FR2791887A1 - COSMETIC OR DERMOPHARMACEUTICAL COMPOSITIONS CONTAINING PLANT EXTRACTS FROM PINUS LAMBERTANIA AGAINST SKIN DROUGHT OF ANY ORIGIN - Google Patents

Abstract

The invention relates to extracts of Pinus Lambertania in which we have found concentrations of pinitol compatible with industrial use in cosmetic or dermopharmaceutical compositions, or for the preparation of medicaments, for all care of the skin, mucous membranes, integuments or scalp against the consequences of skin dryness whatever its origin (physiological, climatic, pollution, exposure to natural or artificial UV rays) and thus obtain anti-aging and anti-wrinkle effects, thus prolonging the flexibility and the protective function of the skin.

Description

To fully ensure its physiological barrier function against

  external aggressions, the skin, and more particularly the stratum corneum, must have a

  perfect integrity and a good state of hydration.

  Skin hygroscopy is linked to a mixture of different hygroscopic substances contained in horny cells, the Natural Moisturizing Factor or NMF, consisting of inorganic ions, organic acids, urea and amino acids. The NMF seems to be protected by a semi-permeable lipid membrane which allows it to attract water by osmosis but which prevents it from leaving the cells. In addition, sebum constitutes with sweat a water-in-oil emulsion which exerts a regulating role in the evaporation of insensible perspiration, which

  maintains the hydration of the horny cells at its best level.

  The imbalance of these factors results in skin dehydration or skin dryness. The latter is initially accompanied by a feeling of discomfort with tightness of the skin, then by roughness and

  skin peeling with most often, signs of inflammation.

  The causes of skin dryness are multiple, for example: * more or less excessive exposure to ultraviolet radiation, * atmospheric pollution, 2 0. hot, cold, wind, * untimely use of detergents, prolonged baths, * overheated housing, * various skin reactions to synthetic fibers, * consumption of tobacco and / or alcohol, or pathophysiology such as aging, diabetes, ichthyosis, hormonal disturbances, abuse of certain drugs (laxatives , diuretics ...);

  this list is by no means exhaustive.

  Skin dryness not only represents discomfort for the person affected, but it also causes the skin to lose its mechanical barrier properties, between the internal environment of the organism and the outside world. Indeed, the skin then loses its elasticity, becomes dry, rough, brittle, which promotes excessive flaking. The loss of this integrity promotes the appearance of cracks and crevices, which increases the insensitive loss of water and facilitates the installation of local infections, the severity of which depends on two factors which add up: the location and size of the cutaneous surface as well as the virulence of the contaminating micro-organism (the above data correspond to a synthesis of various articles including Laurence FRITEAU (1998) Cosmetology

  19: 11-13; Catherine DESMOULIN (1999) Cosmetology 21: 20-21).

  The cosmetic industry is therefore fully in its role when it is constantly looking for new concepts and products capable of preventing or reducing

  skin dryness of all origins.

  The object of this patent application lies in the discovery, and in the demonstration, that a new solution can be proposed in the cases of

  dry skin, and this, whatever the causes.

  Indeed, we have discovered that when applied topically at appropriate concentrations, a polyol, the pinitol (3-Omethyl-inositol) precursor

  of inositol, was able to counter dryness of the skin.

  In addition, we discovered that it was interesting to extract this pinitol from Pinus Lambertiana because this tree contains large quantities of easily extractable pinitol, the cost price of the extracted pinitol is compatible with its industrial use. To date, pinitol was known as an inhibitor of phospholipase A2 (for example: Cu'ellar MJ et al. (1997) J Nat. Prod. 60: 1158-1160), as an anti-diabetic in mice (for example: Narayanan CR et al. (1987) Curr. Sci. 56: 139-144) or as a regulator of sodium in the plant world (for example:

  Nelson DE et al. (1999) Plant Physiol. 119: 165-172).

  Pinitol is extracted from the root, resin, pine nuts, bark or

Pinus Lambertiana needles.

  Pinus Lambertiana is the largest member of the coniferous family since some reach a height of 65 to 70 meters, which are found at altitudes of 1350 to 2700 meters, mainly in southern California, Oregon or

  New Zealand. Its top is flattened, its bark is smooth and brown in color.

  red, its bundles have 5 short needles and its pine nuts are long and soft. For roots, pine nuts and bark, after grinding using standard equipment (knife or hammer mill), the particle size of the material obtained must be

between 0.2 and 5.0 mm.

  The extraction can then be carried out by maceration, for 4 to 10 days, at the

  temperature of 15-20 C, 25 grams of ground product in 100 ml of purified water.

