Personal Care Compositions
A personal care composition with a carboxymethylcysteine and retinoid at a specific ratio effectively enhances COL1A1 expression, addressing skin aging by improving elasticity and reducing wrinkles and sagging.
Patent Information
- Application Number
- JP2025526431
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2022-12-09
- Filing Date
- 2023-10-16
- Publication Date
- 2025-10-24
AI Technical Summary
Existing personal care compositions fail to effectively enhance the expression of collagen synthesis genes, particularly type I collagen αI chain (COL1A1), which is crucial for addressing skin aging issues such as wrinkles and sagging.
A personal care composition comprising a carboxymethylcysteine compound and a retinoid at a specific weight ratio of 1:1.6 to 25:1, which synergistically promotes the expression of COL1A1.
The composition significantly enhances COL1A1 expression by 1.45 to 3.5 times, improving skin elasticity, reducing wrinkles, and reducing sagging.
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Abstract
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 1:1.6 to 25:1. It has been unexpectedly found that such a composition significantly promotes the expression of type I collagen αI chain. [Background technology]
[0002] Skin is the primary barrier of the human body. It protects internal organs from external stimuli. Skin is subject to intrinsic and extrinsic aging. Skin aging is a complex process, and age-related changes in human skin have distinct characteristics compared to other organs. Characteristics of intrinsic or chronological skin aging include dryness, visible fine lines and wrinkles, uneven skin pigmentation, loss of elasticity, and sagging skin. Extrinsic factors such as sun exposure, pollutants, and cigarette smoke can accelerate the skin aging process, especially on the face.
[0003] Collagen, the main protein matrix of skin, is known to provide tensile strength to the skin. It has been shown that collagen is significantly reduced with aging and UV exposure. The degradation and destruction of collagen architecture reduces the tensile strength of the skin, leading to wrinkles and sagging. Collagen destruction is thought to be responsible for the characteristic changes in the appearance of aged skin.
[0004] One of the most effective ways to achieve anti-aging effects is to promote collagen production, which is typically achieved by increasing the expression of collagen synthesis genes. Summary of the Invention [Problem to be solved by the invention]
[0005] Therefore, the present inventors recognized the need for developing a solution to enhance the expression of collagen synthesis genes, such as type I collagen αI chain (COL1A1). Surprisingly, they found that combining carboxymethylcysteine and retinoids at a specific weight ratio significantly enhanced the expression of COL1A1. [Means for solving the problem]
[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 for providing a skin benefit selected from the group consisting of promoting collagen production in the skin, improving skin elasticity, reducing the appearance of wrinkles, reducing sagging, anti-aging, and increasing the expression of collagen synthesis genes, the method comprising topically applying to the skin a composition of the present invention.
[0008] In a third aspect, the present invention relates to the use of the composition of the present invention to provide a skin benefit selected from the group consisting of promoting collagen production in the skin, improving skin elasticity, reducing the appearance of wrinkles, reducing sagging, anti-aging, and increasing the expression of collagen synthesis genes.
[0009] All other aspects of the present invention will become more readily apparent in light of the following detailed description and examples. DETAILED DESCRIPTION OF THE INVENTION
[0010] Except in the examples, or where expressly indicated otherwise, all numbers in this description expressing quantities of materials or reaction conditions, physical properties of materials, and / or uses may be understood to be modified by the word "about."
[0011] Unless otherwise specified, all amounts are by weight of the composition. It should be noted that when specifying a range of values, a particular upper limit can be associated with a particular lower limit.
[0012] 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.
[0013] Notwithstanding the fact that claims may be found without multiple dependency or overlap, the disclosure of the invention found herein should be considered to cover all embodiments found in claims that are multiple dependent from one another.
[0014] Where a feature is disclosed with respect to a particular embodiment of the invention (e.g., a composition of the invention), such disclosure should be deemed to also apply mutatis mutandis to any other embodiment of the invention (e.g., a method of the invention).
[0015] The carboxymethylcysteine compound refers to a compound selected from carboxymethylcysteine, a salt of carboxymethylcysteine, an ester of carboxymethylcysteine, an amide of carboxymethylcysteine, or a mixture thereof. Preferably, the carboxymethylcysteine compound includes carboxymethylcysteine, an ester of carboxymethylcysteine, and / or a salt of carboxymethylcysteine. More preferably, the carboxymethylcysteine compound includes carboxymethylcysteine and / or a salt of carboxymethylcysteine. Even more preferably, the carboxymethylcysteine compound includes a salt of carboxymethylcysteine. Even more preferably, the carboxymethylcysteine compound includes lysine carboxymethylcysteinate, and most preferably, the carboxymethylcysteine compound is lysine carboxymethylcysteinate.
