can be used in combination with other emulsifiers to achieve a combined effective weight average HLB within this range.

Emulsified silicone elastomers are preferably used here, as described in detail above. Other silicone emulsifiers are also preferred. Combinations of emulsified silicone elastomers with silicone emulsifiers are also suitable for use herein.

A variety of silicone emulsifiers are used herein. These silicone emulsifiers are generally organically modified organopolysiloxanes, also known as silicone surfactants by those skilled in the art. Suitable silicone emulsifiers include dimethicone copolyols. These materials are polydimethylsiloxanes which have been modified to include polyether side chains such as polyethylene oxide chains, polypropylene oxide chains, mixtures of these chains, and Polyether chains that are part of ethylene oxide and propylene oxide. Other examples include alkyl-modified dimethicone copolyols, ie, compounds containing C2-C30 side chains. Other suitable dimethicone copolyols include those having various pendant cationic, anionic, amphoteric and zwitterionic moieties.

The dimethicone copolyol emulsifier used here can be represented by the following formula:

Wherein R is C1-C30 linear, branched or cyclic alkyl, and ^R2 is selected from groups consisting of:

--(CH ₂ ) _n --O --(CH ₂ CHR ³ O) _m --H,

and

--(CH ₂ ) _n --O--(CH ₂ CHR ³ O) _m --(CH ₂ CHR ⁴ O) _o --H,

wherein n is an integer from ^{3 to} about 10; R and R are ^selected from groups consisting of H and C1-C16 straight or branched chain alkyl such that R and ^R are not simultaneously the same; and m, o, x and y are selected such that the molecule has an overall molecular weight of from about 200 to about 10,000,000, and m, o, x, and y are each selected from zero or greater integers such that m and o are not simultaneously zero, and z is independently selected from 1 or Larger integer. It is recognized that positional isomers of these copolyols are available. The above chemical representation of the ^R2 moiety containing the ^R3 and ^R4 groups is not limiting, but is shown for convenience.

The silicone surfactants shown in the structure in the previous paragraph, where ^R2 is -( _CH2 ) _n - ^OR5 , where ^R5 is a cationic, anionic, amphoteric or zwitterionic moiety, may also be used, although It is not strictly classified as a dimethicone copolyol.

Non-limiting examples of dimethicone copolyols and other silicone surfactants useful herein as emulsifiers include: Dimethicone polyether copolymers having polyethylene oxide side chains, Polydimethylsiloxane polyether copolymer with polypropylene oxide side chain, polydimethylsiloxane polyether copolymer with polyethylene oxide and polypropylene oxide mixed side chain, (Ethylene)(propylene) mixed side chain polydimethylsiloxane polyether copolymer, polydimethylsiloxane polyether copolymer with organobetaine side chain, carboxylate (salt) side chain Polydimethylsiloxane polyether copolymers, polydimethylsiloxane polyether copolymers with quaternary ammonium salt side chains, and side groups containing C2-C30 linear, branched or cyclic alkyl moieties Further modifications of the above-mentioned copolymers. Examples of dimethicone copolyols sold by Dow Corning for use herein are Dow Corning® 190 ^, 193, Q2-5220, 2501 Wax, 2-5324 Fluid, and 3225C (the latter known as Cyclomethicone sold as a mixture). Cetyl dimethicone copolyol is commercially available as a mixture with polyglyceryl-4 isostearate (and) hexyl laurate as ABIL ^(R) WE-09 (available from Goldschmidt). Cetyl dimethicone copolyol is also commercially available as a mixture with hexyl laurate (and) polyglyceryl-3 oleate (and) cetyl dimethicone, sold as ABIL ^(R) WS-08 is sold (also from Goldschmidt). Other non-limiting examples of dimethicone copolyols include lauryl dimethicone copolyol, dimethicone copolyol acetate, dimethicone copolyol Alcohol Adipate, Dimethicone Copolyol Amine, Dimethicone Copolyol Behenate Dimethicone Copolyol Butyl Ether, Dimethicone Copolyol Hydroxystearate, Dimethicone Copolyol Isostearate, Dimethicone Copolyol Laurate, Dimethicone Copolyol Methyl Ether, Dimethicone Copolyol Methyl Ether, Methicone Copolyol Phosphate, and Dimethicone Copolyol Stearate. See International Cosmetic Ingredient Dictionary , 5th Edition, 1993.

Silicone-free emulsifiers used here include various nonionic and anionic emulsifiers, such as sugar esters and polyesters, alkoxylated sugar esters and polyesters, C1-C30 fatty acid esters of C1-C30 fatty alcohols, Alkoxylated derivatives of C1-C30 fatty acid esters of C1-C30 fatty alcohols, alkoxylated ethers of C1-C30 fatty alcohols, polyglyceryl esters of C1-C30 fatty acids, C1-C30 esters of polyols, C1-C30 ethers of polyols, alkyl phosphates, polyoxyalkylene fatty ether phosphates, fatty acid amides, acyl lactylates, soaps and mixtures thereof.

Non-limiting examples of silicon-free emulsifiers suitable herein include: Polyethylene glycol 20 sorbitan monolaurate (Polysorbate 20), Macrogol 5 soy sterol, Steareth-20, Ceteareth-20, PPG -2 Methyl Glucose Ether Distearate, Ceteth-10, Polysorbate 80, Cetyl Phosphate, Potassium Cetyl Phosphate, Diethanolamine Cetyl Phosphate, Polysorbate 60, Glyceryl Stearate, PEG-100 Hard Fatty acid ester, polyoxyethylene 20 sorbitan trioleate (Polysorbate 85), sorbitan monolaurate, polyoxyethylene 4 lauryl ether sodium stearate, polyglyceryl-4 isostearate, Hexyl laurate, steareth-20, ceteareth-20, PPG-2 methyl glucose ether distearate, ceteth-10, diethanolamine cetyl phosphate, glyceryl stearate, PEG-100 stearate and mixtures thereof.

non-essential ingredients

The compositions of the present invention may contain a wide variety of other ingredients, which are customary in a given product type, so long as they do not unacceptably alter the benefits of the present invention.

