WO2023126169A1 - Use of carboxymethyl cysteine compound - Google Patents
Use of carboxymethyl cysteine compound Download PDFInfo
- Publication number
- WO2023126169A1 WO2023126169A1 PCT/EP2022/085612 EP2022085612W WO2023126169A1 WO 2023126169 A1 WO2023126169 A1 WO 2023126169A1 EP 2022085612 W EP2022085612 W EP 2022085612W WO 2023126169 A1 WO2023126169 A1 WO 2023126169A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- skin
- carboxymethyl cysteine
- carboxymethyl
- inflammation
- composition
- Prior art date
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Classifications
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- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
- A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
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- A—HUMAN NECESSITIES
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
- A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
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- A—HUMAN NECESSITIES
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- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/10—Anti-acne agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
- A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q5/00—Preparations for care of the hair
- A61Q5/006—Antidandruff preparations
Definitions
- the present invention relates to new use of carboxymethyl cysteine compound or a personal care composition comprising carboxymethyl cysteine compound.
- Inflammation may cause various personal care problems including gingivitis/periodontitis (in the oral cavity), dandruff (on scalp/ hair) and eczema/acnes (on skin).
- gingivitis/periodontitis in the oral cavity
- dandruff on scalp/ hair
- eczema/acnes on skin.
- the carboxymethyl cysteine compound is capable of providing a skin brightening and/or exhibiting an improved effect for inhibiting release of pro-inflammatory mediators.
- the present invention is directed to use of carboxymethyl cysteine compound or a personal care composition comprising carboxymethyl cysteine compound for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin.
- the present invention is directed to carboxymethyl cysteine compound or a personal care composition comprising carboxymethyl cysteine compound for use in the treatment for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin.
- the present invention is directed to use of a personal care composition for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin
- the personal care composition comprises carboxymethyl cysteine compound as agent for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin.
- the present invention is directed to a method for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin comprising topical application of a personal care composition comprising a carboxymethyl cysteine compound.
- the present invention is directed to use of carboxymethyl cysteine compound in a method for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin, the method comprising topical application of a cosmetic composition comprising the carboxymethyl cysteine compound.
- the present invention is directed to use of a carboxymethyl cysteine compound in the manufacture of medicants for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin.
- 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.
- the carboxymethyl cysteine compound comprises carboxymethyl cysteine, ester of carboxymethyl cysteine, and/or salt of carboxymethyl cysteine.
- the carboxymethyl cysteine compound comprises carboxymethyl cysteine, and/or salt of carboxymethyl cysteine.
- carboxymethyl cysteine compound comprises salt of carboxymethyl cysteine.
- the carboxymethyl cysteine compound comprises lysine carboxymethyl cysteinate and most preferably, the carboxymethyl cysteine compound is lysine carboxymethyl cysteinate.
- 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.
- 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.
- 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.
- 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.
- the use is non-therapeutic.
- the method is non-therapeutic.
- non-therapeutic typically means for cosmetic purposes and not curative or therapeutic purposes.
- the personal care composition of the present invention typically provides a greater benefit for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin in comparison to a personal care composition that does not contain carboxymethyl cysteine compound.
- the benefit is selected from anti-inflammation, anti-aging, skin brightening or a combination thereof.
- the carboxymethyl cysteine compound is used as agent for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin in the personal care composition.
- skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin in the personal care composition.
- the present invention provides use of lysine carboxymethyl cysteinate or a personal care composition comprising lysine carboxymethyl cysteinate for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin.
- a personal care composition comprising lysine carboxymethyl cysteinate for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin.
- the present invention provides lysine carboxymethyl cysteinate or a personal care composition comprising lysine carboxymethyl cysteinate for use in the treatment for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin.
- skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin.
- the present invention provides use of a personal care composition for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin
- the personal care composition comprises lysine carboxymethyl cysteinate as agent for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin.
- the present invention provides a method for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin comprising topical application of a personal care composition comprising lysine carboxymethyl cysteinate.
- the present invention provides use of lysine carboxymethyl cysteinate in a method for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin, the method comprising topical application of a cosmetic composition comprising the lysine carboxymethyl cysteinate.
- the present invention provides use of a lysine carboxymethyl cysteinate in the manufacture of medicants for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin.
- a skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin.
- the lysine carboxymethyl cysteinate is used as agent for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin in the personal care composition.
