COSMETIC PROCESS USING MICRO-NEEDLES

Abstract

COSMETIC PROCESS USING MICRO-NEEDLES The present invention relates to a cosmetic process for a keratinous substance such as skin and lips, comprising the steps of: applying, to the keratinous substance, at least one composition comprising at least one cosmetic active substance; and applying, to the keratinous substance, a micro-needle sheet comprising a substrate sheet and a plurality of micro-needles on the substrate sheet such that the micro-needles can penetrate the keratinous substance, with a linear movement of the micro-needle sheet on the keratinous substance to perform at least one pass of the micro-needle sheet on the keratinous substance, wherein the frequency of application of the micro-needle sheet to the keratinous substance is 3 times or less per week,and the number of passes of the microneedle sheet over the keratinous substance during each application is 5 or fewer, provided that, if the frequency of application of the microneedle sheet to the keratinous substance is 3 times per week, the number of passes of the microneedle sheet over the keratinous substance during each application is not 5, and, if the number of passes of the microneedle sheet over the keratinous substance during each application is 5, the frequency of application of the microneedle sheet to the keratinous substance is not 3 times per week. Thanks to the present invention, the risk of pigmentation due to the use of microneedles can be reduced. Figure for abstract: 2,

Description

Title of the invention: COSMETIC PROCESS USING MICRO-NEEDLES technical field

[0001] The present invention relates to the use of a plurality of microneedles for cosmetic treatments of a keratinous substance such as skin and lips. PRIOR TECHNOLOGY

[0002] The use of different types of microneedles, such as metallic, soluble, and hollow microneedles, to improve the permeability of cosmetic active substances in the skin is well known. For example, document WO 2019 / 100902 discloses a transdermal penetration dermo-cosmetic process that uses microneedles in combination with a cosmetic composition including certain cosmetic active substances. In document WO 2019 / 100902, the microneedles are used nightly for 28 days. DISCLOSURE OF THE INVENTION

[0003] It is known that the use of such microneedles can cause skin inflammation and, consequently, a risk of skin pigmentation, known as post-inflammatory hyperpigmentation. This can become particularly important when microneedles are used to treat skin hyperpigmentation, such as melasma, dark circles, and brown spots.

[0004] An objective of the present invention is to provide a cosmetic process which uses microneedles which reduces the risk of pigmentation of a keratinous substance, such as skin and lips, due to the use of microneedles.

[0005] The above objective can be achieved by a cosmetic process intended for a keratinous substance such as skin and lips, comprising the steps of:

[0006] - application, on the keratinous substance, of at least one composition comprising at least one active cosmetic substance; and

[0007] - application of a sheet of micro-needles to the keratinous substance comprising a substrate sheet and a plurality of microneedles on the substrate sheet such that the microneedles can penetrate the keratinous substance, with a linear movement of the microneedle sheet over the keratinous substance in order to perform at least one pass of the microneedle sheet over the keratinous substance,

[0008] in which

[0009] - the frequency of application of the microneedle sheet to the substance keratin treatment is 3 times or less per week, and

[0010] - the number of passes of the micro-needle sheet over the keratinous substance Each application is 5 or less.

[0011] - provided that

[0012] - if the frequency of application of the microneedle sheet on the substance keratinous is 3 times per week, the number of passes of the microneedle sheet over the keratinous substance during each application is not 5,

[0013] and

[0014] - if the number of passes of the microneedle sheet over the substance keratinous during each application is 5, the frequency of application of the micro-needle sheet on the keratinous substance is not 3 times per week.

[0015] The above step of applying the composition comprising at least one cosmetic active substance can be carried out before the step of applying the microneedle sheet to the keratinous substance.

[0016] The cosmetic active substance may be chosen from skin care active substances, preferably chosen from the group consisting of depigmenting or brightening agents, anti-aging agents and mixtures thereof, and more preferably chosen from the group consisting of vitamin B3 and its derivatives, ascorbic acid and its derivatives, resorcinol derivatives, tranexamic acid and its derivatives, hyaluronic acid substances and mixtures thereof.

[0017] The cosmetic active substance may be chosen from depigmenting or lightening agents, and preferably chosen from the group consisting of niacinamide, phenylethyl resorcinol, tranexamic acid and a mixture thereof.

[0018] The quantity of the cosmetic active substance(s) may be from 0.001% to 20% by weight, preferably from 0.01% to 15% by weight, and more preferably from 0.1% to 10% by weight, relative to the total weight of the composition.

[0019] The microneedle can have a height between 10 and 300 micrometers, preferably between 30 and 200 micrometers, and more preferably between 50 and 100 micrometers.

[0020] The micro-needle can be in the shape of a pyramid.

[0021] The base of the microneedle can have a width of 10 to 150 micrometers, of preferably from 15 to 100 micrometers, and more preferably from 20 to 50 micrometers.

[0022] The ratio (pyramid height) / (pyramid base width) of the microneedle can be greater than or equal to 1, preferably greater than or equal to 1.5, and more preferably greater than or equal to 2.0.

[0023] Microneedles can be made from inorganic materials, preferably metals or non-metals, and more preferably silicon.

[0024] The present invention also relates to a device for cosmetically treating a keratinous substance, such as skin and lips, comprising:

[0025] - at least one composition comprising at least one cosmetic active substance;

[0026] - a sheet of microneedles, comprising

[0027] - a substrate sheet, and

[0028] - a plurality of micro-needles on the substrate sheet

[0029] - so that the micro-needles can penetrate the keratinous substance, with a linear movement over the keratinous substance to make at least one pass over the keratinous substance when applied to the keratinous substance; and

[0030] - an instruction support including instructions which

[0031] - if the frequency of application of the microneedle sheet on the substance The keratin treatment is performed 3 times per week, with the number of passes of the microneedle sheet over the keratinous substance during each application not exceeding 5.

[0032] and

[0033] - if the number of passes of the microneedle sheet over the substance keratinous during each application is 5, the frequency of application of the micro-needle sheet on the keratinous substance is not 3 times per week.

[0034] The necessary may further include a device for applying the microneedle sheet to the keratinous substance so that the microneedles can penetrate the keratinous substance.

[0035] The above-mentioned device may be capable of applying the microneedle sheet repeatedly.

[0036] The present invention also relates to the use of a microneedle sheet, comprising

[0037] - a substrate sheet, and

[0038] - a plurality of micro-needles on the substrate sheet,

[0039] - so that the micro-needles can penetrate a keratinous substance, such as the skin and lips, with a linear movement of the microneedle sheet over the keratinous substance to perform at least one pass of the microneedle sheet over the keratinous substance, when applied to the keratinous substance,

[0040] - provided that

[0041] - if the frequency of application of the microneedle sheet on the substance The keratin treatment is performed 3 times per week, with the number of passes of the microneedle sheet over the keratinous substance during each application not exceeding 5.

[0042] and

[0043] - if the number of passes of the microneedle sheet over the substance keratinous during each application is 5, the frequency of application of the micro-needle sheet on the keratinous substance should not be 3 times per week,

[0044] - in combination with

[0045] - at least one composition comprising at least one cosmetic active substance,

[0046] - in order to reduce the risk of pigmentation of the keratinous substance. Brief description of the drawings

[0047] Fig. 1 shows a schematic view of a microneedle device which is preferably used for the present invention.

[0048] Fig. 2 shows the pigmentation scores of cosmetic treatments according to examples 1 and 2 and comparative examples 1 to 4.

[0049] Fig. 3 shows the pigmentation scores of cosmetic treatments according to example 3 and comparative examples 5 to 7. Best embodiment of the invention

[0050] After careful research, the inventors discovered that it was possible to propose a cosmetic process which uses microneedles which can reduce the risk of pigmentation of a keratinous substance such as skin and lips due to the use of microneedles.