In a preferred embodiment, when the composition will be in contact with human keratinous tissue, these optional components should be suitable for keratinous tissue, that is, when they are introduced into the composition, they are suitable for contacting human keratinous tissue without reasonable medical reason. Undue toxicity, incompatibility, instability, denaturation, etc. within the scope of judgment. The CTFA Cosmetic Ingredient Handbook , 2nd Edition (1992) describes a wide variety of non-limiting cosmetic and pharmaceutical ingredients commonly used in the skin care industry, which are suitable for use in the compositions of the present invention. Examples of these classes of ingredients include: abrasives, absorbents, aesthetic components such as fragrances, pigments, colorants, essential oils, skin sensates, astringents, etc. (e.g. clove oil, menthol, camphor, eucalyptus, Eugenol, Menthyl Lactate, Witch Hazel Distillate), Anti-Acne Agents, Anti-Caking Agents, Antifoaming Agents, Antimicrobials (such as Iodopropyl Butylcarbamate), Antioxidants (such as BHT, BHA, tocopherol), binders, biological additives, buffers, bulking agents, chelating agents, chemical additives, colorants, cosmetic astringents, cosmetic biocides, denaturants, drug astringents, external analgesics, film-forming Agents such as polymers (such as eicosene and vinylpyrrolidone copolymers), sunscreens, pH regulators, propellants, reducing agents, sequestrants, skin Whitening and brightening agents (eg, hydroquinone, kojic acid, ascorbic acid, ascorbyl phosphate, ascorbyl glucosamine, pyridoxine), skin conditioning agents (eg, humectants, including various and non-occlusive ingredients) , skin comforting and/or healing agents (such as panthenol and its derivatives such as ethyl panthenol), aloe vera, pantothenic acid and its derivatives, allantoin, bisabolol, and dipotassium glycyrrhizinate), skin treatment agents ( Vitamin D compounds, mono-, di-, and triterpenoids, beta-ionol, cedrol), thickeners, and vitamins and vitamin derivatives.

Desquamation Actives

Safe and effective amounts of desquamation actives may be incorporated into the compositions of the present invention, more preferably from about 0.1% to about 10%, more preferably from about 0.2% to about 5%, by weight of the composition, and also preferably is about 0.5% to about 4%. The skin appearance benefits of the present invention are enhanced by desquamation actives. For example, desquamation actives help improve skin texture (eg, smoothness). One class of desquamation systems useful herein contains mercapto compounds and zwitterionic surfactants and is described in US Patent No. 5,681,852 to Bissett (incorporated by reference). Another class of exfoliating systems useful herein comprises salicylic acid and zwitterionic surfactants and is described in US Patent No. 5,652,228 to Bissett (incorporated by reference). Zwitterionic surfactants such as those described in these applications are also useful as desquamation agents herein, cetyl betaine being especially preferred.

Anti-Wrinkle Actives/Anti-Atrophy Actives

The compositions of the present invention may contain a safe and effective amount of one or more anti-wrinkle or anti-atrophy actives. Examples of such actives suitable here are sulfur-containing D and L amino acids and their derivatives and salts, especially N-acetyl derivatives, a preferred example of which is N-acetyl-L-cysteine; sulfur Alcohols, such as ethanethiol; hydroxy alcohols (such as alpha-hydroxy acids, such as lactic acid and glycolic acid, or beta-hydroxy acids), phytic acid, lipoic acid; lysophosphatidic acid, peeling agents (such as phenol, etc.), which enhance this The benefits of inventing the appearance of keratinous tissue, especially in regulating the condition of keratinous tissue such as skin condition.

water soluble vitamins

The compositions of the present invention may contain a safe and effective amount of one or more water-soluble vitamins, examples of which include, but are not limited to, water-soluble vitamin B, vitamin B derivatives, vitamin C, vitamin C derivatives, vitamin K, vitamin K derivatives , vitamin D, vitamin D derivatives, vitamin E, vitamin E derivatives, and mixtures thereof.

Vitamin _B3 Compound

Compositions of the present invention may contain a safe and effective amount of a vitamin _B3 compound. When it is present in the compositions of the present invention, the compositions preferably comprise from about 0.01% to about 50%, more preferably from about 0.1% to about 10%, more preferably from about 1% to about 5%, and more preferably from about 2% to about 5% vitamin _B3 compound.

Here "vitamin _B3 compound" means a compound having the following formula:

wherein R is _-CONH2 (ie nicotinamide), -COOH (ie nicotinic acid) or _-CH2OH (ie nicotinic alcohol); derivatives thereof; and salts of any of the foregoing.

Exemplary derivatives of the aforementioned vitamin _B3 compounds include nicotinic acid esters, including non-vasodilating esters of nicotinic acid (such as nicotinamide), nicotinyl amino acids, nicotinic acid N-oxide, and nicotinamide N-oxide.

