A personal care composition
Patent Information
- Authority / Receiving Office
- EP · EP
- Patent Type
- Applications
- Current Assignee / Owner
- UNILEVER IP HLDG BV
- Filing Date
- 2024-07-24
- Publication Date
- 2026-07-01
AI Technical Summary
There is a growing need for a personal care composition that can effectively upregulate the expression of the OR10A6 gene, which is involved in epidermal differentiation, skin barrier homeostasis, and stress response mechanisms, to provide benefits such as improved skin barrier health, strengthened skin barrier, and stress reduction.
A personal care composition comprising carboxymethyl cysteine compound and vitamin C compound, with a molar ratio of at least 14:1, is topically applied to the skin to achieve the upregulation of the OR10A6 gene expression.
The composition significantly upregulates the expression of the OR10A6 gene, leading to improved skin barrier health, strengthened skin barrier, and stress reduction, as demonstrated by the increase in gene expression fold change compared to compositions without these ingredients.
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Abstract
Description
[0001] A PERSONAL CARE COMPOSITION
[0002] Field of the Invention
[0003] The present invention relates to a personal care composition comprising carboxymethyl cysteine compound and vitamin C compound, wherein the molar ratio of the carboxymethyl cysteine compound to the vitamin C compound is at least 14:1. It was unexpectedly found that such composition is capable of significantly upregulating the expression of OR10A6 (Olfactory Receptor Family 10 Subfamily A Member 6) gene.
[0004] Background of the Invention
[0005] Skin is an organ that protects the body from external stressors like heat, UV, pollutants, allergens, pathogens etc. It also prevents loss of moisture. The protective role of skin is carried out by epidermal or skin barrier. The skin barrier consists of different layers of stratified cells and the outermost layer consists of corneocytes embedded in a layer of lipids.
[0006] It was reported that OR10A6 are involved in epidermal differentiation, water-impermeable barrier homeostasis, 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 may be a potential target for modulation of keratinization, to provide benefits of stress reduction, strengthening skin barrier.
[0007] Therefore, the present inventors have acknowledged that there is increasing needs to develop a personal care composition capable of upregulating the expression of OR10A6 gene. It was surprisingly found that by combining carboxymethyl cysteine compound and vitamin C compound with a molar ratio of at least 14:1 . of the Invention
[0008] In a first aspect, the present invention is directed to a personal care composition comprising carboxymethyl cysteine compound and vitamin C compound, wherein the molar ratio of the carboxymethyl cysteine compound to the vitamin C compound is at least 14:1 , wherein the composition comprises water in amount of 10 to 96% by weight of the composition.
[0009] In a second aspect, the present invention is directed to a method of providing the skin benefits selected from the group consisting of improving skin barrier health, strengthening skin barrier, and stress reduction comprising a step of topically applying to the skin the composition of the present invention.
[0010] In a third aspect, the present invention is directed to use of the composition of the present invention for providing the skin benefits selected from the group consisting of improving skin barrier health, strengthening skin barrier, and stress reduction.
[0011] All other aspects of the present invention will more readily become apparent upon considering the detailed description and examples which follow.
[0012] Detailed Description of the Invention
[0013] Except in the examples, or where otherwise explicitly indicated, all numbers in this description indicating amounts of material or conditions of reaction, physical properties of materials and / or use may optionally be understood as modified by the word “about”.
[0014] All amounts are by weight of the composition, unless otherwise specified.
[0015] It should be noted that in specifying any range of values, any particular upper value can be associated with any particular lower value.
[0016] 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.
[0017] The disclosure of the invention as found herein is to be considered to cover all embodiments as found in the claims as being multiply dependent upon each other irrespective of the fact that claims may be found without multiple dependency or redundancy.
[0018] Where a feature is disclosed with respect to a particular aspect of the invention (for example a composition of the invention), such disclosure is also to be considered to apply to any other aspect of the invention (for example a method of the invention) mutatis mutandis.
