Personal care composition

Abstract

Disclosed is a personal care composition comprising a carboxymethyl cysteine compound and a retinoid, wherein the weight ratio of carboxymethyl cysteine compound to retinoid is from 1: 1.6 to 25: 1.

Description

Technical Field

[0001] The present invention relates to a personal care composition comprising a carboxymethylcysteine compound and a retinoid, wherein the weight ratio of the carboxymethylcysteine compound to the retinoid is from 1:1.6 to 25:1. Unexpectedly, it has been found that such a composition significantly enhances the expression of the αI chain of type I collagen (COL1A1). Background Art

[0002] The skin is the main barrier of the human body. It protects the body organs from external stimuli. It undergoes intrinsic aging and extrinsic aging. Skin aging is a complex process and, compared to other organs, the changes in human skin caused by aging have different characteristics. The characteristics of intrinsic or chronological skin aging include dryness, visible fine lines and wrinkles, uneven skin pigmentation, loss of elasticity, and skin sagging. Extrinsic factors, including exposure to sunlight, pollutants, and cigarette smoke, can accelerate the skin aging process, especially on the face.

[0003] It is known that collagen, the main matrix of skin proteins, imparts tensile strength to the skin. It has been shown that collagen significantly decreases with age and UV exposure. Degradation or disruption of the collagen structure reduces the tensile strength of the skin and thus results in wrinkles and sagging. Collagen breakdown is considered to be the basis for the characteristic changes in the appearance of aging skin.

[0004] One of the most effective ways to provide anti-aging effects is to promote collagen production. Upregulation of the expression of collagen synthesis genes generally leads to an increase in collagen production.

[0005] Therefore, the present inventors have recognized the need to develop a solution that enhances the expression of collagen synthesis genes, such as the αI chain of type I collagen (COL1A1). Surprisingly, it has been found that by combining carboxymethylcysteine and retinoid in a specific weight ratio, the expression of COL1A1 is significantly upregulated. Summary of the Invention

[0006] In a first aspect, the present invention relates to a personal care composition comprising a carboxymethylcysteine compound and a retinoid, wherein the weight ratio of the carboxymethylcysteine compound to the retinoid is from 1:1.6 to 25:1.

[0007] In a second aspect, the present invention relates to a method of providing skin benefits selected from enhancing collagen production in the skin, improving skin elasticity, reducing the appearance of wrinkles, reducing sagging, anti-aging, and upregulating the expression of collagen synthesis genes, the method comprising the step of topically applying the composition of the present invention to the skin.

[0008] In a third aspect, the present invention relates to the use of the compositions of the present invention for providing skin benefits selected from the group consisting of enhancing collagen production in the skin, improving skin elasticity, reducing the appearance of wrinkles, reducing sagging, anti-aging, and upregulating the expression of collagen synthesis genes.

[0009] All other aspects of the present invention will become more readily apparent after considering the detailed description and the following examples. Detailed Description

[0010] Except where otherwise indicated in the examples or otherwise explicitly stated, all numbers expressing amounts of materials or reaction conditions, physical properties of materials, and / or use in this specification are optionally understood to be modified by the word "about".

[0011] Unless otherwise specified, all amounts are by weight of the composition.

[0012] It should be noted that when specifying any range of values, any particular upper value can be associated with any particular lower value.

[0013] For the avoidance of doubt, the word "comprising" is intended to mean "including" but not necessarily "consisting of" or "composed of". In other words, the listed steps or options need not be exhaustive.

[0014] The disclosure of the present invention as found herein is considered to cover all embodiments found to be mutually multiply dependent in the claims, regardless of the fact that the claims may be found to have no multiple dependencies or redundancies.

[0015] Where features are disclosed in relation to a particular aspect of the present invention (such as the compositions of the present invention), with the necessary modifications, such disclosure is also considered applicable to any other aspect of the present invention (such as the methods of the present invention).