[0016] Preferably, the carboxymethylcysteine compound is present in an amount of at least 0.00001% by weight of the composition, more preferably at least 0.0001% by weight, even more preferably at least 0.001% by weight, even more preferably at least 0.01% by weight, and most preferably at least 0.1% by weight. Preferably, the carboxymethylcysteine compound is present in an amount of no more than 10% by weight of the composition, more preferably no more than 5% by weight, even more preferably no more than 3% by weight, even more preferably no more than 1% by weight, and most preferably no more than 0.5% by weight.
[0017] Preferably, lysine carboxymethyl cysteinate is present in an amount of 10% or less by weight of the composition, more preferably 5% or less, even more preferably 3% or less, even more preferably 1% or less, and most preferably 0.5% or less. Preferably, lysine carboxymethyl cysteinate is present in an amount of at least 0.00001% by weight of the composition, more preferably at least 0.0001% by weight, even more preferably at least 0.001% by weight, even more preferably at least 0.01% by weight, and most preferably at least 0.1% by weight.
[0018] The composition of the present invention comprises a retinoid. Typically, the retinoid is selected from a retinyl ester, retinol, retinal, retinoic acid, or a mixture thereof. More preferably, the retinoid comprises retinol, a retinyl ester, or a mixture thereof, and even more preferably, the retinoid is selected from retinol, a retinyl ester, or a mixture thereof.
[0019] The term "retinol" includes the following retinol isomers: all-trans-retinol, 13-cis-retinol, 11-cis-retinol, 9-cis-retinol, 3,4-didehydro-retinol, 3,4-didehydro-13-cis-retinol, 3,4-didehydro-11-cis-retinol, and 3,4-didehydro-9-cis-retinol. Preferred isomers are all-trans-retinol, 13-cis-retinol, 3,4-didehydro-retinol, and 9-cis-retinol. The most preferred retinol is all-trans-retinol due to its widespread commercial availability.
[0020] Retinyl esters are esters of retinol. The term "retinol" is defined above. Retinyl esters suitable for use in the present invention are preferably C1-C6 esters of retinol. 30 esters, more preferably C2-C of retinol 20 esters, most preferably C2, C3 and C of retinol 16 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, and 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 esters are selected from retinyl palmitate, retinyl acetate, retinyl propionate, or mixtures thereof. Even more preferably, the retinyl esters are selected from retinyl palmitate, retinyl propionate, or mixtures thereof.
[0021] Particularly preferred retinoids are selected from all-trans-retinol, retinyl palmitate, retinyl acetate, retinyl propionate, or mixtures thereof. More preferably, the retinoid is selected from retinyl palmitate, retinyl propionate, or mixtures thereof. Even more preferably, the retinoid is retinyl propionate.
[0022] The amount of retinoid is preferably in the range of 0.00001 to 10% by weight, more preferably 0.0001 to 8% by weight, even more preferably 0.001 to 5% by weight, even more preferably 0.02 to 2% by weight, and most preferably 0.1 to 0.6% by weight of the total composition. The total amount of retinol and retinyl esters in the composition is preferably in the range of 0.00001 to 10% by weight, more preferably 0.0001 to 8% by weight, even more preferably 0.001 to 5% by weight, even more preferably 0.02 to 2% by weight, and most preferably 0.1 to 0.6% by weight of the total composition. The total amount of retinyl palmitate and retinyl propionate in the composition is preferably in the range of 0.00001 to 10% by weight, more preferably 0.0001 to 8% by weight, even more preferably 0.001 to 5% by weight, even more preferably 0.02 to 2% by weight, and most preferably 0.1 to 0.6% by weight of the total composition. The amount of retinyl propionate in the composition is preferably in the range of 0.00001 to 10% by weight, more preferably 0.0001 to 8% by weight, even more preferably 0.001 to 5% by weight, even more preferably 0.02 to 2% by weight, and most preferably 0.1 to 0.6% by weight of the total weight of the composition.