  Regarding the resin and needles of Pinus Lambertiana, the extraction can be done directly without grinding, which does not exclude this step if you wish

  however, do it for the needles.

  After filtration of the extract obtained, about 75 ml of a light brown to yellow-orange liquid is collected. The extraction solvents mentioned above are not limiting and can be chosen from water, propylene glycol, butylene glycol, glycerin, polyethylene glycol, methyl or ethyl ethers of diglycols, cyclic polyols, ethoxylated or propoxylated diglycols, alcohols (methanol, ethanol, propanol, butanol),

or any mixture of these solvents.

  Furthermore, it is possible to produce these extracts by other methods such as, for example, simple decoction, leaching, reflux extraction, extraction by means of ultrasound or microwaves or finally by means of techniques against

  current, without this list being exhaustive.

  The extracts obtained with any protocol set out above, or by any other means provided that they contain pinitol at concentrations identical to those described in this patent application, can be used in preparations like those given below by way of example, without this being limiting. Analysis of these extracts, by whatever appropriate methodology, demonstrates on the one hand, the presence of pinitol at concentrations which vary from 0.5% to 5.0% depending on the part of the tree used, l origin of the tree and the season in which the plant material is obtained and, on the other hand, that pinitol is the major constituent of the extract obtained. Example 1: Brij 721 face care cream 2.4 VolopoR S72 2.6 Prostéayl- 15 8.0 Beeswax 0.5 Abil ZP2434 3.0 Propylene glycol 3.0 Carbopol 941 0.25 Triethanolamine 0.25 Pinus Lambertania extract 3.0 Water & preservatives QSP 1 OOg Example 2: Anti-wrinkle cream Polysorbate 60 3.8 Sorbitan stearate 2.0 Cetyl alcohol 1.5 Vaseline oil 13 Pinus Lambertania extract 5.0 Water & preservatives QSP 1 00g Example 3: Deodorant body milk Polysorbate 60 2.5 Oleic acid 0.9 Lanolin oil 2.5 Carbopol 940 0.3 Beeswax 2.0 Triethanolamine 0.1 Glycerin 5.0 Pinus Lambertania extract 2.5 Water & preservatives QSP 00lg The effects of Pinus Lambertania extracts are demonstrated in the following examples. Example 4: Hydrating effect in vivo This example demonstrates the hydrating skin effect obtained, in vivo, on the legs of 15 adult female volunteers. The hydrating power of the Pinus Lambertania extract previously described, incorporated at the concentrations of 0.3, 1.0 and 3.0% in the facial care cream described in the NI example, was compared with that of a placebo (i.e. the same cream but without Pinus Lambertania extract) and

lack of treatment.

  This test can be briefly described as follows. The skin's hydration level is measured by the skin's electrical capacity using a corneometer (Courage

  and Khazaka, model CM 820), a technique conventionally used in cosmetology.

  Indeed, the electrical properties of the surface layers of the skin are

  strongly linked to its water content.

  Five independent sites are identified using adhesives and pen markings and then, after a period of 20 minutes of rest in a seated position, the same

  measurements as those made at the TO are carried out in triplicate, on each site.

  Each cream studied (placebo and Pinus Lambertania extract at different concentrations) is then applied until complete penetration, on a site

  independent, 20 jil per site.

  The fifth site previously identified does not receive any product.

The volunteers remain at rest.

  Three measurements per site are carried out every hour, and this, for 6 hours.

  The temperature and humidity of the room where the test is carried out are maintained

constants throughout the test.

  Two different tests were carried out: the first used an extract made from roots (table 4-1) when the second tested a needle extract (table 4-2);

  the concentrations of pinitol in the two extracts were comparable.

  The two tables show the percentage changes in TO of the

  measurements carried out for 6 hours.

  The values indicated correspond to the averages calculated from the 3 measurements carried out.

