Beauty method using microneedle
A controlled cosmetic method using microneedles with specific application frequency and pyramidal silicon microneedles addresses the risk of hyperpigmentation, delivering active ingredients for improved skin treatment efficacy and safety.
Patent Information
- Application Number
- JP2024020286
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- Filing Date
- 2024-02-14
- Publication Date
- 2025-08-26
AI Technical Summary
The use of microneedles for cosmetic treatments can induce inflammation and risk of skin hyperpigmentation, particularly in treating conditions like hyperpigmentation, dark circles, and age spots.
A cosmetic method using microneedles that applies a composition with cosmetic active ingredients, followed by a microneedle sheet with controlled frequency and number of passes, reducing the risk of pigmentation by penetrating the skin with pyramidal microneedles made from silicon, typically 10-300 microns tall and 10-150 microns wide, and using a kit with instructions for safe application.
The method effectively delivers cosmetic active ingredients into the skin layers, reducing the risk of pigmentation and providing painless, efficient cosmetic treatments with improved aesthetic outcomes.
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Figure 2025124318000001_ABST
Abstract
Description
[Technical Field]
[0001] The present invention relates to the use of multiple microneedles for the cosmetic treatment of keratinous materials such as the skin and lips. [Background technology]
[0002] The use of different types of microneedles, such as metal, soluble, and hollow microneedles, to enhance the penetration of cosmetic active ingredients into the skin is well known. For example, WO2019 / 100902 discloses a transdermal penetration dermal cosmetic method using microneedles in combination with a cosmetic composition containing several cosmetic active ingredients. In WO2019 / 100902, the microneedles are used every night for 28 days.
[0003] It is known that when using such microneedles, inflammation can be induced in the skin, thus running the risk of causing skin hyperpigmentation, known as post-inflammatory hyperpigmentation, which can be particularly important when microneedles are used to treat hyperpigmentation of the skin, such as melanotic lesions, dark circles, and age spots. [Prior art documents] [Patent documents]
[0004] [Patent Document 1] WO2019 / 100902 [Patent Document 2] EP-A-0487404 [Patent Document 3] EP-A-0425066 [Patent Document 4] Japanese Patent Application Publication No. 05213736 [Patent Document 5] EP0667145 [Patent Document 6] EP1430883 [Patent Document 7] U.S. Patent No. 6,219,574 [Patent Document 8] Canadian Patent Application No. 2226718 [Patent Document 9] U.S. Patent No. 6,652,478 [Patent Document 10] WO2011 / 115602 [Non-patent literature]
[0005] [Non-Patent Document 1] Meylan and Howard: Atom / Fragment contribution method for estimating octanol-water partition coefficients, J. Pharm. Sci., 84: pp. 83-92, 1995. [Non-patent document 2] Exploring QSAR: hydrophobic, electronic and steric constants (ACS professional reference book, 1995) [Non-patent document 3] http: / / esc.syrres.com / interkow / kowdemo.htm Summary of the Invention [Problem to be solved by the invention]
[0006] The object of the present invention is to provide a cosmetic method using microneedles that reduces the risk of pigmentation on keratinous materials such as the skin and lips due to the use of microneedles. [Means for solving the problem]
[0007] The object of the present invention is to provide a cosmetic method for keratinous materials such as the skin and lips, comprising: applying at least one composition comprising at least one cosmetic active ingredient onto keratinous materials; applying a microneedle sheet onto the keratinous material, the microneedle sheet comprising a substrate sheet and a plurality of microneedles on the substrate sheet, the microneedles being capable of penetrating into the keratinous material by linear movement of the microneedle sheet over the keratinous material, passing the microneedle sheet over the keratinous material at least once; Including, The frequency of applying the microneedle sheet to the keratin material is 3 times per week or less; the number of passes of the microneedle sheet during each application over the keratin material is 5 or less; however, If the frequency of application of the microneedle sheet onto the keratinous material is three times per week, the number of passes of the microneedle sheet during each application onto the keratinous material is not five, If the number of passes of the microneedle sheet during each application onto the keratinous material is 5, the frequency of applying the microneedle sheet onto the keratinous material is not 3 times per week; This can be achieved through cosmetic procedures.
[0008] The above step of applying a composition containing at least one cosmetic active ingredient may be carried out before the step of applying a microneedle sheet onto the keratin material.
[0009] The cosmetic active ingredient may be selected from skin care active ingredients, preferably from the group consisting of depigmenting or whitening agents, anti-aging agents, and mixtures thereof, and more preferably from the group consisting of vitamin B3 and derivatives thereof, ascorbic acid and derivatives thereof, resorcinol derivatives, tranexamic acid and derivatives thereof, hyaluronic acid components, and mixtures thereof.
[0010] The cosmetic active ingredient may be selected from depigmenting or whitening agents, preferably from the group consisting of niacinamide, phenylethyl resorcinol, tranexamic acid, and mixtures thereof.
[0011] The amount of the cosmetically active ingredient may be 0.001% to 20% by mass, preferably 0.01% to 15% by mass, and more preferably 0.1% to 10% by mass, relative to the total mass of the composition.
[0012] The microneedles may have a height of 10 to 300 microns, preferably 30 to 200 microns, more preferably 50 to 100 microns.
[0013] The microneedles may be pyramidal in shape.
[0014] The base of the microneedle may have a width of 10 to 150 microns, preferably 15 to 100 microns, and more preferably 20 to 50 microns.
[0015] The ratio of (height of pyramid) / (width of base of pyramid) of the microneedle may be 1 or more, preferably 1.5 or more, and more preferably 2.0 or more.
[0016] The microneedles may be made from an inorganic material, preferably a metal or non-metal, more preferably silicon.
[0017] The present invention also provides a kit for the cosmetic treatment of keratinous materials such as the skin and lips, comprising: at least one composition comprising at least one cosmetic active ingredient; a base sheet, and A plurality of microneedles on the base sheet A microneedle sheet comprising: a microneedle sheet that, when applied to a keratinous material, allows the microneedles to penetrate the keratinous material by a linear movement on the keratinous material that passes the microneedle sheet over the keratinous material at least once; It is a medium of instruction, If the frequency of application of the microneedle sheet onto the keratinous material is three times per week, the number of passes of the microneedle sheet during each application onto the keratinous material is not five, If the number of passes of the microneedle sheet during each application onto the keratinous material is 5, the frequency of applying the microneedle sheet onto the keratinous material is not 3 times per week; and an instruction medium containing the instruction Including, It also concerns kits.
[0018] The kit may further comprise a device for applying the microneedle sheet onto the keratinous material so that the microneedles can penetrate into the keratinous material.
[0019] The device in the kit allows repeated application of the microneedle sheet.
[0020] The present invention also relates to the use of a microneedle sheet in combination with at least one composition comprising at least one cosmetic active ingredient for reducing the risk of pigmentation on keratinous materials, the microneedle sheet comprising: A base sheet; a plurality of microneedles on the base sheet; and when applied to a keratinous material, the microneedles can penetrate into the keratinous material, such as the skin and lips, by linear movement of the microneedle sheet on the keratinous material, passing the microneedle sheet over the keratinous material at least once; however, If the frequency of application of the microneedle sheet onto the keratinous material is three times per week, the number of passes of the microneedle sheet during each application onto the keratinous material is not five, but If the number of passes of the microneedle sheet during each application onto the keratinous material is 5, the frequency of applying the microneedle sheet onto the keratinous material is not 3 times per week; It also relates to the use of microneedle sheets. [Brief explanation of the drawings]
[0021] [Figure 1]1 is a schematic diagram showing a microneedle device preferably used for the present invention. FIG. [Figure 2] 1 is a graph showing pigmentation scores for beauty treatments according to Examples 1-2 and Comparative Examples 1-4. [Figure 3] 1 is a graph showing pigmentation scores for beauty treatments according to Example 3 and Comparative Examples 5 to 7. DETAILED DESCRIPTION OF THE INVENTION
[0022] As a result of intensive research, the present inventors have discovered that it is possible to provide a cosmetic method using microneedles that can reduce the risk of pigmentation on keratinous materials such as the skin and lips due to the use of microneedles.
