Personal care composition

Abstract

The present application discloses a personal care comprising a carboxymethyl cysteine compound and a resorcinol derivative.

Description

Technical Field

[0001] The present invention relates to a personal care composition comprising a carboxymethylcysteine compound and a resorcinol derivative. It has surprisingly been found that by combining a carboxymethylcysteine compound with a resorcinol derivative, the expression of the TXNRD1 gene is synergistically increased. Background Art

[0002] Human skin can provide physicochemical protection against environmental damage through its barrier function, mechanical strength, and impermeability to water. It is frequently exposed to harmful environments and extreme conditions such as ultraviolet radiation, blue light, pollution, etc. Such harmful environmental exposures may lead to the overproduction of reactive oxygen species (ROS), resulting in oxidative stress conditions. Oxidative stress can affect our skin in many ways, including signs of premature aging such as wrinkles, fine lines, and uneven skin tone.

[0003] Thioredoxin reductase 1 (TXNRD1) is a redox enzyme encoded by the TXNRD1 gene in humans and is a member of the antioxidant thioredoxin system. TXNRD1 plays an important role in the control of oxidative stress. It reduces and activates thioredoxin, which is a redox enzyme containing a dithiol-disulfide active site. Thioredoxin binds to ROS before ROS can damage cells, thus protecting cells from oxidative stress.

[0004] The inventors have recognized the need to develop personal care compositions that can improve the gene expression of TXNRD1. Accordingly, the inventors have developed a personal care composition comprising a carboxymethylcysteine compound and a resorcinol derivative. It has surprisingly been found that by combining a carboxymethylcysteine compound with a resorcinol derivative, the expression of the TXNRD1 gene is synergistically increased. 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 of providing antioxidant and / or anti-aging benefits, reducing oxidative stress, and / or upregulating the gene expression of thioredoxin reductase 1, the method comprising the step of topically applying the composition of the present invention to the skin.

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

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

[0010] Unless otherwise indicated in the Examples or specifically stated otherwise, all numbers in this specification indicating amounts of materials or reaction conditions, physical properties of materials, and / or uses may optionally be understood to be modified by the word "about".

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

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

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

[0014] The disclosure of the present invention as found herein is considered to cover all embodiments as found in the claims as they cross-reference each other, regardless of the fact that the claims may be found to be without cross-reference or redundant.

[0015] In the case of disclosing features with respect to a particular aspect of the present invention (e.g., a composition of the present invention), such disclosure is also considered applicable to any other aspect of the present invention (e.g., a method of the present invention) with necessary modifications.

[0016] 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 contains a salt of carboxymethylcysteine. Still even more preferably, the carboxymethylcysteine compound contains lysine carboxymethylcysteine salt, and most preferably, the carboxymethylcysteine compound is lysine carboxymethylcysteine salt.

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

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

[0019] As used herein, a resorcinol derivative refers to a compound in which at least one hydrogen on the ring structure and / or hydroxyl group of resorcinol is substituted, usually by an alkyl and / or 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-C 12 alkylresorcinol. The resorcinol derivative useful in the present invention preferably has the following formula (I):

[0020]

[0021] wherein each of R1 and R2 independently represents a hydrogen atom, a C1-C 18 alkyl group, and R3 represents an alkyl group or a phenylalkyl group having 1 to 18 carbon atoms. In a preferred embodiment, both R1 and R2 represent hydrogen, and R3 represents an alkyl group or a phenylalkyl group having 1-18 carbon atoms. More preferably, both R1 and R2 represent hydrogen, and R3 represents an alkyl group or a phenylalkyl group having 2 to 12 carbon atoms.

[0022] Preferably, the resorcinol derivative includes thiazolyl resorcinol (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 a mixture thereof. More preferably, the resorcinol derivative includes thiazolyl resorcinol, 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. Still even more preferably, the resorcinol derivative is selected from 4-ethylresorcinol, 4-hexylresorcinol, or a combination thereof. Most preferably, the resorcinol derivative is 4-hexylresorcinol.

