Personal care product

By setting the molar ratio of carboxymethylcysteine ​​compound to vitamin C compound to 14:1 in a personal care composition and applying it topically to the skin, the problem of existing products being unable to effectively upregulate OR10A6 gene expression was solved, achieving the effects of strengthening the skin barrier and reducing stress.

CN121712482APending Publication Date: 2026-03-20UNILEVER IP HLDG BV
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Patent Information

Application Number
CN202480054061.8
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Priority Date
2023-10-05
Filing Date
2024-07-24
Publication Date
2026-03-20

AI Technical Summary

Technical Problem

Existing personal care products are unable to effectively upregulate the expression of the OR10A6 gene, leading to insufficient skin barrier function and failing to significantly improve skin barrier health and reduce stress.

Method used

A personal care composition is prepared by combining a carboxymethylcysteine ​​compound and a vitamin C compound in a molar ratio of at least 14:1 and applying it topically to the skin.

Benefits of technology

It significantly upregulates OR10A6 gene expression, enhances skin barrier function, and provides skin benefits such as improved skin barrier health and stress reduction.

✦ Generated by Eureka AI based on patent content.

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Abstract

A personal care composition comprising a carboxymethyl cysteine compound and a vitamin C compound wherein the molar ratio of carboxymethyl cysteine compound to vitamin C compound is at least 14: 1, and the composition comprises 10 to 96% by weight of water.
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Description

Technical Field

[0001] This invention relates to personal care compositions comprising a carboxymethylcysteine ​​compound and a vitamin C compound, wherein the molar ratio of the carboxymethylcysteine ​​compound to the vitamin C compound is at least 14:1. Unexpectedly, it has been found that the compositions can significantly upregulate... OR10A6 Expression of genes (member 6 of subfamily A of olfactory receptor family 10). Background Technology

[0002] The skin is an organ that protects the body from external stimuli such as heat, ultraviolet radiation, pollutants, allergens, and pathogens. It also prevents moisture loss. The skin's protective function is mainly achieved by the epidermis or skin barrier. The skin barrier is composed of layers of cells, with the outermost layer consisting of keratinocytes embedded in the lipid layer.

[0003] According to reports, OR10A6 Involved in epidermal differentiation, homeostasis of the water-impermeable barrier, and stress response mechanisms (Shinobu Nakanishi et al., Frontiers in Cell and Developmental Biology , 11:1102585.doi: 10.3389 / fcell.2023.1102585; Romain Duroux et al., Molecules 2020, 25,4743; doi:10.3390 / molecules25204743). OR10A6 It could be a potential target for regulating keratinization, providing benefits such as stress reduction and strengthening the skin barrier.

[0004] Therefore, the inventors of this invention recognized that it was possible to increase the efficiency of development. OR10A6 The growing demand for personalized care compositions based on gene expression. Surprisingly, it was found that combining carboxymethylcysteine ​​compounds and vitamin C compounds in a molar ratio of at least 14:1 is effective. Summary of the Invention

[0005] In a first aspect, the present invention relates to a personal care composition comprising a carboxymethylcysteine ​​compound and a vitamin C compound, wherein the molar ratio of the carboxymethylcysteine ​​compound to the vitamin C compound is at least 14:1, and the composition comprises water in an amount of 10 to 96% by weight of the composition.

[0006] In a second aspect, the present invention relates to a method for providing skin benefits selected from improving skin barrier health, strengthening the skin barrier, and reducing stress, the method comprising the step of topically applying the composition of the present invention to the skin.

[0007] Thirdly, the present invention relates to the use of the compositions of the present invention for providing skin benefits selected from improving skin barrier health, strengthening the skin barrier, and reducing stress.

[0008] All other aspects of the invention will become more apparent by considering the following detailed description and examples. Detailed Implementation

[0009] Unless explicitly stated in the examples or otherwise, all figures in this description representing material amounts or reaction conditions, material physical properties and / or uses may optionally be understood to be modified by the word “about”.

[0010] Unless otherwise stated, all amounts are calculated by weight of the composition.

[0011] It is important to note that when specifying any numerical range, any particular upper limit value can be associated with any particular lower limit value.

[0012] To avoid ambiguity, the word "includes" here means "to include," but does not necessarily mean "composed of" or "consisting of." In other words, the listed steps or options do not need to exhaust all possibilities.

[0013] The invention disclosed herein should be considered to cover all embodiments described in the claims, which have multiple dependencies on each other, even if there may be no multiple dependencies or redundancy in the claims.

[0014] If a feature is disclosed for a particular aspect of the invention (e.g., a composition of the invention), that disclosure should also be considered as applicable to any other aspect of the invention (e.g., a method of the invention) with necessary modifications.