Hydroxy acid

The compositions of the present invention also contain a safe and effective amount of a hydroxy acid. Preferred hydroxy acids for use in the present invention include alpha-hydroxy acids such as lactic acid and glycolic acid. When present in the compositions of the present invention, hydroxy acids are preferably present at levels of from about 0.01% to about 50%, more preferably from about 0.1% to about 10%, still more preferably from about 0.5% to about 2%.

peptide

The compositions of the present invention may contain a safe and effective amount of peptides, including but not limited to di-, tri-, tetra- and penta-peptides and their derivatives. "Peptide" herein refers to naturally occurring as well as synthetic peptides. Naturally occurring and commercially available compositions containing peptides can also be used herein.

Tripeptides suitable for use herein include carnosine (beta-ala-his). Useful tripeptides herein include gly-his-lys, arg-lys-arg, his-gly-gly. Preferred tripeptides and derivatives thereof include palmitoyl-gly-his-lys, which can be commercially available Biopeptide CL® (100 ppm palmitoyl-gly-his-lys available from Sederma, France); Peptide CK (arg- lys-arg); PeptideCK+ (ac-arg-lys-arg-NH ₂ ); and copper derivatives of his-gly-gly (Iamin, available from Sigma, St. Louis, MO). Tetrapeptides suitable for use herein include Peptide E, arg-ser-arg-lys (SEQ ID NO: 1). Pentapeptides suitable for use herein include lys-thr-thr-lys-ser. A preferred commercially available pentapeptide derivative composition is Matrixyl(R), which contains 100 ppm of palmitoyl-lys-thr-thr-lys-ser (SEQ ID NO: 2, available from Sederma, France).

The peptide is preferably selected from palmitoyl-lys-thr-thr-lys-ser, palmitoyl-gly-his-lys, derivatives thereof and combinations thereof.

When included in the compositions of the present invention, peptides are preferably present at levels of from about 1 x 10-6% to about 10%, more preferably from about 0.001% to about 10%, still more preferably from about 0.1% to about 10%, by weight of the composition .

Antioxidant/Free Radical Scavenger

The compositions of the present invention may contain an antioxidant/radical scavenger in a safe and effective amount, preferably at a level of from about 0.1% to about 10%, more preferably from about 1% to about 5%, by weight of the composition. Antioxidants/radical scavengers are especially useful in protecting the skin from UV rays and other environmental factors that can cause increased scaling or changes in the texture of the stratum corneum.

Antioxidants/radical scavengers that can be used are, for example, ascorbic acid (vitamin C) and its salts, ascorbic acid derivatives (eg, magnesium ascorbyl phosphate, sodium ascorbyl phosphate), tocotrienol, butylated hydroxybenzene Formate, Urate, Sorbate, Dihydroxyfumarate, Lysine, Methionine, Proline, Superoxide Dismutase, Silymarin, Tea Extract, Grape Skin/Seed Extract extracts, melanin and rosemary. A preferred antioxidant/radical scavenger is vitamin C.

water soluble flavonoids

The compositions of the present invention may contain a safe and effective amount of a water-soluble flavonoid. Preferred examples are o-glycosides.

Anti-cellulite agent

The compositions of the present invention also contain a safe and effective amount of an anti-celling agent. Suitable agents include, but are not limited to, xanthine compounds (eg, theophylline, theobromine, and aminobases).

tanning actives

The compositions of the present invention may contain a safe and effective amount of a tanning active, preferably the compositions contain from about 0.1% to about 20% dihydroxyacetone artificial tanning active.

Dihydroxyacetone, also known as DHA or 1,3-dihydroxy-2-propanone, is a white to off-white crystalline powder.

skin brightener

Skin lightening agents may be included in the compositions of the present invention. When used, the compositions preferably contain from about 0.1% to about 10%, more preferably from about 0.2% to about 5%, and likewise preferably from about 0.5% to about 2%, by weight of a skin lightening agent. Suitable skin lightening agents include those known in the art, including kojic acid, arbutin, ascorbic acid and its derivatives (such as magnesium ascorbyl phosphate, sodium ascorbyl phosphate) and extracts (such as mulberry tree extract, placenta extract).

Skin Comforting and Skin Healing Agents

The compositions of the present invention may contain a safe and effective amount of a skin comforting or skin healing agent, preferably comprising from about 0.1% to about 30% by weight of the formed composition, more preferably from about 0.5% to about 20%, and also preferably is from about 0.5% to about 10% of a skin comforting or skin healing agent. Skin comforting or skin healing agents suitable for use herein include pantothenic acid derivatives (including panthenol, dexpanthenol, ethyl panthenol), aloe vera, allantoin, and dipotassium glycyrrhizinate.

Antimicrobial and antifungal actives

Compositions of the present invention may contain antimicrobial or antifungal actives. A safe and effective amount of an antimicrobial or antifungal active may be incorporated into the compositions of the present invention, preferably from about 0.001% to about 10%, more preferably from about 0.01% to about 5%, still more preferably from about 0.05% to about 2%.

Examples of preferred antimicrobial and antifungal actives herein include glycolic acid, lactic acid, phytic acid, N-acetyl-L-cysteine, phenoxyethanol, phenoxypropanol, phenoxyisopropanol , and their compounds.

sunscreen actives

Skin exposure to UV rays can cause excessive scales and changes in the stratum corneum tissue. Accordingly, the compositions of the present invention optionally contain sunscreen actives. "Sunscreen active" as used herein includes sunscreens and physical sunscreens. Suitable sunscreen actives can be organic or inorganic.

Non-limiting examples of inorganic sunscreen actives for use herein include the following metal oxides: titanium dioxide with an average primary particle size of about 15 nm to about 100 nm, zinc oxide with an average primary particle size of about 15 nm to about 150 nm, Zirconia is about 15 nm to about 150 nm, iron oxide is about 15 nm to about 500 nm in average primary particle size, and mixtures thereof. When used herein, inorganic sunscreen actives comprise from about 0.1% to about 20%, preferably from about 0.5% to about 10%, more preferably from about 1% to about 5%, by weight of the composition.

