Composition for lightening and / or whitening keratinous materials - Patents.com
The composition, featuring a hydrophilic phase with specific glycol and surfactant components, addresses the poor penetration issue of lightening and whitening agents in conventional emulsions, thereby enhancing skin lightening and whitening effects.
Patent Information
- Application Number
- JP2023538126
- Authority / Receiving Office
- JP · JP
- Patent Type
- Patents
- Current Assignee / Owner
- Filing Date
- 2020-12-22
- Publication Date
- 2025-04-15
- Estimated Expiration
- 2040-12-22
AI Technical Summary
Conventional oil-in-water emulsions are not satisfactory for skin lightening and/or whitening due to poor penetration of lightening and/or whitening components, such as niacinamide, into the stratum corneum.
A composition comprising a hydrophilic phase with at least one glycol having a logP of -0.5 to 4, at least one surfactant with an HLB value of 8-20 at 25°C, and at least one lightening and/or whitening component selected from vitamin B3 and its derivatives, which improves the penetration of these components into the skin.
The composition effectively enhances the penetration of vitamin B3 and its derivatives into the stratum corneum, improving the lightening and/or whitening effects on the skin.
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Abstract
Description
[Technical field]
[0001] Technical Field The present invention relates to a composition and its use. In particular, the present invention relates to a composition for lightening and / or whitening keratinous materials, especially skin. The present invention also relates to a non-therapeutic method for lightening and / or whitening keratinous materials and to the use of a combination of at least one glycol with a logP between -0.5 and 4 and at least one surfactant with an HLB value between 8 and 20 at a temperature of 25°C to improve the penetration of lightening and / or whitening ingredients selected from vitamin B3 and its derivatives into keratinous materials. [Background technology]
[0002] Background technology The color of human skin depends on various factors, in particular the season of the year, race and sex, but is primarily determined by the nature and concentration of melanin produced by melanocytes, which are specialized cells that synthesize melanin by means of specific organelles, the melanocytes. In addition, at various times in life, certain individuals experience skin heterogeneity, with the appearance of dark and / or colored areas on the skin, and more particularly on the hands.
[0003] For various reasons, in particular related to improving comfort (softness and emollient properties, etc.), current compositions for caring for and / or making up keratinous materials, and in particular the skin, are usually in the form of oil-in-water (O / W) emulsions consisting of an aqueous dispersible continuous phase and an oily dispersed discontinuous phase, or of water-in-oil (W / O) emulsions consisting of an oily dispersed continuous phase and an aqueous dispersed discontinuous phase.
[0004] O / W emulsions are the most sought after emulsions in the cosmetic field because they contain an aqueous phase as the outer phase and provide a fresher, less greasy and lighter feel when applied to the skin than W / O emulsions.
[0005] However, due to their inherent properties, conventional oil-in-water emulsions have not been entirely satisfactory, especially in terms of skin lightening and / or whitening.
[0006] Efforts have been made to introduce lightening and / or whitening ingredients, such as niacinamide or its derivatives, into cosmetics. However, for many products for lightening and / or whitening the skin, it is difficult for the lightening and / or whitening ingredients contained therein to penetrate the skin. [Prior art documents] [Non-patent literature]
[0007] [Non-Patent Document 1] Meylan and Howard: Atom / Fragment contribution method for estimating octanol-water partition coefficients, J. Pharm. Sci., 84: 83-92, 1995. [Non-Patent Document 2] Exploring QSAR: hydrophobic, electronic and steric constants (ACS professional reference book, 1995) [Non-Patent Document 3] J. Ploughshare. Cosm. Chem., 1954 (Vol. 5), pp. 249-256 Summary of the Invention [Problem to be solved by the invention]
[0008] For compositions containing lightening and / or whitening ingredients, penetration of the active ingredient into the stratum corneum is one of the most important properties.
[0009] Thus, there remains a need to formulate compositions for lightening and / or whitening the skin that have improved effectiveness in terms of penetration of the contained lightening and / or whitening ingredient, e.g., niacinamide or its derivatives, into the stratum corneum. [Means for solving the problem]
[0010] SUMMARY OF THE PRESENT APPLICATION The inventors have now discovered that such compositions can be formulated which have improved effectiveness in terms of penetration of the contained cosmetically active ingredient, such as niacinamide or a derivative thereof, into the stratum corneum.