[0019] The carboxymethyl cysteine compound refers to compound selected from carboxymethyl cysteine, salt of carboxymethyl cysteine, ester of carboxymethyl cysteine, amide of carboxymethyl cysteine or a mixture thereof. Preferably, the carboxymethyl cysteine compound comprises carboxymethyl cysteine, ester of carboxymethyl cysteine, and / or salt of carboxymethyl cysteine. More preferably, the carboxymethyl cysteine compound comprises carboxymethyl cysteine, and / or salt of carboxymethyl cysteine. Even more preferably, carboxymethyl cysteine compound comprises salt of carboxymethyl cysteine. Still even more preferably the carboxymethyl cysteine compound comprises lysine carboxymethyl cysteinate and most preferably, the carboxymethyl cysteine compound is lysine carboxymethyl cysteinate.
[0020] Preferably, the carboxymethyl cysteine compound is present in 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 % by weight of the composition. Preferably, the carboxymethyl cysteine compound is present in amount of no greater than 10%, more preferably no greater than 5%, even more preferably no greater than 3%, still even more preferably no greater than 1 %, and most preferably no greater than 0.5% by weight of the composition.
[0021] Preferably, the lysine carboxymethyl cysteinate is present in amount of no greater than 10%, more preferably no greater than 5%, even more preferably no greater than 3%, still even more preferably no greater than 1 %, and most preferably no greater than 0.5% by weight of the composition. Preferably, the lysine carboxymethyl cysteinate is present in 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 % by weight of the composition.
[0022] The vitamin C compound refers to compound selected from ascorbic acid (also known as vitamin C), salt, ester, and ether thereof. Any physiologically acceptable salt of ascorbic acid may be used. Salts of ascorbic acid comprise alkali metal, alkaline earth metal salts, ammonium salt, those derived from monoethanolamine, diethanolamine, amino acids salt such as arginine or lysine, or combination thereof. Suitable ascorbic acid esters are those in which one or more hydroxy groups in the 2-, 3-, 5- and / or 6-positions are fatty acid ester, sulphate or phosphate. Preferably, the Vitamin C compound is ester of ascorbic acid. More preferably the vitamin C compound is ascorbyl phosphate. Still even more preferably, vitamin C compound is magnesium ascorbyl phosphate and / or sodium ascorbyl phosphate.
[0023] Preferably, the vitamin C compound comprises ascorbic acid, calcium ascorbate dihydrate, sodium ascorbate, ascorbyl glycoside, glyceryl ascorbate, 3-O-ethyl-L-ascorbic acid, methoxy peg-7 ascorbic acid, ascorbyl stearate, ascorbyl tetraisopalmitate, tetrahexyldecyl ascorbate, ascorbyl phosphate, ascorbyl palmitate, or a mixture thereof. More preferably, the vitamin C compound comprises ascorbic acid, ascorbyl phosphate, sodium ascorbate, ascorbyl glucoside, ascorbyl tetraisopalmitate, ascorbyl palmitate, or a mixture thereof. Even more preferably, the vitamin C compound comprises ascorbic acid, ascorbyl phosphate, ascorbyl glucoside, glyceryl ascorbate, ascorbyl tetraisopalmitate, ascorbyl palmitate, or a mixture thereof. Even more preferably, the vitamin C compound comprises ascorbyl phosphate, ascorbyl glucoside, ascorbyl tetraisopalmitate, ascorbyl palmitate, or a mixture thereof. Still even more preferably, the vitamin C compound comprises ascorbyl phosphate.
[0024] Preferably, the amount of the vitamin C compound of the is 0.0001 to 8% by weight of the composition, more preferably 0.005 to 5% by weight, even more preferably 0.02 to 2% and most preferably 0.1 to 1 .2% by weight of the composition. Preferably, the amount of ester of ascorbic acid is 0.0001 to 8% by weight of the composition, more preferably 0.005 to 5% by weight, even more preferably 0.02 to 2% and most preferably 0.1 to 1.2% by weight of the composition. Preferably, the amount of ascorbyl phosphate is 0.0001 to 8% by weight of the composition, more preferably 0.005 to 5% by weight, even more preferably 0.02 to 2% and most preferably 0.1 to 1 .2% by weight of the composition.