[0016] A carboxymethylcysteine compound refers to a compound selected from the group consisting of carboxymethylcysteine, salts of carboxymethylcysteine, esters of carboxymethylcysteine, amides of carboxymethylcysteine, or mixtures thereof. Preferably, the carboxymethylcysteine compound includes carboxymethylcysteine, esters of carboxymethylcysteine, and / or salts of carboxymethylcysteine. More preferably, the carboxymethylcysteine compound includes carboxymethylcysteine and / or salts of carboxymethylcysteine. Even more preferably, the carboxymethylcysteine compound includes salts of carboxymethylcysteine. Still even more preferably, the carboxymethylcysteine compound includes lysine carboxymethylcysteine salt, and most preferably, the carboxymethylcysteine compound is lysine carboxymethylcysteine salt.

[0017] Preferably, the carboxymethylcysteine compound is present in an amount of at least 0.00001%, more preferably at least 0.0001%, even more preferably at least 0.001%, still even more preferably at least 0.01%, and most preferably at least 0.1% based on the weight of the composition. Preferably, the carboxymethylcysteine compound is present in an amount of not more than 10%, more preferably not more than 5%, even more preferably not more than 3%, still even more preferably not more than 1%, and most preferably not more than 0.5% based on the weight of the composition.

[0018] Preferably, the lysine carboxymethylcysteine salt is present in an amount of not more than 10%, more preferably not more than 5%, even more preferably not more than 3%, still even more preferably not more than 1%, and most preferably not more than 0.5% based on the weight of the composition. Preferably, the lysine carboxymethylcysteine salt is present in an amount of at least 0.00001%, more preferably at least 0.0001%, even more preferably at least 0.001%, still even more preferably at least 0.01%, and most preferably at least 0.1% based on the weight of the composition.

[0019] The composition of the present invention comprises a retinoid. Typically, the retinoid is selected from retinyl esters, retinol, retinal, retinoic acid, or a mixture thereof. More preferably, the retinoid comprises retinol, retinyl esters, or a mixture thereof, and even more preferably the retinoid is selected from retinol, retinyl esters, or a mixture thereof.

[0020] The term "retinol" includes the following isomers of retinol: all-trans retinol, 13-cis-retinol, 11-cis-retinol, 9-cis-retinol, 3,4-dehydro-retinol, 3,4-dehydro-13-cis-retinol, 3,4-dehydro-11-cis-retinol, 3,4-dehydro-9-cis-retinol. Preferred isomers are all-trans retinol, 13-cis-retinol, 3,4-dehydro-retinol, 9-cis-retinol. The most preferred retinol is all-trans retinol because of its wide commercial availability.

[0021] Retinyl esters are esters of retinol. The term "retinol" is defined as above. The retinyl esters suitable for the present invention are preferably C1-C 30 esters of retinol, more preferably C2-C 20 esters of retinol, and most preferably C2, C3, and C 16Esters. Examples of retinyl esters include, but are not limited to: retinyl palmitate, retinyl formate, retinyl acetate, retinyl propionate, retinyl butyrate, retinyl valerate, retinyl isovalerate, retinyl hexanoate, retinyl heptanoate, retinyl octanoate, retinyl nonanoate, retinyl decanoate, retinyl undecanoate, retinyl laurate, retinyl tridecanoate, retinyl myristate, retinyl pentadecanoate, retinyl heptadecanoate, retinyl stearate, retinyl isostearate, retinyl nonadecanoate, retinyl arachidonate, retinyl behenate, retinyl linoleate, retinyl oleate. The retinyl esters used in the present invention are preferably selected from retinyl palmitate, retinyl acetate, retinyl linoleate, retinyl oleate, retinyl propionate or mixtures thereof. More preferably, the retinyl ester is selected from retinyl palmitate, retinyl acetate, retinyl propionate or mixtures thereof. Even more preferably, the retinyl ester is selected from retinyl palmitate, retinyl propionate or mixtures thereof.

[0022] Particularly preferred retinoids are selected from all-trans retinol, retinyl palmitate, retinyl acetate, retinyl propionate or mixtures thereof. Most preferably, the retinoid is selected from retinyl palmitate, retinyl propionate or mixtures thereof. Even more preferably, the retinoid is retinyl propionate.