[0011] Thus, in a first aspect, the present invention relates to a composition for lightening and / or whitening keratinous materials, comprising in the hydrophilic phase: (i) at least one glycol having a logP of -0.5 to 4; (ii) at least one surfactant having an HLB value of 8 to 20 at a temperature of 25° C., and (iii) at least one lightening and / or whitening component selected from vitamin B3 and its derivatives; Including, An oil-free composition is provided.
[0012] The composition of the present invention may be in the form of a liquid, for example a toner or serum.
[0013] In a second aspect, the present invention provides a non-therapeutic method for lightening and / or whitening keratinous materials comprising the step of applying to the keratinous materials a composition according to the first aspect of the invention.
[0014] It has been found that vitamin B3 and / or its derivatives contained in the composition according to the invention are able to easily penetrate the stratum corneum.
[0015] In a third aspect, the present invention provides the use of a combination of at least one glycol having a logP between -0.5 and 4 and at least one surfactant having an HLB value between 8 and 20 at a temperature of 25°C, for improving the penetration into keratinous materials of a lightening and / or whitening ingredient selected from vitamin B3 and its derivatives.
[0016] Other objects, features, aspects and advantages of the present invention will become more apparent from the following detailed description and examples.
[0017] BRIEF DESCRIPTION OF THE DRAWINGS An implementation of the present invention will now be described, by way of example only, with reference to the accompanying drawings, in which: [Brief description of the drawings]
[0018] [Figure 1] 1 is a graph showing the permeation profile of niacinamide for compositions 1-2 having the formulation of the present invention and composition 1 having the formulation of a comparative example. [Diagram 2] 1 is a graph showing the permeation profile of niacinamide for compositions 3-4 of the present invention and composition 1 of the comparative formulation. [Diagram 3] 1 is a graph showing the permeation profile of niacinamide for compositions 5-6 having the formulation of the present invention and composition 1 having the formulation of a comparative example. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS
[0019] Detailed Description of the Invention Unless otherwise defined, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this invention belongs. In the event that a definition of a term in this description conflicts with a meaning commonly understood by one of ordinary skill in the art to which this invention belongs, the definition set forth herein shall apply.
[0020] Hereinafter, unless otherwise indicated, the limits of value ranges are included within the ranges, in particular in the expressions "between ... to ..." and "within ... to ...".
[0021] Furthermore, as used in this description, the term "at least one" is equivalent to the term "one or more."
[0022] Throughout this application, the term "comprising" should be interpreted to encompass all specifically mentioned features as well as optional, additional, unspecified features. As used herein, use of the term "comprising" also discloses embodiments in which no features are present (i.e., "consisting of") other than those features specifically mentioned.
[0023] Unless otherwise specified, all numbers expressing quantities of ingredients and the like used in the description and claims are understood to be modified by the term "about." Accordingly, unless indicated to the contrary, the numbers and parameters set forth herein are approximations that can be varied depending upon the desired objectives required.
[0024] All percentages in this invention refer to percentages by weight unless otherwise specified.
[0025] For the purposes of the present invention, the term "keratinous materials" is intended to include human skin, mucous membranes, such as the lips. The skin of the face is particularly considered by the present invention.
[0026] By "oil-free" it is meant that no oil is intentionally added and that the composition contains less than 0.5% oil by weight, based on the total weight of the composition. In particular, there is no oil present in the composition.
[0027] According to a first aspect, the present invention relates to a composition for lightening and / or whitening keratinous materials, comprising in the hydrophilic phase: (i) at least one glycol having a logP of -0.5 to 4; (ii) at least one surfactant having an HLB value of 8 to 20 at a temperature of 25° C., and (iii) at least one lightening and / or whitening component selected from vitamin B3 and its derivatives; Including, An oil-free composition is provided.
[0028] hydrophilic phase According to a first embodiment, the composition of the invention comprises a hydrophilic phase.
[0029] The hydrophilic phase comprises water.
[0030] Preferably, the hydrophilic phase comprises at least one organic solvent that is miscible with water (at room temperature 25° C.), such as a monohydric alcohol having 2 to 6 carbon atoms, such as ethanol, isopropanol, a triol, such as glycerin.
[0031] Advantageously, water is present in the composition according to the invention in an amount ranging from 60% to 90% by weight relative to the total weight of the composition.
[0032] Glycol According to a first embodiment, the composition of the invention comprises at least one glycol having a logP between -0.5 and 4.