[0023] Therefore, one aspect of the present invention is a cosmetic method for keratinous materials such as the skin and lips, comprising: applying at least one composition comprising at least one cosmetic active ingredient onto keratinous materials; applying a microneedle sheet onto the keratinous material, the microneedle sheet comprising a substrate sheet and a plurality of microneedles on the substrate sheet, the microneedles being able to penetrate into the keratinous material by linear movement of the microneedle sheet over the keratinous material, passing the microneedle sheet over the keratinous material at least once; Including, The frequency of applying the microneedle sheet to the keratin material is 3 times per week or less; the number of passes of the microneedle sheet during each application over the keratin material is 5 or less; however, If the frequency of application of the microneedle sheet onto the keratinous material is three times per week, the number of passes of the microneedle sheet during each application onto the keratinous material is not five, but If the number of passes of the microneedle sheet during each application onto the keratinous material is 5, the frequency of applying the microneedle sheet onto the keratinous material is not 3 times per week; It is a beauty method.
[0024] According to the present invention, the risk of pigmentation due to the use of microneedles can be reduced, and therefore, possible pigmentation after the use of microneedles can be prevented or suppressed by the present invention.
[0025] The cosmetic method according to the present invention can achieve the above-mentioned effects regardless of the combined use of a composition containing at least one cosmetic active ingredient, such as a depigmenting agent or a whitening agent. However, when the cosmetic method according to the present invention is combined with a composition containing at least one cosmetic active ingredient, the risk of pigmentation can be further reduced.
[0026] According to the present invention, microneedles can penetrate keratinous materials such as skin. Therefore, the microneedles can puncture the surface of the keratinous material to create tiny holes or passages through which cosmetically active ingredients can enter the keratinous material, such as skin. Therefore, the cosmetically active ingredients can penetrate the keratinous material through the tiny holes or passages so that they can enter the stratum corneum and / or reach the bottom of the stratum corneum. Furthermore, the cosmetically active ingredients can pass through the stratum corneum to reach any one of the lower layers of the epidermis, such as the stratum granulosum, stratum spinosum, and stratum basale. Therefore, the cosmetically active ingredients can be easily delivered into the keratinous material. This can result in effective cosmetic effects, such as depigmentation or whitening.
[0027] Furthermore, cosmetic active ingredients that pass through the stratum corneum can diffuse relatively easily onto or into the epidermis and be uniformly distributed throughout the keratinous material, thereby providing a uniform cosmetic effect.
[0028] Since microneedles do not cause any pain, the cosmetic method according to the present invention can provide a painless cosmetic treatment.
[0029] In addition, the cosmetic method according to the present invention can be performed in a relatively short period of time.
[0030] The present invention is therefore advantageous for cosmetic or non-therapeutic treatments.
[0031] The cosmetic method, kit, etc. according to the present invention will be described in detail below.
[0032] [Beauty method] The cosmetic method according to the invention for keratinous materials such as the skin and lips comprises: applying at least one composition comprising at least one cosmetic active ingredient onto keratinous materials; applying a microneedle sheet onto the keratinous material, the microneedle sheet comprising a substrate sheet and a plurality of microneedles on the substrate sheet, the microneedles being able to penetrate into the keratinous material by linear movement of the microneedle sheet over the keratinous material, passing the microneedle sheet over the keratinous material at least once; Including, The frequency of applying the microneedle sheet to the keratin material is 3 times per week or less; the number of passes of the microneedle sheet during each application over the keratin material is 5 or less; however, If the frequency of application of the microneedle sheet onto the keratinous material is three times per week, the number of passes of the microneedle sheet during each application onto the keratinous material is not five, but If the number of passes of the microneedle sheet during each application over the keratinous material is 5, then the frequency of applying the microneedle sheet over the keratinous material is not 3 times per week.
[0033] The cosmetic method according to the invention can be intended for the cosmetic treatment of keratinous materials such as the skin and lips, preferably the skin, more preferably the skin of the face.
[0034] The cosmetic method according to the invention can be used to improve the aesthetic appearance of keratinous materials, for example by depigmenting or whitening the keratinous materials.
[0035] The cosmetic method according to the present invention can reduce the risk of pigmentation in keratinous materials. Thus, for example, when microneedles are used for the cosmetic treatment of hyperpigmentation of the skin, such as melanin pigmented lesions, dark circles, and age spots, the cosmetic treatment can be made safer due to the reduced risk of new pigmentation caused by the use of microneedles.
[0036] Hereinafter, examples of microneedle sheets used for the cosmetic method according to the present invention and examples of how to carry out the cosmetic method according to the present invention will be described in detail.
[0037] {composition} The cosmetic method according to the present invention comprises the step of applying at least one composition containing at least one cosmetic active ingredient onto keratinous materials such as the skin and lips.
[0038] The step of applying at least one composition comprising at least one cosmetic active ingredient onto the keratinous material can be carried out by using any application device, such as a brush.
[0039] It may be preferable that a composition containing at least one cosmetic active ingredient be applied onto the keratinous material in combination with at least one porous sheet, such as a woven or nonwoven fabric, for better contact of the composition with the keratinous material and better cosmetic effect on the desired area of the keratinous material.
[0040] The porous sheet can absorb and retain the composition containing at least one cosmetic active ingredient.Therefore, applying the porous sheet can facilitate the composition to contact well with keratinous materials, which can contribute to good cosmetic effects on keratinous materials.
[0041] The type of the above combination is not limited. Therefore, the porous sheet can be applied to the keratinous material before applying the composition to the keratinous material. Alternatively, the porous sheet can be applied to the keratinous material after applying the composition to the keratinous material.
[0042] The step of applying at least one composition containing at least one cosmetic active ingredient onto keratinous materials such as the skin and lips may be performed before or after the step of applying the microneedle sheet onto the keratinous materials.
[0043] Preferably, the step of applying at least one composition containing at least one cosmetic active ingredient to keratinous materials such as skin and lips is carried out before the step of applying the microneedle sheet to the keratinous materials, i.e., the composition is used as a pre-treatment composition for the keratinous materials.
[0044] When the composition is used as a pre-treatment composition, it may be preferable that the microneedle sheet is applied to the keratinous substance without a step of drying the composition on the keratinous substance.In other words, it may be preferable that the composition is applied to the keratinous substance before it is dried or while the keratinous substance is wet so that the microneedles can penetrate into the keratinous substance.
[0045] When the cosmetic method according to the present invention further comprises a step of removing the microneedles from the surface of the keratinous material, after the step of removing the microneedles from the surface of the keratinous material, the composition containing at least one cosmetic active ingredient may be removed from the surface of the keratinous material.
[0046] However, it is preferable that the cosmetic method according to the present invention further comprises a step of maintaining or leaving a composition containing at least one cosmetic active ingredient on the keratinous material after the step of removing the microneedles from the surface of the keratinous material and before the step of removing the composition from the surface of the keratinous material, because the composition can effectively penetrate into the keratinous material through the holes formed on and in the keratinous material by the microneedles.