Table 4-1

  0O T-1H T + 2H T + 3H T + 4H T-5H T + 6 Nothing 0 - 0.2 - 1.0 - 0.5 0.0 + 0.6 + 0.9 Placebo 0 + 0.5 0.2 + 1.4 + 1.0 + 2.2 + 0.9 Extract 0.3% 0 +10.3 +11.2 +15.3 +12.7 +13.2 +11.0 Extract 1.0% 0 +15.6 +19.2 +25.5 +27.8 +25, 1 +20.2 Extract 3.0% 0 +25.1 +28.3 +29.4 +28.2 +27.9 + 26.4 Table 4-2

O T.1H T + 2H T * 3H T + 4H T + 5H T + 6

  Nothing 0 - 0.5 - 0.5 + 0.1 + 0.7 + 0.4 + 0.7 Placebo 0 - 0.4 0.0 + 0.8 + 1.2 + 0.9 + 1, 1 Extract 0.3% 0 +12.0 +13.9 +14.1 +19.8 +19.7 +17.4 Extract 1.0% 0 +17.8 +21.2 +26.8 +30.2 + 29.6 +24.8 Extract 3.0% 0 + 26.2 + 26.1 + 32.7 + 35.8 +33.1 + 28.7 The two creams containing extracts of Pinus Lambertania clearly demonstrate strong power moisturizing since not only, depending on the type of extract tested, skin hydration is increased from 30% to 35% compared to the start of the test but, moreover, it is sustained since the effect is particularly evident during

  at least the six hours of the test.

  In addition, for the two extracts, the measured moisturizing effect is clearly concentration dependent. This, added to the fact that the pinitol concentrations of the two extracts were very close, confirm that the effect observed is

  2 5 actually due to the pinitol extracted.

  A final argument which confirms the role of pinitol in extracts of Pinus Lambertania in the observed effect lies in the fact that, under the same conditions, the placebo cream (without extract of Pinus Lambertania), has no hydrating effect, just as it can be seen when no product is

applied.

  Example N 5 Anti-wrinkle effect in vivo This example reports the anti-wrinkle effect obtained, in vivo, on a panel made up of 13

  adult female volunteers.

  The anti-wrinkle power of the previously described extract, incorporated at 5% in the anti-wrinkle cream of Example 2, containing an extract obtained from Pinus Lambertania resin, is compared to that of a placebo (the same cream but without the extract of Pinus Lambertania). The creams are applied to precisely identified sites, located on the corner of the right or left eye, according to a

  randomized, twice daily, for 28 days.

  The parameter taken into account is the skin relief, at the level of the eye contour (wrinkles called crow's feet). The quantifications of the various relief variables are carried out by computer-video analysis of silicone impressions taken on the surface.

  of the skin according to the protocols described by Corcuff et al. (1985, Int. J Cosm.

  Sci. 7: 117-126) and Corcuff et al. (1995, in Handbook of non-invasive methods and the skin, Serup & Jemec eds., CRC Press: 89-96). The table below indicates the difference, in percentage, of the average values obtained between T +28 days and TO for the average depth of the main wrinkle (column A) or for all the folds (column B), for the density main folds (column C) as well as for

  roughness measurement (column D).

  ABC b Placebo 0.4 - 0.3 + 0.7 + 1.1 Extract - 15.3 - 19.2 - 25.6 - 15.2 The cream containing pinitol extracted from Pinus Lambertania clearly demonstrates a powerful anti-wrinkle effect since there is a significant difference between the start and the end of the in vivo study and this, on all four parameters

  conventionally used in this indication.

  Due to the activities demonstrated above, such preparations can be used for all skin care and especially in cases of dry skin of any origin, thus producing anti-aging and anti-wrinkle effects, this

  which prolong the suppleness and the protective function of the skin.

  The concentration of pinitol in Pinus Lambertania extracts (known as

  Extracts in the rest of this description) can vary between 0.5% to 5.0% depending on the

  part of the tree used, the geographical origin of the tree and the season in which the material was obtained. The concentration of the Extracts can vary between 0.01% and 50% (w / w), preferably between 0.1% and 10% (w / w) in the finished cosmetic or dermopharmaceutical composition. The Extracts can be used in any dosage form used in cosmetics or dermopharmacy: O / W and W / O emulsions, milks, lotions, gelling and viscous polymers, surfactants and emulsifiers, ointments, hair lotions, shampoos,

  soaps, sticks and pencils, sprays, body oils, without this list being exhaustive.

  It is possible to incorporate the Extracts into cosmetic vectors such as liposomes, chylomicrons, macro-, micro- and nanoparticles as well as macro-, micro- and nanocapsules, to absorb them on organic polymers

  powdery, talcs, bentonites and other mineral supports.

  The Extracts can be combined in cosmetic compositions with any other ingredient usually used in cosmetics: extraction and / or synthetic lipids, gelling and viscosifying polymers, surfactants and emulsifiers, hydro- or liposoluble active principles, extracts from other plants, tissue extracts, marine extracts. The Extracts are used in cosmetic or dermnopharmaceutical compositions for all care of the skin, mucous membranes, dander or scalp against the consequences of cutaneous dryness whatever its origin (physiological, climatic, pollution, exposure natural or artificial UV rays) and thus obtain anti-aging and anti-wrinkle effects,

  which prolongs the suppleness and the protective function of the skin.

