KR100654844B1 - Cosmetics on Nano-size Oil-in-water Phospholipid Emulsions Using Polyprotose-based Polymers Modified with Lipophilic Type - Google Patents

Abstract

The present invention includes a polyprotose-based polymer material and a natural phospholipid modified with a lipophilic type of a polymer extracted from a chicory root as a stabilizer on a phospholipid emulsion, and an emulsifier of 60 to 160 nm. The present invention relates to an oil-in-water type phospholipid emulsion-like cosmetic and a method for preparing the same. Oil-in-water type of bulky size by primary emulsification at high temperature together with oil phase ingredients including emulsifier, emulsifying oil and oil-soluble bioactive ingredients ) Make an emulsion phase and cool it to make an oil-in-water phospholipid emulsion phase with nanosize using high pressure emulsifier Stabilize emollient oils and oil-soluble bioactives in lipid bi-layers consisting of phospholipids, cholesterol, and ceramides, and steric hindrance effects of polyprotose modified with nanolipophilic phospholipid emulsions. Thereby preventing the coalescence of particles and preventing and stabilizing the release of water-soluble and oil-soluble bioactive ingredients.

Polyprotose, stabilizer, nanosize emulsion, stabilization, steric hindrance, high pressure emulsifier

Description

Cosmetic composition having a nano-size phospholipid emulsion of oil in water type using a hydrophobically modified polyfroctose polymeric emulsifier and manufacturing method kind}

1 is a diagram showing the chemical structure of polyprotose modified to be lipophilic as used as a stabilizer on a nanosized phospholipid emulsion in the present invention.

2 is a view showing the chemical structure of the phospholipid used as the main emulsifier in the present invention.

3 is a schematic diagram showing a structure in which the nano-sized phospholipid emulsion phase is stabilized by lipophilic modified polyprotose.

4 to 6 are particle size analysis data showing the particle size and distribution thereof on the nanosized phospholipid emulsion stabilized by lipophilic modified polyprotose according to the present invention.

The present invention includes a polyprotose-based polymer material transformed from a chicory root into a lipophilic polymer and a phospholipid extracted from natural soybean that is not chemically synthesized. The present invention relates to a composition having an oil-in-water type phospholipid emulsion phase having a fine size and a preparation method thereof. More specifically, the present invention does not use a chemically synthesized emulsifier that is easy to cause irritation to sensitive skin by using a high pressure emulsifier, and uses natural phospholipids, especially natural phospholipids extracted from soybean, cholesterol, and ceramides as emulsifiers. It is hypoallergenic to the skin and stabilizes to low viscosity type using polyprotose modified into lipophilic nanosized phospholipid emulsion phase having nano size and easy skin delivery of pharmacological substance with excellent skin similarity, This nanosize phospholipid emulsion phase is stabilized by the lipophilic modified polyprotose steric hindrance effect, which prevents the integration of nanosize particles and prevents the release of water-soluble and oil-soluble bioactive components. Nano-size Oil-in-water Phospholipid Emulsion Using Polyprotose-based Polymer The present invention relates to a cosmetic and a method of manufacturing the same.

In general, nano-sized cosmetics using high pressure emulsifiers are used in drug delivery systems that make particles easier to deliver to the skin than normal micro-sized cosmetics by preparing particles having a size similar to or smaller than the skin gap. It is used. In these technologies, the innermost phase is an aqueous phase, the nanosized liposomes and the most endogenous are oil phases, and the phospholipid bilayers are easy to stabilize, and the soluble phospholipids are easily stabilized. It can be divided into nanosized emulsion phases. In addition, there is an emulsification system in which a nano-sized liposome and an emulsion phase exist simultaneously using a composite particle forming technology that is recently developed.

In general, surfactants conventionally used in basic cosmetics include 1) polysorbate 20 and polysorbate 60 as hydrophilic, and 2) glyceryl stearate and sorbent as lipophilic. Non-elastic oleate, sorbitan stearate, etc. 3) Self-emulsifying types such as POE (polyoxyethylene) 100-stearate / glyceryl stearate.

In the conventional emulsification method using these, the particle size is about several micrometers (micrometer), and the interface is formed in the uni-layer mainly by a nonionic surfactant. Therefore, the skin affinity is not good, due to the particle size very large than the gap of the skin is not easy to transfer the active ingredient to the skin, even if prepared in the nano-size has a disadvantage that can cause irritation on the skin.