[0047] The cosmetic active ingredients in the compositions used for the cosmetic method according to the invention can be selected from skin care active ingredients.
[0048] Therefore, it is preferred that the composition used for the cosmetic method according to the present invention is a cosmetic composition, more preferably a skin care cosmetic composition.
[0049] (Skin care active ingredient) The composition used for the cosmetic method according to the invention comprises at least one skin care active ingredient as the cosmetic active ingredient. When two or more skin care active ingredients are used, they may be the same or different.
[0050] Skin care active ingredients are intended herein to mean ingredients for enhancing the aesthetic appearance and / or comfort of the skin. In particular, skin care active ingredients may be intended to reduce visible (dyschromia, hyperpigmentation, etc.) and / or tactile (wrinkles, subcutaneous fat, comedones, acne scars, etc.) irregularities of the skin, and / or to make the skin healthier, less oily and / or less dry.
[0051] Skin care actives, as used herein, are not intended to mean ingredients for imparting color to the skin, and as such, do not include pigments or dyes.
[0052] It may be preferred that the skin care active ingredient has a log P value in the range of -4.5 to 4.5, preferably -4.0 to 4.0, more preferably -3.5 to 3.5.
[0053] The log P value is the base 10 logarithm of the apparent octanol / water partition coefficient. Log P values are known and are determined by standard tests that determine the concentration of a compound in octanol 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 may also be calculated using a number of commercially available software packages that determine log P as a function of the structure of a molecule. An example is Epiwin software from the U.S. Environmental Protection Agency.
[0054] This value can be calculated using, inter alia, ACD (Advanced Chemistry Development) Solaris software V4.67, and 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).
[0055] The skin care actives may be in the form of salts. Salts of the skin care actives include the conventional, non-toxic salts of the compounds, for example, formed from acids or bases.
[0056] Preferably, the skin care active ingredient is a depigmenting or whitening agent, or an anti-aging agent such as an anti-wrinkle agent.
[0057] A depigmenting or whitening agent is herein intended to mean a substance capable of lightening the skin color or enhancing the lightness of the skin surface.
[0058] Mention may be made as depigmenting or whitening agents: vitamin B3 and derivatives.
[0059] Vitamin B3, also known as vitamin PP, has the formula:
[0060] [ka]
[0061] wherein R may be -CONH (niacinamide), -COOH (nicotinic acid or niacin), or CHOH (nicotinyl alcohol), -CO-NH-CH-COOH (nicotinuric acid), or -CO-NH-OH (nicotinylhydroxamic acid). Niacinamide is preferred. is a compound of
[0062] 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 group of -CONH2, products from the reaction of carboxylic acids with amino acids, and esters of nicotinyl alcohol with carboxylic acids such as acetic acid, salicylic acid, glycolic acid or palmitic acid.
[0063] 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.
[0064] Other vitamin B3 derivatives that may also be mentioned are its inorganic salts, such as the chlorides, bromides, iodides or carbonates, and its organic salts, such as those obtained by reaction with carboxylic acids, such as acetates, salicylates, glycolates, lactates, malates, citrates, mandelates, tartrates, etc.
[0065] As depigmenting or whitening agents, mention may be made of ascorbic acid and its derivatives.
[0066] Ascorbic acid is generally in the L-form because it is usually extracted from natural sources.
[0067] Due to its chemical structure (α-keto lactone), which makes it highly 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 selected, for example, from sugar esters of ascorbic acid, or metal salts, alkali metal salts, esters and sugars of phosphoryl ascorbic acid.
[0068] Sugar esters of ascorbic acid that can be used in the present invention are, inter alia, glycosyl, mannosyl, fructosyl, fucosyl, galactosyl, N-acetylglucosamine and N-acetylmuramic acid derivatives of ascorbic acid, as well as mixtures thereof, more particularly ascorbyl glucosides, such as ascorbyl-2-glucoside, 2-O-α-D-glucopyranosyl L-ascorbic acid, or 6-O-β-D-galactopyranosyl L-ascorbic acid. The latter compounds and methods for their preparation are described, inter alia, in documents EP-A-0487404, EP-A-0425066, and JP-A-05213736.
[0069] As regards the metal salt of phosphoryl ascorbic acid, it can be chosen from alkali metal salts, especially sodium ascorbyl phosphate, alkaline earth metal ascorbyl phosphate and transition metal ascorbyl phosphate.
[0070] Ascorbic acid precursors can also be used, such as activator amides and activator sugar derivatives, which require proteases or peptidases and glycosidases, respectively, as enzymes to release ascorbic acid in situ. Such compounds are described in patent EP 0 667 145.
[0071] The active agent sugar derivative is especially selected from C3-C6 sugar derivatives, especially glucosyl, mannosyl, fructosyl, fucosyl, N-acetylglucosamine, galactosyl, and N-acetylgalactosamine derivatives, N-acetylmuramic acid derivatives, and sialic acid derivatives, and mixtures thereof.
[0072] The second ascorbic acid precursor can be selected from derivatives that have been hydrolyzed by other enzymes, such as esterases, phosphatases, and sulfatases. According to the present invention, the second active agent precursor can be selected from, for example, phosphates, sulfates, palmitates, acetates, propionates, ferulates, and generally active agent alkyl or acyl esters; acyl or alkyl ethers. The acyl and alkyl groups preferably contain 1 to 30 carbon atoms. An example of a skin care active ingredient is 3-O-ethyl ascorbic acid.
[0073] In particular, the second precursor may be an ester derived from reaction with a mineral acid, such as a sulfate or phosphate ester, which reacts with sulfatases or phosphatases on contact with the skin, or the second precursor may be an acyl or alkyl ester derived from reaction with an organic acid, such as palmitic acid, acetic acid, propionic acid, nicotinic acid, 1,2,3-propanetricarboxylic acid, or ferulic acid, which reacts with specific skin esterases.
[0074] Other derivatives are described, for example, in patent EP1430883.
[0075] Ascorbic acid analogues are more particularly salts thereof, especially alkali metal salts such as sodium ascorbate, esters thereof, especially acetate, propionate or palmitate esters, or sugars thereof, especially glycosyl ascorbic acids.
[0076] Mention may be made as depigmenting components or whitening agents: resorcinol derivatives.
[0077] The resorcinol derivatives may preferably be derivatives substituted at the 4-position, such as 4-alkylresorcinols, more preferably phenylethylresorcinol, 4-n-butylresorcinol and 4-(tetrahydro-2H-pyran-4-yl)benzene-1,3-diol, and in particular phenylethylresorcinol for its whitening effect. Phenylethylresorcinol, also known as 4-(1-phenylethyl)-1,3-benzenediol, has the chemical formula:
[0078] [ka]
[0079] Phenylethyi resorcinol is available, for example, from Symrise Corp. (product name: Symwhite 377®).
[0080] Other examples of resorcinol derivatives that may be mentioned are: 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. alcohol, 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-di Hydroxyanisole 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, 3,5-dihydroxyacetophenone monohydrate, 3,5-dihydroxybenzylamine hydrochloride, 4,6-dichlororesorcinol, 2',4'-dihydroxy-3'-methylpropiophenone, 1-(3-ethyl-2,6-dihydroxyphenyl)ethan-1-one, 2',6'-dihydroxy-4'-methoxyacetophenone, 1-(2,6-dihydroxy-3-methoxyphenyl)ethan-1-one, 3-(2,4-dihydroxyphenylpropionic acid), and 2,4-dihydroxy-3,6-dimethylbenzoic acid.