[0051] Thus, one aspect of the present invention is a cosmetic process for a keratinous substance such as skin and lips, comprising the steps of:

[0052] - application, on the keratinous substance, of at least one composition comprising at least one active cosmetic substance; and

[0053] - application of a sheet of micro-needles to the keratinous substance comprising a substrate sheet and a plurality of microneedles on the substrate sheet such that the microneedles can penetrate the keratinous substance, with a linear movement of the microneedle sheet over the keratinous substance in order to perform at least one pass of the microneedle sheet over the keratinous substance,

[0054] in which

[0055] - the frequency of application of the microneedle sheet to the substance keratin treatment is 3 times or less per week, and

[0056] - the number of passes of the micro-needle sheet over the keratinous substance Each application is 5 or less.

[0057] - provided that

[0058] - if the frequency of application of the microneedle sheet on the substance keratinous is 3 times per week, the number of passes of the microneedle sheet over the keratinous substance during each application is not 5,

[0059] and

[0060] - if the number of passes of the microneedle sheet over the substance keratinous during each application is 5, the frequency of application of the micro-needle sheet on the keratinous substance is not 3 times per week.

[0061] According to the present invention, the risk of pigmentation due to the use of microneedles can be reduced. Thus, any pigmentation that may occur after the use of microneedles can be avoided or eliminated by the present invention.

[0062] The cosmetic process according to the present invention can provide the above effects independently of the combined use of a composition including at least one cosmetic active substance such as a depigmenting or lightening agent. However, if the cosmetic process according to the present invention is combined with a composition including at least one cosmetic active substance, the risk of pigmentation can be further reduced.

[0063] According to the present invention, microneedles can penetrate a keratinous substance such as skin. Thus, the microneedles can pierce the surface of the keratinous substance to create tiny holes or passages through which the cosmetic active substance can penetrate the keratinous substance. The cosmetic active substance can then penetrate the keratinous substance through these tiny holes or passages, thereby passing through the stratum corneum and / or reaching the base of the stratum corneum. Furthermore, the cosmetic active substance can pass through the stratum corneum to reach one of the lower layers of the epidermis, such as the stratum granulosum, stratum spinosum, and stratum basale. Consequently, the cosmetic active substance can be easily delivered into the keratinous substance. This can provide effective cosmetic effects such as depigmenting or brightening effects.

[0064] Furthermore, the cosmetic active substance that penetrates the stratum corneum can diffuse quite easily onto or into the epidermis to distribute itself uniformly in the keratinous substance. This therefore makes it possible to obtain uniform cosmetic effects.

[0065] Since microneedles do not cause pain, the cosmetic process according to the present invention can offer painless cosmetic treatments.

[0066] Furthermore, the cosmetic process according to the present invention can be carried out in a relatively short time.

[0067] Thus, the present invention is suitable for cosmetic or non-therapeutic treatments.

[0068] The cosmetic process, the necessary and similar according to the present invention will be described in detail below. [Cosmetic process]

[0069] The cosmetic process according to the present invention for a keratinous substance such as skin and lips comprises the steps of:

[0070] - application, on the keratinous substance, of at least one composition comprising at least one active cosmetic substance; and

[0071] - application of a sheet of micro-needles to the keratinous substance comprising a substrate sheet and a plurality of microneedles on the substrate sheet such that the microneedles can penetrate the keratinous substance, with a linear movement of the microneedle sheet over the keratinous substance in order to perform at least one pass of the microneedle sheet over the keratinous substance,

[0072] in which

[0073] - the frequency of application of the microneedle sheet to the substance keratin treatment is 3 times or less per week, and

[0074] - the number of passes of the microneedle sheet over the keratinous substance Each application is 5 or less.

[0075] - provided that

[0076] - if the frequency of application of the microneedle sheet on the substance The keratin treatment is performed 3 times per week, with the number of passes of the microneedle sheet over the keratinous substance during each application not exceeding 5.

[0077] and

[0078] - if the number of passes of the microneedle sheet over the substance keratinous during each application is 5, the frequency of application of the micro-needle sheet on the keratinous substance is not 3 times per week.

[0079] The cosmetic process according to the present invention can be intended for cosmetic treatments of a keratinous substance such as skin and lips, preferably skin, and more preferably facial skin.

[0080] The cosmetic process according to the present invention can be used to improve the aesthetic appearance of a keratinous substance, for example, by depigmenting or lightening the keratinous substance.

[0081] The cosmetic process according to the present invention can reduce the risk of pigmentation of a keratinous substance. Therefore, for example, when microneedles are used to cosmetically treat skin hyperpigmentation, such as melasma, dark circles, and brown spots, the cosmetic treatments can be safe because of the reduced risk of new pigmentation when using microneedles.

[0082] The microneedle sheet and similar devices used for the cosmetic process according to the present invention, as well as examples of implementation of the cosmetic process according to the present invention, will be explained in detail below. {Composition}

[0083] The cosmetic process according to the present invention includes the step of applying, on a keratinous substance such as skin and lips, at least one composition comprising at least one cosmetic active substance.

[0084] The step of applying at least one composition comprising at least one cosmetic active substance to a keratinous substance can be carried out using any applicator such as a brush.

[0085] It may be preferable that the composition including at least one cosmetic active substance be applied to the keratinous substance in combination with at least one porous sheet such as a woven or non-woven fabric, in order to obtain good contact of the composition with the keratinous substance and good cosmetic effects on the desired site of the keratinous substance.

[0086] A porous sheet can absorb and retain the composition comprising at least one cosmetic active substance. Therefore, the application of a porous sheet can facilitate contact of the composition with the keratinous substance, which can contribute to good cosmetic effects on the keratinous substance.

[0087] The type of combination described above is not limited. Thus, a porous sheet can be applied to the keratinous substance after the composition has been applied to the keratinous substance. It is also possible to apply a porous sheet to the keratinous substance after the composition has been applied to the keratinous substance.

[0088] The step of applying at least one composition comprising at least one cosmetic active substance to a keratinous substance such as skin and lips can be carried out before or after the step of applying the microneedle sheet to the keratinous substance.

[0089] It is preferable that the application step, on a keratinous substance such as skin and lips, of at least one composition comprising at least one cosmetic active substance be carried out before or after the application step of the microneedle sheet on the keratinous substance. In other words, it is preferable that the composition be used as a pretreatment composition for a keratinous substance.

[0090] If the composition is used as a pretreatment composition, it may be preferable for the microneedle sheet to be applied to the keratinous substance without a drying step of the composition on the keratinous substance. In other words, it may be preferable for the microneedle sheet to be applied to the keratinous substance so that the microneedles can penetrate the keratinous substance before the composition dries or when the keratinous substance is wet.

[0091] If the cosmetic process according to the present invention further includes the step of removing microneedles from the surface of the keratinous substance, after the step of removing microneedles from the surface of the keratinous substance, the composition comprising at least one cosmetic active substance can be removed from the surface of the keratinous substance.

[0092] However, it is preferable that the cosmetic process according to the present invention further include the step of maintaining or resting the composition comprising at least one cosmetic active substance on the keratinous substance after the step of removing the microneedles from the surface of the keratinous substance and before the step of removing the composition from the surface of the keratinous substance, because the composition can effectively penetrate the keratinous substance through the holes formed on and in the keratinous substance by the microneedles.

[0093] The cosmetic active substance in the composition to be used for the cosmetic process according to the present invention can be chosen from skin care active substances.

[0094] Thus, it is preferable that the composition to be used for the cosmetic process according to the present invention be a cosmetic composition, and more preferably a skin care cosmetic composition.

[0095] (active skin care substance)

[0096] The composition to be used for the cosmetic process according to the present invention may include, as a cosmetic active substance, at least one skin-care active substance. If two or more skin-care active substances are used, they may be identical or different.