A wide variety of conventional sunscreen actives are suitable for use here. A number of suitable actives are disclosed by Sagarin et al. in Cosmetic Science and Technology (1972), Chapter VIII, pp. 189ff. Specific suitable sunscreen actives include, for example, p-aminobenzoic acid, its salts and derivatives (ethyl, isobutyl, glyceryl esters, p-dimethylaminobenzoic acid), anthranilic acid esters (i.e. anthranil esters, methyl, menthyl, phenyl, benzyl, phenylethyl, linalyl, terpinyl and cyclohexenyl esters); salicylates (pentyl, phenyl, benzyl, menthyl dipropylene glycol esters); cinnamic acid derivatives (menthyl and benzyl esters, (alpha-phenylcinnamonitrile; butylcinnamoyl acetonate); dihydroxycinnamic acid derivatives (umbrelliform ketone, methyl umbelliferone, methyl acetyl umbelliferone); trihydroxycinnamic acid derivatives (escin, methyl esculetin, daphnetin, and glucoside, escin and daphnetin); hydrocarbons (diphenylbutadiene, 1,2-stilbene); dibenzylideneacetone and benzylideneacetophenone; naphthol sulfonate (2-naphthol-3,6-disulfonic acid and 2- Naphthol-6,8-disulfonic acid sodium salt); dihydroxynaphthoic acid and its salts; o- and p-hydroxybiphenyl disulfonates; coumarin derivatives (7-hydroxy, 7-methyl , 3-phenyl); diazoles (2-acetyl-3-bromoindazole, phenylbenzoxazole, methylnaphthazole, various arylbenzothiazoles); quinine salts (bisulfate , sulfate, chloride, oleate and tannate); quinoline derivatives (8-hydroxyquinolinate, 2-phenylquinoline); hydroxyl or methoxy substituted benzophenones; uric acid and vilouric acid; tannic acid and its derivatives (e.g. hexaethyl ether); (butyl carbotol) (6-propyl piperonyl) ether; hydroquinone; Oxybenzone, benzoresorcinol, 2,2',4,4'-tetrahydroxybenzophenone, 2,2'-dihydroxy-4,4'-dimethoxybenzophenone, Otto Benzophenone; 4-Isopropyl-dibenzoylmethane; Butylmethoxybenzoylmethane; Ethyl cyanodiphenylacrylate; Octocrylene; [3-(4'-Methylbenzylidene camphor alkan-2-one), and 4-isopropyl-dibenzoylmethane.

Among them, 2-ethylhexyl p-methoxycinnamate (commercially available as PARSOL MCX), 4,4'-tert-butylmethoxydibenzoylmethane (commercially available as PARSOL 1789), 2-hydroxy-4-methoxy benzophenone, octyldimethyl-p-aminobenzoic acid, digalloyl trioleate, 2,2-dihydroxy-4-methoxybenzophenone, 4-(bis(hydroxypropyl)) Ethyl aminobenzoate, 2-ethylhexyl 2-cyano-3,3-diphenylacrylate, 2-ethylhexyl salicylate, glyceryl p-aminobenzoate, 3,3 salicylic acid , 5-trimethylcyclohexyl ester, methyl anthranisate, p-dimethylaminobenzoic acid or aminobenzoate, 2-ethylhexyl p-dimethylaminobenzoate, 2-phenylbenzene Imidazole-5-sulfonic acid, 2-(p-dimethylaminophenyl)-5-sulfobenzoxazoic acid, octocrylene and mixtures of these compounds are preferred.

Also suitable for use in the compositions of the present invention are sunscreens having two different chromophore moieties in one molecule which exhibit different absorption spectra of ultraviolet radiation. One of the chromophore moieties absorbs primarily in the UVB radiation range and the other chromophore moiety absorbs primarily in the UVA radiation range.

When present in the compositions, the sunscreen actives are used in a safe and effective amount, typically from about 1% to about 20%, more preferably from about 2% to about 10%, by weight of the composition. The exact amount used will depend on the sunscreen active selected and the desired Sun Protection Factor (SPF).

particulate matter

Compositions of the present invention may in some embodiments comprise particulate materials, preferably metal oxides. These particles may be coated or uncoated, charged or uncharged. Charged particulate matter is disclosed in US Patent No. 5997887 (Ha et al.), incorporated by reference. Particulate materials useful for this include bismuth oxychloride, iron oxide, mica, barium sulfate treated mica, titanium dioxide ( _TiO2 ), zinc oxide, zirconia, silica, nylon, polyethylene, talc, styrene, polypropylene , ethylene/acrylic acid copolymer, silk mica, aluminum oxide, polysiloxane resin, barium sulfate, calcium carbonate, cellulose acetate, polymethyl methacrylate, and mixtures thereof.

Inorganic particulate materials such as _TiO2 , ZnO, or _ZrO2 are available from many commercial sources. An example of a suitable particulate material includes that available from US Cosmetics (TRONOX _TiO2 series, SAT-T CR837, rutile _TiO2 ). Preferably, the particulate material is present in the composition at a level of from about 0.01% to about 2%, more preferably from about 0.05% to about 1.5%, still more preferably from about 0.1% to about 1%, by weight of the composition. There are no particular limitations on the pigments, colorants, or fillers employed in the composition.