[0033] The logP value is the logarithm to the base 10 of the apparent partition coefficient of octan-1-ol / water. The logP value is known and is determined by standard tests to determine the concentration of glycols in octan-1-ol and water. The logP can be calculated by the method described in the article by Meylan and Howard: Atom / Fragment contribution method for estimating octanol-water partition coefficients, J. Pharm. Sci., 84:83-92, 1995. This value may be calculated using a number of commercially available software packages, which determine the logP as a function of the structure of the molecule. An example is the Epiwin software from the United States Environmental Protection Agency.
[0034] This value can be calculated using, inter alia, ACD (Advanced Chemistry Development) Solaris software V4.67, and it can also be obtained from Exploring QSAR: hydrophobic, electronic and steric constants (ACS professional reference book, 1995). There is also an internet site that provides approximate values (address: http: / / esc.syrres.com / interkow / kowdemo.htm).
[0035] Preferably, the glycol is selected from C4 to C10 glycols.
[0036] More preferably, the glycol is selected from C4 to C8 glycols.
[0037] Thus, in some preferred embodiments, the compositions of the present invention comprise at least one C4-C10 glycol, preferably a C4-C8 glycol.
[0038] Examples of C4 to C10 glycols that can be used in the composition of the present invention include butylene glycol, pentylene glycol, hexylene glycol, dipropylene glycol, heptanediol, octanediol, nonanediol, and decylene glycol.
[0039] In the present invention, the definition of glycol includes all possible isomers, for example pentylene glycol includes 1,5-pentylene glycol, 2,4-pentylene glycol, etc.
[0040] In a more preferred embodiment, the composition comprises a combination of butylene glycol, pentylene glycol and dipropylene glycol.
[0041] Advantageously, the glycol is present in an amount ranging from 2% to 40% by weight, preferably from 5% to 30% by weight and even better still from 8% to 20% by weight relative to the total weight of the composition.
[0042] Surfactants According to a first embodiment, the composition of the invention comprises at least one surfactant having an HLB value of between 8 and 20 at a temperature of 25°C.
[0043] The HLB (hydrophilic-lipophilic balance) value is defined according to the method of Griffin in J. Ploughshare. Cosm. Chem., 1954 (vol. 5), pp. 249-256.
[0044] Advantageously, the surfactant has an HLB value of between 10 and 15, preferably between 12 and 15, at a temperature of 25°C.
[0045] Preferably, the surfactant is selected from a nonionic surfactant, an anionic surfactant, an amphoteric or zwitterionic surfactant, or mixtures thereof.
[0046] Nonionic surfactants suitable for the composition may be selected from: polyoxyethylenated sorbitol fatty esters, such as the product sold under the name TWEEN 20 by the company ICI; polyoxyethylenated fatty alcohols, such as the product sold under the name REMCOPAL 21912 AL by the company Gerland; - polyoxyethylenated alkylphenols, such as the products sold under the name TRITON X 100 by the company Rohm-Haas, condensates of ethylene oxide with propylene oxide, such as those sold under the name SYNPERONIC PE by the company ICI, in particular those referenced L 31, L 64, F 38, F 88, L 92, P 103, F 108 and F 127; - Esters of fatty acids with glycerol or polyglycerol, preferably C6-C 30 , more preferably C8 to C 16 with glycerol or polyglycerol, for example glyceryl stearate, glyceryl isostearate, polyglyceryl-3 diisostearate, glyceryl caprylate, polyglyceryl-4 caprate, polyglyceryl-10 laurate or mixtures thereof. Such products are available on the market, for example the mixture of glyceryl stearate and PEG-100 stearate sold under the trade name Simulsol™ 165 by the company Seppic, or polyglyceryl-4 caprate, the product sold under the trade name Tegosoft® PC 41 by the company Evonik Goldshmidtc. ethers of polyethylene glycol and / or polypropylene glycol with glycerol, such as glycereth-26 and PPG-24 glycereth-24; - esters derived from the reaction of a) fatty acids with b) polyethylene glycol and / or polypropylene glycol glycerol ethers, such as, for example, glycereth-7 