[0097] The skin care active substance is intended here to refer to a substance for improving the aesthetic appearance and / or comfort of the skin. In particular, the skin care active substance may be intended to reduce visible irregularities (dyschromia, hyperpigmentation, etc.) and / or irregularities to the touch (wrinkles, subcutaneous fat, blackheads, acne scars, etc.) of the skin, and / or to make the skin healthier, less oily and / or less dry.

[0098] The active skin care substance is not intended here to refer to a substance intended to impart a chromatic color to the skin. Thus, the active skin care substance does not include any pigment or colorant.

[0099] It may be preferable for the active skin care substance to have a log P value ranging from -4.5 to 4.5, preferably from -4.0 to 4.0, and more preferably from -3.5 to 3.5.

[0100] A log P value is the base-ten logarithm of the apparent octan-l-ol / water partition coefficient. Log P values ​​are known and are determined by a standard test that determines the concentration of the compound in octan-l-ol and water. Log P can be calculated according to 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 can also be calculated using many commercially available software packages that determine log P based on the structure of a molecule. For example, the U.S. Environmental Protection Agency's Epiwin software.

[0101] The values ​​can be calculated using the ACD (Advanced Chemistry Development) Solaris V4.67 software; they can also be obtained from Exploring QSAR: hydrophobia, electronic and steric constants (a reference work for professionals, ACS, 1995). There is also a website that provides estimated values ​​(address: http: / / esc.syrres.com / interkow / kowdemo.htm).

[0102] The skin care active substance may be in the form of a salt. Salts of the skin care active substance include conventional non-toxic salts of said compounds, such as those formed from an acid or a base.

[0103] It is preferable that the active skin care substance be a depigmenting or brightening agent, or an anti-aging agent such as an anti-wrinkle agent.

[0104] The depigmenting or lightening agent here means any substance that can lighten the color of the skin or enhance the radiance of the skin surface.

[0105] As a depigmenting or lightening agent, vitamin B3 and its derivatives can be mentioned.

[0106] Vitamin B3, also known as vitamin PP, is a compound with the following formula:

[0107] wherein R may be -CONH2 (niacinamide), -COOH (nicotinic acid or niacin), or CH2OH (nicotinic alcohol), -CO-NH-CH2-COOH (nicotinuric acid) or -CO-NH-OH (niconityl hydroxamic acid). Niacinamide is preferred.

[0108] Vitamin B3 derivatives that may be mentioned include, for example, nicotinic acid esters such as tocopherol nicotinate, amides derived from niacinamide by substitution of the hydrogen groups of -CONH2, reaction products with carboxylic acids and amino acids, esters of nicotinyl alcohol and carboxylic acids such as acetic acid, salicylic acid, glycolic acid or palmitic acid.

[0109] The following derivatives may also be mentioned: 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.

[0110] Other derivatives of vitamin B3 that may also be cited include its inorganic salts, such as chlorides, bromides, iodides or carbonates, and its organic salts, such as salts obtained by reaction with carboxylic acids, such as acetate, salicylate, glycolate, lactate, malate, citrate, mandelate, tartrate, etc.

[0111] Ascorbic acid and its derivatives may be mentioned as a depigmenting or lightening agent.

[0112] Ascorbic acid is generally in L form, since it is usually extracted from natural products.

[0113] Because of its chemical structure (α-keto lactone) which makes it very sensitive to certain environmental parameters such as light, heat and aqueous media, it may be advantageous to use ascorbic acid in the form of a derivative or analogue chosen, for example, from ascorbic acid saccharide esters or phosphoryl ascorbic acid metal salts, alkali metal salts, esters and sugars.

[0114] The saccharide esters of ascorbic acid that can be used in the present invention include, in particular, glycosylated, mannosyl, fructosyl, fucosyl, galactosyl, N-acetylucosamine, and N-acetylmuramic derivatives of ascorbic acid, and mixtures thereof, and more particularly ascorbyl glucoside such as ascorbyl-2 glucoside, 2-OaD-glucopyranosyl L-ascorbic acid, or 6-O-[3-D-galactopyranosyl L-ascorbic acid. These latter compounds and the processes for their preparation are described in particular in documents EP-A-0 487 404, EP-A-0 425 066, and JP 05 213 736.

[0115] As regards the metallic salt of phosphoryl ascorbic acid, it may be chosen from alkali metals and in particular sodium, ascorbyl phosphates, alkaline earth metal ascorbyl phosphates and transition metal ascorbyl phosphates.

[0116] It is also possible to use ascorbic acid precursors such as active agent amides and active agent saccharide derivatives, which respectively involve proteases or peptidases and glycosidases as enzymes to release ascorbic acid in situ. These compounds are described in patent EP 0 667 145.

[0117] The saccharide derivatives of the active agent are particularly selected from C3 to C6 saccharide derivatives. They are particularly selected from glucosyl, mannosyl, fructosyl, fucosyl, N-acetylglucosamine, galactosyl and N-acetylgalactosamine derivatives, N-acetylmuramic acid derivatives and sialic acid derivatives, and mixtures thereof.

[0118] Secondary precursors of ascorbic acid may be selected from derivatives that are hydrolyzed by other enzymes, for example, esterases, phosphatases, sulfatases, etc. According to the present invention, secondary precursors of the active agent may be selected, for example, from phosphates; sulfates; palmitates; acetates; propionates; ferulates and, in general, alkyl or acyl esters; alkyl or acyl ethers of the active agent. The acyl and alkyl radicals, in particular, contain from 1 to 30 carbon atoms. 3-O-ethyl ascorbic acid may be cited as an active ingredient in skincare products.

[0119] In particular, the second precursor may be an ester derived from the reaction with a mineral acid such as a sulfate or a phosphate to react with a sulfatase or a phosphatase on contact with the skin, and the second precursor may be an acyl or alkyl ester derived from the reaction with an organic acid, for example palmitic acid, acetic acid, propionic acid, nicotinic acid, 1,2,3-propanetricarboxylic acid or ferulic acid to react with a specific skin esterase.

[0120] Other derivatives are described, for example, in patent EP 1 430 883.

[0121] Analogues of ascorbic acid are more particularly its salts, especially alkali metal salts, for example sodium ascorbate, its esters, especially its acetic, propionic or palmitic esters, or its sugars, especially glycosyl ascorbic acid.

[0122] As a depigmenting or lightening agent, mention may be made of resorcinol derivatives.

[0123] The resorcinol derivative may preferably be derivatives substituted at position 4, such as 4-alkylresorcinols, more preferably phenylethyl resorcinol, 4-n-butylresorcinol, and 4-(tetrahydro-2H-pyran-4-yl)benzene-1,3-diol, and in particular phenylethyl resorcinol because of its lightening effect. Phenylethyl resorcinol is also called 4-(l-phenylethyl)-1,3-benzenediol and is represented by the following chemical formula. Phenylethyl resorcinol may be obtained, for example, from Symrise Corp (product name: Symwhite 377®). HQ v OH