[0023] Preferably, the weight ratio of the carboxymethylcysteine compound to the retinoid is 1:1.6 to 20:1, more preferably 1:1.6 to 10:1, even more preferably, even more preferably 1:1.5 to 3:1, and most preferably 1:1.3 to 2:1. Preferably, the weight ratio of the lysine carboxymethylcysteinate to the retinoid is 1:1.6 to 20:1, more preferably 1:1.6 to 10:1, even more preferably, even more preferably 1:1.5 to 3:1, and most preferably 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 1:1.6 to 20:1, more preferably 1:1.6 to 10:1, even more preferably, even more preferably 1:1.5 to 3:1, and most preferably 1:1.3 to 2:1. Preferably, the weight ratio of lysine carboxymethyl cysteinate to the total amount of retinyl propionate and retinyl palmitate in the composition is 1:1.6 to 20:1, more preferably 1:1.6 to 10:1, even more preferably, even more preferably, 1:1.5 to 3:1, and most preferably, 1:1.3 to 2:1. Preferably, the weight ratio of lysine carboxymethyl cysteinate to retinyl propionate in the composition is 1:1.6 to 20:1, more preferably 1:1.6 to 10:1, even more preferably, even more preferably, 1:1.5 to 3:1, and most preferably, 1:1.3 to 2:1.
[0024] 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 1:1.6 to 25:1. Preferably, the molar ratio of the carboxymethylcysteine compound to the retinoid is 1:1.6 to 20:1, more preferably 1:1.6 to 10:1, even more preferably 1:1.5 to 3:1, and most preferably 1:1.3 to 2:1. Preferably, the molar ratio of lysine carboxymethylcysteinate to the retinoid is 1:1.6 to 20:1, more preferably 1:1.6 to 10:1, even more preferably 1:1.5 to 3:1, and most preferably 1:1.3 to 2:1. Preferably, the molar ratio of the carboxymethylcysteine compound to the total amount of retinol and retinyl ester in the composition is 1:1.6 to 20:1, more preferably 1:1.6 to 10:1, even more preferably 1:1.5 to 3:1, and most preferably 1:1.3 to 2:1. Preferably, the molar ratio of lysine carboxymethylcysteine to the total amount of retinyl propionate and retinyl palmitate in the composition is 1:1.6 to 20:1, more preferably 1:1.6 to 10:1, even more preferably 1:1.5 to 3:1, and most preferably 1:1.3 to 2:1. Preferably, the molar ratio of lysine carboxymethylcysteine to retinyl propionate in the composition is 1:1.6 to 20:1, more preferably 1:1.6 to 10:1, even more preferably 1:1.5 to 3:1, and most preferably 1:1.3 to 2:1.
[0025] The composition may optionally contain a whitening pigment. The whitening pigment is typically a particle of a high refractive index material. For example, the whitening pigment may have a refractive index greater than 1.3, more preferably greater than 1.8, and most preferably between 2.0 and 2.7. Examples of such whitening pigments include bismuth oxychloride, boron nitride, barium sulfate, mica, silica, titanium dioxide, zirconium oxide, aluminum oxide, zinc oxide, or a combination thereof. More preferred whitening pigments are particles containing titanium dioxide, zinc oxide, zirconium oxide, mica, iron oxide, or a combination thereof. Even more preferred whitening pigments are particles containing zinc oxide, zirconium oxide, titanium dioxide, or a combination thereof, since these materials have particularly high refractive indices. More preferably, the whitening pigment is selected from titanium dioxide, zinc oxide, or a mixture thereof, with titanium dioxide being the most preferred whitening pigment. The average diameter of the whitening pigment is typically 15 nm to 1 micron, more preferably 35 nm to 800 nm, even more preferably 50 nm to 500 nm, and even more preferably 100 to 300 nm. The amount of whitening pigment can be 0.1 to 15% by weight, preferably 0.5 to 5% by weight, of the composition.
[0026] Preferably, the composition comprises a glutamic acid source selected from the group consisting of glutamine, glutamine esters, glutamic acid, pyroglutamic acid, salts, and mixtures thereof. More preferably, the composition comprises pyroglutamic acid and / or a salt of pyroglutamic acid. Even more preferably, the composition comprises sodium pyroglutamic acid. Preferably, the glutamic acid source is present in an amount of 0.0001 to 10% by weight of the composition, more preferably 0.001 to 6% by weight of the composition, and even more preferably 0.01 to 3% by weight.