PCA isostearate or glycereth-25 PCA isostearate, - esters of sucrose with fatty acids containing from 12 to 30 carbon atoms, in particular from 14 to 20 carbon atoms, said esters optionally containing from 2 to 5 fatty chains, such as sucrose distearate, sucrose tristearate and sucrose palmitate, - alkyl polyglucosides, preferably those containing an alkyl group containing from 6 to 30 carbon atoms, preferably from 8 to 16 carbon atoms, and preferably those containing a hydrophilic group (glucoside) containing from 1.2 to 3 sugar units, such as decyl glucoside (alkyl-C9 / C 11- polyglucosides (1.4)), such as the product sold under the name Plantacare® 2000 UP by Cogins (BASF), the product sold under the name MYDOL 10® by Kao Chemicals, the product sold under the name PLANTAREN® 2000 UP by Cognis and the product sold under the name ORAMIX® NS 10 by Seppic; caprylyl / capryl glucoside, such as the product sold under the name ORAMIX® CG 110 by Seppic; lauryl glucoside, such as the product sold under the name PLANTAREN® 1200 by Cognis. Mention may also be made of cocoglucosides, such as the products sold under the names PLANTACARE® 818 / UP by the company Cognis, cetostearyl glucoside, optionally in a mixture with cetostearyl alcohol, such as that sold under the name MONTANOV 68 by the company Seppic, under the name TEGO® CARE CG90 by the company Goldschmidt and under the name EMULGADE KE3302 by the company Henkel, arachidyl glucoside, for example in the form of a mixture of arachidyl alcohol and behenyl alcohol with arachidyl glucoside, sold under the name MONTANOV 202 by the company Seppic; cocoyl ethyl glucoside, for example in the form of a (35 / 65) mixture with cetyl alcohol and stearyl alcohol, sold under the name MONTANOV 82 by the company Seppic, and mixtures thereof.
[0047] Among the anionic surfactants, mention may be made of: - alkyl sulfates, alkyl ether sulfates and their salts, in particular the sodium salts, such as the sodium laureth sulfate / magnesium laureth sulfate / sodium laureth-8 sulfate / magnesium laureth-8 sulfate mixture sold under the name TEXAPON ASV by the company Henkel; sodium lauryl ether sulfate (C 2 ), sold under the name SIPON AOS 225 or under the name TEXAPON® N702 PASTE by the company Henkel; 12~14 70 / 30) (2.2EO); Ammonium lauryl ether sulfate (C 2.2EO) sold under the name SIPON LEA 370 by Henkel 12~14 70 / 30)(3EO); alkyl (C 12~C14 ) ether (9EO) ammonium sulfate, alkyl sulfoacetates, such as those sold under the name LATHANOL® LAL by the company Stepan; - alkyl sulfosuccinates, such as oxyethylenated (3 EO) lauryl alcohol (C 2 ), sold under the names SETACIN 103 SPECIAL or REWOPOL SB-FA 30 K 4 by the company Witco; 12 / C 14 70 / 30) Monosulfosuccinate, sold under the name SETACIN F SPECIAL PASTE by Zschimmer Schwarz C 12 ~C 14disodium salts of hemisulfosuccinate esters of alcohols, such as the disodium oxyethylenated (2 EO) oleamide sulfosuccinate sold under the name STANDAPOL SH 135 by Henkel, the disodium oxyethylenated (5 EO) lauramide monosulfosuccinate sold under the name LEBON A-5000 by Sanyo, the disodium salt of oxyethylenated (10 EO) lauryl citrate monosulfosuccinate sold under the name REWOPOL® SB CS 50 by Witco, or the disodium salt of ricinoleic acid monoethanolamide monosulfosuccinate sold under the name REWODERM® S 1333 by Witco, - polypeptides obtained by condensation of fatty chains with cereal amino acids, in particular wheat and oat amino acids, such as the potassium salt of lauroyl hydrolyzed wheat protein sold under the name AMINOFOAM® WOR by the company Croda, the triethanolamine salt of cocoyl hydrolyzed soy protein sold under the name MAY-TEIN SY by the company Maybrook, the sodium salt of lauroyl oat amino acid sold under the name PROTEOL® OAT by the company Seppic, the hydrolysate of collagen grafted onto coconut fatty acids sold under the name GELIDERM 3000 by the company Deutsche Gelatine or the soy protein acylated with hydrogenated coconut fatty acids sold under the name PROTEOL VS 22 by the company Seppic, amino acid derivatives, such as the salts of amino acids, for example especially the sarcosine salts, in particular the acyl sarcosine salts, such as sodium lauroyl sarcosine sold under the name SARKOSYL NL 97 by the