[0124] Other examples of resorcinol derivatives include: 2-methylresorcinol, 5-methylresorcinol, 4-methylresorcinol, 4-ethylresorcinol, 2,5-dimethylresorcinol, 4,5-dimethylresorcinol, 2,4-dimethyl-1,3-benzenediol, 3,5-dihydroxybenzylamine, 5-methoxyresorcinol, 3,5-dihydroxybenzyl alcohol, 2-methoxyresorcinol, 4-methoxyresorcinol, 3,5-dihydroxytoluene monohydrate, 4-chlororesorcinol, 2-chlororesorcinol, 2',4'-dihydroxyacetophenone, 3',5'-dihydroxyacetophenone, 2,6-Dihydroxy-4-methylbenzaldehyde, 4-propylresorcinol, 2,4-dihydroxy-1,3,5-trimethylbenzene, 3,5-dihydroxybenzamide, 2,6-dihydroxybenzamide, 2,4-dihydroxybenzamide, 2,4-dihydroxybenzoic acid, 2,6-dihydroxybenzoic acid, 3,5-dihydroxybenzoic acid, 2,6-dihydroxy-4-methylbenzyl alcohol, 3,5-dihydroxyanisole hydrate, 4-aminoresorcinol hydrochloride, 2-aminoresorcinol hydrochloride,5-Aminobenzene-1,3-diol hydrochloride, 2',4'-dihydroxypropiophenone, 2',4'-dihydroxy-3'-methylacetophenone, (2,4-dihydroxyphenyl)acetone, (3,5-dihydroxyphenyl)acetone, 2,6-dihydroxy-4'-methylacetophenone, 4-n-butylresorcinol, 2,4-diethyl-1,3-benzenediol, 3,5-dihydroxy-4-methylbenzoic acid, 2,6-dihydroxy-4-methylbenzoic acid, 2,4-dihydroxy-6-methylbenzoic acid, 3,5-dihydroxyphenylacetic acid, 2-ethyl-5-methoxybenzene-1,3-diol, 4-amino-3,5-dihydroxybenzoic acid, monohydrate of 3,5-Dihydroxyacetophenone, 3,5-Dihydroxybenzylamine hydrochloride, 4,6-Dichlororesorcinol, 2',4'-Dihydroxy-3'-methylpropiophenone, L-(3-ethyl-2,6-dihydroxyphenyl)ethan-l-one, 2',6'-Dihydroxy-4'-Methoxyacetophenone, L-(2,6-Dihydroxy-3-Methoxyphenyl)ethan-l-one, 3(2,4-Dihydroxyphenylpropionic acid and 2,4-Dihydroxy-3,6-Dimethylbenzoic acid.

[0125] Tranexamic acid and its derivatives can also be cited as a depigmenting or lightening agent.

[0126] Examples of tranexamic acid derivatives include tranexamic acid dimers (such as trans-4-(trans-aminomethylcyclohexanecarbonyl)aminomethylcyclohexane carboxylic acid), tranexamic acid and hydroquinone esters (such as trans-4-aminomethylcyclohexane carboxylate), and tranexamic acid and acid esters. gentisic acid (such as 2-(trans-4-aminomethylcyclohexanecarbonyloxy)-5-hydroxybenzoic acid and its salts), tranexamic amides (such as trans-4-aminomethylcyclohexane carboxylic acid methylamide and its salts, and trans-4-(p-methoxybenzoyl)aminomethylcyclohexane carboxylic acid and its salts, and trans-4-guanidinomethylcyclohexane carboxylic acid and its salts), and the like.

[0127] It is preferable that the depigmenting or lightening agent be chosen from the group consisting of niacinamide, phenylethyl resorcinol, tranexamic acid and a mixture thereof.

[0128] Hyaluronic acid substances can be cited as an anti-aging agent.

[0129] The hyaluronic acid substance may be selected from the group consisting of hyaluronic acid, hyaluronic acid salts, hyaluronic acid derivatives, hyaluronic acid derivative salts and mixtures thereof.

[0130] Hyaluronic acid is a predominant glucosaminoglycan found in the skin. Fibroblasts primarily synthesize collagen, matrix glycoproteins other than collagen (fibronectin, laminin), proteoglycans, and elastin. Keratinocytes, on the other hand, primarily synthesize sulfated glycosaminoglycans and hyaluronic acid. Hyaluronic acid is also called hyaluronan.

[0131] Hyaluronic acid is present in its free state in the epidermis and dermis and is responsible for skin turgor. This polysaccharide can actually retain a large volume of water, corresponding to 1,000 times its weight. In this sense, hyaluronic acid plays an important role in increasing the amount of bound water in tissues, as well as in the mechanical properties of the skin and in the formation of wrinkles.

[0132] Hyaluronic acid can be represented by the following chemical formula.

[0134] In the context of the present invention, the term "hyaluronic acid" specifically covers the basic unit of hyaluronic acid of formula:

[0135] This is the smallest fraction of hyaluronic acid comprising a disaccharide dimer, namely D-glucuronic acid and N-acetylglucosamine.

[0136] Hyaluronic acid derivatives may be selected from the group consisting of hydrolyzed hyaluronic acid, acetylated hyaluronic acid, cationic hyaluronic acid and mixtures thereof.

[0137] Cationic hyaluronic acid comprises at least one cationic fraction. The cationic fraction may be a trialkyl ammonium group such as -N+(CH3)3. The cationic fraction may include at least one hydroxyl group. Examples of the cationic group include -CH2-CH(OH)-CH2-N+(CH3)3.

[0138] Examples of cationic hyaluronic acid include hydroxypropyltrimonium hyaluronate.

[0139] Examples of hyaluronic acid salts or salts of hyaluronic acid derivatives include alkali metal salts such as sodium salt and potassium salt, alkaline earth metal salts such as magnesium salts, ammonium salts and mixtures thereof.

[0140] The molecular weight of the hyaluronic acid substance is not limited. The molecular weight of the hyaluronic acid substance may be greater than or equal to 5 kDa, preferably greater than or equal to 20 kDa, and more preferably greater than or equal to 100 kDa. The molecular weight of the hyaluronic acid substance may be less than or equal to 20 MDa, preferably less than or equal to 10 MDa, and more preferably less than or equal to 2,000 kDa. Thus, the molecular weight of the hyaluronic acid substance may be from 5 kDa to 20 MDa, preferably from 20 kDa to 10 MDa, and more preferably from 100 kDa to 2,000 kDa.

[0141] Unless otherwise specified in the descriptions, "molecular weight" means an average number molecular mass.

[0142] The hyaluronic acid substance may in particular be hyaluronic acid supplied by Hyactive under the trade name CPN (MW: 10 to 150 kDa), by Soliance under the trade name Cristalhyal (MW: 1 to 1.4 MDa), by Bioland under the name Nutra HA (MW: 820,000 Da), by Bioland under the name Nutra AF (MW: 69,000 Da), or by Bioland under the name Oligo HA (MW: 6,100 Da).

[0143] A single hyaluronic acid substance of a single molecular weight, or a combination of two or more hyaluronic acid substances of different molecular weights, may be used.

[0144] In one embodiment of the present invention, the cosmetic active substance may be chosen from skin care active substances, preferably from the group consisting of depigmenting or brightening agents, anti-aging agents and mixtures thereof, and more preferably from the group consisting of vitamin B3 and its derivatives, ascorbic acid and its derivatives, resorcinol derivatives, tranexamic acid and its derivatives, hyaluronic acid substances and mixtures thereof.

[0145] In another embodiment of the present invention, the cosmetic active substance may be chosen from depigmenting or lightening agents, and preferably from the group consisting of niacinamide, phenylethyl resorcinol, tranexamic acid and a mixture thereof.

[0146] (Quantity of cosmetic active substance)

[0147] The quantity of the cosmetic active substance(s) in the composition used for the cosmetic process according to the present invention is not limited.

[0148] The quantity of the cosmetic active substance(s) in the composition to be used for the cosmetic process according to the present invention may be greater than or equal to 0.001% by weight, preferably greater than or equal to 0.01% by weight, and more preferably greater than or equal to 0.1% by weight, relative to the total weight of the composition.

[0149] The quantity of the cosmetic active substance(s) in the composition to be used for the process according to the present invention may be less than or equal to 20% by weight, preferably less than or equal to 15% by weight, and more preferably less than or equal to 10% by weight, relative to the total weight of the composition.

[0150] Thus, the quantity of the cosmetic active substance(s) in the composition to be used for the cosmetic process according to the present invention can range from 0.001% to 20% by weight, preferably from 0.01% to 15% by weight, and more preferably from 0.1% to 10% by weight, relative to the total weight of the composition.

[0151] (Vehicle)

[0152] The composition to be used for the cosmetic process according to the present invention may include at least one vehicle.