[0023] Based on the weight of the total amount of the composition, the amount of retinoid is preferably from 0.00001 to 10%, more preferably from 0.0001 to 8%, even more preferably from 0.001 to 5%, still even more preferably from 0.02 to 2%, and most preferably from 0.1 to 0.6%. Based on the weight of the total amount of the composition, the total amount of retinol and retinyl esters in the composition is preferably from 0.00001 to 10%, more preferably from 0.0001 to 8%, even more preferably from 0.001 to 5%, still even more preferably from 0.02 to 2%, and most preferably from 0.1 to 0.6%. Based on the weight of the total amount of the composition, the total amount of retinyl palmitate and retinyl propionate in the composition is preferably from 0.00001 to 10%, more preferably from 0.0001 to 8%, even more preferably from 0.001 to 5%, still even more preferably from 0.02 to 2%, and most preferably from 0.1 to 0.6%. Based on the weight of the total amount of the composition, the total amount of retinyl propionate in the composition is preferably from 0.00001 to 10%, more preferably from 0.0001 to 8%, even more preferably from 0.001 to 5%, still even more preferably from 0.02 to 2%, and most preferably from 0.1 to 0.6%.

[0024] Preferably, the weight ratio of the carboxymethylcysteine compound to the retinoid is from 1:1.6 to 20:1, more preferably from 1:1.6 to 10:1, even more preferably, still even more preferably from 1:1.5 to 3:1, and most preferably from 1:1.3 to 2:1. Preferably, the weight ratio of the lysine carboxymethylcysteine salt to the retinoid is from 1:1.6 to 20:1, more preferably from 1:1.6 to 10:1, even more preferably, still even more preferably from 1:1.5 to 3:1, and most preferably from 1:1.3 to 2:1. Preferably, the weight ratio of the carboxymethylcysteine compound to the total amount of retinol and retinyl esters in the composition is from 1:1.6 to 20:1, more preferably from 1:1.6 to 10:1, even more preferably, still even more preferably from 1:1.5 to 3:1, and most preferably from 1:1.3 to 2:1. Preferably, the weight ratio of the lysine carboxymethylcysteine salt to the total amount of retinyl propionate and retinyl palmitate in the composition is from 1:1.6 to 20:1, more preferably from 1:1.6 to 10:1, even more preferably, still even more preferably from 1:1.5 to 3:1, and most preferably from 1:1.3 to 2:1. Preferably, the weight ratio of the lysine carboxymethylcysteine salt to retinyl propionate in the composition is from 1:1.6 to 20:1, more preferably from 1:1.6 to 10:1, even more preferably, still even more preferably from 1:1.5 to 3:1, and most preferably from 1:1.3 to 2:1.

[0025] The present invention also provides a personal care composition comprising a carboxymethylcysteine compound and a retinoid, wherein the molar ratio of the carboxymethylcysteine compound to the retinoid is from 1:1.6 to 25:1. Preferably, the molar ratio of the carboxymethylcysteine compound to the retinoid is from 1:1.6 to 20:1, more preferably from 1:1.6 to 10:1, even more preferably, still even more preferably from 1:1.5 to 3:1, and most preferably from 1:1.3 to 2:1. Preferably, the molar ratio of lysine carboxymethylcysteine salt to the retinoid is from 1:1.6 to 20:1, more preferably from 1:1.6 to 10:1, even more preferably, still even more preferably from 1:1.5 to 3:1, and most preferably from 1:1.3 to 2:1. Preferably, the molar ratio of the carboxymethylcysteine compound to the total amount of retinol and retinyl esters in the composition is from 1:1.6 to 20:1, more preferably from 1:1.6 to 10:1, even more preferably, still even more preferably from 1:1.5 to 3:1, and most preferably from 1:1.3 to 2:1. Preferably, the molar ratio of lysine carboxymethylcysteine salt to the total amount of retinyl propionate and retinyl palmitate in the composition is from 1:1.6 to 20:1, more preferably from 1:1.6 to 10:1, even more preferably, still even more preferably from 1:1.5 to 3:1, and most preferably from 1:1.3 to 2:1. Preferably, the molar ratio of lysine carboxymethylcysteine salt to retinyl propionate in the composition is from 1:1.6 to 20:1, more preferably from 1:1.6 to 10:1, even more preferably, still even more preferably from 1:1.5 to 3:1, and most preferably from 1:1.3 to 2:1.