company Ciba or under the name ORAMIX® L 30 by the company Seppic, sodium myristoyl sarcosine sold under the name NIKKOL SARCOSINATE MN by the company Nikkol or sodium palmitoyl sarcosine sold under the name NIKKOL SARCOSINATE PN by the company Nikkol; alaninates, such as sodium N-lauroyl-N-methylamidopropionate sold under the name SODIUM NIKKOL ALANINATE LN 30 by the company Nikkol or under the name ALANONE ALE by the company Kawaken, and sodium N-lauroyl-N-methylamidopropionate sold under the name ALANONE ALE by the company Kawaken. N-lauroyl-N-methylalanine triethanolamine sold under the name ALTA; N-acyl glutamates, such as monococoyl glutamate triethanolamine sold under the name ACYLGLUTAMATE CT-12 by the company Ajinomoto, and lauroyl glutamate triethanolamine sold under the name ACYLGLUTAMATE LT-12 by the company Ajinomoto; aspartates, such as the mixture of N-lauroyl aspartate triethanolamine and N-myristoyl aspartate triethanolamine sold under the name ASPARACK LM-TS2 by the company Mitsubishi; or glycine derivatives, such as sodium N-cocoyl glycine and potassium N-cocoyl glycine, such as the products sold under the names AMILITE GCS-12 and AMILITE GCK-12 by the company Ajinomoto; lysins, such as sodium dilauramidoglutamide lysine, such as the product sold under the name PELLICER L-30 by the company ASAHI KASEI, sulfonates, such as α-olefin sulfonates, such as those sold under the name BIO-TERGE® AS-40 by the company Stepan, those sold under the name WITCONATE AOS PROTEGE and SULFRAMINE AOS PH 12 by the company Witco, or α-olefin (C ) sulfonates sold under the name BIO-TERGE® AS-40 CG by the company Stepan; 14~16 ) sodium sulfonate, or the secondary olefin sulfonate sold under the name HOSTAPUR® SAS 30 by Clariant; or linear alkylaryl sulfonates, for example sodium xylene sulfonate sold under the names MANROSOL SXS30, MANROSOL SXS40 or MANROSOL SXS93 by Manro, - isethionates, in particular acyl isethionates, such as sodium cocoyl isethionate, for example the product sold under the name JORDAPON CI P by the company Jordan.
[0048] Among the amphoteric or zwitterionic surfactants, mention may in particular be made of: - alkylamidoalkylamine derivatives, such as N-disodium N-cocoyl-N-carboxymethoxyethyl-N-(carboxymethyl)ethylenediamine (CTFA name: disodium cocoamphodiacetate), sold as an aqueous solution of salts under the name MIRANOL C2M CONC NP by the company Rhodia Chimie; N-sodium N-cocoyl-N-hydroxyethyl-N-(carboxymethyl)ethylenediamine (CTFA name: sodium cocoamphodiacetate) and the mixture of coconut fatty acid ethanolamide (CTFA name: cocamide DEA); betaines, such as coco betaine, for example the product sold under the name DEHYTON® AB-30 by the company Henkel, lauryl betaine, for example the product sold under the name GENAGEN® KB by the company Clariant and the product sold under the name EMPIGEN BB / LS by the company INNOSPEC ACTIVE CHEMICALS, oxyethylenated (10 EO) lauryl betaine, for example the product sold under the name Lauryl Ether (10 EO) Betaine by the company Shin Nihon Rica, or oxyethylenated (10 EO) stearyl betaine, for example the product sold under the name Stearyl Ether (10 EO) Betaine by the company Shin Nihon Rica, etc. alkylamidopropyl betaines and their derivatives, such as, for example, the cocamidopropyl betaine sold under the name LEBON 2000 HG by the company Sanyo or under the name EMPIGEN® BB by the company Albright & Wilson, lauramidopropyl betaine sold under the name REWOTERIC AMB12P® by the company Witco, such as, for example, the product sold under the name TEGO BETAINE by the company Goldschmidt, - imidazoline derivatives, such as the products sold under the name CHIMEXANE HD by the company Chimex, - A mixture of these.
[0049] Preferably, the surfactants are chosen from esters of fatty acids with glycerol or polyglycerol, salts of amino acids; betaines and mixtures thereof.
[0050] More preferably, the surfactant is a C6-C 30 , preferably C8 to C 16 of saturated or unsaturated fatty acids with glycerol or polyglycerol, lysinates, betaines and mixtures thereof.
[0051] According to a preferred embodiment, the surfactant is selected from sodium dilauramidoglutamidolysine, polyglyceryl-4 caprate, polyglyceryl-10 laurate, lauryl betaine and mixtures thereof.