[0153] The vehicle in the composition to be used for the cosmetic process according to the present invention is not limited.

[0154] For example, the vehicle can be chosen from hydrophilic and hydrophobic media.

[0155] Hydrophilic media can be alcohols: in particular monovalent alcohols such as ethyl alcohol, isopropyl alcohol, benzyl alcohol and phenylethyl alcohol; diols such as ethylene glycol, propylene glycol and butylene glycol; other polyols such as glycerol, sugar and carbohydrate alcohols; and ethers such as monomethyl, monoethyl and monobutyl ethers of ethylene glycol, monomethyl, monoethyl and monobutyl ethers of propylene glycol, and monomethyl, monoethyl and monobutyl ethers of butylene glycol.

[0156] Hydrophobic media can be chosen from oils.

[0157] It may be preferable for the composition to be used for the cosmetic process according to the present invention to include water.

[0158] The quantity of the vehicle(s) in the composition to be used for the present invention may be greater than or equal to 50% by weight, preferably greater than or equal to 55% by weight, and more preferably greater than or equal to 60% by weight, relative to the total weight of the composition.

[0159] The quantity of the vehicle(s) in the composition to be used for the present invention may be less than or equal to 99% by weight, preferably less than or equal to 95% by weight, and more preferably less than or equal to 90% by weight, relative to the total weight of the composition.

[0160] The quantity of the vehicle(s) in the composition to be used for the present invention may be from 50% to 99% by weight, preferably from 55% to 95% by weight, and more preferably from 60% to 90% by weight, relative to the total weight of the composition.

[0161] (Optional substances)

[0162] The composition to be used for the cosmetic process according to the present invention may include, in addition to the aforementioned substances, additives generally used in cosmetics, more specifically, surfactants or emulsifiers, hydrophilic or lipophilic thickeners, natural extracts derived from animals or plants, waxes and the like, within a range which does not affect the effects of the present invention.

[0163] The composition to be used for the cosmetic process according to the present invention may include the above optional additive(s) in an amount of 0.01% to 50% by weight, preferably 0.05% to 30% by weight, and more preferably 0.1% to 10% by weight, relative to the total weight of the composition.

[0164] (Preparation)

[0165] The composition to be used for the present invention can be prepared, for example, by mixing one or more cosmetic active substances such as one or more depigmenting or lightening agents, and one or more vehicles, as essential substances, and one or more optional substances, if necessary, as explained above.

[0166] The method and means for mixing the above essential and optional substances are not limited. Any conventional method and means may be used to mix the above essential and optional substances to prepare the composition to be used for the present invention. {Micro-needle sheet}

[0167] The cosmetic process according to the present invention includes the step of applying a sheet of microneedles to a keratinous substance, such as skin and lips.

[0168] The microneedle sheet to be used for the cosmetic process according to the present invention comprises a substrate sheet and a plurality of microneedles on the substrate sheet.

[0169] The microneedle sheet to be used for the present invention can be considered as a cosmetic device, preferably a cosmetic device for a keratinous substance, and more preferably a cosmetic device for the skin, in particular the skin of the face, as well as the lips.

[0170] According to the cosmetic process according to the present invention, a microneedle sheet comprising a substrate sheet and a plurality of microneedles on the substrate sheet is applied to a keratinous substance, such as skin and lips, so that the microneedles can penetrate the keratinous substance, with a linear movement on the keratinous substance in order to make at least one pass on the keratinous substance.

[0171] It is preferable that the linear movement be carried out over a desired area on the keratinous substance. For example, it is preferable that the application site of the microneedle sheet be able to move in a linear direction over a desired area of ​​the surface of the keratinous substance, provided that the microneedles can penetrate the desired area on the keratinous substance.

[0172] The cosmetic process according to the present invention may further include the step of removing micro-needles from the surface of the keratinous substance.

[0173] (Microneedles)

[0174] The microneedle sheet to be used for the present invention comprises a plurality of microneedles.

[0175] The microneedles are present on the surface of a substrate sheet. The microneedles may be present on 50% or more, preferably 70% or more, and more preferably 90% or more of the surface of the substrate sheet.

[0176] It is preferable that the microneedles be present on one of the surfaces of a substrate sheet.

[0177] It is preferable that the microneedles of the microneedle sheet to be used for the present invention be designed to penetrate or enter the stratum corneum of the skin, in particular the skin of the face, as well as the lips.

[0178] A microneedle can be of any size and shape suitable for perforating the stratum corneum. It may be preferable for microneedles to be designed to pierce and penetrate the stratum corneum. Microneedles can create openings or passages in the stratum corneum.

[0179] If necessary, the height of the microneedles can be adjusted to allow penetration of the epidermis and / or dermis of the skin, preferably the epidermis, and more preferably one of the layers of the epidermis.

[0180] The shape of the microneedles is not limited as long as the shape is a "needle." It will be apparent to those skilled in the art that the microneedles for the present invention can take any reasonable shape, including, but not limited to, pyramids, cones, rods, and / or pillars. As such, the microneedles may have the same diameter at the tip as at the base or may be tapered in the direction from base to tip.

[0181] For example, the shape of the microneedle may be a triangular pyramid, a square pyramid, or a pentagonal pyramid. Alternatively, the microneedle may be cylindrical, preferably with a point that can be formed by cutting the cylinder diagonally. The cross-section of the microneedle may take any geometric shape, including circular, triangular, square, rectangular, polyhedral, regular or irregular, and the like. In one embodiment, a group of microneedles may take the form of hollow microcapillaries. However, for the present invention, solid (non-hollow) microneedles may be preferable.

[0182] Reference is therefore made to "microneedles" as the type of microprotrusion or microprojection used. It will be understood by those skilled in the art that in many cases, the same inventive principles apply to the use of other microprotrusions or microprojections for penetrating the skin. Other microprotrusions or microprojections may include, for example, microblades as described in US Patent No. 6,219,574 and Canadian Patent Application No. 2,226,718 and sharp microneedles as described in US Patent No. 6,652,478.

[0183] The height or length of the microneedle of the microneedle sheet to be used for the present invention can be from 10 to 300 micrometers, preferably from 30 to 200 micrometers, and more preferably from 50 to 100 micrometers.

[0184] According to one embodiment of the present invention, the micro-needle is in the form of a cone.

[0185] The cone may include a distal end such as a point and a base. The base may be a circle or an oval.

[0186] The height or length of the microneedle cone of the microneedle sheet to be used for the present invention can be from 10 to 300 micrometers, preferably from 30 to 200 micrometers, and more preferably from 50 to 100 micrometers.

[0187] The base of the microneedle cone of the microneedle sheet to be used for the present invention may have a diameter or width of 10 to 150 micrometers, preferably 15 to 100 micrometers, and more preferably 20 to 50 micrometers. If the base of the microneedle cone of the microneedle sheet to be used for the present invention is oval or elliptical in shape, the length of the major axis or the width of the oval may be 10 to 150 micrometers, preferably 15 to 100 micrometers, and more preferably 20 to 50 micrometers.

[0188] The microneedle may have an aspect ratio (length / width at the base) of at least about 3:1, at least about 2:1 or at least about 1:1. The ratio (height of the cone) / (diameter of the base of the cone) of the microneedle may be greater than or equal to 1, preferably greater than or equal to 1.5, and more preferably greater than or equal to 2.0.

[0189] According to another embodiment of the present invention, the micro-needle is pyramid-shaped, such as a triangular pyramid and a square pyramid.

[0190] The pyramid may include a distal end such as a point and a base. The shape of the base may be a triangle or a square.

[0191] The height or length of the pyramid of the microneedle of the microneedle sheet to be used for the present invention can be from 10 to 300 micrometers, preferably from 30 to 200 micrometers, and more preferably from 50 to 100 micrometers.