In general, the surfactants used on the nano-sized liposomes and emulsions having excellent biocompatibility and high pressure emulsifiers are mainly phospholipids extracted from soybean or egg yolk, which are saturated and unsaturated types. In these two types, there are phosphatidylcholin, phosphatidylethanolamine, and phosphatidylinositol depending on the type of each functional group. These phospholipids have good advantages due to their high skin safety, biocompatibility, and similarity to skin structure, but they have problems due to their emulsifying power and their unique interfacial properties. The high-energy emulsifier (high-pressure homogenizer) to compensate for the above disadvantages by using these components can be used to prepare an emulsion phase having a nano-size using these components. However, according to the conventional method described above, even when a nano-sized emulsion phase is prepared, the oil amount is not a small amount, and when it is increased, its stability is increased by Ostwald ripening; Interfacial phenomena) may ultimately lead to instability of the nanoscale phospholipid emulsion phase, separation of the formulation itself, and release of the stabilized useful bioactive substance. There was a disadvantage that there is no choice.

Therefore, using a high-pressure emulsifier, the nano-sized oil-in-water phospholipid emulsion using phospholipid, which is the main component of the skin lipid membrane and cell membrane, is stabilized by preventing the Oswald living phenomenon and encapsulated into nano-sized phospholipid emulsion. Compositions and methods that can deliver effectively as a result have still needed to be improved.

Therefore, the present invention, as a result of the efforts to solve the above problems, using a polyprotose-based polymer material modified in the lipophilic polymer material extracted from the lettuce roots as a stabilizer extracted from natural soybean not chemically synthesized Nano-sized phospholipid emulsion phase containing phospholipid as emulsifier, having oil-in-water phospholipid emulsion phase with fine size of 60-160 nm, soft to skin, and easy delivery of pharmacological substance to skin The present invention is intended to provide a cosmetic and a method for producing the same, comprising a low viscosity and stabilized excess oil components to ensure stable delivery to the skin.

In addition, in the present invention, using polyprotose made by extracting polysaccharides of pentose sugar from the root of lettuce, which is a source of polysaccharide intake of humans, including sugarcane, is very mild to the skin and has excellent moisturizing power. And many chains of polyprotose modified to lipophilic not only at low temperatures but also at high temperatures are small in the oil phase due to the hydration force due to the strong hydrogen bond with water and the numerous lipophilic groups oriented in the oil phase. The small loop prevents the desorption of oil and, moreover, the excellent steric hindrance effect of the large loop of polyprotose, which has a long chain from the water phase to the polymer. Provides a method of stabilizing by preventing the unification of the liver, preventing the separation of the formulation and desorption of the useful bioactive components, smoothing without irritation to sensitive skin, and encapsulated in the nano-sized phospholipid emulsion to stabilize the desired It is an object to build a drug delivery system deliverable to the site.

In the present invention, to prepare a cosmetic such as skin, lotion, essence on the nano-sized phospholipid emulsion as a moisturizer, water-modified polyprotose-based stabilizer, water-soluble bioactive components Bulk sized oil-in-water type by primary emulsification at high temperature with oil phase components including phospholipids, cholesterol, ceramides, preservatives, alcohol phases, emulsified oils, oil soluble active ingredients Emulsion phase is made and cooled to form an oil-in-water type phospholipid emulsion phase using a high pressure emulsifier to stabilize emulsified oils and oil-soluble bioactive substances in lipid bi-layers consisting of phospholipids, cholesterol and ceramides. And a lipophilic polyprotose polymer as a stabilizer Blocking the sum of using particles, the water solubility and availability for the phospholipid composition of the emulsion of the nano-size to prevent the glass of the physiologically active ingredient and a method of manufacturing for the purpose of providing.

Nano-size oil-in-water phospholipid emulsion phase cosmetics using polyprotose-based polymer materials modified with lipophilic type according to the present invention, alcohol 2.0 to 20.0% by weight, phospholipid 0.5 to 8.0% by weight, ceramide 0.03 to 2.0% by weight, cholesterol An alcohol portion including 0.03 to 2.0 wt%, and 0.1 to 0.5 wt% preservative; An oil phase including 2.0 to 20.0 wt% of emollient oil and 0.05 to 5 wt% of an oil-soluble bioactive substance; And an aqueous phase including 0.5 to 10% by weight of a moisturizing agent, 0.1 to 5% by weight of a polyprotose-based polymer material modified into a lipophilic type, 0.01 to 3.0% by weight of a water-soluble physiologically active material, and water remaining.