- the personal care composition comprising lysine carboxymethyl cysteinate typically provides a greater benefit for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin in comparison to a personal care composition that does not contain lysine carboxymethyl cysteinate.
- the composition comprises Vitamin B3 compounds (including derivatives of vitamin B3).
- the vitamin B3 compounds comprises niacin, nicotinic acid, niacinamide or a mixture thereof.
- the most preferred vitamin B3 compound is niacinamide.
- Amount of Vitamin B3 compounds may be 0.1 to 10%, preferably 0.5 to 5% by weight of the composition.
- 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.
- 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.
- the composition may optionally comprise whitening pigment.
- Whitening pigments are typically particles of high refractive index materials.
- 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.
- 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.
- 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.
- the composition comprises moisturizing agents.
- 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.
- compositions may include thickeners. These may be selected from cellulosics, natural gums and acrylic polymers but not limited by this thickening agent types.
- cellulosics sodium carboxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl methylcellulose and combinations thereof.
- Suitable gums include xanthan, pectin, karaya, agar, alginate gums and combinations thereof.
- 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.
- 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.
- 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.
- the composition may 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.
- 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 .
- the composition is in the form of fluid.
- the composition is an emulsion, more preferably an oil-in-water emulsion.
- the 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.
- leave-on as used with reference to compositions herein means a composition that is applied to or rubbed on the skin, and left thereon.
- 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 skin care composition means a fluid liquid, and particularly a moisturizer rather than a make-up product.
- the personal care composition is a skin care composition.
- skin as used herein includes the skin on the face, neck, chest, abdomen, back, arms, under arms, hands, and legs.
- skin means includes the skin on the face and under arms, more preferably skin means skin on the face other than lips and eyelids.
- This Example demonstrates skin brightening effect and anti-aging effect of lysine carboxymethyl cysteinate.
- the skin brightening efficacy were evaluated by using MelaKuits® living skin equivalent models (Biocell, Xi’an, China). A series of identical living skin equivalent models were constructed by following manufacturer’s instruction. After the models were constructed, the models were irradiated by UVB with an energy density of 50 mJ/cm 2 , followed by culturing in the fresh medium either together with active or without active for one day. Such irradiating and culturing process were repeated by using refreshed same medium for seven times. The lightness (L*) of each model was measured by using a DSM II Color Meter. The measurements of lightness were repeated at least three times.
- the live tissues of each skin model were detached by 0.25% trypsin to form a mixture.
- the mixture was centrifuged at 2000 r/min at low temperature.
- the pellets were lysed by lysis buffer at 80°C.
- the lysates were then transferred to a new 96-well plate and absorbance was measured at 405 nm using a TECAN plate reader.
- Serial dilutions of pure melanin were prepared as references. The melanin content was calculated from the melanin standard curve.
- IL1a interleukin 1a
- PGE2 prostaglandin E2
- IL1 a and PGE2 are both pro-inflammatory mediators.
- concentrations of IL1 a and PGE2 in the medium were determined using commercial DY200 and PGE2 Enzyme-linked immunosorbent assay (ELISA) kits (both from R&D systems, Minneapolis, USA).
- lysine carboxymethyl cysteinate is capable of inhibiting I L1 a and PGE2 and therefore reducing or preventing inflammation of the skin.
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Abstract
Disclosed is use of carboxymethyl cysteine compound or a personal care composition comprising carboxymethyl cysteine compound for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin.
Description
USE OF CARBOXYMETHYL CYSTEINE COMPOUND
Field of the Invention
The present invention relates to new use of carboxymethyl cysteine compound or a personal care composition comprising carboxymethyl cysteine compound.
Background of the Invention
Many consumers are concerned with the characteristics of their skin. For example, consumers may wish to reduce skin darkening caused by exposure to sunlight or to lighten their natural skin color. Other consumer may wish to reduce skin inflammatory problems.
Inflammation may cause various personal care problems including gingivitis/periodontitis (in the oral cavity), dandruff (on scalp/ hair) and eczema/acnes (on skin). The skin experiences many conditions like aging, pigmentation, photo-damage, and skin irritation which are all accompanied by inflammation. Additionally, inflammation has been implicated in many problems like skin wrinkling, acne, age spots, eczema, dandruff, and hyper-pigmentation.
Many attempts have been made to develop products that improve skin characteristics. The products developed thus far, however, often tend to have low efficacy or undesirable side effects, such as, for example, toxicity or skin irritation.