Preferred organic powders/fillers include, but are not limited to, polymer particles selected from methylsilsesquioxane resin microspheres such as those sold by Toshiba silicone under the trade name Tospearl 145A; microspheres of polymethyl methacrylate; spheres, such as microspheres sold under the trade name Micropearl M 100 by Seppic; spherical particles of cross-linked polydimethylsiloxane, especially those sold under the trade names Trefil E 506C or Trefil E 505C by Dow Corning Toray Silicone; Spherical particles of amides and more particularly Nylon 12, especially as sold under the trade name Orgasol 2002D Nat C05 by Atochem; polystyrene microspheres such as those sold by Dyno Particles under the trade name Dynospheres; Kobo under the trade name FloBead Ethylene acrylate copolymers and mixtures thereof sold as EA209.

Also useful here are pigment and/or dye capsules, such as nanocolorants from BASF, and multilayer interference pigments, such as Sicopearls from BASF.

Pigments/powders are preferably surface treated to provide additional color stability and ease of formulation. Hydrophobically treated pigments are preferred because they are more easily dispersed in the delivery medium. Additionally, it may be useful to treat the pigment with a material that is compatible with the polysiloxane. Hydrophobic pigment treatments particularly suitable for use in water-in-silicone emulsions include silicone treatments as described in US Patent No. 5,143,722, which is hereby incorporated by reference in its entirety. Also preferred are pigments/powders having an average primary particle size of from about 10 nm to about 100,000 nm, more preferably from about 50 nm to about 5,000 nm, most preferably from about 100 nm to about 1000 nm. Mixtures of the same or different pigments/powders with different particle sizes are also suitable for use here (eg, TiO2 having a primary particle size of about 100 nm to about 400 nm and TiO2 having a primary particle size of about 10 nm to about 50 nm).

conditioner

Compositions of the present invention may contain conditioning agents selected from humectants, moisturizers or skin conditioning agents. A variety of materials are useful herein, each present at from about 0.01% to about 40%, more preferably from about 0.1% to about 30%, still more preferably from about 0.5% to about 10%, by weight of the composition. Non-limiting examples of conditioning agents include guanidine, urea, glycolic acid and glycolic acid salts (such as ammonium and quaternary alkyl ammonium salts); salicylic acid; lactic acid and lactate salts (such as ammonium and quaternary alkyl ammonium salts) ; various forms of aloe vera (such as aloe vera gel); polyols such as sorbitol, mannitol, xylitol, erythritol, glycerin, hexanetriol, butanetriol, propylene glycol, butylene glycol, hexylene glycol, etc. ; polyethylene glycol; sugars (eg, melibiose) and starches; sugar and starch derivatives (eg, alkoxylated glucose, fructose, glucosamine); hyaluronic acid; lactamide monoethanolamine; acetamide monoethanolamine; Panthenol; Allantoin; and mixtures thereof. Also suitable for use herein are the propoxylated glycerols of US Patent No. 4976953 (December 11, 1990) to Orr et al.

Also suitable herein are the various C ₁ -C ₃₀ mono- or polyesters of sugars and related materials. These esters are derived from a sugar or polyol moiety and one or more carboxylic acid moieties.

Preferably, the conditioning agent is selected from the group consisting of urea, guanidine, sucrose polyesters, panthenol, dexpanthenol, allantoin and combinations thereof.

Thickening agents (including thickeners and gelling agents)

The compositions of the present invention may comprise one or more thickening agents, preferably from about 0.1% to about 5%, more preferably from about 0.1% to about 3%, and still more preferably from about 0.25% to about 2%, by weight of the composition. Thick reagent. The compositions of the present invention may also contain mixtures of thickeners.

Non-limiting examples of thickening agents include materials selected from the group consisting of:

a) Carboxylic acid polymer

Nonlimiting examples of commercially available carboxylic acid polymers useful in the present invention include carbomers, which are homopolymers of acrylic acid crosslinked with sucrose or allyl ethers of pentaerythritol. Commercially available carbopol formulations are ^Carbopol® 900 series (such as ^Carbopol® 954) produced by Goodrich Corporation. Additionally, other suitable carboxylic acid polymer reagents include copolymers of C _10-30 alkyl acrylates with one or more monomers such as acrylic acid, methacrylic acid, or short chains thereof (i.e., C _{1 -4} alcohol) ester, wherein the cross-linking agent is allyl ether of sucrose or pentaerythritol. These copolymers are known as acrylates/C _10-30 alkyl acrylate cross-linked polymers and are commercially available as ^Carbopol® 1342, ^Carbopol® 1382, Pemulen TR-1 and Pemulen® from Goodrich Corporation. TR-2.

b) Cross-linked polyacrylate polymer

U.S.P 5,100,660 issued March 31, 1992 to Hawe et al; U.S.P 4,849,484 issued July 18, 1989 to Heard; U.S.P 4,835,206 issued May 30, 1989 to Farrar et al; issued December 9, 1986 to Glover et al U.S.P 4,628,078 to Flesher et al.; U.S. Patent 4,599,379 to Flesher et al., issued July 8, 1986; EP 228,868 to Farrar et al., published July 15, 1987. Non-limiting examples of acrylate polymers and crosslinked cationic polyacrylate polymers, which are incorporated by reference.

c) Polyacrylamide polymer

A non-limiting example of a polyacrylamide nonionic polymer herein is the product having the CTFA designation polyacrylamide and isoparaffin and lauryl ether-7, available under the tradename Sepigel 305 from Seppic Corporation (Fairfield, NJ).