In the preparation method of the nano-sized oil-in-water phospholipid emulsion phase cosmetics using the polyprotose-based polymer material modified into a lipophilic type according to the present invention, in preparing cosmetics by emulsification, (1) 2.0 to 20.0% by weight of alcohol, Alcohol part preparation step of preparing an alcohol part by heating the phospholipid 0.5 to 8.0% by weight, ceramide 0.03 to 2.0% by weight, cholesterol 0.03 to 2.0% by weight, preservative 0.1 to 0.5% by weight to 40 to 70 ℃; (2) an oil phase preparation step of preparing an oil phase by heating 2.0 to 20.0 wt% of an emulsified oil and 0.05 to 5 wt% of an oil-soluble bioactive substance at 70 to 85 ° C .; (3) 0.5 to 10% by weight of a moisturizing agent, 0.1 to 5% by weight of polyprotose-based polymer material modified into a lipophilic type, 0.01 to 3.0% by weight of a water-soluble physiologically active material, and the remaining amount of water to 70-85 ° C. A water phase preparation stage for preparing; (4) The oil-in-water emulsion phase of a bulky size was first emulsified by mixing the water phase portion, the alcohol portion and the oil phase portion and stirring at a rotational speed of 2,000 to 3,500 rpm in a normal vacuum emulsion tank. Forming a first emulsion; (5) a cooling step of cooling the bulky oil-in-water emulsion phase to 45-65 ° C .; (6) a lipid consisting of phospholipids, cholesterol, and ceramides by adding the bulky oil-in-water emulsion phase of the bulky size to a commercially available high-pressure emulsifier at a temperature of 5 to 65 ° C. and second emulsifying at a pressure of 500 to 1,500 bar. A second emulsion forming step of forming an oil-in-water phospholipid emulsion phase having a nano-sized stabilization of an emollient oil and an oil-soluble bioactive substance in a bilayer; And (7) a second cooling step of stabilizing the oil-in-water phospholipid emulsion phase having a nano-sized stabilization of the emollient oil and the oil-soluble bioactive substance at 25 to 30 ° C .; This is done including.

Hereinafter, exemplary embodiments of the present invention will be described in detail with reference to the accompanying drawings.

According to the present invention, in the preparation of nano-sized oil-in-water phospholipid emulsion phase using phospholipid, the physiological stability of nano-size phospholipid emulsion ultimately becomes unstable, and the formulation itself is separated and stabilized. In order to prevent the active substance from being detached, it is characterized in that it comprises the use of polyprotose modified into a lipophilic type as a stabilizer. Here, polyprotose modified into a lipophilic type as a stabilizer for stabilization of an emulsion phase has an oily phase due to the numerous lipophilic groups in which its numerous chains are hydrated by a strong hydrogen bond with water and orientated to an oil phase. Enables the formation of small loops in the membrane, thereby preventing desorption of oil, and the greater steric hindrance effect of large loops of polyprotose with longer chains in the water phase and polymers It is one of the main features to prevent the unity between the particles due to the Ostwald lifeening phenomenon, to prevent the separation of the formulation and desorption of the useful bioactive component, as described above.

Nano-size phospholipid emulsion phase composition using the lipophilic polymer modified emulsifier according to the present invention is composed of alcohol portion, oil phase portion and water phase portion, alcohol 2.0 to 20.0% by weight, phospholipid 0.5 to 8.0% by weight, ceramide An alcohol portion comprising 0.03 to 2.0 wt%, cholesterol 0.03 to 2.0 wt%, and 0.1 to 0.5 wt% preservative; An oil phase including 2.0 to 20.0 wt% of emollient oil and 0.05 to 5 wt% of an oil-soluble bioactive substance; And an aqueous phase including 0.5 to 10% by weight of a moisturizing agent, 0.1 to 5% by weight of a lipophilic polyprotose-based polymer material, 0.01 to 3.0% by weight of a water-soluble physiologically active substance, and water remaining. It is done.

The alcohol part comprises 2.0 to 20.0% by weight of alcohol, 0.5 to 8.0% by weight of phospholipid, 0.03 to 2.0% by weight of ceramide, 0.03 to 2.0% by weight of cholesterol, and 0.1 to 0.5% by weight of preservative. In the alcohol, ethanol, which is generally used, is suitable, and is used for dissolving phospholipids, ceramides, cholesterol, and preservatives that are poorly soluble in water, and when used in less than 2.0% by weight, the above-mentioned phospholipids, If it is difficult to dissolve ceramides and cholesterol and, on the contrary, exceeds 20.0% by weight, there may be problems such as bad smell of alcohol and irritation to the skin. In addition, the phospholipid has a structure as shown in FIG. 2, and serves to form a lipid membrane that stably encapsulates an emollient oil and an oil-soluble physiologically active ingredient, preferably hydrogenated lecithin, unsaturated lecithin ( It can be selected and used from the natural phospholipid extracted from soybean such as unsaturated lecithin, lyso lecithin, preferably 0.5 to 8.0% by weight based on the total composition. The content of the phospholipid is an amount found experimentally by testing the amount of the aqueous phase including the physiologically active component, emulsifier, and moisturizer to be emulsified, and if the phospholipid content is less than 0.5% by weight, it is not easily emulsified, so that encapsulation is not easy. On the contrary, if it exceeds 8% by weight, excessive gelation (gel) may cause a problem that the viscosity is too high and difficult to process with a high pressure type emulsifier. In addition, the ceramide and cholesterol is used for the purpose of strengthening the interface on the nano-size oil-in-water phospholipid emulsion formed by using phospholipids, and to restore moisture and barrier function to the skin, preferably ceramide 0.03 to 2.0 weight %, Cholesterol 0.03 to 2.0% by weight can be used. However, when the content is less than the above content, the function of strengthening the interface and the effect of restoring moisture and barrier function to the skin are insignificant, and when the content is more than the above content, it is difficult to dissolve and gelation due to excessive in-orientation. There may be a problem that lowers the stability. In addition, the preservative comprises 0.1 to 0.5% by weight, and functions to improve the preservation of the cosmetic.

