Personal Care Compositions

Abstract

A personal care composition comprising a carboxymethylcysteine ​​compound and a resorcinol derivative is disclosed.

Description

[Technical Field]

[0001] The present invention relates to a personal care composition comprising a carboxymethylcysteine ​​compound and a resorcinol derivative. Surprisingly, it has been found that combining a carboxymethylcysteine ​​compound with a resorcinol derivative synergistically increases the expression of the TXNRD1 gene. [Background technology]

[0002] Human skin may provide physicochemical protection against environmental insults through its barrier function, mechanical strength, and water impermeability. Skin is constantly exposed to harmful environmental and extreme conditions, such as ultraviolet radiation, blue light, and pollution. Such harmful environmental exposure can cause excessive production of reactive oxygen species (ROS), thereby resulting in a state of oxidative stress. Oxidative stress can affect the skin in many ways, including signs of premature aging such as wrinkles, fine lines, and uneven skin tone.

[0003] Thioredoxin reductase 1 (TXNRD1) is an oxidoreductase encoded by the human TXNRD1 gene and a member of the antioxidant thioredoxin system. TXNRD1 plays an important role in oxidative stress regulation. TXNRD1 reduces and activates thioredoxin, an oxidoreductase containing a dithiol-disulfide active site. Thioredoxin binds ROS before they can harm cells, thus protecting cells from oxidative stress.

[0004] The present inventors have recognized the need to develop a personal care composition that can improve the expression of TXNRD1 gene. Therefore, the present inventors have developed a personal care composition comprising a carboxymethylcysteine ​​compound and a resorcinol derivative. Surprisingly, it has been found that the combination of a carboxymethylcysteine ​​compound and a resorcinol derivative synergistically increases the expression of TXNRD1 gene. Summary of the Invention

[0005] In a first aspect, the present invention relates to a personal care composition comprising a carboxymethylcysteine ​​compound and a resorcinol derivative.

[0006] In a second aspect, the present invention relates to a method for providing antioxidant and / or anti-aging benefits, reducing oxidative stress and / or upregulating expression of the thioredoxin reductase 1 gene, comprising topically applying to the skin a composition of the present invention.

[0007] In a third aspect, the present invention relates to the use of the composition of the present invention to provide antioxidant and / or anti-aging benefits, to reduce oxidative stress and / or to upregulate expression of the thioredoxin reductase 1 gene.

[0008] 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

[0009] Except in the examples, or where otherwise expressly indicated, all numbers herein expressing quantities of ingredients or reaction conditions, physical properties of ingredients and / or uses may be understood to be modified by the word "about."

[0010] All amounts are by weight of the composition unless otherwise specified.

[0011] It should be noted that in specifying any range of values, any particular upper limit value can be associated with any particular lower limit value.

[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] The disclosure of the present invention found herein should be considered to cover all embodiments found in the claims as being multiple dependent on one another, regardless of the fact that the claims may be found without multiple dependency or redundancy.

[0014] Where features are disclosed with respect to a particular embodiment of the invention (e.g., a composition of the invention), such disclosure should be deemed to 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 comprises carboxymethylcysteine, an ester of carboxymethylcysteine, and / or a salt of carboxymethylcysteine. More preferably, the carboxymethylcysteine ​​compound comprises carboxymethylcysteine ​​and / or a salt of carboxymethylcysteine. Even more preferably, the carboxymethylcysteine ​​compound comprises a salt of carboxymethylcysteine. Even more preferably, the carboxymethylcysteine ​​compound comprises carboxymethylcysteine ​​lysine, and most preferably, the carboxymethylcysteine ​​compound is carboxymethylcysteine ​​lysine.

[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, carboxymethylcysteine ​​lysine is present in an amount of 10% by weight or less of the composition, more preferably 5% by weight or less, even more preferably 3% by weight or less, even more preferably 1% by weight or less, and most preferably 0.5% by weight or less. Preferably, carboxymethylcysteine ​​lysine 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] As used herein, a resorcinol derivative refers to one in which at least one hydrogen atom on the ring structure and / or hydroxy group of resorcinol has been substituted, typically with an alkyl group and / or a phenylalkyl group. Preferably, the resorcinol derivative is a 4-substituted resorcinol, more preferably, the resorcinol derivative is a 4-alkylresorcinol, and even more preferably, the resorcinol derivative is a 4-C1-C2 alkylresorcinol. 12 The resorcinol derivatives useful in the present invention preferably have the following formula (I): [ka] wherein each R and R independently represents a hydrogen atom, a C-C 18In a preferred embodiment, R1 and R2 both represent hydrogen and R3 represents an alkyl group or a phenylalkyl group having 1 to 18 carbon atoms. More preferably, R1 and R2 both represent hydrogen and R3 represents an alkyl group or a phenylalkyl group having 2 to 12 carbon atoms.