[0052] Advantageously, the surfactant is present in an amount ranging from 0.001% to 3% by weight, preferably from 0.003% to 2% by weight and even better still from 0.005% to 1% by weight relative to the total weight of the composition.
[0053] Vitamin B3 and its derivatives According to a first aspect, the composition of the invention comprises at least one lightening and / or whitening ingredient chosen from vitamin B3 and its derivatives.
[0054] Niacinamide, also known as vitamin B3 and vitamin PP, has the following structure: [ka]
[0055] Vitamin B3 derivatives that may be mentioned include, for example, nicotinic acid esters, such as tocopherol nicotinate, amides derived from niacinamide by replacement of the hydrogen group of -CONH2, products from the reaction with carboxylic acids and amino acids, esters of nicotinyl alcohol with carboxylic acids, such as acetic acid, salicylic acid, glycolic acid or palmitic acid.
[0056] Mention may also be made of the following derivatives: 2-chloronicotinamide, 6-methylnicotinamide, 6-aminonicotinamide, N-methylnicotinamide, N,N-dimethylnicotinamide, N-(hydroxymethyl)nicotinamide, quinolinic acid imide, nicotinanilide, N-benzylnicotinamide, N-ethylnicotinamide, nifenazone, nicotinaldehyde, isonicotinic acid, methylisonicotinic acid, thionicotinamide, nialamide, 2-mercaptonicotinic acid, nicomol and niaprazine, methyl nicotinate and sodium nicotinate.
[0057] Other vitamin B3 derivatives that may also be mentioned include its inorganic salts, such as the chlorides, bromides, iodides or carbonates, and its organic salts, such as the salts obtained by reaction with carboxylic acids, such as the acetates, salicylates, glycolates, lactates, malates, citrates, mandelates, tartrates, etc.
[0058] Advantageously, the lightening and / or whitening component chosen from vitamin B3 and its derivatives is present in an amount ranging from 0.1% to 15% by weight, preferably from 0.5% to 10% by weight and more preferably from 1% to 8% by weight relative to the total weight of the composition.
[0059] Additional cosmetic active ingredients Depending on the final purpose, the composition according to the invention may contain one or more additional cosmetically active ingredients.
[0060] Examples of cosmetically active ingredients that may be used in the compositions of the present invention include enzymes; flavonoids; moisturizing agents, anti-inflammatory agents; exfoliants; anti-aging agents; antioxidants; depigmenting agents; alpha-hydroxy acids; tensioning agents; and mixtures thereof.
[0061] One skilled in the art can readily adjust the amount of additional cosmetically active ingredients based on the end use of the composition according to the present invention.
[0062] Additional adjuvants or additives The compositions of the present invention may also include conventional cosmetic adjuvants or additives, such as fragrances, chelating agents (e.g., disodium EDTA), preservatives (e.g., hydroxyacetophenone, chlorphenesin, and phenoxyethanol) as well as bactericides, thickeners, fillers, pH adjusters (e.g., citric acid, sodium hydroxide, potassium hydroxide), and mixtures thereof.
[0063] A person skilled in the art can select the amount of additional adjuvants or additives so as not to adversely affect the end use of the composition according to the present invention.
[0064] According to a particularly preferred embodiment, the present invention relates to a composition for lightening and / or whitening keratinous materials, comprising in the hydrophilic phase: (i) 8% by weight to 20% by weight of a combination of butylene glycol, pentylene glycol, and dipropylene glycol; (ii) 0.005% to 1% by weight of at least one surfactant selected from sodium dilauramidoglutamidolysine, polyglyceryl-4 caprate, polyglyceryl-10 laurate, lauryl betaine, and mixtures thereof; and (iii) 1% to 8% by mass of vitamin B3 Including, An oil-free composition is provided.
[0065] Galenic form The compositions of the present invention are preferably in the form of a liquid.
[0066] Preferably, the composition according to the present invention has a low viscosity.
[0067] According to a preferred embodiment, the compositions of the invention have a viscosity of less than 50 UD (Deviation Units), measured at 25° C. using a Rheomat 180 viscometer equipped with spindle M1 rotating at 200 rpm.
[0068] Methods and Uses According to a second aspect, the present invention provides a non-therapeutic method for lightening and / or whitening keratinous materials comprising the step of applying to the keratinous materials a composition according to the first aspect of the invention.
[0069] In particular, keratinous materials are intended to mean the skin, especially the face.