The emulsifier of the oil phase portion may preferably be made of 3.0 to 8.0 wt% of ester oil, 4.0 to 12.0 wt% of squalane, and 2.0 to 10.0 wt% of silicone oil.

The oil phase portion is 2.0 to 20.0% by weight of the emulsified oil, 0.05 to 5.0% by weight of the oil-soluble bioactive components. The emulsified oil is used to impart a moisturizing effect to the skin and to dissolve oil-soluble physiologically active ingredients, preferably squalane, natural oils including jojoba oil, trioctanoate, cetearyloctanoate, Esters including cetearylisononanoate, dicaprylcarbonate, capric / caprylic triglyceride, isostearylisostearate, octyldodecyl myristate, isopropyl palmitate, isopropyl myristate, octyl palmitate Those selected from the group consisting of system oils, cyclomethicone, silicone oils including dimethicone, or mixtures of two or more thereof can be used. If the content is less than the above, the moisturizing effect is insignificant, and there is a problem that it is difficult to dissolve the useful bioactive substance. If the content is more than the above, it is difficult to encapsulate stably even when using a high pressure type emulsifier, and the feeling is too oily. There may be a problem. In addition, the oil-soluble bioactive substance is tocopherol and its derivatives, coenzyme Q10, vitamin C oil-soluble derivatives, oleanolic acid, ursolic acid, diacetyl boldine, oil-soluble licorice, retinol (retinol) and derivatives thereof or those selected from the group consisting of two or more thereof can be used.

The water phase part comprises 0.5 to 10.0% by weight of a moisturizing agent, 0.1 to 5.0% by weight of polyprotose modified into lipophilic, 0.01 to 3.0% by weight of water-soluble bioactive components. The moisturizing agent is glycerin, 1,3-butylene glycol, propylene glycol, polyethylene glycol, pentylene glycol or two or more of these for the purpose of preventing freezing at low temperature and to help the penetration of stabilized water-soluble bioactive components It can select from the group which consists of mixtures, and can use. In addition, the polylactose modified with the lipophilic type prevents desorption of oil due to its excellent hydration ability and a small loop in the oil phase, and polyprotose having a long chain from a water phase to a polymer. It is an excellent steric hindrance of the large loop, which prevents particle and particle coalescing caused by the Ostwald life-saving phenomenon, and prevents separation of the formulation and desorption of useful bioactive components. An amount of 0.1 to 5.0% by weight is used. The polyprotose polymer material modified into the lipophilic type has a structure as shown in FIG. 1. When the polyprotose polymer material modified by the lipophilic type is smaller than the above content, the amount thereof is insignificant to prevent the oil particles dispersed in the water phase from being oriented in a dense structure on the oil interface including the useful bioactive substance. There may be a problem that becomes difficult, and difficult to give a steric hindrance effect. In addition, when the content is greater than the above, there is a problem in solubility, gelation may cause a viscosity increase, or agglomeration of itself may impair stability, and the use may be too sticky.

The water-soluble bioactive components include arbutin, water-soluble vitamin C derivatives including AA2G (ascorbic acid-2-glucoside), niacinamide, adenosine, N-acetylglucosamine, and N-acetylglucosamine. It may be selected from the group consisting of a variety of water-soluble extracts or mixtures of two or more of them, including the lettuce extract, the above range is an example applied in the range that can exhibit the solubility and efficacy of these physiologically active ingredients, When used, the content is not limited to the above range.

The nanosize phospholipid emulsion phase technology and manufacturing method using the lipophilic modified polyprotose-based polymer emulsifier according to the present invention comprising the above components will be described in more detail step by step.