[0081] As depigmenting or whitening agents, mention may also be made of tranexamic acid and its derivatives.
[0082] Examples of tranexamic acid derivatives include tranexamic acid dimers (e.g., trans-4-(trans-aminomethylcyclohexanecarbonyl)aminomethylcyclohexanecarboxylic acid hydrochloride), esters of tranexamic acid and hydroquinone (e.g., 4'-hydroxyphenyl trans-4-aminomethylcyclohexanecarboxylate), esters of tranexamic acid and gentisic acid (e.g., 2-(trans-4-aminomethylcyclohexanecarbonyloxy)-5-hydroxybenzoic acid and its salts), and tranexamic acid amides (e.g., trans-4-aminomethylcyclohexanecarboxylic acid methylamide and its salts, trans-4-(p-methoxybenzoyl)aminomethylcyclohexanecarboxylic acid and its salts, and trans-4-guanidinomethylcyclohexanecarboxylic acid and its salts).
[0083] Preferably, the depigmenting or whitening agent is selected from the group consisting of niacinamide, phenylethyl resorcinol, tranexamic acid, and mixtures thereof.
[0084] Hyaluronic acid components may be mentioned as anti-aging agents.
[0085] The hyaluronic acid component may be selected from the group consisting of hyaluronic acid, hyaluronate salts, hyaluronic acid derivatives, hyaluronic acid derivative salts, and mixtures thereof.
[0086] Hyaluronic acid is the main glycosaminoglycan found in the skin. Therefore, fibroblasts predominantly synthesize collagen, non-collagenous matrix glycoproteins (fibronectin, laminin), proteoglycans, and elastin. Keratinocytes, for their part, predominantly synthesize sulfated glycosaminoglycans and hyaluronic acid. Hyaluronic acid is also called hyaluronan.
[0087] Hyaluronic acid exists in the epidermis and dermis in a free state and is responsible for the turgor of the skin. This polysaccharide can actually hold a large volume of water, up to 1000 times its mass. In this sense, hyaluronic acid plays an important role in increasing the amount of water bound in tissues, as well as in the mechanical properties of the skin and wrinkle formation.
[0088] Hyaluronic acid has the chemical formula:
[0089] [ka]
[0090] It can be expressed as:
[0091] In the context of the present invention, the term "hyaluronic acid" specifically refers to the compound of the formula:
[0092] [ka]
[0093] It includes the basic unit of hyaluronic acid. It is the smallest part of hyaluronic acid, containing a disaccharide dimer, namely D-glucuronic acid and N-acetylglucosamine.
[0094] The hyaluronic acid derivative may be selected from the group consisting of hydrolyzed hyaluronic acid, acetylated hyaluronic acid, cationic hyaluronic acid, and mixtures thereof.
[0095] Cationic hyaluronic acid contains at least one cationic moiety. The cationic moiety is -N + The cationic moiety may be a trialkylammonium group such as (CH3)3. The cationic moiety may contain at least one hydroxyl group. Examples of cationic groups include -CH2-CH(OH)-CH2-N + (CH3)3 is an example.
[0096] Examples of cationic hyaluronic acids include hydroxypropyltrimonium hyaluronate.
[0097] Hyaluronic acid salts or hyaluronic acid derivative salts that may be mentioned are alkali metal salts such as sodium salts and potassium salts, alkaline earth metal salts such as magnesium salts, ammonium salts, and mixtures thereof.
[0098] The molecular weight of the hyaluronic acid component is not limited. The molecular weight of the hyaluronic acid component may be 5 kDa or more, preferably 20 kDa or more, and more preferably 100 kDa or more. The molecular weight of the hyaluronic acid component may be 20 MDa or less, preferably 10 MDa or less, and more preferably 2,000 kDa or less. Therefore, the molecular weight of the hyaluronic acid component may be 5 kDa to 20 MDa, preferably 20 kDa to 10 MDa, and more preferably 100 kDa to 2,000 kDa.
[0099] Unless otherwise defined in the description, "molecular weight" may mean number average molecular weight.
[0100] The hyaluronic acid component may be specifically hyaluronic acid supplied by Hyactive under the trade name CPN (MW: 10-150 kDa), by Soliance under the trade name Cristalhyal (MW: 1-1.4 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: 6100 Da).
[0101] A single hyaluronic acid component having a single molecular weight or a combination of two or more hyaluronic acid components having different molecular weights can be used.
[0102] In one embodiment of the present invention, the cosmetic active ingredient may be selected from skin care active ingredients, preferably from the group consisting of depigmenting or whitening agents, anti-aging agents, and mixtures thereof, and more preferably from the group consisting of vitamin B3 and derivatives thereof, ascorbic acid and derivatives thereof, resorcinol derivatives, tranexamic acid and derivatives thereof, hyaluronic acid components, and mixtures thereof.
[0103] In another embodiment of the present invention, the cosmetic active ingredient may be selected from a depigmenting or whitening agent, preferably selected from the group consisting of niacinamide, phenylethyl resorcinol, tranexamic acid, and mixtures thereof.
[0104] (Amount of active beauty ingredients) The amount of the cosmetic active ingredient in the composition used for the cosmetic method according to the present invention is not limited.
[0105] The amount of the cosmetic active ingredient in the composition used for the cosmetic method according to the present invention may be 0.001% by mass or more, preferably 0.01% by mass or more, more preferably 0.1% by mass or more, relative to the total mass of the composition.
[0106] The amount of cosmetically active ingredient in the composition used for the cosmetic method according to the present invention may be 20% by weight or less, preferably 15% by weight or less, more preferably 10% by weight or less, based on the total weight of the composition.
[0107] Therefore, the amount of the cosmetic active ingredient in the composition used for the cosmetic method according to the present invention may be in the range of 0.001% by mass to 20% by mass, preferably 0.01% by mass to 15% by mass, and more preferably 0.1% by mass to 10% by mass, relative to the total mass of the composition.
[0108] (Vehicle) The composition used for the cosmetic method according to the present invention may contain at least one vehicle.
[0109] The vehicle in the composition used for the cosmetic method according to the present invention is not limited.
[0110] For example, the vehicle can be selected from hydrophilic and hydrophobic media.
[0111] The hydrophilic medium may be alcohols, especially monohydric 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, sugars and sugar alcohols; and ethers such as ethylene glycol monomethyl, monoethyl and monobutyl ether, propylene glycol monomethyl, monoethyl and monobutyl ether, and butylene glycol monomethyl, monoethyl and monobutyl ether.
[0112] The hydrophobic medium may be selected from oils.
[0113] The composition used for the cosmetic method according to the present invention may preferably contain water.
[0114] The amount of vehicle in the composition used for the present invention may be 50% by weight or more, preferably 55% by weight or more, more preferably 60% by weight or more, based on the total weight of the composition.
[0115] The amount of vehicle in the composition used for the present invention may be up to 99% by weight, preferably up to 95% by weight, more preferably up to 90% by weight, based on the total weight of the composition.
[0116] The amount of vehicle in the composition used for the present invention may be in the range of 50% to 99% by mass, preferably 55% to 95% by mass, and more preferably 60% to 90% by mass, based on the total mass of the composition.
[0117] (Optional Ingredients) In addition to the above-mentioned components, the composition used for the cosmetic method according to the present invention may contain additives typically used in cosmetics, specifically surfactants or emulsifiers, hydrophilic or lipophilic thickeners, natural extracts of animal or plant origin, waxes, etc., within ranges that do not impair the effects of the present invention.