[0026] The composition may optionally comprise a brightening pigment. Brightening pigments are typically particles of high refractive index materials. For example, the brightening pigment may have a refractive index greater than 1.3, more preferably greater than 1.8 and most preferably from 2.0 to 2.7. Examples of such brightening pigments are those comprising bismuth oxychloride, boron nitride, barium sulfate, mica, silica, titanium dioxide, zirconium oxide, alumina, zinc oxide or combinations thereof. More preferred brightening pigments are particles comprising titanium dioxide, zinc oxide, zirconium oxide, mica, iron oxide or combinations thereof. Even more preferred brightening pigments are particles comprising zinc oxide, zirconium oxide, titanium dioxide or combinations thereof, as these materials have particularly high refractive indices. Still even more preferably, the brightening pigment is selected from titanium dioxide, zinc oxide or mixtures thereof, and the most preferred brightening pigment is titanium dioxide. The average diameter of the brightening pigment is typically from 15 nm to 1 micron, more preferably from 35 nm to 800 nm, even more preferably from 50 nm to 500 nm, still even more preferably from 100 nm to 300 nm. The amount of the brightening pigment, based on the weight of the composition, may be from 0.1 to 15%, preferably from 0.5 to 5%.

[0027] Preferably, the composition comprises a glutamate source selected from glutamine, glutamine esters, glutamic acid, pyroglutamic acid, salts thereof, and mixtures thereof. More preferably, the composition comprises pyroglutamic acid and / or a salt of pyroglutamic acid. Even more preferably, the composition comprises the sodium salt of pyroglutamic acid. Preferably, the glutamate source is present in an amount of from 0.0001 to 10%, more preferably from 0.001 to 6%, even more preferably from 0.01 to 3% by weight of the composition.

[0028] Preferably, the composition comprises a polyol. The polyol may be selected from glycerol, propylene glycol, dipropylene glycol, polypropylene glycol, polyethylene glycol, sorbitol, hydroxypropyl sorbitol, hexylene glycol, 1,3 - butanediol, isopentylene glycol, ethoxylated glycerol, propoxylated glycerol, or mixtures thereof. The most preferred polyol is glycerol, also known as glycerin. The amount of the polyol may be from 0.1 to 20%, preferably from 0.5 to 15%, more preferably from 2 to 10% by weight of the composition.

[0029] Preferably, the composition comprises an emollient material. Suitable emollient materials include silicones, hydrocarbons, triglycerides, or mixtures thereof. These silicones can be organic, silicone - containing or fluorine - containing, volatile or non - volatile, polar or non - polar. Hydrocarbons may include mineral oil, petrolatum, and polyalpha - olefins. Examples of preferred volatile hydrocarbons include polydecane such as isododecane and isodecane (e.g., Permethyl - 99A, which is purchased from Presperse Inc.) and C7 - C8 to C12 - C15 isoparaffins (e.g., the Isopar series, purchased from Exxon Chemicals). Exemplary but non - limiting triglycerides are sunflower oil, cottonseed oil, rapeseed oil, soybean oil, castor oil, borage oil, olive oil, shea butter, jojoba oil, and mixtures thereof. Glycerol monoesters and glycerol diesters may also be useful. Particularly preferred are glycerol monostearate and glycerol distearate.

[0030] Preferably, the composition comprises a humectant. Particularly preferred humectants include: petrolatum, aquaporin - modulating active substances, oat kernel flour, substituted ureas such as hydroxyethyl urea, hyaluronic acid and / or its precursor N - acetylglucosamine, hyaluronic acid and / or its precursor N - acetylglucosamine or mixtures thereof.