In the preparation method of the nano-sized oil-in-water phospholipid emulsion phase cosmetics using the polyprotose-based polymer material modified into a lipophilic type according to the present invention, in preparing cosmetics by emulsification, (1) 2.0 to 20.0% by weight of alcohol, Alcohol part preparation step of preparing alcohol part by heating phospholipid 0.5 to 8.0 wt%, ceramide 0.03 to 2.0 wt%, cholesterol 0.03 to 2.0 wt%, and preservative 0.1 to 0.5 wt% at 40 to 70 ° C .; (2) an oil phase preparation step of preparing an oil phase by heating 2.0 to 20.0 wt% of an emulsified oil and 0.05 to 5 wt% of an oil-soluble bioactive substance at 70 to 85 ° C .; (3) 0.5 to 10% by weight of a moisturizing agent, 0.1 to 5% by weight of polyprotose-based polymer material modified into a lipophilic type, 0.01 to 3.0% by weight of a water-soluble physiologically active material, and the remaining amount of water to 70-85 ° C. A water phase preparation stage for preparing; (4) The oil-in-water emulsion phase of a bulky size was first emulsified by mixing the water phase portion, the alcohol portion and the oil phase portion and stirring at a rotational speed of 2,000 to 3,500 rpm in a normal vacuum emulsion tank. Forming a first emulsion; (5) a cooling step of cooling the bulky oil-in-water emulsion phase to 45-65 ° C .; (6) a lipid consisting of phospholipids, cholesterol, and ceramides by adding the bulky oil-in-water emulsion phase of the bulky size to a commercialized high-pressure emulsifier at a temperature of 5 to 65 ° C. and second emulsifying to a pressure of 500 to 1,500 bar. A second emulsion forming step of forming an oil-in-water phospholipid emulsion phase having a nano-sized stabilization of an emollient oil and an oil-soluble bioactive substance in a bilayer; And (7) a second cooling step of stabilizing the oil-in-water phospholipid emulsion phase having a nano-sized stabilization of the emollient oil and the oil-soluble bioactive substance at 25 to 30 ° C .; Characterized by including them.

First, the alcohol part preparation step of (1) is 2.0 to 20.0% by weight of alcohol, phospholipid 0.5 to 8.0% by weight, ceramide 0.03 to 2.0% by weight, cholesterol 0.03 to 2.0% by weight, preservative 0.1-0.5 weight% is prepared, it warms at 40-70 degreeC, and melt | dissolves and consists of preparing an alcohol part. Next, the oil phase preparation step of (2) comprises 2.0 to 20.0% by weight of the emulsified oil, 0.05 to 5.0% by weight of the soluble physiologically active components to prepare the oil phase to dissolve by heating to a temperature of 70 to 85 ??. Next, the water phase preparation step of (3) is 0.5 to 10.0% by weight of moisturizing agent, 0.1 to 5.0% by weight of polylactose modified into lipophilic, 0.01 to 3.0% by weight of water-soluble physiologically active ingredients and the balance by adding water And heating to a temperature of 70 to 85 ° C. to dissolve the aqueous phase to prepare.

Next, the first emulsion forming step of (4) is performed by mixing the alcohol portion, the oil phase portion and the water phase portion by mixing, stirring at a rotational speed of 2,000 to 3,500 rpm in a vacuum emulsion tank capable of temperature control and stirring. Emulsification to form a bulky oil-in-water emulsion phase. Next, the cooling step (5) consists of cooling the bulky oil-in-water emulsion phase to 45-65 ° C. to adjust it to a temperature suitable for emulsification. Subsequently, in the secondary emulsification step (6), the bulky oil-in-water emulsion phase is introduced into a commercially available high-pressure emulsifier at a temperature of 50 to 65 ° C. to be second emulsified at a pressure of 500 to 1,500 bar. It consists of forming an oil-in-water phospholipid emulsion phase with nanosized stabilizing emollient oil and oil-soluble bioactives in a lipid bilayer consisting of hypercholesterol and ceramide. In the second emulsion forming step (6), the bulky oil-in-water emulsion phase formed in the first emulsion forming step (4) is introduced into a commercially available high pressure type emulsifier at a temperature of 50 to 65 ° C to 500 to 1,500. Secondary emulsification at a pressure of bar yields an oil-in-water phospholipid emulsion phase with nanosize. In this step, the oil-in-water emulsion phase of the bulk size formed in the first emulsion forming step of (4) is introduced into a high pressure type emulsifier in the above temperature range, and treated 2 to 3 times at a pressure of 500 to 1,500 bar for the second time. Emulsification results in the oil-soluble bioactives and the emulsified oils being encapsulated within the phospholipid bilayer to form a stabilized nanosized oil-in-water phospholipid emulsion phase. The secondary emulsification is a step of making the formed, large, bulky oil-in-water phospholipid emulsion phase to nanosize, wherein if the treatment temperature is less than 50 ° C., it is lower than the phase inversion temperature of the phospholipid itself. Formation of the phospholipid emulsion phase of the size is not easy, and if it exceeds 50 ℃ there may be a problem that the structure of the phospholipid emulsion phase is modified to form a nano-sized homogeneous emulsion phase. In addition, the treatment pressure is an important factor in the preparation of the nano-sized composition. If the treatment pressure is less than 500 bar, the oil-in-water-encapsulated oil-soluble particles encapsulated with the soluble bioactive substance cannot be divided into nano-sized particles. Due to the friction caused by the force, the temperature rises rapidly, causing damage to the bioactive material and the phospholipid itself, and rather there may be a problem that the particles cannot be made into a nano size by uniting the particles. On the other hand, the high pressure type emulsifier can be understood to be known to those skilled in the art to the extent that it can be used to buy a commercially available emulsifier, such as Microfluidics (US, model name: M-110F). This high pressure type emulsifier applies a very high pressure in the pressure pump, passes it through an interaction chamber made of hollow micro-sized diamonds such as pipes to change the high pressure to high speed, and cavitation into a unique structure in the interaction chamber. It is a device that can produce nano-sized particles by using a kind of vacuum phenomenon and a crushing effect by collision, and the force for crushing the particles is much stronger than that of a conventional mixer.