[0025] Preferably the molar ratio of the carboxymethyl cysteine 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 , still even more preferably 16:1 to 30:1. Preferably the molar ratio of the carboxymethyl cysteine compound to ester of ascorbic acid is 14:1 to 500:1 , more preferably 14:1 to 200:1, even more preferably 15:1 to 70:1 , still even more preferably 16:1 to 30:1. Preferably the molar ratio of the carboxymethyl cysteine compound to ascorbyl phosphate acid is 14:1 to 500:1 , more preferably 14:1 to 200:1 , even more preferably 15:1 to 70:1 , still even more preferably 16:1 to 30:1. Preferably the molar ratio of the lysine carboxymethyl cysteinate to ascorbyl phosphate acid is 14:1 to 500:1 , more preferably 14:1 to 200:1 , even more preferably 15:1 to 70:1 , still even more preferably 16:1 to 30:1.
[0026] The composition may optionally comprise whitening pigment. Whitening pigments are typically particles of high refractive index materials. For example, the whitening pigment may have a refractive index of greater than 1.3, more preferably greater than 1.8 and most preferably from 2.0 to 2.7. Examples of such whitening pigment are those comprising bismuth oxy-chloride, boron nitride, barium sulfate, mica, silica, titanium dioxide, zirconium oxide, aluminium oxide, zinc oxide or combinations thereof. More preferred whitening pigment are particles comprising titanium dioxide, zinc oxide, zirconium oxide, mica, iron oxide or a combination thereof. Even more preferred whitening pigment are particles comprising zinc oxide, zirconium oxide, titanium dioxide or a combination thereof as these materials have especially high refractive index. Still even more preferably the whitening pigment is selected from titanium dioxide, zinc oxide or a mixture thereof and most preferred whitening pigment is titanium dioxide. The average diameter of whitening pigment is typical from 15 nm to 1 micron, more preferably from 35 nm to 800 nm, even more preferably from 50 nm to 500 nm and still even more preferably from 100 to 300 nm. Amount of whitening pigment may be 0.1 to 15%, preferably 0.5 to 5% by weight of the composition.
[0027] Preferably, the composition comprises a glutamate source selected from the group consisting of glutamine, glutamine ester, glutamic acid, pyroglutamic acid, salts, and mixtures thereof. More preferably, the composition comprises pyroglutamic acid and / or salt of pyroglutamic acid. Even more preferably, the composition comprises sodium salt of pyroglutamic acid. Preferably, the glutamate source is present in amount of 0.0001 to 10% by weight of the composition, more preferably 0.001 to 6%, even more preferably 0.01 to 3% by weight of the composition.
[0028] Preferably, the composition comprises polyhydric alcohol. Polyhydric alcohols may be selected from group of glycerin, propylyene glycol, dipropylene glycol, polypropylene glycol, polyethylene glycol, sorbitol, hydroxypropyl sorbitol, hexylene glycol, 1 ,3-butylene glycol, isoprene glycol, ethoxylated glycerol, propoxylated glycerol or a mixture thereof. Most preferred polyhydric alcohol is glycerol known also as glycerin. The amount of polyhydric alcohol may range anywhere from 0.1 to 20%, preferably 0.5 to 15% and more preferably 2 and 10% by weight of the composition.
[0029] Preferably, the composition comprises emollient materials. Suitable emollient materials include silicones, hydrocarbons, triglycerides or a mixture thereof. These silicones may 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 polydecanes such as isododecane and isodecane (e.g. Permethyl- 99A which is available from Presperse Inc.) and the C7-C8 through C12-C15 isoparaffins (such as the Isopar Series available from Exxon Chemicals). Illustrative triglycerides but not limiting are sunflower seed oil, cotton oil, canola oil, soybean oil, castor oil, borage oil, olive oil, shea butter, jojoba oil and mixtures thereof. Mono- and di- glycerides may also be useful. Particularly preferable are glyceryl monostearate and glyceryl distearate.