[0192] The base of the microneedle pyramid of the microneedle sheet to be used for the present invention may have a width or side length of 10 to 150 micrometers, preferably 15 to 100 micrometers, and more preferably 10 to 50 micrometers. If the base of the microneedle pyramid of the microneedle sheet to be used for the present invention is triangular or square, the length of the width or side length of the triangle or square may be 10 to 150 micrometers, preferably 15 to 100 micrometers, and more preferably 20 to 50 micrometers.

[0193] The microneedle may have an aspect ratio (length / width at the base) of at least about 3:1, at least about 2:1 or at least about 1:1. The ratio (height of the pyramid) / (width of the base of the pyramid) of the microneedle may be greater than or equal to 1, preferably greater than or equal to 1.5, and more preferably greater than or equal to 2.0.

[0194] It may be preferable that the microneedle be able to penetrate into a keratinous substance, such as skin and lips, to a depth of less than or equal to 200 micrometers, preferably less than or equal to 180 micrometers, and more preferably less than or equal to 160 micrometers.

[0195] A very narrow spacing of microneedles may not provide the microneedles with sufficient surface area to prevent them from penetrating the skin. On the other hand, a spacing that is too wide may also lead to a problem whereby the individual microneedle may not have sufficient pressure for penetration. Thus, it may be preferable for a microneedle array spacing of 400 to 700 micrometers, and more preferably 400 to 500 micrometers.

[0196] The number of microneedles and the spacing between microneedles depend on certain factors such as the desired color pattern and the width of a microneedle. For example, if a color pattern with a width of 0.5 micrometers is desired, the use of a microneedle sheet with a (2x2) microneedle array with a spacing of 0.5 mm may be the most appropriate.

[0197] In one embodiment, the density of microneedles can be from 100 to 2,000 microneedles / cm2, preferably 200 to 1,000 microneedles / cm2, and even more preferably 200 to 500 microneedles / cm2.

[0198] It is preferable that the microneedles not be soluble.

[0199] The microneedle “non-soluble” means that the microneedle cannot decompose or disintegrate inside a keratinous substance such as skin and lips, for example, by a natural hydrating factor or external moisture.

[0200] It is preferable that the microneedles not be water-soluble.

[0201] Microneedles can be made of organic or inorganic materials. Examples of organic materials include synthetic polymers, such as polyethylene, polypropylene, and photosensitive resins, biodegradable plastics, cellulose derivatives, and mixtures thereof. Examples of inorganic materials include metals, such as stainless steel, nonmetals such as silicon, glass, and ceramics, and mixtures thereof. Any other material suitable for implantation in the skin or body may also be used.

[0202] It is preferable that microneedles be sterile or sterilized before use. It is preferable that microneedles be used only once and therefore be disposable.

[0203] It is preferable that the microneedles be composed of inorganic materials, more preferably of metals or non-metals, and even more preferably of silicon (in particular, monocrystalline silicon).

[0204] It is also preferable that the microneedles be solid (not hollow).

[0205] (Substrate sheet)

[0206] The microneedle sheet to be used for the present invention comprises a substrate sheet on which the microneedles are present or placed.

[0207] The substrate sheet and the microneedles can be separated or integrated.

[0208] For example, the substrate sheet and the microneedles may comprise at least one common material. Thus, in one embodiment, the substrate sheet and the microneedles may be a single element comprising at least one common material. Preferably, the single element may be prepared using the same material.

[0209] On the other hand, the substrate sheet may be different from or distinct from the microneedles. For example, the substrate sheet and the microneedles may be made of different materials. In this case, the substrate sheet may be chosen, for example, from masks, wipes, patches, and, in general, all types of porous substrate sheets. Preferably, these substrate sheets have an oblong structure, that is, a thickness less than the dimensions of the plane in which they are defined.

[0210] The substrate sheet can be cut to take the form of a stamp, a disc, a mask, a towel, a glove, a pre-cut roll or any other shape suitable for cosmetic use.

[0211] (Preparation)

[0212] There are no limitations as to how the microneedle sheet for use in the cosmetic process according to the present invention can be prepared. It is possible to prepare the microneedle sheet for use in the cosmetic process according to the present invention using conventional technologies such as molding, 3D printing, metalworking, and the like.

[0213] The shape of the microneedle sheet to be used for the cosmetic process according to the present invention is not limited and can be any shape such as the shape of the lips or a shape suitable for application under the eyes, depending on the target of application of the microneedle sheet. {Device}

[0214] In the cosmetic process according to the present invention, the microneedle sheet is applied to a keratinous substance, such as skin and lips, so that the microneedles can penetrate the keratinous substance.

[0215] It is preferable that the microneedles be able to penetrate the keratinous substrate repeatedly.

[0216] The method of performing repeated microneedle penetrations into a keratinous substance is not limited. For example, repeated penetrations can be performed by tapping the back surface of the microneedle sheet's substrate sheet several times with the fingers so that the microneedles on the front surface of the substrate sheet can repeatedly penetrate the keratinous substance.

[0217] In addition, it is preferable to perform repeated microneedle penetrations using vibrations towards a keratinous substance such as skin and lips.

[0218] For example, as shown in [Fig. 1], a sheet of microneedles 1 can be connected to an oscillator 2 that can produce vibrations toward the surface of a keratinous substance, corresponding to the up and down direction in [Fig. 1]. The type of oscillator 2 is not limited as long as it can produce vibrations. For example, oscillator 2 can be made of a piezoelectric element. Of course, any other actuator that can move repeatedly, preferably vibrate, toward a keratinous substance can be used instead of oscillator 2.

[0219] In [Fig.1], the microneedle sheet 1 can move up and down according to the vibrations caused by the oscillator 2, and thus the microneedles on the microneedle sheet 1 can repeatedly penetrate a keratinous substance such as skin and lips.

[0220] It is preferable that the oscillator 2 be connected to a head that can serve as a receiver for the microneedle sheet 1, and that the substrate sheet of the microneedle sheet 1 be attached to the head. In this way, the vibrations caused by the oscillator 2 can be transmitted to the head. The microneedle sheet 1 can then also vibrate via the head.

[0221] It is preferable to use a device to vibrate the microneedle sheet 1. For example, the device may include the oscillator 2 and the head which is connected to the oscillator 2, as well as a battery, such as a dry cell battery, which can drive the oscillator 2 and a control means for controlling the frequency of the vibrations caused by the oscillator 2. By way of example, a device disclosed in document WO 2011 / 115602, the contents of which are incorporated herein by reference, may be used as the above device.

[0222] When using the above device, the microneedle sheet 1 can be mounted on the head of the device and can be applied to a keratinous substance such as skin and lips so that the microneedles of the microneedle sheet 1 can repeatedly penetrate the keratinous substance.

[0223] The frequency of vibration or tapping is not limited. For example, the frequency may be from 1,000 to 10,000 per minute, preferably from 1,000 to 8,000 per minute, and more preferably from 3,000 to 6,000 per minute.

[0224] It may be preferable to regulate the pressure used to penetrate the microneedles into a keratinous substance. The pressure may depend on certain factors such as the type of microneedles.

[0225] Tapping or vibrating the microneedles allows for continuous and stable skin perforation and can reduce the force required to drive the microneedle into the keratinous substance. It can also provide a massaging effect on the treated area of ​​the keratinous substance.

[0226] {How to perform the cosmetic process}

[0227] According to the cosmetic process according to the present invention, a microneedle sheet comprising a substrate sheet and a plurality of microneedles on the substrate sheet is applied to a keratinous substance, such as the skin, so that the microneedles can penetrate the keratinous substance, with a linear movement over the keratinous substance in order to make at least one pass over the keratinous substance.

[0228] According to the present invention, the above application satisfies the following conditions:

[0229] - the frequency of application of the microneedle sheet to the substance keratin treatment is 3 times or less per week, and

[0230] - the number of passes of the microneedle sheet over the keratinous substance Each application is 5 or less.