The present inventors have acknowledged that there is an increasing interest and therefore developed new actives to deliver skin benefit. It was surprisingly found that the carboxymethyl cysteine compound is capable of providing a skin brightening and/or exhibiting an improved effect for inhibiting release of pro-inflammatory mediators.
Summary of the Invention
In a first aspect, the present invention is directed to use of carboxymethyl cysteine compound or a personal care composition comprising carboxymethyl cysteine compound for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin.
In a second aspect, the present invention is directed to carboxymethyl cysteine compound or a personal care composition comprising carboxymethyl cysteine compound for use in the treatment
for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin.
In a third aspect, the present invention is directed to use of a personal care composition for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin, wherein the personal care composition comprises carboxymethyl cysteine compound as agent for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin.
In a fourth aspect, the present invention is directed to a method for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin comprising topical application of a personal care composition comprising a carboxymethyl cysteine compound.
In a fifth aspect, the present invention is directed to use of carboxymethyl cysteine compound in a method for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin, the method comprising topical application of a cosmetic composition comprising the carboxymethyl cysteine compound.
In a sixth aspect, the present invention is directed to use of a carboxymethyl cysteine compound in the manufacture of medicants for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin.
All other aspects of the present invention will more readily become apparent upon considering the detailed description and examples which follow.
Detailed Description of the Invention
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”.
All amounts are by weight of the composition, unless otherwise specified.
It should be noted that in specifying any range of values, any particular upper value can be associated with any particular lower value.
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.
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.
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.
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.
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.
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.
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.
The personal care composition of the present invention typically provides a greater benefit for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin in comparison to a personal care composition that does not contain carboxymethyl cysteine compound.
Preferably the benefit is selected from anti-inflammation, anti-aging, skin brightening or a combination thereof.
Preferably, the carboxymethyl cysteine compound is used as agent for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin in the personal care composition.
Preferably, the present invention provides use of lysine carboxymethyl cysteinate or a personal care composition comprising lysine carboxymethyl cysteinate for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin.
Preferably, the present invention provides lysine carboxymethyl cysteinate or a personal care composition comprising lysine carboxymethyl cysteinate for use in the treatment for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin.
Preferably, the present invention provides use of a personal care composition for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin, wherein the personal care composition comprises lysine carboxymethyl cysteinate as agent for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin.
Preferably, the present invention provides a method for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin comprising topical application of a personal care composition comprising lysine carboxymethyl cysteinate.
Preferably, the present invention provides use of lysine carboxymethyl cysteinate in a method for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin, the method comprising topical application of a cosmetic composition comprising the lysine carboxymethyl cysteinate.
Preferably, the present invention provides use of a lysine carboxymethyl cysteinate in the manufacture of medicants for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin.
Preferably, the lysine carboxymethyl cysteinate is used as agent for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin in the personal care composition.
The personal care composition comprising lysine carboxymethyl cysteinate typically provides a greater benefit for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin in comparison to a personal care composition that does not contain lysine carboxymethyl cysteinate.
Preferably, the composition comprises Vitamin B3 compounds (including derivatives of vitamin B3). The vitamin B3 compounds comprises niacin, nicotinic acid, niacinamide or a mixture thereof. The most preferred vitamin B3 compound is niacinamide. Amount of Vitamin B3 compounds may be 0.1 to 10%, preferably 0.5 to 5% by weight of the composition.
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.
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.
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.
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.
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.
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.
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.
The composition may 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.
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. Preferably, the composition is in the form of fluid.
Preferably, the composition is an emulsion, more preferably an oil-in-water emulsion. The 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. Preferably the skin care composition means a fluid liquid, and particularly a moisturizer rather than a make-up product.
Preferably, the personal care composition is a skin care composition. 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 following examples are provided to facilitate an understanding of the invention. The examples are not intended to limit the scope of the claims.
Examples
Materials
Example 1
This Example demonstrates skin brightening effect and anti-aging effect of lysine carboxymethyl cysteinate.
The skin brightening efficacy were evaluated by using MelaKuits® living skin equivalent models (Biocell, Xi’an, China). A series of identical living skin equivalent models were constructed by following manufacturer’s instruction. After the models were constructed, the models were irradiated by UVB with an energy density of 50 mJ/cm2, followed by culturing in the fresh medium either together with active or without active for one day. Such irradiating and culturing process were repeated by using refreshed same medium for seven times. The lightness (L*) of each model was measured by using a DSM II Color Meter. The measurements of lightness were repeated at least three times.