  The Extracts are used as such, or in cosmetic or dermopharmaceutical compositions, for the preparation of a medicament for all care of the skin, mucous membranes, integuments or scalp against the consequences of cutaneous dryness whatever either the origin (physiological, climatic, pollution, exposure to natural or artificial UV rays) and thus obtain anti-aging and anti-wrinkle effects, which prolongs flexibility and function

protective of the skin.

  The Extracts can be used either in liquid form or in dry form obtained by conventional techniques of precipitation, drying, evaporation,

atomization or freeze-drying.

Claims (13)

  1. Use of extracts of Pinus Lambertania in cosmetic compositions or dermopharmaceuticals.   2. Cosmetic or dermopharmaceutical compositions according to claim 1 characterized in that the extracts contain between 0.5% and 5.0% (w / w) of pinitol. 3. Cosmetic or dermopharmaceutical compositions according to the   Claims 1 to 2, characterized in that the extraction solvents used   for obtaining the extract are chosen from water, propylene glycol, butylene glycol, glycerin, polyethylene glycol, methyl or ethyl ethers of diglycols, cyclic polyols, ethoxylated or propoxylated diglycols, alcohols (methanol, ethanol, propanol, butanol), or any mixture of these solvents.   4. Cosmetic or dermopharmaceutical compositions according to one of the   Claims 1 to 3, characterized in that the extraction can be replaced by   maceration techniques or by other methods such as, for example, simple decoction, leaching, extraction under reflux, extraction by means   ultrasound or microwave or finally countercurrent techniques.   5. Cosmetic or dermopharmaceutical compositions according to one of the   Claims 1 to 4, characterized in that the extract is obtained from   root, resin, pine, bark or needles.   6. Cosmetic or dermopharmaceutical compositions according to one of the   Claims 1 to 5, characterized in that the extract is used either in the form   liquid, either in dry form obtained by conventional techniques of   precipitation, drying, evaporation, atomization or lyophilization.   7. Cosmetic or dermopharmaceutical compositions according to one of the   Claims 1 to 6, characterized in that the concentration of the extract can   vary between 0.01% and 50% (w / w), preferably between 0.1% and 10% (w / w)   in the finished cosmetic or dermopharmaceutical composition.   8. Cosmetic or dermopharmaceutical compositions according to one of the   Claims 1 to 7, characterized in that they are in any form   dosage form used in cosmetics or dermopharmacy: O / W and W / O emulsions, milks, lotions, gelling and viscosifying polymers, surfactants and emulsifiers, ointments, hair lotions, shampoos, soaps, sticks and pencils, sprays, body oils.   9. Cosmetic or dermopharmaceutical compositions according to one of the   Claims 1 to 8, characterized in that the extract is incorporated in   cosmetic vectors such as liposomes, chylomicrons, macro-, micro- and nanoparticles as well as macro-, micro- and nanocapsules, to absorb them on powdery organic polymers, talcs, bentonites and others mineral supports.   10. Cosmetic or dermopharmaceutical compositions according to one of the   Claims 1 to 9, characterized in that the extract is used with any other   ingredient usually used in cosmetics: extraction and / or synthetic lipids, gelling and viscosifying polymers, surfactants and emulsifiers, water- or liposoluble active ingredients, extracts of other plants, extracts tissues, marine extracts.   11. Cosmetic or dermopharmaceutical compositions according to one of claims 1 to 10 for all care of the skin, mucous membranes, integuments or scalp against the consequences of skin dryness whatever its origin (physiological, climate, pollution, exposure   natural or artificial UV rays) and thus obtain anti-   aging and anti-wrinkle, which prolongs flexibility and protective function skin.   12. Cosmetic or dermopharmaceutical compositions according to one of claims I to 10 for the preparation of a medicament for all care of the skin, mucous membranes, integuments or scalp against the consequences of cutaneous dryness whatever either the origin (physiological, climatic, pollution, exposure to natural or artificial solar UV rays) and thus obtain anti-aging and anti-wrinkle effects, which   prolongs the suppleness and the protective function of the skin.   13. Use of the extract according to claims 1 and 7 for the preparation of a   medication for all skin, mucous membrane, skin appendage or scalp care against the consequences of skin dryness whatever its origin (physiological, climatic, pollution, exposure to natural or artificial UV rays) and obtain thus anti-aging effects and   anti-wrinkle, which prolongs the suppleness and the protective function of the skin.