[0118] The composition used for the cosmetic method according to the present invention may contain the above-mentioned optional additives in an amount of 0.01% by mass to 50% by mass, preferably 0.05% by mass to 30% by mass, and more preferably 0.1% by mass to 10% by mass, relative to the total mass of the composition.
[0119] (preparation) The composition used for the present invention can be prepared, for example, by mixing a cosmetic active ingredient such as a depigmenting or whitening agent as an essential ingredient and a vehicle, and, if necessary, the optional ingredients described above.
[0120] The method and means for mixing the above essential components and optional components are not limited. Any conventional method and means can be used to mix the above essential components and optional components to prepare the composition used in the present invention.
[0121] {Microneedle sheet} The cosmetic method according to the present invention includes a step of applying a microneedle sheet onto keratinous materials such as the skin and lips.
[0122] The microneedle sheet used for the cosmetic method according to the present invention comprises a base sheet and a plurality of microneedles on the base sheet.
[0123] The microneedle sheet used for the present invention may be considered a cosmetic device, preferably a cosmetic device for keratinous materials, more preferably a cosmetic device for the skin, in particular for the facial skin and lips.
[0124] According to the cosmetic method of the present invention, a microneedle sheet comprising a substrate sheet and a plurality of microneedles on the substrate sheet is applied onto keratinous material such as skin and lips so that the microneedles penetrate the keratinous material with a linear movement on the keratinous material and make at least one pass over the keratinous material.
[0125] It is preferable that the linear movement is performed over the desired area on the keratinous material. For example, it is preferable that the application site of the microneedle sheet can be moved in a linear direction over the desired area on the surface of the keratinous material, as long as the microneedles can penetrate into the desired area on the keratinous material.
[0126] The cosmetic method according to the present invention may further comprise the step of removing the microneedles from the surface of the keratinous material.
[0127] (microneedle) The microneedle sheet used for the present invention includes a plurality of microneedles.
[0128] The microneedles are present on the surface of the base 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 base sheet.
[0129] Preferably, the microneedles are present on one of the surfaces of the substrate sheet.
[0130] The microneedles of the microneedle sheet used for the present invention are preferably designed to penetrate or enter the stratum corneum of the skin, particularly the facial skin and lips.
[0131] The microneedles may be of any size and shape suitable for piercing the stratum corneum. It may be preferable for the microneedles to be designed to pierce and traverse the stratum corneum. The microneedles may be capable of creating openings or passageways in the stratum corneum.
[0132] If necessary, the height of the microneedles can be adapted to allow penetration into the epidermis and / or dermis of the skin, preferably the epidermis, more preferably any of the layers in the epidermis.
[0133] The shape of the microneedle is not limited as long as it has a "needle" shape. It will be apparent to those skilled in the art that the microneedles for the present invention can have any reasonable shape, including, but not limited to, pyramidal, conical, rod-like, and / or columnar. Thus, the microneedle may have the same diameter at the tip as at the base, or the diameter may taper from the base to the tip.
[0134] For example, the shape of the microneedles may be in the form of a triangular pyramid, a square pyramid, or a pentagonal pyramid. Alternatively, the microneedles may preferably be in the form of a cylinder with a tip formed by cutting a cylinder diagonally. The cross section of the microneedles may take any geometric shape, including circular, triangular, square, rectangular, polygonal, regular or irregular, etc. In one embodiment, the group of microneedles may take the form of hollow microcapillaries. However, solid (non-hollow) microneedles may be preferred in the present invention.
[0135] As such, reference is made to "microneedles" as the type of microprojection or microprotrusion utilized. Those skilled in the art will understand that in many cases the same inventive principles apply to the use of other microprojections or microprojections to penetrate the skin. Other microprojections or microprojections may include, for example, microblades, as described in U.S. Pat. No. 6,219,574 and Canadian Patent Application No. 2,226,718, and edged microneedles, as described in U.S. Pat. No. 6,652,478.
[0136] The height or length of the microneedles of the microneedle sheet used in the present invention may be 10 to 300 microns, preferably 30 to 200 microns, and more preferably 50 to 100 microns.
[0137] According to one embodiment of the present invention, the microneedles are in the form of cones.
[0138] The cone may have a distal end, such as a tip and a base, which may be circular or elliptical in shape.
[0139] The height or length of the cones of the microneedles of the microneedle sheet used in the present invention may be 10 to 300 microns, preferably 30 to 200 microns, and more preferably 50 to 100 microns.
[0140] The conical bases of the microneedles of the microneedle sheet used for the present invention may have a diameter or width of 10 to 150 microns, preferably 15 to 100 microns, and more preferably 20 to 50 microns. When the conical bases of the microneedles of the microneedle sheet used for the present invention are elliptical or oval in shape, the length or width of the major axis of the ellipse may be 10 to 150 microns, preferably 15 to 100 microns, and more preferably 20 to 50 microns.
[0141] The microneedles may have an aspect ratio (length / width at base) of at least about 3: 1, at least about 2: 1, or at least about 1: 1. The ratio of the microneedle's (cone height) / (cone base diameter) may be 1 or greater, preferably 1.5 or greater, and more preferably 2.0 or greater.
[0142] According to another embodiment of the present invention, the microneedles are in the form of pyramids, for example triangular and square pyramids.
[0143] The pyramid may have a distal end, such as a tip and a base. The base may be triangular or rectangular in shape.
[0144] The height or length of the pyramids of the microneedles of the microneedle sheet used in the present invention may be 10 to 300 microns, preferably 30 to 200 microns, and more preferably 50 to 100 microns.
[0145] The bases of the pyramidal microneedles of the microneedle sheet used for the present invention may have a width or side length of 10 to 150 microns, preferably 15 to 100 microns, and more preferably 10 to 50 microns. When the bases of the pyramidal microneedles of the microneedle sheet used for the present invention are triangular or rectangular, the width or side length of the triangle or rectangle may be 10 to 150 microns, preferably 15 to 100 microns, and more preferably 20 to 50 microns.
[0146] The microneedles may have an aspect ratio (length / width at base) of at least about 3: 1, at least about 2: 1, or at least about 1: 1. The ratio of the height of the pyramid to the width of the base of the pyramid of the microneedle may be 1 or greater, preferably 1.5 or greater, and more preferably 2.0 or greater.
[0147] It may be preferred that the microneedles are capable of penetrating into keratinous materials such as skin and lips to a depth of 200 microns or less, preferably 180 microns or less, more preferably 160 microns or less.
[0148] An extremely narrow pitch of the microneedles cannot provide the microneedles with a sufficient surface area, and as a result, the microneedles cannot penetrate into the skin. On the other hand, a pitch that is too wide can also cause the problem that the individual microneedles cannot obtain sufficient pressure to penetrate. Therefore, it may be preferable that the pitch of the microneedle array is 400 to 700 microns, more preferably 400 to 500 microns.
[0149] The number of microneedles and the pitch between them depend on several factors, such as the desired color pattern and the width of the microneedles. For example, if a color pattern with a width of 0.5 microns is desired, the use of a microneedle sheet having a microneedle array (2x2) with a 0.5 mm pitch may be most appropriate.
[0150] In one embodiment, the density of the microneedles is between 100 and 2000 microneedles / cm 2 , preferably 200 to 1000 microneedles / cm 2 , and even more preferably 200 to 500 microneedles / cm 2 may be.
[0151] Preferably, the microneedles are not dissolvable.