[0015] Carboxymethylcysteine ​​compounds refer to compounds selected from 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. Even more preferably, the carboxymethylcysteine ​​compound includes lysine carboxymethylcysteine ​​ester, and most preferably, the carboxymethylcysteine ​​compound is lysine carboxymethylcysteine ​​ester.

[0016] Preferably, the content of the carboxymethylcysteine ​​compound is at least 0.00001% of the weight of the composition, more preferably at least 0.0001%, even more preferably at least 0.001%, even more preferably at least 0.01%, and most preferably at least 0.1%. Preferably, the content of the carboxymethylcysteine ​​compound is no more than 10% of the weight of the composition, more preferably no more than 5%, even more preferably no more than 3%, even more preferably no more than 1%, and most preferably no more than 0.5%.

[0017] Preferably, the content of lysine carboxymethyl cysteine ​​ester is no more than 10% of the weight of the composition, more preferably no more than 5%, even more preferably no more than 3%, even more preferably no more than 1%, and most preferably no more than 0.5%. Preferably, the content of lysine carboxymethyl cysteine ​​ester is at least 0.00001% of the weight of the composition, more preferably at least 0.0001%, even more preferably at least 0.001%, even more preferably at least 0.01%, and most preferably at least 0.1%.

[0018] Vitamin C compounds are compounds selected from ascorbic acid (also known as vitamin C) and its salts, esters, and ethers. Any physiologically acceptable salt of ascorbic acid can be used. Salts of ascorbic acid include alkali metal salts, alkaline earth metal salts, ammonium salts, and salts derived from monoethanolamine, diethanolamine, amino acid salts such as arginine or lysine, or combinations thereof. Suitable ascorbic acid esters are compounds in which one or more hydroxyl groups at the 2-, 3-, 5-, and / or 6-positions are fatty acid esters, sulfate esters, or phosphate esters. Preferably, the vitamin C compound is an ester of ascorbic acid. More preferably, the vitamin C compound is ascorbic acid phosphate. Even more preferably, the vitamin C compound is magnesium ascorbic acid phosphate and / or sodium ascorbic acid phosphate.

[0019] Preferably, the vitamin C compound comprises ascorbic acid, calcium ascorbate dihydrate, sodium ascorbate, ascorbate glucoside, ascorbate glyceryl ester, 3-O-ethyl-L-ascorbic acid, methoxyPEG-7 ascorbic acid, ascorbate stearate, ascorbate tetraisopalmitate, ascorbate tetrahexyldecyl ester, ascorbate phosphate, ascorbate palmitate, or mixtures thereof. More preferably, the vitamin C compound comprises ascorbic acid, ascorbate phosphate, sodium ascorbate, ascorbate glucoside, ascorbate tetraisopalmitate, ascorbate palmitate, or mixtures thereof. Even more preferably, the vitamin C compound comprises ascorbic acid, ascorbate phosphate, ascorbate glucoside, ascorbate glyceryl ester, ascorbate tetraisopalmitate, ascorbate palmitate, or mixtures thereof. Even more preferably, the vitamin C compound comprises ascorbate phosphate, ascorbate glucoside, ascorbate tetraisopalmitate, ascorbate palmitate, or mixtures thereof. Even more preferably, the vitamin C compound comprises ascorbate phosphate.

[0020] Preferably, the amount of the vitamin C compound is 0.0001 to 8% of the weight of the composition, more preferably 0.005 to 5%, even more preferably 0.02 to 2%, and most preferably 0.1 to 1.2%. Preferably, the amount of ascorbic acid ester is 0.0001 to 8% of the weight of the composition, more preferably 0.005 to 5%, even more preferably 0.02 to 2%, and most preferably 0.1 to 1.2%. Preferably, the amount of ascorbic acid phosphate is 0.0001 to 8% of the weight of the composition, more preferably 0.005 to 5%, even more preferably 0.02 to 2%, and most preferably 0.1 to 1.2%.

[0021] Preferably, the molar ratio of the carboxymethylcysteine ​​compound to the vitamin C compound is 14:1 to 500:1, more preferably 14:1 to 200:1, even more preferably 15:1 to 70:1, and even more preferably 16:1 to 30:1. Preferably, the molar ratio of the carboxymethylcysteine ​​compound to the ascorbic acid ester is 14:1 to 500:1, more preferably 14:1 to 200:1, even more preferably 15:1 to 70:1, and even more preferably 16:1 to 30:1. Preferably, the molar ratio of the carboxymethylcysteine ​​compound to the ascorbic acid phosphate ester is 14:1 to 500:1, more preferably 14:1 to 200:1, even more preferably 15:1 to 70:1, and even more preferably 16:1 to 30:1. Preferably, the molar ratio of lysine carboxymethyl cysteine ​​ester to ascorbic acid phosphate ester (acid) is 14:1 to 500:1, more preferably 14:1 to 200:1, even more preferably 15:1 to 70:1, and even more preferably 16:1 to 30:1.