[0023] The amount of the resorcinol derivative is preferably 0.000001 - 8% by weight of the total amount of the composition, more preferably 0.00001 - 4% by weight, even more preferably 0.0005 - 3% by weight, still even more preferably 0.005 - 1% by weight, and most preferably 0.02 - 0.5% by weight. Preferably, the amount of 4-alkylresorcinol is 0.000001 to 8% by weight of the total amount of the composition, more preferably 0.00001 to 4% by weight, even more preferably 0.0005 to 3% by weight, still even more preferably 0.005 to 1% by weight, and most preferably 0.02 to 0.5% by weight. Preferably, the amount of 4-alkylresorcinol is 0.000001 to 8% by weight of the total amount of the composition, more preferably 0.00001 to 4% by weight, even more preferably 0.0005 to 3% by weight, still even more preferably 0.005 to 1% by weight, and most preferably 0.02 to 0.5% by weight. Preferably, the total amount of 4-ethylresorcinol and 4-hexylresorcinol is 0.000001 to 8% by weight of the total amount of the composition, more preferably 0.00001 to 4% by weight, even more preferably 0.0005 to 3% by weight, still even more preferably 0.005 to 1% by weight, and most preferably 0.02 to 0.5% by weight. Preferably, the amount of 4-hexylresorcinol is 0.000001 to 8% by weight of the total amount of the composition, more preferably 0.00001 to 4% by weight, even more preferably 0.0005 to 3% by weight, still even more preferably 0.005 to 1% by weight, and most preferably 0.02 to 0.5% by weight.

[0024] Preferably, the weight ratio of the carboxymethylcysteine compound to the resorcinol derivative is from 1:40 to 1000:1, more preferably from 1:12 to 200:1, even more preferably from 1:3 to 50:1, still even more preferably from 1:1 to 20:1, and most preferably from 2:1 to 8:1. Preferably, the weight ratio of the carboxymethylcysteine compound to the 4-alkylresorcinol is from 1:40 to 1000:1, more preferably from 1:12 to 200:1, even more preferably from 1:3 to 50:1, still even more preferably from 1:1 to 20:1, and most preferably from 2:1 to 8:1. Preferably, the carboxymethylcysteine compound and 4-C 1-12 The weight ratio of the alkylresorcinol is from 1:40 to 1000:1, more preferably from 1:12 to 200:1, even more preferably from 1:3 to 50:1, still even more preferably from 1:1 to 20:1, and most preferably from 2:1 to 8:1.

[0025] Preferably, the weight ratio of lysine carboxymethylcysteine salt to 4-alkylresorcinol is from 1:40 to 1000:1, more preferably from 1:12 to 200:1, even more preferably from 1:3 to 50:1, still even more preferably from 1:1 to 20:1, and most preferably from 2:1 to 8:1. Preferably, the weight ratio of lysine carboxymethylcysteine salt to the total amount of 4-ethylresorcinol and 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, still even more preferably from 1:1 to 20:1, and most preferably from 2:1 to 8:1. Preferably, the weight ratio of lysine carboxymethylcysteine salt 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.

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

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

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

[0029] Preferably, the composition comprises an emollient material. Suitable emollient materials include silicones, hydrocarbons, triglycerides, or mixtures thereof. These silicones can be organic, silicone-containing, or fluorine-containing, volatile or non-volatile, polar or non-polar. Hydrocarbons can include mineral oil, petrolatum, and polyalphaolefins. Examples of preferred volatile hydrocarbons include polydecane, 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 but non-limiting triglycerides are sunflower oil, cottonseed oil, canola oil, soybean oil, castor oil, borage oil, olive oil, shea butter, jojoba oil, and mixtures thereof. Monoglycerides and diglycerides can also be used. Particularly preferred are glycerol monostearate and glycerol distearate.

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

[0031] Some compositions may contain a thickening agent. These can be selected from cellulose, natural gums, and acrylic polymers, but are not limited to these thickening agent types. Cellulose types include sodium carboxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl methyl cellulose, and combinations thereof. Suitable gums include xanthan gum, pectin, karaya gum, agar, alginate gums, and combinations thereof. Acrylic thickening agents are homopolymers and copolymers of acrylic acid and methacrylic acid, including carbomers, such as Carbopol 1382, Carbopol 982, Ultrez, Aqua SF-1, and Aqua SF-2 available from Lubrizol Corporation. The amount of the thickening agent can be 0.01-3% by weight of the active polymer (other than solvent or water) in the composition.