[0031] Some compositions may contain thickeners. These may be selected from celluloses, natural gums, and acrylic polymers, but are not limited to this type of thickener. Among the celluloses are sodium carboxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl methyl cellulose, and combinations thereof. Suitable gums include xanthan gum, pectin, karaya gum, agar, alginic acid gum, and combinations thereof. Among the acrylic thickeners are homopolymers and copolymers of acrylic acid and methacrylic acid, including carbomers, such as Carbopol 1382, Carbopol 982, Ultrez, Aqua SF-1, and Aqua SF-2 available from Lubrizol Corporation. The amount of the thickener may be from 0.01 to 3% by weight of the active polymer (excluding solvents or water) in the composition.

[0032] In addition, the compositions of the present invention may further comprise 0.5 to 10% by weight of a chelating agent, such as tetrasodium ethylenediaminetetraacetate (EDTA), EHDP, or a mixture; opacifying agents and pearlescent agents, such as ethylene glycol distearate, titanium dioxide, or Lytron 621 (styrene / acrylic ester copolymer); all of which may be used to enhance the appearance or performance of the product.

[0033] The composition may contain water in an amount of 10 to 96%, more preferably 25 to 92%, even more preferably 42 to 88%, and most preferably 55 to 82% by weight of the composition.

[0034] Preferably, when measured at a relatively high shear rate of about 20 s -1 at 20 °C, the composition has a viscosity of at least 10 mPa·s, more preferably 30 to 10000 mPa·s, even more preferably 50 to 5000 mPa·s, and most preferably 100 to 2000 mPa·s.

[0035] Preferably, the composition is an emulsion, more preferably an oil-in-water emulsion. Preferably, the composition is a fluid liquid at 25 °C and atmospheric pressure.

[0036] Preferably, the personal care composition is a skin care composition. A skin care composition refers to a composition suitable for topical application to human skin, including leave-on and rinse-off products, but preferably leave-on compositions. As used herein, the term "leave-on" in relation to the composition means a composition applied or rubbed onto the skin and left thereon. The term "rinse-off" in relation to the compositions herein means a skin cleanser applied or rubbed onto the skin and substantially rinsed off immediately after application. The term "skin" as used herein includes the skin on the face, neck, chest, abdomen, back, arms, underarms, hands, and legs. Preferably, "skin" means the skin including the face and underarms, and more preferably, the skin means the skin on the face excluding the lips and eyelids. The composition is particularly preferably a moisturizer rather than a cosmetic product.

[0037] Preferably, the composition is a topical composition. Preferably, the composition can be in the form of a cream, lotion, ointment, solution, suspension, emulsion, paste, gel, powder, foundation, liquid foundation, wax foundation, or spray. More preferably, the composition can be formulated in the form of a cream, lotion, ointment, emulsion, gel, or spray.

[0038] Preferably, the use is non-therapeutic. Preferably, the method is non-therapeutic. The term non-therapeutic generally means for cosmetic purposes rather than curative or therapeutic purposes.

[0039] Preferably, the composition is capable of upregulating the expression of the alpha-1 chain of type I collagen (COL1A1) gene by at least 1.45-fold change, more preferably 1.55 to 5 and most preferably 1.75 to 3.5 and most preferably 1.75 to 2.5-fold change, typically compared to a personal care composition that contains neither a carboxymethylcysteine compound nor a retinoid.

[0040] The following examples are provided to facilitate understanding of the present invention. These examples are not intended to limit the scope of the claims.

[0041] Examples

[0042] Materials

[0043]

[0044] Example 1

[0045] This example demonstrates the synergistic anti-aging effect by combining lysine carboxymethylcysteine salt and retinyl propionate in a specific ratio.

[0046] Normal human dermal fibroblasts (NHDF) (Biocell, Xi'an, China, lot number: Fb20081902) were incubated in medium with or without the active substance for 48 hours. After incubation, total RNA of each NHDF was extracted using RNAex Pro reagent (Accurate Biotechnology, product number: AG21102) according to the manufacturer's protocol.