[0231] - provided that

[0232] - if the frequency of application of the microneedle sheet to the substance keratinous is 3 times per week, the number of passes of the microneedle sheet over the keratinous substance during each application is not 5,

[0233] and

[0234] - if the number of passes of the microneedle sheet over the substance keratinous during each application is 5, the frequency of application of the micro-needle sheet on the keratinous substance is not 3 times per week.

[0235] Regulating the application frequency and the number of passes in each application in the cosmetic process according to the present invention can reduce the risk of pigmentation due to the use of microneedles.

[0236] Thus, for example, if the frequency of application of the microneedle sheet to the keratinous substance is 3 times per week, the number of passes of the microneedle sheet over the keratinous substance during each application may be less than or equal to 4, preferably less than or equal to 3, and more preferably less than or equal to 2.

[0237] On the other hand, for example, if the number of passes of the microneedle sheet on the keratinous substance during each application is 5, the frequency of application of the microneedle sheet on the keratinous substance can be 2 times per week, and preferably 1 time per week.

[0238] It may be preferable that, in the cosmetic process according to the present invention,

[0239] the frequency of application of the microneedle sheet to the keratinous substance either 3 times a week, and

[0240] that the number of passes of the micro-needle sheet over the keratinous substance during each application is 2.

[0241] It may be preferable that, in the cosmetic process according to the present invention,

[0242] the frequency of application of the microneedle sheet to the keratinous substance either twice a week, and

[0243] that the number of passes of the micro-needle sheet over the keratinous substance during each application is 5. [Necessary and use]

[0244] The present invention also relates to a device for cosmetically treating a keratinous substance, such as skin and lips, comprising:

[0245] - at least one composition comprising at least one cosmetic active substance;

[0246] - a sheet of microneedles, comprising

[0247] - a substrate sheet, and

[0248] - a plurality of micro-needles on the substrate sheet

[0249] - so that the micro-needles can penetrate the keratinous substance, with a linear movement over the keratinous substance to make at least one pass over the keratinous substance when applied to the keratinous substance; and

[0250] - an instruction support including instructions that

[0251] - if the frequency of application of the microneedle sheet to the substance keratinous is 3 times per week, the number of passes of the microneedle sheet over the keratinous substance during each application is not 5,

[0252] and

[0253] - if the number of passes of the microneedle sheet over the substance keratinous during each application is 5, the frequency of application of the micro-needle sheet on the keratinous substance is not 3 times per week.

[0254] The above support can be, for example, a sheet made from any material such as paper.

[0255] The above explanations for the composition and the microneedle sheet for the cosmetic process according to the present invention can also be applied to those of the device according to the present invention.

[0256] The necessary may further include a device for applying the microneedle sheet to the keratinous substance so that the microneedles can penetrate the keratinous substance.

[0257] The above explanations for the device that can be used for the cosmetic process according to the present invention can also be applied to the device that can be used for the necessary purpose according to the present invention.

[0258] Preferably, the device should be capable of repeatedly applying the microneedle sheet. For example, the device may include at least one element capable of vibrating or tapping the microneedle sheet. This element may correspond to the back surface of the substrate sheet if tapping with the fingers is used to repeatedly penetrate the microneedles into a keratinous substance, and to oscillator 2 of [Fig. 1] explained above if vibration is used to repeatedly penetrate the microneedles into a keratinous substance.

[0259] The composition comprising at least one cosmetic active substance may be contained in any container such as a container commonly used for cosmetic purposes.

[0260] The necessary equipment can preferably be used to carry out a cosmetic process according to the present invention.

[0261] The present invention also relates to a use of a microneedle sheet, comprising

[0262] - a substrate sheet, and

[0263] - a plurality of micro-needles on the substrate sheet,

[0264] - so that the microneedles can penetrate a keratinous substance, such as the skin and lips, with a linear movement of the microneedle sheet over the keratinous substance to perform at least one pass of the microneedle sheet over the keratinous substance, when applied to the keratinous substance,

[0265] - provided that

[0266] - if the frequency of application of the microneedle sheet to the substance keratinous is 3 times per week, the number of passes of the microneedle sheet over the keratinous substance during each application is not 5,

[0267] and

[0268] - if the number of passes of the microneedle sheet over the substance keratinous during each application is 5, the frequency of application of the microneedle sheet to the keratinous substance is not 3 times per week,

[0269] - in combination with

[0270] - at least one composition comprising at least one cosmetic active substance,

[0271] - in order to reduce the risk of pigmentation of the keratinous substance.

[0272] The above explanations for the composition and the microneedle sheet for the cosmetic process according to the present invention can also be applied to those of the use according to the present invention.

[0273] More specifically, the use according to the present invention may include

[0274] the first application, on the keratinous substance, of at least one composition comprising at least one cosmetic active substance; and

[0275] the second application, on the keratinous substance, on which the composition has been applied, of a microneedle sheet comprising a substrate sheet and a plurality of microneedles on the substrate sheet so that the microneedles are able to penetrate the keratinous substance, in order to reduce the risk of pigmentation of the keratinous substance.

[0276] It is preferable that the microneedles be able to penetrate the keratinous substrate repeatedly. The repetitions can be based on vibration or tapping of the microneedle foil.

[0277] Another aspect of use according to the present invention may be a composition comprising at least one cosmetic active substance, preferably at least one depigmenting or lightening agent, intended to be used to reduce the risk of pigmentation, in combination with a microneedle sheet comprising a substrate sheet and a plurality of microneedles on the substrate sheet, in which the microneedles can penetrate the keratinous substance.

[0278] According to the above-mentioned application and use of the present invention, the microneedles of a microneedle sheet can deliver the cosmetic active substance to a keratinous substance such as skin and lips to provide the keratinous substance with cosmetic effects. If the cosmetic active substance is a depigmenting or lightening agent, the above-mentioned application and use of the present invention can provide a keratinous substance such as skin with depigmenting or lightening effects. If the cosmetic active substance is an anti-aging agent, such as an anti-wrinkle agent, the above-mentioned application and use of the present invention can provide a keratinous substance such as skin with anti-aging effects, such as anti-wrinkle effects. EXAMPLES

[0279] The present invention will be described in more detail by means of examples. However, these examples shall not be construed as limiting the scope of the present invention. The examples below are presented as non-limiting illustrations within the field of the present invention. Examples 1 and 2 and comparative examples 1 to 4

[0280] (Microneedle device)

[0281] A square microneedle sheet (5 mm x 5 mm square) with 7 x 7 microneedles on a substrate sheet was used. Each microneedle was pyramidal in shape with a length or height of 80 pm and a base width of 40 pm. The microneedles were made of monocrystalline silicon.

[0282] The square microneedle sheet has been mounted on a head (first end) of a device as shown in document WO 2011 / 115602, wherein the head can vibrate with the axis of the device, to prepare a microneedle device which can apply the microneedle sheet to the skin with a vibration action towards the skin so that the microneedles can penetrate the skin repeatedly.

[0283] (Composition)

[0284] The following composition A shown in Table 1 was prepared by mixing the ingredients shown in Table 1.

[0285] [Table 1] Table 1 Composition by weight (%) Glycerin 5 Sodium hyaluronate 1.5 Preservative qs Hydrogenated castor oil PEG-60 0.32 Water qsp 100

[0286] (Evaluation)

[0287] First, for examples 1 and 2 and comparative examples 1 to 4, a human cadaver skin of a shape of 1.5 cm x 1.5 cm square was provided as a skin sample.

[0288] Secondly, for examples 1 and 2 and comparative examples 2 and 4, composition A was applied to a site (1 cm x 1 cm square) on the above skin sample.