[0152] "Non-dissolvable" microneedles means that the microneedles cannot be destroyed or disintegrated within keratinous materials such as skin and lips, for example, by natural moisturizing agents or external moisture.
[0153] More preferably, the microneedles are not water soluble.
[0154] The microneedles may be made of organic or inorganic materials. Examples of organic materials include synthetic polymers, including polyethylene, polypropylene, and photoresist, biodegradable plastics, cellulose derivatives, and mixtures thereof. Examples of inorganic materials include metals, including stainless steel, non-metals, such as silicon, glass, and ceramics, and mixtures thereof. Furthermore, any other material that can be implanted into the skin or body can also be used.
[0155] Preferably, the microneedles are sterile or sterilized prior to use, more preferably the microneedles are single use and therefore disposable.
[0156] It is preferred that the microneedles are made from an inorganic material, more preferably a metal or non-metal, even more preferably silicon (especially single crystal silicon).
[0157] It is also preferred that the microneedles are solid (non-hollow).
[0158] (Base sheet) The microneedle sheet used for the present invention comprises a substrate sheet on which the microneedles reside or are placed.
[0159] The substrate sheet and the microneedles may be separate or integrated.
[0160] For example, the base sheet and the microneedles may contain at least one common material. Therefore, in one embodiment, the base sheet and the microneedles can be a single element containing at least one common material. Preferably, this single element can be prepared using the same material.
[0161] On the other hand, the substrate sheet may be different or separate 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 selected from, for example, masks, wipes, patches, and generally all types of porous substrate sheets.Preferably, these substrate sheets have an oval structure, i.e., have a thickness smaller than the dimensions of the plane in which they are defined.
[0162] The substrate sheet may be cut into the form of a patch, disc, mask, towel, glove, pre-cut roll, or any other form suitable for cosmetic use.
[0163] (preparation) There are no limitations on how to prepare the microneedle sheet used for the cosmetic method according to the present invention. The microneedle sheet used for the cosmetic method according to the present invention can be prepared based on conventional techniques such as molding, 3D printing, metal processing, etc.
[0164] The shape of the microneedle sheet used for the cosmetic method according to the present invention is not limited, and it can be any shape, such as the shape of the lips or a shape suitable for application under the eyes, depending on the target to which the microneedle sheet is applied.
[0165] {device} In the cosmetic method according to the present invention, the microneedle sheet is applied onto keratinous materials such as skin and lips so that the microneedles can penetrate into the keratinous materials.
[0166] Preferably, the microneedles are capable of repeatedly penetrating the keratinous material.
[0167] There is no limitation on how the microneedles are repeatedly penetrated into the keratinous material. For example, the repeated penetration can be performed by tapping the back surface of the substrate sheet of the microneedle sheet with a finger several times so that the microneedles on the front surface of the substrate sheet can repeatedly penetrate into the keratinous material.
[0168] Furthermore, repeated penetration of the microneedles is preferably performed by using vibrations directed at keratinous materials such as the skin and lips.
[0169] For example, as shown in FIG. 1, the microneedle sheet 1 can be coupled to a vibrator 2 capable of generating vibrations toward the surface of the keratinous material, which corresponds to the up-down direction in FIG. 1. The type of vibrator 2 is not limited as long as it can generate vibrations. For example, the vibrator 2 may be constituted by a piezoelectric element. Naturally, any other actuator capable of repeatedly moving, preferably vibrating, toward the keratinous material can be used instead of the vibrator 2.
[0170] In Figure 1, the microneedle sheet 1 can move up and down based on the vibration caused by the vibrator 2, and therefore the microneedles on the microneedle sheet 1 can repeatedly penetrate into keratinous materials such as the skin and lips.
[0171] It is preferable that the vibrator 2 is connected to a head that can function as a receptor for the microneedle sheet 1, and that the base sheet of the microneedle sheet 1 is attached to the head. Therefore, the vibrations caused by the vibrator 2 can be transmitted to the head. In this way, the microneedle sheet 1 can also vibrate via the head.
[0172] It is preferable to use a device to vibrate the macroneedle sheet 1. For example, the device may include a vibrator 2, a head connected to the vibrator 2, a battery such as a dry cell capable of driving the vibrator 2, and a control means for controlling the frequency of the vibration caused by the vibrator 2. For example, the device disclosed in WO2011 / 115602, the contents of which are incorporated herein by reference, can be used as the device.
[0173] When using the above device, the microneedle sheet 1 can be placed on the head of the device and applied to keratinous materials such as the skin and lips so that the microneedles of the microneedle sheet 1 can repeatedly penetrate into the keratinous material.
[0174] The vibration or tapping frequency is not limited, and may be, for example, 1,000 to 10,000 per minute, preferably 1,000 to 8,000 per minute, and more preferably 3,000 to 6,000 per minute.
[0175] It may be desirable to control the pressure used to penetrate the microneedles into the keratinous material, which may depend on several factors, such as the type of microneedle.
[0176] Tapping or vibrating penetration of the microneedles allows for continuous and stable penetration of the skin and may reduce the force required to drive the microneedles into the keratinous material, which may further provide a massaging effect to the treated area of the keratinous material.
[0177] {How to implement beauty treatments} According to the cosmetic method of the present invention, a microneedle sheet comprising a substrate sheet and a plurality of microneedles on the substrate sheet is applied onto a keratinous material such as skin so that the microneedles penetrate the keratinous material with a linear movement on the keratinous material and make at least one pass over the keratinous material.
[0178] According to the present invention, the application satisfies the following conditions: The frequency of applying the microneedle sheet to the keratinous material is 3 times per week or less; the number of passes of the microneedle sheet during each application over the keratin material is 5 or less; however, If the frequency of application of the microneedle sheet onto the keratinous material is three times per week, the number of passes of the microneedle sheet during each application onto the keratinous material is not five, but If the number of passes of the microneedle sheet during each application over the keratinous material is 5, then the frequency of applying the microneedle sheet over the keratinous material is not 3 times per week.
[0179] Controlling the frequency of application and the number of passes in each application in the cosmetic method according to the present invention may reduce the risk of pigmentation due to the use of microneedles.
[0180] Therefore, for example, if the frequency of application of the microneedle sheet to the keratinous material is three times per week, the number of passes of the microneedle sheet during each application over the keratinous material may be four or less, preferably three or less, and more preferably two or less.
[0181] On the other hand, for example, if the number of passes of the microneedle sheet over the keratinous material during each application is 5, the frequency of applying the microneedle sheet over the keratinous material may be 2 times per week, preferably 1 time per week.
[0182] In the cosmetic method according to the present invention, The frequency of applying the microneedle sheet to the keratin material is three times per week; and The number of passes of the microneedle sheet during each application over the keratin material is two. However, there are cases where this is preferable.
[0183] In the cosmetic method according to the present invention, The frequency of applying the microneedle sheet to the keratin material is twice per week; and The number of passes of the microneedle sheet during each application over the keratin material is 5 However, there are cases where this is preferable.
[0184] [Kit and Use] The present invention also provides a kit for cosmetic treatment of keratinous materials such as the skin or lips, comprising: at least one composition comprising at least one cosmetic active ingredient; a base sheet, and A plurality of microneedles on a substrate sheet A microneedle sheet comprising: a microneedle sheet, wherein when applied onto a keratinous material, the microneedles can penetrate into the keratinous material by linear movement on the keratinous material that passes the microneedle sheet over the keratinous material at least once; It is a medium of instruction, If the frequency of application of the microneedle sheet onto the keratinous material is three times per week, the number of passes of the microneedle sheet during each application onto the keratinous material is not five, If the number of passes of the microneedle sheet during each application onto the keratinous material is 5, the frequency of application of the microneedle sheet onto the keratinous material is not 3 times per week. and an instruction medium containing the instruction The present invention relates to a kit comprising:
[0185] The medium can be, for example, a sheet made of any material, such as paper.