After the measurement of lightness, the live tissues of each skin model were detached by 0.25% trypsin to form a mixture. The mixture was centrifuged at 2000 r/min at low temperature. The pellets were lysed by lysis buffer at 80°C. The lysates were then transferred to a new 96-well plate and absorbance was measured at 405 nm using a TECAN plate reader. Serial dilutions of pure melanin were prepared as references. The melanin content was calculated from the melanin standard curve.
The medium from each model was collected to measure the interleukin 1a (IL1a) and prostaglandin E2 (PGE2) secretion. IL1 a and PGE2 are both pro-inflammatory mediators. The concentrations of IL1 a and PGE2 in the medium were determined using commercial DY200 and PGE2 Enzyme-linked immunosorbent assay (ELISA) kits (both from R&D systems, Minneapolis, USA).
Each test was repeated at least three times. The results of lightness and melanin content were summarised in Table 1 and the results of concentrations of I L1 a and PGE2 were summarised in Table 2.
Table 1
#: the concentration of LCC is based on the medium, a: Significant different with those for model 2 (p<0.05). As indicated in Table 1, it was surprisingly found that lysine carboxymethyl cysteinate is capable of improving the lightness and reducing the level of melanin.
Table 2
*Significant different with those for model 2 (p<0.05).
As indicated in Table 2, it was surprisingly found that lysine carboxymethyl cysteinate is capable of inhibiting I L1 a and PGE2 and therefore reducing or preventing inflammation of the skin.
Claims
1. Use of carboxymethyl cysteine compound or a personal care composition comprising carboxymethyl cysteine compound for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin.
2. The use according to claim 1 wherein the carboxymethyl cysteine compound comprises carboxymethyl cysteine, ester of carboxymethyl cysteine, and/or salt of carboxymethyl cysteine.
3. The use 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 use 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 use according to any one of the preceding claims wherein the composition is an emulsion, preferably an oil-in-water emulsion.
6. The use according to any one of the preceding claims wherein the composition comprises water in amount of 10 to 96% by weight of the composition, preferably from 42 to 88% by weight of the composition.
7. The use according to any one of the preceding claims is non-therapeutic.
8. The use according to any one of the preceding claims wherein the carboxymethyl cysteine compound is used as agent for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin in the personal care composition.
9. The use according to any one of the preceding claims wherein the personal care composition provides a greater benefit for alleviating, inhibiting and/or reducing at least one skin conditions
selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin in comparison to a personal care composition that does not contain the carboxymethyl cysteine compound. A carboxymethyl cysteine compound or a personal care composition comprising carboxymethyl cysteine compound for use in the treatment for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin. Use of a personal care composition for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin, wherein the personal care composition comprises carboxymethyl cysteine compound as agent for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin. A method for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin comprising topical application of a personal care composition comprising a carboxymethyl cysteine compound. The method according to claim 12 is non-therapeutic. Use of carboxymethyl cysteine compound in a method for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin, the method comprising topical application of a cosmetic composition comprising the carboxymethyl cysteine compound. Use of a carboxymethyl cysteine compound in the manufacture of medicants for alleviating, inhibiting and/or reducing at least one skin conditions selected from inflammation, gingivitis, periodontitis, dandruff, pigmentation, hyperpigmentation, discoloration, age spots, acne and eczema; and/or brightening skin.
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| CNPCT/CN2021/143515 | 2021-12-31 | ||
| CN2021143515 | 2021-12-31 | ||
| EP22153547 | 2022-01-27 | ||
| EP22153547.9 | 2022-01-27 |
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| US4217914A (en) * | 1974-05-16 | 1980-08-19 | L'oreal | Quaternized polymer for use as a cosmetic agent in cosmetic compositions for the hair and skin |
| US6153649A (en) * | 1995-10-30 | 2000-11-28 | L'oreal | Use of carboxylic acids having a sulphur function for promoting skin exfoliation or stimulating epidermal regeneration |
| US20090062340A1 (en) * | 2002-11-19 | 2009-03-05 | Galderma Research & Development | Novel biaromatic compounds which activate ppary type receptors and cosmetic/pharmaceutical compositions comprised thereof |
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