[0022] The composition may optionally contain a whitening pigment. The whitening pigment is typically composed of particles of a high refractive index material. For example, the refractive index of the whitening pigment may be greater than 1.3, more preferably greater than 1.8, and most preferably 2.0 to 2.7. Examples of such whitening pigments are those comprising bismuth oxychloride, boron nitride, barium sulfate, mica, silicon dioxide, titanium dioxide, zirconium oxide, aluminum oxide, zinc oxide, or combinations thereof. More preferably, the whitening pigment is composed of particles comprising titanium dioxide, zinc oxide, zirconium oxide, mica, iron oxide, or combinations thereof. Even more preferably, the whitening pigment is composed of particles comprising zinc oxide, zirconium oxide, titanium dioxide, or combinations thereof, because these materials have particularly high refractive indices. Even more preferably, the whitening pigment is selected from titanium dioxide, zinc oxide, or mixtures thereof, with titanium dioxide being the most preferred whitening pigment. The average particle size of the whitening pigment is typically 15 nm to 1 micrometer, more preferably 35 nm to 800 nm, even more preferably 50 nm to 500 nm, and even more preferably 100 nm to 300 nm. The amount of the whitening pigment can be 0.1 to 15% of the weight of the composition, preferably 0.5 to 5%.

[0023] Preferably, the composition comprises a glutamate (salt) source selected from glutamine, glutamine esters, glutamic acid, pyroglutamic acid, their salts, and mixtures thereof. More preferably, the composition comprises pyroglutamic acid and / or salts of pyroglutamic acid. More preferably, the composition comprises a sodium salt of pyroglutamic acid. Preferably, the content of the glutamate (salt) source is 0.0001 to 10% by weight of the composition, more preferably 0.001 to 6%, and even more preferably 0.01 to 3%.

[0024] Preferably, the composition comprises a polyol. The polyol may be selected from glycerol, propylene glycol, dipropylene glycol, polypropylene glycol, polyethylene glycol, sorbitol, hydroxypropyl sorbitol, hexanediol, 1,3-butanediol, isopentyl glycol, ethoxylated glycerol, propoxylated glycerol, or mixtures thereof. The most preferred polyol is glycerol (also known as glycerol). The amount of the polyol may be 0.1% to 20% by weight of the composition, preferably 0.5% to 15%, more preferably 2% to 10%.

[0025] Preferably, the composition comprises an emollient material. Suitable emollient materials include silicones, hydrocarbons, triglycerides, or mixtures thereof. These silicones may be organic, silicone-containing, or fluorine-containing, volatile or non-volatile, polar or non-polar. Hydrocarbons may include mineral oils, petrolatum, and polyalphaolefins. Preferred examples of volatile hydrocarbons include polydecanes, such as isododecane and isodecane (e.g., Permethyl-99A, available from Presperse), and C7-C8 to C64 hydrocarbons. 12 -C 15Isoalkanes (e.g., the Isopar series, available from Exxon Chemicals). Exemplary triglycerides include, but are not limited to, sunflower oil, cottonseed oil, rapeseed oil, soybean oil, castor oil, borage oil, olive oil, shea butter, jojoba oil, and mixtures thereof. Monoglycerides and diglycerides are also available. Glyceryl monostearate and glyceryl distearate are particularly preferred.

[0026] Preferably, the composition comprises a moisturizer. Particularly preferred moisturizers include petrolatum, aquaporin-regulating active ingredients, oat kernel powder, substituted ureas such as hydroxyethyl urea, hyaluronic acid and / or its precursor N-acetylglucosamine, or mixtures thereof.

[0027] Some compositions may contain a thickener. This thickener may be selected from, but is not limited to, cellulose, natural gums, and acrylic polymers. Cellulose includes sodium carboxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl methyl cellulose, and combinations thereof. Suitable gums include xanthan gum, pectin, carrageenan, agar, alginate gum, and combinations thereof. Acrylic thickeners include 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. The amount of thickener in the composition may be from 0.01 to 3% by weight of the active polymer (excluding solvent or water).

[0028] In addition, the compositions of the present invention may also contain 0.5 to 10% by weight of a chelating agent, such as tetrasodium ethylenediaminetetraacetate (EDTA), EHDP or a mixture thereof; an opacifier and a pearlescent agent, such as ethylene glycol distearate, titanium dioxide or Lytron 621 (styrene / acrylate copolymer); all of which contribute to enhancing the appearance or performance of the product.

[0029] The composition comprises 10 to 96%, more preferably 25 to 92%, even more preferably 42 to 88%, and most preferably 55 to 82% of water by weight of the composition.