[0070] According to a third aspect, the present invention provides the use of a combination of at least one glycol with a logP between -0.5 and 4 and at least one surfactant with an HLB between 10 and 20, for improving the penetration into keratinous materials of a lightening and / or whitening ingredient selected from vitamin B3 and its derivatives.
[0071] The glycols having a log P between -0.5 and 4 and the surfactants having an HLB value between 8 and 20 at a temperature of 25°C are as defined above.
[0072] Preferably, the at least one glycol is selected from C4 to C10 glycols and the at least one surfactant is selected from esters of C6 to C30 saturated or unsaturated fatty acids with glycerol or polyglycerol, lysinates, betaines and mixtures thereof.
[0073] More preferably, the at least one glycol is a combination of butylene glycol, pentylene glycol and dipropylene glycol, and the at least one surfactant is selected from sodium dilauramidoglutamido lysine, polyglyceryl-4 caprate, polyglyceryl-10 laurate, lauryl betaine, and mixtures thereof.
[0074] The following examples serve to illustrate the invention and are not limiting in nature. EXAMPLES
[0075] The main raw materials used, their trade names and their suppliers are listed in Table 1.
[0076] [Table 1]
[0077] Example 1 Preparation of the Composition Compositions (Comp.) 1-2 according to the formulation of the comparative example and compositions (Inv.) 1-6 according to the formulation of the invention were prepared according to the contents given in Tables 2-3 (unless otherwise indicated, the contents are expressed as the mass percentage of active substance relative to the total mass of each composition).
[0078] [Table 2]
[0079] Composition 1, which is a comparative formulation, does not contain a surfactant having an HLB value of 8 to 20 at a temperature of 25°C.
[0080] [Table 3]
[0081] The comparative formulation, Composition 2, contains a surfactant with an HLB value of 7.3 at a temperature of 25° C., instead of a surfactant with an HLB value of 8-20. The resulting composition is not stable, separates into two phases, and is unable to form a homogeneous liquid.
[0082] Preparation method The compositions listed above, taking composition 1 of the formulation of the present invention as an example, were prepared as follows: 1) Dissolve niacinamide in water by stirring to obtain the main phase; 2) Dissolve the hydroxyacetophenone in the glycol by stirring until a clear phase is obtained; 3) Add the clear phase containing hydroxyacetophenone and glycol to the main phase while stirring until a clear mixture is obtained; 3) With stirring, carefully add the surfactant to the clear mixture to obtain the composition.
[0083] Example 2 Evaluation of the composition The permeation of niacinamide in each of the compositions prepared in Example 1 was characterized through an In-vitro skin permeation test (Strat-M test) using Strat-M (a synthetic membrane that mimics the lipophilic components of the stratum corneum, available from Merck).
[0084] The steps are as follows: - The receptor fluid (RF, pH 7.4 in PBS) is subjected to an ultrasonic bath for 15 minutes to remove gases; - for each composition, three Franz cells are placed in parallel on shelves; - To homogenize the temperature for each cell, connect the cells in parallel to a fluid thermostat (T bath = 34 °C, T cells = 32°C), - Introducing a magnetic bar into the cell (RF section), - Mark a line on the sampling port, approximately 1 cm from the entrance of the sampling port to the line (this is the reference for filling the receptor fluid); - Introduce Molykote 111 (valve lubricant and sealant from Dow Corning) into a 5 mL plastic syringe, spread Molykote 111 on the sanded surface of the receptor part of the cell with the syringe, place the donor compartment on the Franz cell and rotate it a full 360° to ensure that Molykote 111 is applied well and homogenously to the periphery of the Franz cell, remove the donor compartment of the cell and remove the excess Molykote inside the cells (donor and receiver compartments) with a cotton swab to avoid any contamination; - Place the Strat-M membrane in the center of the cell, shiny side facing the donor compartment, without touching the edges of the membrane; - Place the donor compartment and gently close the Franz cell with clips, - Introduce the receptor fluid through the sampling port and run the stirrer at 600 rpm; - Invert the diffusion cell and use the stir bar to eliminate any air bubbles under the membrane, - taking 45 mg of the composition to be tested and applying it evenly to the membrane by a 360° rotational movement and careful tapping to accurately determine the amount of composition applied to the membrane; - 200 μL of receptor fluid is sampled using a 250 μL Hamilton syringe, with a minimum of 3 samples per hour from 1 hour to 24 hours; - Slowly fill the sampling port with new receptor fluid until it reaches the mark, - Measuring the amount of active ingredient in the receptor fluid to determine the relationship between the amount of active ingredient and the penetration time.