Other polyacrylamide polymers useful in the present invention include multi-block copolymers of acrylamide and acrylamide substituted with acrylic acid and substituted acrylic acid. Commercially available examples of such multi-block copolymers include HypanSR150H, SS500V, SS500W, SSSA100H from Lipo Chemicals, Inc., (Patterson, NJ).

d) polysaccharide

Non-limiting examples of polysaccharide gelling agents include cellulose, carboxymethyl hydroxyethyl cellulose, cellulose acetate propionate carboxylate, hydroxyethyl cellulose, hydroxyethyl ethyl cellulose, hydroxypropyl cellulose , hydroxypropylmethylcellulose, methylhydroxyethylcellulose, microcrystalline cellulose, sodium cellulose sulfate, and mixtures thereof. Alkyl-substituted celluloses can also be used in the present invention. In these polymers, the hydroxyl groups in the cellulosic polymer are hydroxyalkylated, preferably hydroxyethylated or hydroxypropylated, to form hydroxyalkylated cellulose, which is then formed from The C ₁₀ -C ₃₀ linear or branched alkyl groups are further modified by ether linkages. These polymers are typically ethers of hydroxyalkylcelluloses with C ₁₀ -C ₃₀ linear or branched chain alcohols. The alkyl group used here can be selected from stearyl, isostearyl, lauryl, myristyl, cetyl, isocetyl, cocoyl (that is, the alkyl group derived from the alcohol of coconut oil ), palmityl, oleyl, linoleyl, linolenic, castoryl, behenyl, and mixtures thereof. Preferred among the alkyl hydroxyalkyl cellulose ethers are those having the CTFA designation cetyl hydroxyethyl cellulose, which is an ether of cetyl alcohol and hydroxyethyl cellulose. Aqualon Corporation (Wilmington, DE) sells these materials under the tradename Natrosol ^(R) CS Plus.

Other polysaccharides used include scleroglucans containing (1-3) linked glucose units with linear chains of (1-6) linked glucose units for every three sugar units, a commercial example of which is Michel Clearogel ^(TM) CS11 from Mercier Products Inc. (Mountainside, NJ).

e) Glue

Non-limiting examples of these gelling agent gums include substances selected from the group consisting of gum arabic, agar, alginic acid, ammonium alginate, pullulan, calcium alginate, calcium carrageenan, carnitine, carrageenan , dextrin, gelatin, gellan gum, guar gum, guar hydroxypropyltrimonium chloride (guar hydroxypropyltrimonium chloride), hectorite grease, hyaluronic acid, hydrated silica, hydroxypropyl Chitosan, Hydroxypropyl Guar Gum, Karaya Gum, Seaweed, Locust Bean Gum, Natto Gum, Potassium Alginate, Potassium Carrageenan, Propylene Glycol Alginate, Sclerotin Gum, Carboxymethyl Dextrose Sodium sugar, sodium carrageenan, gum tragacanth, xanthan gum, and mixtures thereof.

Composition preparation method

Methods of preparation of the compositions of the present invention are generally conventional methods known in the art of preparing topical compositions. These methods generally involve mixing the ingredients into a relatively uniform state in one or more steps, with or without heating, cooling, vacuum, and the like.

Instructions

The compositions of the present invention are useful for enhancing the delivery of oil-soluble skin care actives to the skin. The oil-soluble active agents in the compositions of the present invention are delivered to the skin dermis at a higher rate than single application delivery of conventional oil-in-water or water-in-oil emulsions in which the active agent is present in the oil phase. Measurement of such delivery enhancement can be accomplished by any conventional means comparing the delivery of the active agent to a standard topical skin care composition. For example, the ex-vivo skin penetration method that penetrates dead skin using Franz cells is a standard method for measuring the skin penetration ability of skin care actives. 933

The compositions of the present invention are useful for regulating the condition of the skin and/or hair while maintaining good aesthetics, and improving the delivery of oil-soluble skin care actives. Regulating skin condition includes reducing the appearance of fine lines and/or wrinkles on the skin, reducing eye bags and dark circles under the eyes, sagging skin, scars/spots, bumps, pores, extended spots, roughness, skin surface blemishes, forehead The appearance of lines, expression lines, wrinkles, blemishes, photodamage, fissures and/or unevenness.

Modulation of keratinous tissue condition of the skin using these actives in combination with the viscous solvent soluble actives and the improved delivery system can include both prophylactic and therapeutic modulation. For example, such methods of regulation refer to densifying keratinous tissue (i.e. structuring the epidermis and/or dermis of the skin and, where applicable, of the nails and hair shaft), and preventing and/or retarding the atrophy of mammalian skin, preventing and/or Blocks the appearance of capillaries and/or erythema on the skin of mammals, prevents and/or blocks the appearance of dark circles under the eyes, sallow complexion, sagging, softens and/or smoothes lips, hair and nails, prevents and/or Reduces itchy skin, regulates skin texture (eg wrinkles and fine lines) and improves skin tone (eg redness, freckles).

In a preferred embodiment, the composition is applied chronically to the skin. "Long-term topical administration" refers to the continuous application of the composition for an extended period of time in the individual's life, preferably at least about 1 week, more preferably at least about 1 month, more preferably at least about 3 months, and more preferably at least about 6 months. months, and preferably at least about 1 year. Chronic administration over the lifetime of the individual is preferred, although benefits may be obtained after various maximum periods of time, such as after five, ten or twenty years. During these periods, application is generally about once per day, but the rate of application can be from about once per week to about 3 or more times per day.

The compositions of the present invention can be used in a wide range of amounts to provide an appearance and/or sensory benefit to the skin. The composition is generally used in an amount (in milligrams of composition per square centimeter of skin) of about 0.1 mg/cm ² to about 10 mg/cm ² . In particular, the amount applied is from about 1 mg/cm ² to about 2 mg/cm ² .

