Composition and method for applying the same to the skin to strengthen the skin barrier

Abstract

A composition for strengthening the skin barrier is provided, which contains a compound represented by a specific chemical formula as an active ingredient.

Description

[Technical Field]

[0001] This description is ,set product and a method for strengthening the skin barrier by applying the same to the skin. It is related to. [Background technology]

[0002] Skin performs a variety of essential functions for the human body to survive. The most representative functions of skin include the barrier function to maintain internal homeostasis in response to environmental changes, the sensory function to recognize external changes, and the thermoregulatory function. Among these diverse skin functions, the barrier function is primarily achieved by the stratum corneum, the outermost layer of the skin. The stratum corneum has been reported to not only function as a simple barrier but also influence the function, role, and structure of the inner living cell layers, namely the epidermis and dermis, and its importance is continually increasing. The stratum corneum, composed of dead keratinocytes and intercellular lipids, plays a crucial role as a skin barrier, protecting the skin from external stimuli and preventing moisture evaporation from the inside. Furthermore, keratinocytes in the stratum corneum form the skin barrier through differentiation and keratinization processes.

[0003] There are various factors that cause skin aging, but UV rays in particular cause wrinkles, loss of elasticity, pigmentation, and loss of skin moisture due to damage to the skin barrier. When UV damage reduces the moisture content of the skin surface, the stratum corneum loses its flexibility and becomes dry, which ultimately prevents the skin from functioning properly as a barrier. Therefore, maintaining skin moisture is very important for strengthening the skin barrier.

[0004] There are two types of pores in the epidermis that are associated with water homeostasis: aquaporins (AQPs) and tight junctions (TJs). Filaggrin is a precursor protein of natural moisturizing factors (NMFs) that are responsible for skin moisturization, and it is known that the ability to promote filaggrin production plays an important role in moisturizing (J. Invest. Dermatol. 54, 24-31, 1970).

[0005] Meanwhile, many reports suggest that various inflammatory dermatitis is caused by IgE-related immune mechanisms, and that delayed immune responses due to T cell abnormalities are involved in these cases. In particular, the infiltration of immune-related cells, such as macrophages, Th lymphocytes, and mast cells, significantly increases in areas affected by atopic dermatitis. In atopic dermatitis patients, the blood IgE concentration is high in the skin, due to an increase in the number of Th2 cells, which promote IgE secretion through the stimulation of B lymphocytes by Th2 cytokines, such as IL-4 and IL-13, secreted by these cells. In particular, IL-4 and IL-13 play an important role in early atopic dermatitis (Non-Patent Document 1).

[0006] In the treatment and prevention of inflammation, such as atopic dermatitis, it is crucial to ensure that inflammation-resolving factors are actively involved. Inflammation-resolving factors are actively involved in the resolution of inflammation and are naturally produced and secreted by immune cells (neutrophils, macrophages) in the tissues during the late stage of the inflammatory response. Inflammation-resolving factors come in various forms, including lipids, proteins, and gas molecules. Research on specialized pro-resolving lipid mediators (SPMs) has been particularly active recently. These SPMs are metabolites produced during the intracellular metabolism of the omega-3 polyunsaturated fatty acids (PUFAs), eicosapentaenoic acid (EPA) or docosahexaenoic acid (DHA). While numerous studies have reported that these SPMs can alleviate inflammatory responses, their use in strengthening the skin barrier and improving skin moisture remains unknown. Therefore, the present inventors have been developing a natural skin barrier strengthening agent that is safe for the human body, and have discovered that the anti-inflammatory lipid factor has such an effect, leading to the invention of the present invention. [Prior art documents] [Patent documents]

[0007] [Patent Document 1] Korean Patent Publication No. 10-2018-0096158 [Patent Document 2] Korean Patent Publication No. 10-2007-0090928 [Patent Document 3] U.S. Patent Application Publication No. 2011-019389 [Patent Document 4] U.S. Patent Application Publication No. 2015-0126602 [Non-patent literature]

[0008] [Non-Patent Document 1] Donald YMLeung et al., J Clin Invest. 2004, 113, 651-657 Summary of the Invention [Problem to be solved by the invention]

[0009] One embodiment provides a (cosmetic) composition that can strengthen damaged skin barriers, particularly those damaged by ultraviolet rays, and improve skin moisturizing power. [Means for solving the problem]

[0010] According to one embodiment, there is provided a composition for strengthening skin barrier, comprising a compound represented by the following Chemical Formula 1 as an active ingredient:

[0011] [ka]

[0012] In the above chemical formula 1, R 1 ~R 3 are each independently a hydrogen atom, a hydroxyl group, or a carboxyl group, but 1 ~R 3 At least one of the R 1 ~R 3 At least one of the groups is a carboxyl group.

[0013] R 1 and R 2 are each independently a hydroxy group, and 3 may be a carboxyl group.

[0014] The compound represented by Chemical Formula 1 may be contained in a concentration range of 0.01 μM to 100 μM.

[0015] The skin barrier strengthening may be characterized as a decrease in skin water loss and improved skin hydration.

[0016] The skin barrier strengthening can be characterized as strengthening the skin barrier damaged by ultraviolet rays.

[0017] The composition may be a cosmetic composition.