[0047] The extracted RNA was quantified using a Nanodrop spectrometer (Thermo Fisher Scientific, Waltham, MA, US) and reverse transcribed using the Evo M-MLV RT Premix for qPCR (Accurate Biotechnology, product number: AG11706) according to the manufacturer's protocol to generate template cDNA. Using the Green PremixPro Taq HS qPCR kit (Accurate Biotechnology, AG11701), the gene expression of the COL1A1 gene was analyzed by polymerase chain reaction (PCR). The actin beta (ACTB) gene was selected as the housekeeping gene, and all data on the relative expression of the target gene were normalized to the ACTB gene. The fold change in expression was calculated relative to the blank control (medium without the active substance). All tests were performed at least three times, and Table 1 shows the fold change in COL1A1 gene expression.

[0048] Table 1

[0049]

[0050] * The level of the active substance is the weight percentage based on the amount of the medium

[0051] a: Not significantly superior (p < 0.05) to any of the single active substances at the same level. b: Significantly superior (p < 0.05) to any of the single active substances at the same level.

[0052] It can be clearly seen from Table 1 that the expression of COL1A1 was significantly upregulated (1 vs. G and E) only when lysine carboxymethylcysteine salt and retinyl propionate were combined at the specific weight ratio of the present invention. In contrast, when retinyl propionate was combined with lysine carboxymethylcysteine salt at a weight ratio outside the scope of the present invention, the expression of COL1A1 was not significantly upregulated (C vs. A and B; F vs. D and E).

Claims

1. A personal care composition comprising a carboxymethylcysteine compound and a retinoid, wherein the weight ratio of the carboxymethylcysteine compound to the retinoid is from 1:1.6 to 25:

1.

2. The composition according to claim 1, wherein the carboxymethylcysteine compound comprises carboxymethylcysteine, an ester of carboxymethylcysteine and / or a salt of carboxymethylcysteine.

3. The composition according to claim 2, wherein the carboxymethylcysteine compound comprises a salt of carboxymethylcysteine, and preferably the carboxymethylcysteine compound comprises lysine carboxymethylcysteine salt.

4. The composition according to any one of the preceding claims, wherein the carboxymethylcysteine compound is present in an amount of at least 0.00001% and not more than 10% by weight of the composition, preferably the carboxymethylcysteine compound is present in an amount of at least 0.01% and not more than 3% by weight of the composition.

5. The composition according to any one of the preceding claims, wherein the retinoid is selected from retinol, retinyl esters or mixtures thereof, preferably the retinoid is retinyl propionate.

6. The composition according to any one of the preceding claims, wherein the amount of the retinoid is from 0.00001 to 10% by weight of the total amount of the composition, preferably from 0.02 to 2%.

7. The composition according to any one of the preceding claims, wherein the weight ratio of the carboxymethylcysteine compound to the retinoid is from 1:1.6 to 20:1, preferably from 1:1.5 to 3:

1.

8. The composition according to any one of the preceding claims, wherein the weight ratio of lysine carboxymethylcysteine salt to retinyl propionate in the composition is from 1:1.6 to 20:1, preferably from 1:1.5 to 3:

1.

9. The composition according to any one of the preceding claims, wherein the composition is an emulsion, preferably an oil-in-water emulsion.

10. The composition according to any one of the preceding claims, wherein the composition is a fluid liquid at 25 °C and atmospheric pressure.

11. The composition according to any one of the preceding claims, wherein the composition comprises water in an amount of from 10 to 96% by weight of the composition, preferably from 42 to 88% by weight of the composition.

12. A method of providing a skin benefit selected from enhancing collagen production in the skin, improving skin elasticity, reducing the appearance of wrinkles, reducing sagging, anti-aging and upregulating the expression of collagen synthesis genes, the method comprising the step of topically applying the composition according to any one of the preceding claims to the skin.

13. Use of the composition according to any one of claims 1 to 11 for providing a skin benefit selected from enhancing collagen production in the skin, improving skin elasticity, reducing the appearance of wrinkles, reducing sagging, anti-aging and upregulating the expression of collagen synthesis genes.

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