Subsequently, in the secondary cooling step of (7), the oil-in-water phospholipid emulsion phase having a nano-sized stabilization of the emulsified oil and the oil-soluble bioactive substance is cooled to 25-30 ° C. to finally stabilize the oil-soluble bioactive substance and The oily components, including emulsified oils, consist in the form of a nanosized phospholipid emulsion phase in an aqueous phase and obtain a composition stabilized by lipophilic modified polyprotose.

As described above, polyprotose modified with the lipophilic type of the macromolecular substance extracted from the cauliflower root according to the nano-phosphorus emulsion phase technology and manufacturing method using the polylactose-based polymer emulsifier modified according to the present invention. It has an oil-in-water phospholipid emulsion phase with a fine size of 60 to 120 nanometers using a polymeric polymer as a stabilizer, phospholipids extracted from natural soybeans that are not chemically synthesized, and the largest problem particle size in nanosized emulsions. Nano sized phospholipid emulsion phase that prevents unity of particles due to Ostwald life phenomenon due to the relative difference of and keeps it stable and is gentle on skin and easy to transfer pharmacological substance to skin with excellent skin affinity. Has a nano-size, low viscosity and excess oil To be delivered to the skin in the stabilized stabilized stabilized.

Hereinafter, preferred embodiments and comparative examples of the present invention will be described.

The following examples are intended to illustrate the invention and should not be understood as limiting the scope of the invention.

Example  1 to 3 and Comparative example  1 to 4

To prepare a cosmetic composition on a nano-sized phospholipid emulsion using a polyprotose-based polymer material modified into a lipophilic type according to the present invention as an emulsifier in the composition as shown in Table 1, the preparation method is as follows.

In the vacuum emulsion tank capable of temperature control and agitation, each component of the water phase part is added and mixed with the contents shown in Table 1 below, and heated to a temperature of 75 ° C., and separately, a dissolution tank capable of temperature control and stirring, respectively, of the alcohol part and the oil phase part. The alcohol part was heated to a temperature of 65 ° C., and the oil phase was prepared by heating to a temperature of 75 ° C. In the vacuum emulsification tank containing the aqueous phase, while maintaining the temperature of the prepared alcohol portion and oil phase at 75 ℃ by stirring for 5 minutes at a speed of 2,500rpm using a homomixer to make the oil-in-water emulsion phase of the bulky size, It was cooled down to 55 ° C. with a paddle. A bulky oil-in-water emulsion phase was introduced into a high-pressure emulsifier at 55 ° C. and subjected to secondary emulsification by three treatments at a pressure of 1,000 bar to form an oil-in-water phospholipid emulsion phase having nano-sized, and then to 30 ° C. Cooling with paddle was used to obtain an oil-in-water phospholipid emulsion phase with nanosize.

The obtained nano-sized phospholipid emulsion image was photographed using a conventional optical microscope, and as a result, it was impossible to observe due to the fine size of 150 nanometers or less, and separately from the particle size analyzer (NANOPHOX of Sympatec, Germany) As a result of examining the distribution and the size of the particles, the average particle size was formed in the nano size of 60 to 160 nm, and it was confirmed that the particle size was well maintained at 60 to 160 nm as a result of checking stability for a long time at high temperature.

division Ingredient (% by weight) Example 1 Example 2 Example 3 Comparative Example 1 Comparative Example 2 Comparative Example 3 Comparative Example 4 Award Purified water 64.7 71.9 79.9 65.15 66.4 75.3 42.2 glycerin 5.0 5.0 5.0 5.0 5.0 5.0 5.0 Polyprotose Modified to Lipophilic 0.5 2.5 0.3 0.05 8.0 3.0 3.0 Arbutin 2.0 2.0 2.0 2.0 2.0 2.0 2.0 Alcohol ethanol 13.0 6.0 6.0 13.0 6.0 4.0 13.0 Hydrogenated Lecithin 3.0 1.5 1.0 3.0 1.5 0.2 3.0 Ceramide 0.7 0.35 0.2 0.7 0.35 0.05 0.7 cholesterol 0.7 0.35 0.2 0.7 0.35 0.05 0.7 antiseptic 0.2 0.2 0.2 0.2 0.2 0.2 0.2 The upper part Squalane 10.0 10.0 5.0 10.0 10.0 10.0 30.0 Coenzyme Q10 0.2 0.2 0.2 0.2 0.2 0.2 0.2 Properties Viscosity (cps) 200 150 100 150 10,000 100 3,000 pH 6.25 5.96 6.28 6.40 5.70 6.00 6.02 1) Glycerin, Henkel, Germany 2) Polyprotose modified with lipophilic type, Inutec SP1 (Olgati, Belgium) 3) Hydrogenated lecithin, Lecinol S-10, Nico chemical ( Nikko Chemical)), Lipoid S75-3, Lipoid S100-3) 4) Ceramide, DS-CERAMIDE (Korea, Doosan Biotech) 5) Coenzyme Q10, German Carden