[0027] Preferably, the composition comprises a polyhydric alcohol. The polyhydric alcohol may be selected from the group consisting of glycerin, propylene glycol, dipropylene glycol, polypropylene glycol, polyethylene glycol, sorbitol, hydroxypropyl sorbitol, hexylene glycol, 1,3-butylene glycol, isoprene glycol, ethoxylated glycerol, propoxylated glycerol, or mixtures thereof. The most preferred polyhydric alcohol is glycerol, also known as glycerin. The amount of polyhydric alcohol may range from 0.1 to 20% by weight of the composition, preferably from 0.5 to 15% by weight, and more preferably from 2 to 10% by weight.
[0028] Preferably, the composition contains 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, and polar or non-polar. Hydrocarbons may include mineral oil, petrolatum, and polyalphaolefins. Examples of preferred volatile hydrocarbons include polydecanes such as isododecane and isodecane (e.g., Permethyl-99A available from Presperse Inc.) and C7-C8 to C12-C15 isoparaffins (e.g., the Isopar series available from Exxon Chemicals). Exemplary triglycerides include, but are not limited to, sunflower seed oil, cottonseed oil, rapeseed oil, soybean oil, castor oil, borage oil, olive oil, shea butter, jojoba oil, and mixtures thereof. Monoglycerides and diglycerides may also be useful. Particularly preferred are glyceryl monostearate and glyceryl distearate.
[0029] Preferably, the composition comprises a moisturizer, particularly preferred moisturizers include petrolatum, aquaporin manipulating active agents, oat grain 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.
[0030] Some compositions may contain thickeners. These may be selected from cellulose derivatives, natural gums, and acrylic polymers, but are not limited by the type of thickener. Cellulose derivatives include sodium carboxymethylcellulose, hydroxyethylcellulose, hydroxypropylmethylcellulose, and combinations thereof. Suitable gums include xanthan, pectin, karaya, agar, alginate gum, and combinations thereof. Acrylic thickeners include homopolymers and copolymers of acrylic and methacrylic acid, such as carbomers such as Carbopol 1382, Carbopol 982, Ultrez, Aqua SF-1, and Aqua SF-2, available from Lubrizol Corporation. The amount of thickener can range from 0.01 to 3% by weight of the active polymer (excluding solvent or water) in the composition.
[0031] Additionally, the compositions of the present invention may further comprise 0.5 to 10% by weight of a sequestering agent such as tetrasodium ethylenediaminetetraacetic acid (EDTA), EHDP, or mixtures; an opacifying and pearlizing agent such as ethylene glycol distearate, titanium dioxide, or Lytron 621 (styrene / acrylate copolymer), all of which are useful for enhancing the appearance and properties of the product.
[0032] The composition may comprise water in an amount of from 10 to 96%, more preferably from 26 to 92%, even more preferably from 42 to 88%, and most preferably from 55 to 82% by weight of the composition.
[0033] Preferably, the composition is -1 When measured at a relatively high shear rate of 1000 mPa·s at 20°C, the viscosity is preferably at least 10 mPa·s, more preferably in the range of 30 to 10,000 mPa·s, even more preferably 50 to 5,000 mPa·s, and most preferably 100 to 2,000 mPa·s.
[0034] Preferably, the composition is an emulsion, more preferably an oil-in-water emulsion. Preferably, the composition is in fluid form at 25°C and atmospheric pressure.
[0035] 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 products and wash-off products, but is preferably a leave-on composition. The term "leave-on" used in relation to a composition herein means a composition that is applied to or rubbed into the skin and left on. The term "wash-off" used in relation to a composition herein means a skin cleanser that is applied to or rubbed into the skin and is washed off almost immediately after application. Preferably, skin care composition refers to a flowable liquid, and in particular refers to a moisturizer rather than a makeup product.
[0036] The term "skin" as used herein includes the skin of the face, neck, chest, abdomen, back, arms, armpits, hands, and feet. Preferably, "skin" includes the face and armpits, and more preferably, skin refers to the skin of the face other than the lips and eyelids. The composition particularly preferably refers to a moisturizer, not a makeup product.
[0037] Preferably, the composition is a topical composition. Preferably, the composition can be in the form of a cream, lotion, ointment, liquid, suspension, emulsion, paste, gel, powder, powder foundation, emulsion 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 means that the purpose is typically cosmetic, not curative or therapeutic.