[0030] Preferably, at 20°C for approximately 20 seconds -1 When measured at relatively high shear rates, the viscosity of the composition is 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.

[0031] 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.

[0032] 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. The term "leave-on" as used herein refers to a composition applied or rubbed onto the skin and left thereon. The term "rinse-off" as used herein refers to 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 of the face, neck, chest, abdomen, back, arms, armpits, hands, and legs. Preferably, "skin" includes the skin of the face and armpits; more preferably, "skin" refers to the facial skin excluding the lips and eyelids. The composition is particularly preferred as a moisturizer rather than a makeup product.

[0033] Preferably, the composition is a topical application composition. Preferably, the composition may be in the form of a cream, lotion, ointment, solution, suspension, emulsion, paste, gel, powder, powder foundation, emulsion foundation, wax foundation, or spray. More preferably, the composition may be formulated as a cream, lotion, ointment, emulsion, gel, or spray.

[0034] Preferably, the composition is capable of […]. OR10A6 The expression of the gene (member 6 of subfamily A of olfactory receptor family 10) was upregulated by at least 1.2-fold, more preferably 1.2 to 4-fold, and even more preferably 1.3 to 3-fold, typically compared to personal care compositions that contain neither carboxymethylcysteine ​​nor vitamin C compounds.

[0035] Preferably, the use is non-therapeutic. Preferably, the method is non-therapeutic. The term "non-therapeutic" generally refers to use for cosmetic purposes, rather than for curative or therapeutic purposes.

[0036] The following embodiments are provided to aid in understanding the invention. These embodiments are not intended to limit the scope of the claims.

[0037] Example Material

[0038] Example 1 This embodiment demonstrates that the composition of the present invention upregulates gene expression.

[0039] Normal human epidermal keratinocytes (NHEK) (Biocell, Xi'an, China) were cultured in keratinocyte culture medium (KcGrowth, Biocell, Xi'an, China) and seeded in 6-well plates. When the cell confluence reached 40% to 60%, the culture medium was replaced with or without the active ingredient, over a period of 24 hours. After incubation, total RNA was extracted from each well of NHEK cells using RNAex Pro reagent (Accurate Biotechnology, catalog number: AG21102) according to the manufacturer's specifications.

[0040] The extracted RNA was quantified using a Nanodrop spectrometer (Thermo Fisher Scientific, Waltham, MA, US), and reverse transcription was performed using the Evo M-MLV RT Premix for qPCR (AccurateBiotechnology, catalog number: AG11706) to generate template cDNA, following the manufacturer's instructions. Analysis was performed by polymerase chain reaction (PCR) using the SYBR® Green Premix Pro Taq HS qPCR kit (Accurate Biotechnology, AG11701). ATG5 Gene expression. Select β-actin ( ACTB As housekeeping genes, all data on the relative expression of target genes are based on... ACTB Genes were normalized. The fold change in expression was calculated relative to the blank control (medium without active ingredients). All tests were performed at least three times, as shown in Table 1. OR10A6 (Fold change in gene expression of 6 members of subfamily A of olfactory receptor family 10)

[0041] Table 1

[0042] As can be seen from Table 1, only when LCC and Stay-C are combined in the specific molar ratio of this invention, OR10A6 Gene expression will be significantly upregulated (1 relative to A and F). In contrast, when LCC and Stay-C are combined in a molar ratio outside the scope of this invention, OR10A6 The expression is not modulated (C relative to A and B, and E relative to D and A).

Claims

1. A personal care composition comprising a carboxymethylcysteine ​​compound and a vitamin C compound, wherein the molar ratio of the carboxymethylcysteine ​​compound to the vitamin C compound is at least 14:1, wherein the composition comprises water in an amount of 10 to 96% by weight of the composition.

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

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

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

5. The composition according to any one of the preceding claims, wherein the vitamin C compound comprises ascorbic acid, ascorbate phosphate, ascorbate glucoside, ascorbate glyceryl ester, ascorbate tetraisopalmitate, ascorbate palmitate, or a mixture thereof, preferably, the vitamin C compound is ascorbate phosphate.

6. The composition according to any one of the preceding claims, wherein the content of the vitamin C compound is 0.0001 to 8% by weight of the composition, preferably 0.02 to 2%.

7. The composition according to any one of the preceding claims, wherein the molar ratio of the carboxymethylcysteine ​​compound to the vitamin C compound is 14:1 to 500:1, preferably 15:1 to 70:

1.

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

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

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

11. A method of providing skin benefits selected from improving skin barrier health, strengthening the skin barrier, and reducing stress, the method comprising the step of topically applying a composition according to any one of claims 1 to 10 to the skin.

12. The composition according to any one of claims 1 to 10 is used to provide skin benefits selected from improving skin barrier health, strengthening the skin barrier, and reducing stress.