The following facts could be confirmed from the analysis results of Table 1 and FIGS. 4 to 6.

In the case of Examples 1 to 3, a good result of the formation of the stabilized nano-sized phospholipid emulsion phase shown in Figures 4 to 6 was obtained, the average particle size was 85, 130, 120 as a result of the particle size was examined by the particle size analyzer It was confirmed that the nano-size was formed, and the results observed for 1.5 months at 50 ℃ was maintained similar to the above, confirming that the nano-sized phospholipid emulsion phase was stabilized by the lipophilic-modified polyprotose-based polymer material It was. In addition, by analyzing the content by high performance liquid chromatography (HPLC, Japan, Shimadzu, LC-10VP), initially, almost useful bioactive active ingredient, Coenzyme Q10, obtained 0.2% by weight, and 1.5 at 50 ° C. In the month and month, the titer was analyzed at 6 ° C for six months, and the content was maintained at 95% or more. Thus, coenzyme Q10, a useful bioactive substance that was unstable by heat or time, was entrapped on the nanosized phospholipid emulsion. It could be confirmed.

When the amount of polyprotose modified to a lipophilic type is less than 0.1% by weight as in Comparative Example 1, the amount is so small that it is difficult to prevent desorption of oil particles dispersed in the aqueous phase, and it is difficult to impart a steric hindrance effect. When checking, there was a problem in that oil particles were detached and separated, and when the amount of polyprotose modified to a lipophilic type was 5.0 wt% or more as in Comparative Example 2, there was a problem in smooth dissolution thereof. Gelling before emulsifying by treating the emulsifier, the viscosity rises, or agglomeration occurs itself, there is a problem that the feeling of the formulation obtained by treating the high-pressure emulsifier is too sticky, which is not good. When the phospholipid is less than 0.5% by weight as in Comparative Example 4, the content of the phospholipid that basically acts to stabilize the useful physiologically active component to the phospholipid bilayer is insufficient. As a result, the titer of coenzyme cue 10 was not properly maintained and its stability was also poor. When the emulsified oil used as in Comparative Example 4 is less than 20% by weight, the phospholipid emulsion phase could not be obtained in nano size even when using a high pressure type emulsifier, resulting in a phenomenon of separation due to poor stability over time. It was confirmed that there is a problem that is too oily.

Therefore, according to the present invention, by using a high-pressure emulsifier, without using a chemically synthesized emulsifier that is easy to cause irritation to sensitive skin, using natural phospholipids, especially natural phospholipids extracted from soybean, cholesterol, ceramide A nanosized phospholipid emulsion phase that is hypoallergenic to the skin, has a nanosize, and has excellent skin similarity and is easy to transfer pharmacological substances to the skin, is stabilized to a low viscosity type using polyprotose modified with a lipophilic type. Technology that stabilizes nanosized phospholipid emulsion phase by steric hindrance of lipophilic modified polyprotose, prevents coalescence of nanosized particles and prevents release of water-soluble and oil-soluble bioactive ingredients. Nano-sized oil-in-water phospholipids using protopose-based polymers as stabilizers There is an effect of providing an emulsion phase composition and a method of making the same. In particular, as described above, according to the present invention, without using a chemically synthesized emulsifier that is easy to cause irritation to sensitive skin, using a natural phospholipid extracted from soybean, it is a soft, emollient oil and poorly soluble substance, Useful bioactive ingredients such as coenzyme Q10, which are difficult to recrystallize and discolor, and potency retention, are encapsulated in nanosize on phospholipid emulsions, resulting in instability due to ostwald life under external environmental factors such as heat and air. It is possible to maintain the product stably even though it is a low viscosity type without problems, and greatly improve the titer retention of the coenzyme Q10 used by being selected as one of the useful bioactive substances.

Moreover, the nano-sized phospholipid emulsion phase is combined with ceramide and cholesterol to form excellent nanoness and smaller nano size than the skin's lipid gap, so that it can be quickly and easily penetrated into the skin, so that the water-soluble bioactive substances and It can be expected that the effects of oil-soluble bioactive substances can be obtained differently from conventional formulations.