[0019] Preferably, the resorcinol derivative comprises thiazolylresorcinol (thiamidol), 2-methylresorcinol, 4-chlororesorcinol, 4-methylresorcinol, 4-ethylresorcinol, 4-propylresorcinol, 4-butylresorcinol, 4-pentylresorcinol, 4-hexylresorcinol, 4-heptylresorcinol, 4-octylresorcinol, 4-nonylresorcinol, 4-decylresorcinol, phenylethylresorcinol, 4-acetylresorcinol, or mixtures thereof. More preferably, the resorcinol derivative comprises thiazolylresorcinol, 2-methylresorcinol, 4-chlororesorcinol, 4-methylresorcinol, 4-ethylresorcinol, 4-propylresorcinol, 4-butylresorcinol, 4-pentylresorcinol, 4-hexylresorcinol, 4-heptylresorcinol, 4-octylresorcinol, 4-nonylresorcinol, 4-decylresorcinol, phenylethylresorcinol, 4-acetylresorcinol, or a mixture thereof. Even more preferably, the resorcinol derivative is selected from 4-ethylresorcinol, 4-butylresorcinol, 4-hexylresorcinol, phenylethylresorcinol, or a mixture thereof. Even more preferably, the resorcinol derivative is selected from 4-ethylresorcinol, 4-hexylresorcinol, phenylethylresorcinol, or a combination thereof. Most preferably, the resorcinol derivative is 4-hexylresorcinol.

[0020] The amount of the resorcinol derivative is preferably 0.000001 to 8 wt %, more preferably 0.00001 to 4 wt %, even more preferably 0.0005 to 3 wt %, even more preferably 0.005 to 1 wt %, and most preferably 0.02 to 0.5 wt % of the total composition. Preferably, the amount of the 4-alkylresorcinol is 0.000001 to 8 wt %, more preferably 0.00001 to 4 wt %, even more preferably 0.0005 to 3 wt %, even more preferably 0.005 to 1 wt %, and most preferably 0.02 to 0.5 wt % of the total composition. Preferably, the amount of the 4-alkylresorcinol is 0.000001 to 8 wt %, more preferably 0.00001 to 4 wt %, even more preferably 0.0005 to 3 wt %, even more preferably 0.005 to 1 wt %, and most preferably 0.02 to 0.5 wt % of the total composition. Preferably, the amount of total 4-ethylresorcinol and 4-hexylresorcinol is in the range of 0.000001 to 8 wt.%, more preferably 0.00001 to 4 wt.%, even more preferably 0.0005 to 3 wt.%, even more preferably 0.005 to 1 wt.%, and most preferably 0.02 to 0.5 wt.% of the total composition. Preferably, the amount of 4-hexylresorcinol is in the range of 0.000001 to 8 wt.%, more preferably 0.00001 to 4 wt.%, even more preferably 0.0005 to 3 wt.%, even more preferably 0.005 to 1 wt.%, and most preferably 0.02 to 0.5 wt.% of the total composition.

[0021] Preferably, the weight ratio of the carboxymethylcysteine ​​compound to the resorcinol derivative is 1:40 to 1000:1, more preferably 1:12 to 200:1, even more preferably 1:3 to 50:1, even more preferably 1:1 to 20:1, and most preferably 2:1 to 8:1. Preferably, the weight ratio of the carboxymethylcysteine ​​compound to the 4-alkylresorcinol is 1:40 to 1000:1, more preferably 1:12 to 200:1, even more preferably 1:3 to 50:1, even more preferably 1:1 to 20:1, and most preferably 2:1 to 8:1. Preferably, 4-C 1-12The weight ratio of the carboxymethylcysteine ​​compound to the alkylresorcinol is 1:40 to 1000:1, more preferably 1:12 to 200:1, even more preferably 1:3 to 50:1, even more preferably 1:1 to 20:1, and most preferably 2:1 to 8:1.

[0022] Preferably, the weight ratio of carboxymethylcysteine ​​lysine to 4-alkylresorcinol is 1:40 to 1000:1, more preferably 1:12 to 200:1, even more preferably 1:3 to 50:1, even more preferably 1:1 to 20:1, and most preferably 2:1 to 8:1. Preferably, the weight ratio of carboxymethylcysteine ​​lysine to the total amount of 4-ethylresorcinol and 4-hexylresorcinol is 1:40 to 1000:1, more preferably 1:12 to 200:1, even more preferably 1:3 to 50:1, even more preferably 1:1 to 20:1, and most preferably 2:1 to 8:1. Preferably, the weight ratio of carboxymethyl cysteine ​​lysine to 4-hexylresorcinol is from 1:40 to 1000:1, more preferably from 1:12 to 200:1, even more preferably from 1:3 to 50:1, even more preferably from 1:1 to 20:1, and most preferably from 2:1 to 8:1.