Preferably, improving and/or regulating skin appearance, feel, and/or condition is effected through lotions, creams, gels, foams, salves, pastes, emulsions, sprays, conditioners, tonics, cosmetics, Lipsticks, foundations, nail polishes, after-shaves, or other preferred forms of compositions applied to the skin or other keratinous structures for aesthetic, preventive, therapeutic, or other benefits (i.e., " leave-on” composition). After applying the composition to the skin, it is preferably left on the skin for at least about 15 minutes, more preferably at least about 30 minutes, more preferably at least about 1 hour, most preferably at least about several hours, such as up to 12 hours. Can treat any part of the exterior of the face, hair and/or nails, such as face, lips, under-eye area, eyelids, scalp, neck, torso, arms, hands, legs, feet, nails, toenails, scalp hair, eyelashes, eyebrows, etc. . Compositions can be applied with the fingers or with any device such as pads, cotton balls, applicator pens, spray applicators, and the like.

Another way to ensure continued exposure of the skin to at least a minimum amount of phytantriol and bisabolol is to apply the composition using a patch application to, for example, the face. This approach is especially useful for problematic areas of the skin that require more intensive treatment (such as facial creases, frown lines, under-eye area, etc.). The patch can be occlusive, semi-occlusive or non-occlusive and can be adhesive or non-adhesive. The composition can be included in a patch or applied to the skin prior to application of the patch. The patch may also contain other actives such as chemical initiators for exothermic reactions as described in US5821250; 5981547 and 5972957 to Wu et al. Preferably the patch is left on the skin for at least about 5 minutes, more preferably at least about 15 minutes, still more preferably at least about 30 minutes, still more preferably at least about 1 hour, still more preferably about overnight for an overnight treatment.

Example

The following examples will further describe and illustrate specific examples within the scope of the present invention. These embodiments are for the purpose of illustration only, and are not intended to limit the present invention, and many changes are possible without violating the spirit and scope of the present invention.

Example 1-7

Water-in-Silicone Skin Cream

A water-in-silicone skin care cream was prepared by conventional methods from the following ingredients. Amounts of ingredients are listed as percentages by weight of the composition. Element 1 2 3 4 5 6 7 Phase A water Appropriate amount Appropriate amount Appropriate amount Appropriate amount Appropriate amount Appropriate amount Appropriate amount Disodium EDTA 0.10 0.10 0.10 0.10 0.10 0.10 0.10 Methylparaben 0.10 0.10 0.10 0.10 0.10 0.10 0.10 Methylparaben 0.10 0.10 0.10 0.10 0.10 0.10 0.10 Nicotinamide 2.00 7.5 5.0 3.50 10.00 5.0 Dexpanthenol 0.50 1.0 1.0 0.50 1.0 0.50 Allantoin 0.2 0.2 0.2 0.2 benzyl alcohol 0.25 0.25 0.25 0.25 0.25 0.25 0.25 green tea extract 1.00 1.00 1.00 1.00 1.00 1.00 glycerin 6.00 20.00 10.00 7.00 15.00 15 Terephthalidene camphor sulfonic acid 1 5.0 Palmitoyl Lys Thr Thr Lys Ser ² 0.0003 0.0003 Phase B Dow Corning 9040 ³ 11.00 15.00 20.00 10.00 7.50 10 kSG-21 ⁴ 4.00 5.50 15.00 7.00 0.50 10 Cyclomethicone 12.00 17.00 20.00 25.00 20.00 3.00 20 Dimethicone Copolyol (Dow Corning 5225c) 3.00 5.00 2.50 2.00 Vitamin E Acetate 0.50 0.5 0.50 0.50 Titanium dioxide GLW75CAP-MP ⁵ 0.50 0.50 Fragrance 0.20 0.20 0.20 0.20 Farnesol 3.00 5.00 1.00 (-)-α bisabolol 0.50 1.00 Parsol 1789 ⁶ 3.00 2.00 Fytosterol-85 ⁷ 1.00 Octyl Salicylate 5.00 Isopropyl palmitate 7.00 6.00 Tospearl 145 1.00 1.00 Phase C Finsolv TN 2.00 2.00 2.00 Retinol 0.10 retinyl propionate 0.20 0.20

¹ available from Chimex as Mexoryl SX

² peptides available from Sederma

³ 12% Dimethicone/Vinyl Dimethicone Crosspolymer in Cyclomethicone obtained from Dow Corning

⁴ Commercially available from Shin-Etsu; 25% dimethicone/copolyol crosspolymer in dimethicone

⁵ Titanium dioxide GLW75CAP-MP is available from KOBO.

⁶ Parsol 1789 available from Roche.

⁷ Fytosterol-85 is available from Dragoco.

Mix together the ingredients of Phase A in a suitable container and the ingredients of Phase B in a separate suitable container, both using a suitable agitator equipped with a propeller (eg, Tekmar Model RW20DZM). If Phase C is present, its ingredients are mixed together in a separate suitable container (if needed) and added to Phase B. When both phases are homogeneous, slowly add phase A to phase B while stirring phase B by the propeller. Keep stirring until smooth. The resulting emulsion is then ground for a few minutes through a suitable mill (eg Tekmar T25) to ensure homogeneity. The product is then poured into suitable containers. The resulting products can exhibit enhanced penetration of oil-soluble skin care actives and have good aesthetic properties.