In addition, according to the present invention, they were able to confirm that they feel soft on the skin even in the organoleptic test of adults, and have a nano-sized phospholipid emulsion phase that is easy to transfer pharmacological substances to the skin with excellent skin affinity. In addition, there is an effect of providing a cosmetic composition and a manufacturing method of the oil-in-water phospholipid emulsion of nano-size using a polyprotose-based polymer material transformed into a lipophilic type that can stably stabilize and stabilize the excess oil components to be delivered into the skin stably.

Although the present invention has been described in detail only with respect to the described embodiments, it will be apparent to those skilled in the art that various modifications and variations are possible within the technical scope of the present invention, and such modifications and modifications are within the scope of the appended claims.

Claims (6)

Alcohol part comprising 2.0 to 20.0% by weight of alcohol, 0.5 to 8.0% by weight of phospholipid, 0.03 to 2.0% by weight of ceramide, 0.03 to 2.0% by weight of cholesterol, 0.1 to 0.5% by weight of preservative; An oil phase including 2.0 to 20.0 wt% of emollient oil and 0.05 to 5 wt% of an oil-soluble bioactive substance; And an aqueous phase including 0.5 to 10% by weight of a moisturizing agent, 0.1 to 5% by weight of a lipophilic polyprotose-based polymer material, 0.01 to 3.0% by weight of a water-soluble physiologically active substance, and water remaining. Nano-size oil-in-water phospholipid emulsion phase cosmetic composition using a polyprotose-based polymer material modified into a lipophilic type. The method of claim 1, The water-soluble bioactive component of the water phase is arbutin, water-soluble vitamin C derivatives including AA2G (ascorbic acid-2-glucoside), niacinamide (niacinamide), adenosine (adenosine), N-acetylglucosamine (N-acetylglucosamine And a bioactive substance selected from the group consisting of lettuce extract. The method of claim 1, The phospholipid used in the alcohol part is a cosmetic composition, characterized in that the phospholipid selected from the group consisting of hydrogenated lecithin, Unsaturated lecithin and Lyso lecithin. The method of claim 1, The emulsified oil of the oil phase portion is natural oils including squalane, jojoba oil, trioctanoate, cetearyl octanoate, cetearyl isononanoate, dicaprylcarbonate, capric / caprylic triglyceride, iso Oils selected from the group consisting of stearyl isostearate, octyldodecyl myristate, isopropyl palmitate, isopropyl myristate, ester oils including octyl palmitate, silicone oils including cyclomethicone and dimethicone Cosmetic composition, characterized in that. The method of claim 1, The oil-soluble physiologically active component of the oil phase is tocopherol and its derivatives, coenzyme Q10, vitamin C useful derivatives, oleanolic acid, ursolic acid, diacetyl boldine, oil soluble licorice, retinol Cosmetic composition, characterized in that the bioactive component selected from the group consisting of (retinol) and its derivatives. In preparing cosmetics by emulsification, (1) Alcohol 2.0 to 20.0 wt%, phospholipid 0.5 to 8.0 wt%, ceramide 0.03 to 2.0 wt%, cholesterol 0.03 to 2.0 wt%, preservative 0.1 to 0.5 wt% Secondary preparation step; (2) an oil phase preparation step of preparing an oil phase by heating 2.0 to 20.0 wt% of an emulsified oil and 0.05 to 5 wt% of an oil-soluble bioactive substance at 70 to 85 ° C .; (3) 0.5 to 10% by weight of a moisturizing agent, 0.1 to 5% by weight of polyprotose-based polymer material modified into a lipophilic type, 0.01 to 3.0% by weight of a water-soluble physiologically active material, and the remaining amount of water to 70-85 ° C. A water phase preparation stage for preparing; (4) The agent which mixes the said water phase part, an alcohol part, and an oil phase part, and primary-emulsifies by stirring at a rotational speed of 2,000-3,500 rpm in a normal vacuum emulsion tank, and forms the oil-in-water emulsion phase of a bulky size. 1 emulsion forming step; (5) a cooling step of cooling the bulky oil-in-water emulsion phase to 45 to 65 ° C; (6) The bulky oil-in-water emulsion phase was introduced into a commercially available high pressure type emulsifier at a temperature of 5 to 65 ° C. and then emulsified at a pressure of 500 to 1,500 bar to emulsify the lipid bilayer consisting of phospholipids, cholesterol, and ceramides. A second emulsion forming step of forming an oil-in-water phospholipid emulsion phase having a nanosized stabilized oil and an oil soluble bioactive substance; And (7) a second cooling step of stabilizing the oil-in-water phospholipid emulsion phase having a nano-sized stabilization of the emollient oil and the oil-soluble bioactive substance to 25 to 30 ° C; Method for producing a nano-size oil-in-water phospholipid emulsion phase cosmetic using a lipophilic polyprotose-based polymer material characterized in that made.

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