[0023] The composition may contain a white pigment. The white pigment is typically a particle of a high refractive index material. For example, the white 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 white pigments include bismuth oxychloride, boron nitride, barium sulfate, mica, silica, titanium dioxide, zirconium oxide, aluminum oxide, zinc oxide, or a combination thereof. More preferred white pigments are particles containing titanium dioxide, zinc oxide, zirconium oxide, mica, iron oxide, or a combination thereof. Even more preferred white pigments are particles containing zinc oxide, zirconium oxide, titanium dioxide, or a combination thereof, since these materials have particularly high refractive indices. Even more preferably, the white 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 white pigment is typically between 15 nm and 1 micron, more preferably between 35 nm and 800 nm, even more preferably between 50 nm and 500 nm, and even more preferably between 100 and 300 nm. The amount of white pigment may be from 0.1 to 15% by weight of the composition, preferably from 0.5 to 5% by weight.

[0024] Preferably, the composition comprises a glutamate 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 glutamate source is present in an amount of 0.0001 to 10% by weight of the composition, more preferably 0.001 to 6% by weight, and even more preferably 0.01 to 3% by weight of the composition.

[0025] Preferably, the composition contains 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 between 2 and 10% by weight.

[0026] Preferably, the composition contains an emollient. Suitable emollients include silicones, hydrocarbons, triglycerides, or mixtures thereof. These silicones may be organic, silicone-containing, or fluorine-containing, volatile or nonvolatile, and polar or nonpolar. 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, cotton oil, canola oil, soybean oil, castor oil, borage oil, olive oil, shea butter, jojoba oil, and mixtures thereof. Mono- and diglycerides may also be useful. Glyceryl monostearate and glyceryl distearate are particularly preferred.

[0027] Preferably, the composition includes a moisturizer. Particularly preferred moisturizers include petrolatum, an aquaporin manipulating active, oat grain flour, a substituted urea such as hydroxyethyl urea, hyaluronic acid and / or its precursor N-acetylglucosamine, hyaluronic acid and / or its precursor N-acetylglucosamine, or mixtures thereof.

[0028] Some compositions may contain thickeners. These may be selected from cellulosics, natural gums, and acrylic polymers, but are not limited by the type of thickener. Cellulosics include sodium carboxymethylcellulose, hydroxyethylcellulose, hydroxypropylmethylcellulose, and combinations thereof. Suitable gums include xanthan gum, pectin gum, karaya gum, agar gum, alginate gum, and combinations thereof. Acrylic thickeners include homopolymers and copolymers of acrylic 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 thickener may range from 0.01 to 3% by weight of the active polymer (excluding solvent or water) in the composition.

[0029] 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; opacifiers and pearlescent agents, such as ethylene glycol distearate, titanium dioxide, or Lytron 621 (styrene / acrylate copolymer), all of which are useful for improving the appearance or properties of the product.

[0030] The composition may comprise water in an amount of from 10 to 96% by weight of the composition, more preferably from 25 to 92% by weight, even more preferably from 42 to 88% by weight, and most preferably from 55 to 82% by weight of the composition.

[0031] Preferably, the composition is mixed for about 20 seconds.-1 The composition has a viscosity of 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, when measured at a relatively high shear rate of 100 mPa·s at 20° C. Preferably, the composition is in the form of a fluid.

[0032] Preferably, the composition is an emulsion, more preferably an oil-in-water emulsion. Preferably, the composition is a flowable liquid at 25°C and atmospheric pressure.

[0033] 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, preferably leave-on compositions.The term "leave-on" used in relation to the composition herein means a composition that is applied to the skin or rubbed onto the skin and left on.The term "wash-off" used in relation to the composition herein means a skin cleanser that is applied to the skin or rubbed onto the skin and rinsed off substantially immediately after application.The term "skin" used in relation to the composition 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, and more preferably, skin refers to the skin of the face other than the lips and eyelids.It is particularly preferred that the composition is a moisturizer rather than a makeup product.

[0034] 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 spray.

[0035] Preferably, the use is non-therapeutic. Preferably, the method is non-therapeutic. The term non-therapeutic typically refers to cosmetic purposes, not curative or therapeutic purposes.