[0186] The above description of the composition and microneedle sheet for the cosmetic method according to the present invention can also be applied to the description of the kit according to the present invention.
[0187] The kit may further comprise a device for applying the microneedle sheet onto the keratinous material so that the microneedles can penetrate into the keratinous material.
[0188] The above description of the devices that can be used for the cosmetic method according to the present invention also applies to the devices that can be used for the kit according to the present invention.
[0189] Preferably, the device can repeatedly apply the microneedle sheet. For example, the device may include at least one element that can vibrate or tap the microneedle sheet. This element can correspond to the back surface of the substrate sheet if finger tapping is used to repeatedly penetrate the microneedles into the keratinous material, or it can correspond to the vibrator 2 described above in Figure 1 if vibration is used to repeatedly penetrate the microneedles into the keratinous material.
[0190] The composition comprising at least one cosmetic active ingredient may be contained in any container, such as a vessel commonly used for cosmetic purposes.
[0191] The kit can preferably be used to carry out the cosmetic method according to the present invention.
[0192] The present invention also relates to the use of a microneedle sheet in combination with at least one composition comprising at least one cosmetic active ingredient for reducing the risk of pigmentation on keratinous materials, the microneedle sheet comprising: A base sheet; a plurality of microneedles on the base sheet; Including, When applied onto a keratinous material, the microneedles are allowed to penetrate into the keratinous material, such as the skin and lips, by linear movement of the microneedle sheet over the keratinous material, passing the microneedle sheet over the keratinous material at least once; however, If the frequency of application of the microneedle sheet onto the keratinous material is three times per week, the number of passes of the microneedle sheet during each application onto the keratinous material is not five, but If the number of passes of the microneedle sheet during each application onto the keratinous material is 5, the frequency of applying the microneedle sheet onto the keratinous material is not 3 times per week; It also relates to the use of microneedle sheets.
[0193] The above explanations regarding the composition and microneedle sheet for the cosmetic method according to the present invention can also be applied to the explanation regarding the use according to the present invention.
[0194] In particular, the use according to the invention provides a reduced risk of pigmentation on keratinous materials, a first application onto the keratinous material of at least one composition comprising at least one cosmetic active ingredient; a second application of a microneedle sheet comprising a substrate sheet and a plurality of microneedles on the substrate sheet onto the keratinous material to which the composition has been applied, so that the microneedles can penetrate into the keratinous material; may include:
[0195] Preferably, the microneedles can repeatedly penetrate the keratinous material. The repetition can be based on vibration or tapping of the microneedle sheet.
[0196] Another embodiment of the use according to the present invention may be a composition comprising at least one cosmetic active ingredient, preferably at least one depigmenting or whitening agent, for use in reducing the risk of pigmentation, in combination with a microneedle sheet comprising a substrate sheet and a plurality of microneedles on the substrate sheet, the microneedles being capable of penetrating into keratinous materials.
[0197] According to the kit and use of the present invention, the microneedles of the microneedle sheet can deliver cosmetically active ingredients into keratinous materials such as skin and lips, thereby providing cosmetic effects to the keratinous materials. If the cosmetically active ingredient is a depigmenting agent or whitening agent, the kit and use of the present invention can provide a depigmenting or whitening effect to keratinous materials such as skin. If the cosmetically active ingredient is an anti-aging agent, such as an anti-wrinkle agent, the kit and use of the present invention can provide an anti-aging effect, such as an anti-wrinkle effect, to keratinous materials such as skin. [Example]
[0198] The present invention will be described in more detail by way of examples. However, these examples should not be construed as limiting the scope of the present invention. The following examples are presented as non-limiting examples in the field of the present invention.
[0199] (Examples 1 to 2 and Comparative Examples 1 to 4) (microneedle device) A square microneedle sheet (5 mm x 5 mm square) containing 7 x 7 microneedles on a substrate sheet was used. Each microneedle had a pyramidal shape with a length or height of 80 μm and a base width of 40 μm. The microneedles were made from single-crystal silicon.
[0200] A microneedle device can be prepared in which a square microneedle sheet is placed on the head (first end) of the device as shown in WO2011 / 115602, and the head vibrates along the axis of the device to apply the microneedle sheet onto the skin so that the microneedles can repeatedly penetrate into the skin with a vibrating action towards the skin.
[0201] (composition) The following composition A shown in Table 1 was prepared by mixing the ingredients shown in Table 1.
[0202] [Table 1]
[0203] (evaluation) First, for Examples 1 and 2 and Comparative Examples 1 to 4, human cadaver skin having a rectangular shape of 1.5 cm x 1.5 cm was prepared as a skin sample.
[0204] Second, 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 skin sample.
[0205] Third, for Examples 1 and 2 and Comparative Examples 3 and 4, the skin samples were treated with the microneedle device. Specifically, using the microneedle device, microneedles were applied to the site on the skin sample with vibrations at a frequency of 5,000 times per minute and linear movements of two strokes per 8 seconds to cover the site on the skin sample once (one pass), so that the microneedles repeatedly penetrated into the site on the skin sample.
[0206] Next, for Examples 1-2 and Comparative Examples 1-4, the above skin samples were sliced to obtain 12 skin sections (in the form of thin plates). The 12 skin sections were stained with a modified Fontana-Masson stain to stain melanin and argyrophilic granules in the skin sections black / dark gray / brown. The skin sections were then analyzed by pigmentation analysis as follows.
[0207] Pigmentation analysis: The amount of melanin present in each section was assessed by estimating the intensity and distribution of gray tones. Briefly, 8-bit grayscale images were obtained by microscopic observation of the sections. The color space of the images was then converted from the RGB system to L * a * b * system, and each pixel of each image is converted to its L * The results were evaluated according to the L * The values were transformed in rank and then normalized in the ratio between the selected area and the area of the plate to obtain a pigmentation score.
[0208] The results for the skin sections were averaged.
[0209] It should be noted that standardization was performed, which entailed excluding extreme values (minimum and maximum values) from subsequent analysis. This allowed reducing the influence of potential "outliers" and allowing for a proper evaluation of the "authentic data."
[0210] Details of the treatment of the skin samples for Examples 1-2 and Comparative Examples 1-4 are shown in Table 2.
[0211] [Table 2]
[0212] The results are shown in Figure 1.
[0213] (overview) Comparative Examples 3 and 4 show that use of the microneedle device with or without Composition A resulted in an enhanced pigmentation effect on the skin at 3 and 5 passes per week (each use of the microneedle device).
[0214] On the other hand, Examples 1 and 2 show that the enhanced pigmentation effect can be reduced by reducing the frequency of application of the microneedle device or the number of passes of the microneedle device during its application on the skin, so the optimal routine for the microneedle device can be 2 passes 3 times per week or 5 passes 2 times per week.
[0215] (Example 3 and Comparative Examples 5 to 7) (microneedle device) A square microneedle sheet (5 mm x 5 mm square) containing 7 x 7 microneedles on a substrate sheet was used. Each microneedle had a pyramidal shape with a length or height of 80 μm and a base width of 40 μm. The microneedles were made from single-crystal silicon.