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

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

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

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

[0036] Preferably, the personal care composition is a skin care composition. A skin care composition refers to a composition suitable for topical application to human skin, including leave-on and rinse-off products, but preferably leave-on compositions. The term "leave-on" as used herein with respect to the compositions of this invention refers to a composition that is applied to the skin or rubbed on the skin and remains on the skin. The term "rinse-off" as used herein with respect to the compositions of this invention refers to a skin cleanser that is applied to the skin or rubbed on the skin and is rinsed off substantially immediately after application. As used herein, the term "skin" includes the skin on the face, neck, chest, abdomen, back, arms, underarms, hands and legs. Preferably, "skin" is meant to include the skin on the face and underarms, and more preferably, skin is meant to include the skin on the face except for the lips and eyelids. The composition is particularly preferably a moisturizer rather than a cosmetic product.

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

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

[0039] Preferably, compared to a personal care composition that contains neither a carboxymethylcysteine compound nor a resorcinol derivative, the composition is capable of upregulating the expression of the thioredoxin reductase 1 (TXNRD1) gene by at least a 1.3-fold change, more preferably a 1.4- to 5-fold change, most preferably a 1.5- to 3.5-fold change, and most preferably a 1.6- to 2.5-fold change.

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

[0041] Examples

[0042] Materials

[0043]

[0044] Example 1

[0045] This example demonstrates that by combining lysine carboxymethyl cysteine and 4-hexylresorcinol, gene expression can be synergistically upregulated.

[0046] Normal human epidermal keratinocytes (NHEK, lot number Lot: NHS-2021-006) (Archgene Biotechnology, Shanghai, China) were incubated in medium with or without the active ingredient for 24 hours. After incubation, total RNA of each NHEK was extracted using the Qiagen Mini RNeasy kit (Qiagen, Cat. 74106) according to the manufacturer's protocol.

[0047] The extracted RNA was quantified using a Nanodrop 2000 spectrometer (Thermo Fisher Scientific, Waltham, MA, US), and reverse transcription was performed using ABScript III RT Mast Mix (Cat. BK20428, ABclonal) according to the manufacturer's protocol to generate template cDNA. The gene encoding the TXNRD1 (thioredoxin reductase 1) gene was amplified using RT-PCR reagents (Universal SYBR Green Fast qPCR Mix kit, Cat.: 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 activation protein zeta gene (YWHAZ) was selected as the housekeeping gene, and all data on the relative expression of the target gene were normalized to YWHAZ. The fold change in expression was calculated relative to the blank control (medium without the active ingredient). All experiments were performed at least three times, and Table 1 shows the fold change in TXNRD1 gene expression.

[0048] Table 1

[0049]

[0050] #: Based on the level of the active ingredient in the medium.

[0051] a: Significantly better than (p < 0.05) either of the single active ingredients at the same level.

[0052] As shown in Table 1, it was surprisingly found that the fold change when lysine carboxymethyl cysteine and 4-hexylresorcinol were combined was significantly higher than the product of the fold changes of lysine carboxymethyl cysteine alone and 4-hexylresorcinol alone. By combining lysine carboxymethyl cysteine and 4-hexylresorcinol, the expression of the TXNRD1 gene was synergistically upregulated.

Claims

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

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

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

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

5. The composition according to any one of the preceding claims, wherein the resorcinol derivative is 4-alkylresorcinol, preferably 4-C 1-12 alkylresorcinol.

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

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

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

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

1.

10. The composition according to any one of claims 7-9, wherein the weight ratio of the lysine carboxymethylcysteine salt to the 4-hexylresorcinol is from 1:40 to 1000:1, and more preferably from 1:1 to 20:

1.

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

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

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

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

15. Use of the composition according to any one of claims 1-12 preceding for providing antioxidant and / or anti-aging benefits, reducing oxidative stress and / or upregulating the expression of the thioredoxin reductase 1 gene.

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