[0030] Preferably, the composition comprises moisturizing agents. Particularly preferred moisturizing agents includes, petrolatum, aquaporin manipulating actives, oat kernel flour, substituted urea like hydroxyethyl urea, hyaluronic acid and / or its precursor N-acetyl glucosamine, hyaluronic acid and / or its precursor N-acetyl glucosamine, or a mixture thereof.
[0031] Some compositions may include thickeners. These may be selected from cellulosics, natural gums and acrylic polymers but not limited by this thickening agent types. Among the cellulosics are sodium carboxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl methylcellulose and combinations thereof. Suitable gums include xanthan, pectin, karaya, agar, alginate gums and combinations thereof. Among the acrylic thickeners are homopolymers and copolymers of acrylic and methacrylic acids including carbomers such as Carbopol 1382, Carbopol 982, llltrez, Aqua SF-1 and Aqua SF-2 available from the Lubrizol Corporation. Amounts of thickener may range from 0.01 to 3% by weight of the active polymer (outside of solvent or water) in the compositions.
[0032] In addition, the compositions of the invention may further include 0.5 to 10% by weight of sequestering agents, such as tetra sodium ethylenediaminetetraacetate (EDTA), EHDP or mixtures; opacifiers and pearlizers such as ethylene glycol distearate, titanium dioxide or Lytron 621 (Styrene / Acrylate copolymer); all of which are useful in enhancing the appearance or properties of the product.
[0033] The composition comprise water in amount of 10 to 96% by weight of the composition, more preferably from 25 to 92%, even more preferably from 42 to 88%, most preferably from 55 to 82% by weight of the composition.
[0034] Preferably, the composition has a viscosity of at least 10 mPa s, more preferably in the range 30 to 10000 mPa s, even more preferably 50 to 5000 mPa s, and most preferably 100 to 2000 mPa s, when measured at 20 degrees C at a relatively high shear rate of about 20 s'1.
[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. Skin care composition refers to a composition suitable for topical application to human skin, including leave-on and wash-off products but preferably leave-on compositions. The term “leave-on” as used with reference to compositions herein means a composition that is applied to or rubbed on the skin, and left thereon. The term “wash-off” as used with reference to compositions herein means a skin cleanser that is applied to or rubbed on the skin and rinsed off substantially immediately subsequent to application. The term "skin" as used herein includes the skin on the face, neck, chest, abdomen, back, arms, under arms, hands, and legs. Preferably “skin” means includes the skin on the face and under arms, more preferably skin means skin on the face other than lips and eyelids. The composition is particularly preferably a moisturizer rather than a make-up product.
[0037] Preferably, the composition is a topical composition. Preferably, the composition may be in the form of cream, lotion, ointment, solution, suspension, emulsion, paste, gel, powder, powder foundation, emulsion foundation, wax foundation, or spray. More preferably, the composition may be formulated in the form of cream, lotion, ointment, emulsion, gel, or a spray.
[0038] Preferably, the composition is capable of upregulating the expression of OR10A6 (Olfactory Receptor Family 10 Subfamily A Member 6) gene by at least 1.2 fold change, more preferably 1.2 to 4, and even more preferably 1.3 to 3 fold change, typically in comparison to personal care composition comprising neither carboxymethyl cysteine compound nor vitamin C compound.
[0039] Preferably the use is non-therapeutic. Preferably the method is non-therapeutic. The term non- therapeutic typically means for cosmetic purposes and not curative or therapeutic purposes.
[0040] The following examples are provided to facilitate an understanding of the invention. The examples are not intended to limit the scope of the claims.
[0041] Examples
[0042] Materials
[0043] Example 1
[0044] This Example demonstrates that the upregulation of gene expression by the composition of the present invention.