[0216] A microneedle device can be prepared in which a square microneedle sheet is placed on the head (first end) of the device as shown in WO2011 / 115602, and the head vibrates along the axis of the device so that the microneedles can repeatedly penetrate into keratinous material, thereby applying the microneedle sheet onto the skin with a vibrating action toward the skin.
[0217] (composition) The following composition B shown in Table 3 was prepared by mixing the ingredients shown in Table 3.
[0218] [Table 3]
[0219] (evaluation) First, for Example 3 and Comparative Examples 5 to 7, skin from a human cadaver having a rectangular shape of 1.5 cm x 1.5 cm was prepared as a skin sample.
[0220] Second, for Example 3 and Comparative Example 6, Composition B was applied to a site (1 cm x 1 cm square) on the skin sample.
[0221] Third, for Example 3 and Comparative Example 7, the skin samples were treated with the microneedle device. Specifically, using the microneedle device, a microneedle sheet was applied onto the site on the skin sample with vibrations at a frequency of 5,000 times per minute and linear movements of two strokes per 8 seconds to cover the site on the skin sample once (one pass), so that the microneedles repeatedly penetrated into the site on the skin sample.
[0222] Next, for Example 3 and Comparative Examples 5 to 7, the skin samples were sliced to obtain 12 skin sections (in the form of thin plates). The 12 skin sections were stained with a modified Fontana-Masson stain to stain melanin and argyrophilic granules in the skin sections black / dark gray / brown. The skin sections were then analyzed by pigmentation analysis as follows.
[0223] Pigmentation analysis: The amount of melanin present in each section was assessed by estimating the intensity and distribution of gray tones. Briefly, 8-bit grayscale images were obtained by microscopic observation of the sections. The color space of the images was then converted from the RGB system to L * a * b * system, and each pixel of each image is converted to its L * The results were evaluated according to the L * The values were transformed in rank and then normalized in the ratio between the selected area and the area of the plate to obtain a pigmentation score.
[0224] The results for the skin sections were averaged.
[0225] It should be noted that standardization was performed, which entailed excluding extreme values (minimum and maximum values) from subsequent analysis. This allowed reducing the influence of potential "outliers" and allowing for a proper evaluation of the "authentic data."
[0226] Details of the treatment of the skin samples for Example 3 and Comparative Examples 5 to 7 are shown in Table 4.
[0227] [Table 4]
[0228] The results are shown in Figure 2.
[0229] (overview) Example 3 and Comparative Examples 5-7 demonstrate that controlled use of a microneedle device can prevent hyperpigmentation, and that the combination of use of Composition B with controlled use of a microneedle device can provide a synergistic effect in reducing hyperpigmentation on the skin. [Explanation of symbols]
[0230] 1 Microneedle Sheet 2 oscillators
Claims
1. A cosmetic method for keratinous materials such as the skin and lips, comprising: applying at least one composition comprising at least one cosmetic active ingredient onto keratinous materials; applying a microneedle sheet onto the keratinous material, the microneedle sheet comprising a substrate sheet and a plurality of microneedles on the substrate sheet, the microneedles being able to penetrate into the keratinous material by linear movement of the microneedle sheet over the keratinous material, passing the microneedle sheet over the keratinous material at least once; Including, The frequency of applying the microneedle sheet to the keratin material is 3 times per week or less; the number of passes of the microneedle sheet during each application over the keratin material is 5 or less; however, If the frequency of application of the microneedle sheet onto the keratinous material is three times per week, the number of passes of the microneedle sheet during each application onto the keratinous material is not five, If the number of passes of the microneedle sheet during each application onto the keratinous material is 5, the frequency of application of the microneedle sheet onto the keratinous material is not 3 times per week; Beauty method.
2. The cosmetic method according to claim 1, wherein the step of applying a composition containing at least one cosmetic active ingredient is carried out before the step of applying the microneedle sheet onto a keratinous substance.
3. 3. The cosmetic method according to claim 1 or 2, wherein the cosmetic active ingredient is selected from the group consisting of skin care active ingredients, preferably selected from the group consisting of depigmenting or whitening agents, anti-aging agents, and mixtures thereof, more preferably selected from the group consisting of vitamin B3 and derivatives thereof, ascorbic acid and derivatives thereof, resorcinol derivatives, tranexamic acid and derivatives thereof, hyaluronic acid components, and mixtures thereof.
4. 4. The cosmetic method according to claim 1, wherein the cosmetic active ingredient is selected from depigmenting or whitening agents, preferably selected from the group consisting of niacinamide, phenylethyl resorcinol, tranexamic acid, and mixtures thereof.
5. 5. The cosmetic method according to any one of claims 1 to 4, wherein the amount of the cosmetic active ingredient is 0.001% by mass to 20% by mass, preferably 0.01% by mass to 15% by mass, and more preferably 0.1% by mass to 10% by mass, relative to the total mass of the composition.
6. 6. The cosmetic method according to any one of claims 1 to 5, wherein the microneedles have a height of 10 to 300 microns, preferably 30 to 200 microns, more preferably 50 to 100 microns.
7. The cosmetic method according to any one of claims 1 to 6, wherein the microneedles are pyramidal in shape.
8. 8. The cosmetic method according to claim 7, wherein the base of the microneedle has a width of 10 to 150 microns, preferably 15 to 100 microns, more preferably 20 to 50 microns.
9. 9. The cosmetic method according to claim 7 or 8, wherein the ratio of (height of the pyramid) / (width of the base of the pyramid) of the microneedle is 1 or more, preferably 1.5 or more, and more preferably 2.0 or more.
10. 10. The cosmetic method according to any one of claims 1 to 9, wherein the microneedles are made of an inorganic material, preferably a metal or a non-metal, more preferably silicon.
11. The cosmetic method according to any one of claims 1 to 10, wherein the microneedles can be repeatedly penetrated into the keratinous material.
12. 1. A kit for cosmetic treatment of keratinous materials such as skin and lips, comprising: at least one composition comprising at least one cosmetic active ingredient; a base sheet, and A plurality of microneedles on a substrate sheet A microneedle sheet comprising: a microneedle sheet that, when applied onto a keratinous material, allows the microneedles to penetrate into the keratinous material by a linear movement on the keratinous material that passes the microneedle sheet over the keratinous material at least once; It is a medium of instruction, If the frequency of application of the microneedle sheet onto the keratinous material is three times per week, the number of passes of the microneedle sheet during each application onto the keratinous material is not five, but If the number of passes of the microneedle sheet during each application onto the keratinous material is 5, the frequency of applying the microneedle sheet onto the keratinous material is not 3 times per week; and an instruction medium containing the instruction Includes a kit.
13. The kit of claim 12, further comprising a device for applying the microneedle sheet onto the keratinous material so that the microneedles can penetrate into the keratinous material.
14. The kit of claim 13, wherein the device allows repeated application of the microneedle sheet.
15. 1. Use of a microneedle sheet in combination with at least one composition comprising at least one cosmetic active ingredient for reducing the risk of pigmentation on keratinous materials, the microneedle sheet comprising: A base sheet; A plurality of microneedles on a base sheet; Including, When applied to a keratinous material, the microneedles are allowed to penetrate into the keratinous material, such as the skin and lips, by linear movement of the microneedle sheet on the keratinous material, passing the microneedle sheet over the keratinous material at least once; however, If the frequency of application of the microneedle sheet onto the keratinous material is three times per week, the number of passes of the microneedle sheet during each application onto the keratinous material is not five, If the number of passes of the microneedle sheet during each application onto the keratinous material is 5, the frequency of application of the microneedle sheet onto the keratinous material is not 3 times per week; Use of microneedle sheets.
Citation Information
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