Claims (21)

1. Topical compositions for delivering oil-soluble skin care actives to the skin, comprising: a) oil-soluble skin care actives in an amount of from 0.01% to 40% by weight of the composition; b) silicone oil in an amount from 5% to 99% by weight of the composition; and c) silicone elastomers in an amount of from 0.1% to 30% by weight of the composition; Wherein the oil-soluble skin care active agent is selected from oil-soluble terpene alcohols, oil-soluble phytosterols, oil-soluble anti-acne active agents, oil-soluble β-hydroxy acids, oil-soluble vitamin _B3 compounds, oil-soluble retinoids, oil-soluble antioxidants , oil-soluble free radical scavengers, oil-soluble chelating agents, oil-soluble flavonoids, oil-soluble anti-inflammatory agents, oil-soluble anti-cellulite agents and oil-soluble local anesthetics and mixtures thereof. 2. The composition of claim 1, wherein the oil-soluble skin care active agent is selected from the group consisting of oil-soluble terpene alcohols, oil-soluble phytosterols, oil-soluble beta-hydroxy acids, oil-soluble vitamin _B3 compounds, oil-soluble retinoids, oil-soluble Antioxidants, oil-soluble free radical scavengers, oil-soluble chelating agents, oil-soluble flavonoids and mixtures thereof. 3. The composition of claim 1, wherein the silicone oil is selected from the group consisting of cyclomethicone, dimethicone, and mixtures thereof. 4. The composition of claim 1, wherein the silicone elastomer is selected from the group consisting of emulsifying silicone elastomers, non-emulsifying silicone elastomers, and mixtures thereof. 5. The composition of claim 1, wherein the oil-soluble skin care active is selected from the group consisting of farnesol, retinol, retinyl propionate, retinyl palmitate, tocopheryl nicotinate, and mixtures thereof. 6. The composition of claim 1 wherein the silicone elastomer is an emulsified silicone elastomer selected from the group consisting of dimethicone copolyol crosspolymers and the silicone oil is dimethicone. 7. The composition of claim 4 wherein the non-emulsifying silicone elastomer is selected from the group consisting of dimethicone/vinyl dimethicone crosspolymer and mixtures thereof. 8. The composition of claim 1, wherein the composition is anhydrous. 9. The composition of claim 1, further comprising an additional skin care active agent selected from the group consisting of sunscreens, particulate materials, conditioning agents, thickeners, water-soluble vitamins, water-dispersible vitamins, oil-dispersible vitamins and its mixture. 10. The composition of claim 1, wherein the silicone elastomer is selected from the group consisting of emulsifying silicone elastomers, non-emulsifying silicone elastomers, and mixtures thereof. 11. The composition of claim 10, wherein the silicone elastomer is an emulsified silicone elastomer selected from the group consisting of dimethicone copolyol crosspolymers and the silicone oil is dimethicone. 12. The composition of claim 10 wherein the non-emulsifying silicone elastomer is selected from the group consisting of dimethicone/vinyl dimethicone crosspolymer and mixtures thereof. 13. A topical water-in-silicone emulsion composition suitable for delivering an oil-soluble skin care active to the skin, comprising a continuous oil phase and a discontinuous water phase, wherein the oil phase comprises: a) oil-soluble skin care actives in an amount of from 0.01% to 40% by weight of the composition; b) silicone oil in an amount from 5% to 99% by weight of the composition; and c) silicone elastomers in an amount of from 0.1% to 30% by weight of the composition; Wherein the oil-soluble skin care active agent is selected from oil-soluble terpene alcohols, oil-soluble phytosterols, oil-soluble anti-acne active agents, oil-soluble β-hydroxy acids, oil-soluble vitamin _B3 compounds, oil-soluble retinoids, oil-soluble antioxidants , Oil-soluble free radical scavengers, oil-soluble chelating agents, oil-soluble flavonoids, oil-soluble anti-inflammatory agents, oil-soluble anti-cellulite agents, oil-soluble local anesthetics and mixtures thereof. 14. The composition of claim 13, wherein the oil-soluble skin care active agent is selected from the group consisting of oil-soluble terpene alcohols, oil-soluble phytosterols, oil-soluble beta-hydroxy acids, oil-soluble vitamin _B3 compounds, oil-soluble retinoids, oil-soluble Antioxidants, oil-soluble free radical scavengers, oil-soluble chelating agents, oil-soluble flavonoids and mixtures thereof. 15. The composition of claim 13, wherein the oil phase comprises at least 51% silicone oil by weight of the oil phase. 16. The composition of claim 13, wherein the silicone oil is selected from the group consisting of cyclomethicone, dimethicone, and mixtures thereof. 17. The composition of claim 13, wherein the oil-soluble skin care active is selected from the group consisting of farnesol, retinol, retinyl propionate, retinyl palmitate, tocopheryl nicotinate, and mixtures thereof. 18. The composition of claim 13, further comprising an additional skin care active agent selected from the group consisting of sunscreens, particulate materials, conditioning agents, thickeners, water soluble vitamins, water dispersible vitamins, oil dispersible vitamins and its mixture. 19. A topical water-in-silicone emulsion composition suitable for delivering an oil-soluble skin care active to the skin, comprising a continuous oil phase and a discontinuous water phase, wherein the oil phase comprises: a) farnesol in an amount of from 0.01% to 40% by weight of the composition; b) Silicone oil in an amount from 5% to 99% by weight of the composition; c) Silicone elastomers in amounts of from 0.1% to 30% by weight of the composition. 20. A cosmetic method of enhancing the delivery of an oil-soluble skin care active to the skin comprising applying a safe and effective amount of the composition of claim 2 to the skin of a mammal in need of treatment. 21. A cosmetic method of enhancing the delivery of an oil-soluble skin care active to the skin comprising applying a safe and effective amount of the composition of claim 14 to the skin of a mammal in need of treatment.