[0045] The normal human epidermal keratinocytes (NHEKs) (Biocell, Xi’an, China) were cultured in keratinocyte culture medium (KcGrowth, Biocell, Xi’an, China) and plated in 6-well plates. When the cell confluency reached 40% to 60%, the culture medium was replaced with medium together with or without actives for 24 hours. After incubation, the total RNA for each NHEK was extracted using RNAex Pro reagent (Accurate Biotechnology, Cat: AG21102) according to manufacturer’s protocol.
[0046] The extracted RNA was quantified using Nanodrop spectrometer (Thermo Fisher Scientific, Waltham, MA, US) and reverse transcribed to generate the template cDNA using the Evo M-MLV RT Premix for qPCR (Accurate Biotechnology, Cat: AG11706) according to manufacturer’s protocol. Gene expression of ATG5 gene was analyzed by polymerase chain reaction (PCR) using SYBR® Green Premix Pro Taq HS qPCR Kit (Accurate Biotechnology, AG11701). The actin beta (ACTB) gene was selected as the housekeeping gene and all data on relative expression of the target genes was normalized to ACTB gene. The fold changes in expression were calculated relative to the blank control (medium having no active). All tests were conducted at least three times and Table 1 shows the fold change of the gene expression for OR10A6 (Olfactory Receptor Family 10 Subfamily A Member 6).
[0047] Table 1
[0048] #: The level of the active is based on the medium. a: not significantly better (p<0.05) than either of single active at same level. b: significantly better (p<0.05) than either of single active at same level.
[0049] It’s an evident from Table 1 that only when combining LCC with Stay-C in a specific molar ratio of the present invention, the expression of OR10A6 gene is significantly upregulated (1 vs. A and F). In contrast, when combining LCC with Stay-C in a molar ratio not within the range of the present invention, the expression of OR10A6 is not upregulated (C vs. A and B and E vs. D and A).
Claims
Claims1. A personal care composition comprising carboxymethyl cysteine compound and vitamin C compound, wherein the molar ratio of the carboxymethyl cysteine compound to the vitamin C compound is at least 14:1 , wherein the composition comprises water in amount of 10 to 96% by weight of the composition.
2. The composition according to claim 1 wherein the carboxymethyl cysteine compound comprises carboxymethyl cysteine, ester of carboxymethyl cysteine, and / or salt of carboxymethyl cysteine.
3. The composition according to claim 2 wherein the carboxymethyl cysteine compound comprises salt of carboxymethyl cysteine and preferably the carboxymethyl cysteine compound comprises lysine carboxymethyl cysteinate.
4. The composition according to any one of the preceding claims wherein the carboxymethyl cysteine compound is present in amount of at least 0.00001% and no greater than 10% by weight of the composition, preferably carboxymethyl cysteine compound is present in amount of at least 0.01% and no greater than 3% by weight of the composition.
5. The composition according to any one of the preceding claims wherein the vitamin C compound comprises ascorbic acid, ascorbyl phosphate, ascorbyl glucoside, glyceryl ascorbate, ascorbyl tetraisopalmitate, ascorbyl palmitate, or a mixture thereof, preferably the Vitamin C compound is ascorbyl phosphate.
6. The composition according to any one of the preceding claims wherein the amount of the vitamin C compound of the is 0.0001 to 8% preferably 0.02 to 2% by weight of the composition.
7. The composition according to any one of the preceding claims wherein the molar ratio of the carboxymethyl cysteine 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 amount of from 42 to 88% by weight of the composition.
11. A method of providing the skin benefits selected from the group consisting of improving skin barrier health, strengthening skin barrier, and stress reduction comprising a step of topically applying to the skin the composition according to any one of the preceding claims 1 to 10.
12. Use of the composition according to any one of the preceding claims 1 to 10 for providing the skin benefits selected from the group consisting of improving skin barrier health, strengthening skin barrier, and stress reduction.