[0085] FIG. 1 shows the permeation profiles of niacinamide for compositions 1-2 of the inventive formulation and composition 1 of the comparative formulation.
[0086] FIG. 2 shows the permeation profiles of niacinamide for compositions 3-4 of the inventive formulation and composition 1 of the comparative formulation.
[0087] FIG. 3 shows the permeation profiles of niacinamide for compositions 5-6 of the inventive formulation and composition 1 of the comparative formulation.
[0088] From Figures 1-3 it can be seen that the combination of at least one glycol with at least one surfactant having an HLB value of 8-20 at a temperature of 25°C can improve the penetration of niacinamide into the skin after topical application.
[0089] The viscosity of each of the compositions prepared in Example 1 was measured at 25° C. using a ProRheo Rheomat 180 viscometer equipped with spindle M1 or M3 rotating at 200 rpm.
[0090] The results are summarized in Table 4.
[0091] [Table 4]
[0092] From Table 4 it can be seen that the composition according to the invention has a low viscosity.
Claims
1. A composition for lightening and / or whitening keratinous materials, comprising in a hydrophilic phase: (i) at least one glycol having a logP of -0.5 to 4, including pentylene glycol; (ii) at least one surfactant having an HLB value of 8 to 20 at a temperature of 25° C.; and (iii) at least one lightening and / or whitening component selected from vitamin B3 and its derivatives; Including, A composition, wherein the composition is oil-free and glycerin-free.
2. 2. The composition of claim 1, wherein the glycol is a combination of butylene glycol, pentylene glycol and dipropylene glycol.
3. 3. The composition according to claim 1, wherein the glycol is present in an amount ranging from 2% to 40% by weight relative to the total weight of the composition.
4. 4. The composition according to claim 1, wherein the surfactant is chosen from esters of fatty acids with glycerol or polyglycerol, salts of amino acids; betaines and mixtures thereof.
5. 5. The composition according to claim 1, wherein the surfactant is selected from esters of C6 to C30 saturated or unsaturated fatty acids with glycerol or polyglycerol, lysinates, betaines and mixtures thereof.
6. 6. The composition according to claim 1, wherein the surfactant is present in an amount ranging from 0.001% to 3% by weight relative to the total weight of the composition.
7. 7. The composition according to claim 1, wherein the lightening and / or whitening ingredient selected from vitamin B3 and its derivatives is present in an amount ranging from 0.1% to 15% by weight relative to the total weight of the composition.
8. The hydrophilic phase contains, relative to the total weight of the composition: (i) 8% to 20% by weight of a combination of butylene glycol, pentylene glycol, and dipropylene glycol; (ii) 0.005% to 1% by weight of at least one surfactant selected from sodium dilauramidoglutamidolysine, polyglyceryl-4 caprate, polyglyceryl-10 laurate, lauryl betaine, and mixtures thereof; and (iii) 1% to 8% by weight of vitamin B3 Including, The composition of claim 1 , wherein the composition is oil-free and glycerin-free.
9. 9. The composition of claim 1, wherein the hydrophilic phase comprises water.
10. 10. A non-therapeutic method for lightening and / or whitening keratinous materials, comprising the step of applying a composition according to any one of claims 1 to 9 to said keratinous materials.
11. 2. Use of a combination of at least one glycol having a logP of -0.5 to 4, including pentylene glycol, and at least one surfactant having an HLB value of 8 to 20 at a temperature of 25°C, to improve the penetration of a lightening and / or whitening ingredient selected from vitamin B3 and its derivatives into keratinous materials.
12. The at least one surfactant is C 6 ~C 30 12. The use according to claim 11, which is selected from esters of saturated or unsaturated fatty acids with glycerol or polyglycerol, lysinates, betaines and mixtures thereof.
13. 12. The use according to claim 11, wherein the at least one glycol is a combination of butylene glycol, pentylene glycol and dipropylene glycol, and the at least one surfactant is selected from sodium dilauramidoglutamido lysine, polyglyceryl-4 caprate, polyglyceryl-10 laurate, lauryl betaine and mixtures thereof.
Citation Information
Patent Citations
Skin cosmetic
JP2009040694A
External preparations for skin
JP2014084304A
Phosphatidylinositol-containing cosmetic or external preparation for skin
JP2019214537A
External skin preparation for pimpled skin
WO2009084200A1
A method of lightening skin
WO2012152567A2