[0039] Preferably, the composition is capable of increasing expression of the collagen type I alpha chain I (COL1A1) gene by at least 1.45 times, more preferably 1.55 to 5 times, most preferably 1.75 to 3.5 times, and most preferably 1.75 to 2.5 times, typically compared to a personal care composition that does not contain a carboxymethylcysteine compound or a retinoid.
[0040] The following examples are provided to facilitate understanding of the present invention and are not intended to limit the scope of the claims. [Example]
[0041] material [Table 1]
[0042] Example 1 This example demonstrates the synergistic anti-aging effect of combining lysine carboxymethyl cysteinate and retinyl propionate in a specific ratio.
[0043] Healthy human dermal fibroblasts (NHDFs) (Biocell, Xi'an, China, lot number: Fb20081902) were incubated in medium with or without active substances for 48 hours. After incubation, total RNA was extracted from each NHDF using RNAex Pro Reagent (Accurate Biotechnology, catalog number: AG21102) according to the manufacturer's protocol.
[0044] The extracted RNA was quantified using a Nanodrop spectrometer (Thermo Fisher Scientific, Waltham, MA, US) and reverse-transcribed to generate template cDNA using Evo M-MLV RT Premix for qPCR according to the manufacturer's protocol (Accurate Biotechnology, Catalog No. AG11706). Gene expression of the COL1A1 gene was analyzed by polymerase chain reaction (PCR) using the 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 regarding the relative expression of target genes were normalized to the ACTB gene. The percent change in expression was calculated relative to the blank control (medium without active substance). All tests were performed at least three times, and the percent change in gene expression of COL1A1 is shown in Table 1.
[0045] Table 1 [Table 2]
[0046] From Table 1, it is clear that COL1A1 expression was significantly elevated only when lysine carboxymethyl cysteinate and retinyl propionate were combined at a specific weight ratio of the present invention (I vs. G and E). In contrast, when retinyl propionate and lysine carboxymethyl cysteinate were combined at a weight ratio outside the range of the present invention, the elevation of COL1A1 expression was not significant (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. 2. The composition of claim 1, wherein the carboxymethylcysteine compound comprises carboxymethylcysteine, an ester of carboxymethylcysteine, and / or a salt of carboxymethylcysteine.
3. 3. The composition of claim 2, wherein the carboxymethylcysteine compound comprises a salt of carboxymethylcysteine, preferably wherein the carboxymethylcysteine compound comprises lysine carboxymethylcysteinate.
4. 4. The composition of any one of claims 1 to 3, wherein the carboxymethylcysteine compound is present in an amount of at least 0.00001% and no more than 10% by weight of the composition, preferably the carboxymethylcysteine compound is present in an amount of at least 0.01% and no more than 3% by weight of the composition.
5. The composition according to any one of claims 1 to 3, wherein the retinoid is selected from retinol, a retinyl ester or a mixture thereof, preferably the retinoid is retinyl propionate.
6. The composition according to any one of claims 1 to 3, wherein the amount of said retinoid ranges from 0.00001 to 10% by weight, preferably from 0.02 to 2% by weight of the total weight of the composition.
7. The composition according to any one of claims 1 to 3, 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 claims 1 to 3, wherein the weight ratio of lysine carboxymethyl cysteinate 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 claims 1 to 3, wherein the composition is an emulsion, preferably an oil-in-water emulsion.
10. The composition of any one of claims 1 to 3, wherein the composition is fluid at 25°C and atmospheric pressure.
11. A composition according to any one of claims 1 to 3, wherein the composition comprises water in an amount of from 10 to 96% by weight of the composition, preferably in an amount of from 42 to 88% by weight of the composition.
12. 10. A method for providing a skin benefit selected from the group consisting of promoting collagen production in the skin, improving skin elasticity, reducing the appearance of wrinkles, reducing sagging, anti-aging, and increasing the expression of collagen synthesis genes, the method comprising topically applying to the skin a composition according to any one of claims 1 to 3.
13. 4. Use of the composition of any one of claims 1 to 3 to provide a skin benefit selected from the group consisting of promoting collagen production in the skin, improving skin elasticity, reducing the appearance of wrinkles, reducing sagging, anti-aging, and increasing the expression of collagen synthesis genes.