[0036] Preferably, the composition is capable of upregulating expression of the thioredoxin reductase 1 (TXNRD1) gene by at least a fold change of 1.3, more preferably a fold change of 1.4 to 5, most preferably a fold change of 1.5 to 3.5, and most preferably a fold change of 1.6 to 2.5, typically compared to a personal care composition that does not contain a carboxymethylcysteine ​​compound or a resorcinol derivative.

[0037] The following examples are provided to facilitate understanding of the invention and are not intended to limit the scope of the claims.

[0038] [Example] [Table 1]

[0039] [Example 1] This example demonstrates the synergistic upregulation of gene expression by combining carboxymethyl cysteine ​​lysine and 4-hexylresorcinol.

[0040] Normal human epidermal keratinocytes (NHEK, lot: NHS-2021-006) (Archgene Biotechnology, Shanghai, China) were incubated in medium with or without active substances for 24 hours. After incubation, total RNA from each NHEK was extracted using the Qiagen Mini RNeasy kit (Qiagen, catalog 74106) according to the manufacturer's protocol.

[0041] The extracted RNA was quantified using a Nanodrop 2000 spectrometer (Thermo Fisher Scientific, Waltham, MA, USA) and reverse-transcribed to generate template cDNA using ABScript III RT Master Mix (catalog BK20428, ABclonal) according to the manufacturer's protocol. Amplification of the gene encoding TXNRD1 (thioredoxin reductase 1) was performed using RT-PCR reagents (Universal SYBR Green Fast qPCR Mix Kit, catalog RK21203, ABclonal) on an ABI Vii 7 Real-Time PCR System (Applied Biosystems, Thermo Fisher Scientific, Carlsbad, CA, USA). The tyrosine 3-monooxygenase / tryptophan 5-monooxygenase-activating protein ζ gene (YWHAZ) was selected as a housekeeping gene, and all data regarding the relative expression of target genes were normalized to YWHAZ. The fold change in expression was calculated relative to the blank control (medium without active substances). All tests were performed at least three times, and Table 1 shows the fold change in gene expression of TXNRD1. [Table 2]

[0042] As shown in Table 1, surprisingly, the fold change when carboxymethylcysteine ​​lysine and 4-hexylresorcinol were combined was found to be significantly higher than the fold change results for carboxymethylcysteine ​​lysine alone and 4-hexylresorcinol alone. TXNRD1 gene expression was synergistically upregulated by the combination of carboxymethylcysteine ​​lysine and 4-hexylresorcinol.

Claims

1. A personal care or pharmaceutical composition comprising a resorcinol derivative and a carboxymethylcysteine ​​compound.

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 carboxymethylcysteine ​​lysine.

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 resorcinol derivative is a 4-alkylresorcinol, preferably a 4-C １－１２ The composition of any one of claims 1 to 4, which is an alkylresorcinol.

6. 6. The composition according to any one of claims 1 to 5, wherein the amount of the resorcinol derivative is preferably in the range of 0.000001 to 8% by weight, preferably 0.0005 to 3% by weight, more preferably 0.02 to 0.5% by weight of the total amount of the composition.

7. 7. The composition of any one of claims 1 to 6, wherein the resorcinol derivative is selected from 4-ethylresorcinol, 4-hexylresorcinol, or a combination thereof, more preferably the resorcinol derivative is 4-hexylresorcinol.

8. 8. The composition of claim 7, wherein the amount of 4-hexylresorcinol ranges from 0.00001 to 4% by weight, preferably 0.02 to 0.5% by weight, of the total amount of the composition.

9. 9. The composition of any one of claims 1 to 8, wherein the weight ratio of the carboxymethylcysteine ​​compound to the resorcinol derivative is from 1:40 to 1000:1, more preferably from 2:1 to 8:

1.

10. 10. The composition of any one of claims 7 to 9, wherein the weight ratio of said carboxymethyl cysteine ​​lysine to said 4-hexylresorcinol is from 1:40 to 1000:1, more preferably from 1:1 to 20:

1.

11. The composition according to any one of claims 1 to 10, wherein the composition is an emulsion, preferably an oil-in-water emulsion.

12. The composition of any one of claims 1 to 11, wherein the composition is a flowable liquid at 25°C and atmospheric pressure.

13. A composition according to any preceding claim, 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.

14. 14. A method of providing antioxidant and / or anti-aging benefits, reducing oxidative stress and / or upregulating expression of the thioredoxin reductase 1 gene, comprising topically applying to the skin a composition according to any one of claims 1 to 13.

15. 13. Use of a composition according to any one of claims 1 to 12 to provide antioxidant and / or anti-aging benefits, to reduce oxidative stress and / or to upregulate expression of the thioredoxin reductase 1 gene.

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