[0289] Third, for Examples 1 and 2 and Comparative Examples 3 and 4, the above skin sample was treated with the above microneedle device. More specifically, the above microneedle device was used to apply the microneedle sheet on the above site on the skin sample so that the microneedles repeatedly penetrate the above site on the skin sample, with a vibration frequency of 5,000 times per minute, and a linear movement such as 2 strokes every 8 seconds in order to cover once (one pass) the above site on the skin sample.

[0290] Next, for Examples 1 and 2 and Comparative Examples 1 to 4, twelve skin sections (in the form of thin plates) were obtained by slicing the above skin sample. The twelve skin sections were stained with a modified Fontana-Masson stain to stain the melanin and argentaffin granules in the skin sections black / dark gray / brown. The skin sections were then analyzed by pigmentation analysis, as follows.

[0291] Pigmentation analysis: The amount of melanin present in each section was assessed by estimating the intensity and distribution of the gray tint. In short, an 8-bit grayscale image was obtained by microscopic observation of the section. The image's color space was then converted from the RGB system to the L*a*b* system, and each pixel in each image was evaluated according to its L* value. The results were transformed into ranks of L* values ​​and then normalized to the ratio of the selected area to the plate area to obtain the pigmentation score.

[0292] The results for the skin sections were averaged.

[0293] It should be noted that standardization has been carried out. Standardization means that these extreme values ​​(the smallest and largest values) have been excluded from further analysis. This has reduced the influence of potential "unusual values" and allowed for a proper assessment of the "genuine data".

[0294] Details of the treatments on the skin samples for Examples 1 and 2 and Comparative Examples 1 to 4 were as shown in the following Table 2.

[0295] [Table 2]Table 2 Ex. comp. 1 Ex. comp. 2 Ex. comp. 3 Ex. comp. 4 comp. 1 comp. 2 Application of composition A No Yes No Yes Yes Yes Application of the microneedle device No No Yes Yes Yes Yes Number of microneedle device applications (per week) - - 3 3 3 2 Number of microneedle passes during each application - - 5 5 2 5

[0296] The results are shown in [Fig. 1].

[0297] (Summary)

[0298] Comparative examples 3 and 4 show that the use of the above microneedling device with or without composition A 3 times / week and 5 passes (at each use of the microneedling device) caused propagation effects on the skin.

[0299] On the other hand, examples 1 and 2 show that the pro-pigmentation effects can be reduced by decreasing the frequency of application of the microneedling device or the number of passes of the microneedling device during its application to the skin. Thus, the optimal routine for the microneedling device can be 3 times / week with 2 passes or 2 times / week with 5 passes. Example 3 and comparative examples 5 to 7

[0300] (Microneedle device)

[0301] A square microneedle sheet (5 mm x 5 mm square) with 7 x 7 microneedles on a substrate sheet was used. Each microneedle was pyramidal in shape with a length or height of 80 pm and a base width of 40 pm. The microneedles were made of monocrystalline silicon.

[0302] The square microneedle sheet has been mounted on a head (first end) of a device as shown in document WO 2011 / 115602, wherein the head can vibrate with the axis of the device, to prepare a microneedle device which can apply the microneedle sheet to the skin with a vibration action towards the skin so that the microneedles can repeatedly penetrate the skin.

[0303] (Composition)

[0304] The following composition B shown in Table 3 was prepared by mixing the substances shown in Table 3.

[0305] [Table 3]Table 3 Composition B Weight (%) Caprylyl glycol 0.5 Preservative qs Hydroxyethylpiperazine ethanesulfonic acid 5 Propylene Glycol 2 Glycerin 3 Butylene glycol 10 Hydroxyethyl urea 5 Allantoin 0.3 Niacinamide 5 Xanthan gum 0.15 Phenylethyl resorcinol (Symwhite 377®) 0.3 Tranexamic acid 1 Water qsp 100

[0306]

[0307] (Evaluation) First, for example 3 and comparative examples 5 to 7, a human cadaver skin of a shape of 1.5 cm x 1.5 cm square was provided as a skin sample.

[0308] Secondly, for example 3 and comparative example 6, composition B was applied to a site (1 cm x 1 cm square) on the above skin sample.

[0309] Third, for Example 3 and Comparative Example 7, the above skin sample was treated with the above microneedle device. More specifically, the above microneedle device was used to apply the microneedle sheet to the above site on the skin sample so that the microneedles repeatedly penetrate the above site on the skin sample, with a vibration frequency of 5,000 times per minute, and a linear motion such as 2 strokes every 8 seconds in order to cover the above site on the skin sample once (one pass).

[0310] Next, for Example 3 and comparative Examples 5 to 7, twelve skin sections (in the form of thin plates) were obtained by slicing the above skin sample. The twelve skin sections were stained with a modified Fontana-Masson stain to stain the melanin and argentaffin granules in the skin sections black / dark gray / brown. The skin sections were then analyzed by pigmentation analysis, as follows.

[0311] Pigmentation analysis: The amount of melanin present in each section was evaluated by estimating the intensity and distribution of the gray tint. In short, an 8-bit grayscale image was obtained by microscopic observation of the section. Then, the image's color space was transformed from the system RGB in L*a* b* system, and each pixel of each image was evaluated according to its L* value. The results obtained were transformed into ranks of L* values, then normalized on the ratio between the selected area and the area of ​​the plate in order to obtain the pigmentation score.

[0312] The results for the skin sections were averaged.

[0313] It should be noted that standardization has been carried out. Standardization means that these extreme values ​​(the smallest and largest values) have been excluded from further analysis. This has reduced the influence of potential "unusual values" and allowed for a proper assessment of the "genuine data".

[0314] Details of the treatments on the skin samples for Example 3 and comparative examples 5 to 7 were as shown in the following Table 4.

[0315] [Table 4] Table 4 Ex. comp. 5 Ex. comp. 6 Ex. comp. 7 comp. 3 Application of composition B No Yes No Yes Application of the microneedle device No No Yes Yes Number of microneedle device applications (per week) - - 2 2 Number of microneedle passes during each application - - 5 5

[0316] The results are shown in [Fig.2].

[0317] (Summary)

[0318] Example 3 and comparative examples 5 to 7 show that regulated use of the microneedling device can prevent pro-pigmentation, and that a combination of the use of composition B and regulated use of the microneedling device can provide synergistic effects in reducing the effects of pro-pigmentation on the skin.

Claims

Demands

1. Necessary for cosmetically treating a keratinous substance, such as skin and lips, comprising: - at least one composition comprising at least one cosmetic active substance; - a microneedle sheet, comprising - a substrate sheet, and - a plurality of microneedles on the substrate sheet, - such that the microneedles can penetrate the keratinous substance, with a linear movement over the keratinous substance to make at least one pass over the keratinous substance, when applied to the keratinous substance;and - an instruction support including instructions which specify that - if the frequency of application of the microneedle sheet on the keratinous substance is 3 times per week, the number of passes of the microneedle sheet on the keratinous substance during each application is not 5, and - if the number of passes of the microneedle sheet on the keratinous substance during each application is 5, the frequency of application of the microneedle sheet on the keratinous substance is not 3 times per week.;

2. Necessary according to claim 1, wherein the necessary further comprises a device for applying the microneedle sheet to the keratinous substance so that the microneedles can penetrate the keratinous substance.

3. Necessary according to any one of claims 1 to 2, wherein the microneedles have a height of 10 to 300 micrometers, preferably 30 to 200 micrometers, and more preferably 50 to 100 micrometers.

4. Necessary according to claim 3, wherein the base of the microneedles has a width of 10 to 150 micrometers, preferably 15 to 100 micrometers, and more preferably 20 to 50 micrometers.

5. Necessary according to claim 4, wherein the ratio (pyramid height) / (pyramid base width) of the micro- needles is greater than or equal to 1, preferably greater than or equal to 1.5, and more preferably greater than or equal to 2.0.

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