[0018] According to another embodiment, there is provided a method for strengthening the skin barrier by applying to the skin a composition containing an effective amount of the compound represented by Chemical Formula 1 as an active ingredient. [Effects of the Invention]

[0019] According to one embodiment, the skin barrier can be strengthened by reducing water loss from the skin and improving the skin barrier damaged by UV radiation. [Brief explanation of the drawings]

[0020] [Figure 1] 10 is a graph showing the measurement of the effect on the expression of a keratinocyte differentiation marker gene (Keratin 1). [Figure 2] 10 is a graph showing the measurement of the effect on the expression of a keratinocyte differentiation marker gene (Keratin 10). [Figure 3] This is a graph measuring the effect on the expression of DSC1 (Desmocollin-1) gene, which is a component of intercellular junctions (desmosomes). DETAILED DESCRIPTION OF THE INVENTION

[0021] DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS The present invention will now be described in detail with reference to exemplary embodiments thereof so that those skilled in the art can easily practice the present invention. However, as those skilled in the art may realize, the present invention is not limited to the exemplary embodiments set forth herein.

[0022] As used herein, "improving skin barrier function" refers to strengthening the barrier of the stratum corneum, the outer layer of the skin. The stratum corneum, the skin's primary defense, is easily damaged by the external environment. In addition, in people with dry skin, the skin barrier function of the stratum corneum is insufficient or damaged. While moisturizing dry skin can generally be temporarily solved by applying a moisturizer, it is difficult to fundamentally solve the problem. Furthermore, skin barrier damage caused by ultraviolet rays cannot be improved simply by applying a moisturizer. Therefore, the present inventors have completed the present invention by confirming that the compound represented by the specific chemical formula of the present invention can solve the fundamental problem and strengthen the skin barrier.

[0023] In this specification, when a layer, film, region, plate, or other part is said to be "on" another part, this includes not only the case where it is "directly on" another part, but also the case where there is another part between them. Conversely, when a part is said to be "directly on" another part, it means that there is no other part between them.

[0024] Unless otherwise defined herein, "combination" means a mixture or copolymerization, and "copolymerization" means block copolymerization or random copolymerization, and "copolymer" means block copolymerization or random copolymerization.

[0025] A composition for strengthening skin barrier according to one embodiment will be described below.

[0026] A composition for strengthening skin barrier according to one embodiment includes a compound represented by the following Formula 1 as an active ingredient.

[0027] [ka]

[0028] In the above chemical formula 1, R 1 ~R 3 are each independently a hydrogen atom, a hydroxyl group, or a carboxyl group, but 1~R 3 At least one of the R 1 ~R 3 At least one of the groups is a carboxyl group.

[0029] For example, in the above-mentioned Chemical Formula 1, R 1 and R 2 are each independently a hydroxy group, and R 3 may be a carboxyl group.

[0030] The compound represented by Chemical Formula 1 is a specialized pro-resolving lipid mediator (SPM) and can improve UV-induced skin barrier damage, reduce skin moisture loss, and improve skin moisturizing ability. Specifically, when UV-damaged skin is examined, decreased expression of keratinocyte differentiation marker genes and desmosome factor genes can be observed. The compound represented by Chemical Formula 1 can increase the expression of the keratinocyte differentiation marker genes and desmosome factor genes, thereby exhibiting excellent effects in improving UV-damaged skin barriers. That is, a composition according to one embodiment contains the compound represented by Chemical Formula 1 as an active ingredient, and can therefore exhibit excellent effects in strengthening UV-damaged skin barriers.

[0031] In addition, the compound represented by Chemical Formula 1 increases gene expression of aquaporin and filaggrin, which are skin moisturizing factors, and ultimately strengthens the skin barrier by providing moisturizing power to the skin. That is, the composition according to one embodiment contains the compound represented by Chemical Formula 1 as an active ingredient, and thus has an excellent effect of reducing moisture loss from the skin and improving skin moisturizing power.

[0032] In one embodiment, a composition for strengthening skin barrier is provided, which comprises the compound represented by Chemical Formula 1 as an active ingredient, and may comprise a pharmaceutically effective amount of the compound represented by Chemical Formula 1 alone or in combination with one or more pharmaceutically acceptable carriers, excipients, or diluents.

[0033] The compound represented by Chemical Formula 1 in the composition may be contained in a concentration range of 0.01 pM to 100 μM. When the compound represented by Chemical Formula 1 is used at a concentration of less than 0.01 pM, the expression level of keratinocyte differentiation marker genes is minimal, and the effect of improving skin barrier function cannot be achieved. When the compound represented by Chemical Formula 1 is used at a concentration exceeding 100 μM, cytotoxicity may occur, which may be harmful to the human body, and therefore, it is not preferable.

[0034] The term "pharmaceutically effective amount" refers to an amount of the physiologically active ingredient sufficient to exhibit the desired physiological or pharmacological activity when administered to an animal or human. However, the pharmaceutically effective amount may vary depending on the severity of symptoms, the patient's age, weight, health condition, sex, administration route, and treatment period.

[0035] "Pharmaceutically acceptable" means that a substance is physiologically acceptable and does not normally cause gastrointestinal upset, dizziness, or other allergic or similar reactions when administered to humans. Examples of carriers, excipients, and diluents include lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, gum arabic, alginate, gelatin, calcium phosphate, calcium silicate, cellulose, methylcellulose, polyvinylpyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate, and mineral oil. Additionally, fillers, anti-agglomerating agents, lubricants, wetting agents, flavorings, emulsifiers, preservatives, etc. may also be included.

[0036] For example, the composition may be a cosmetic composition.

[0037] In this specification, the term "cosmetic" refers to any substance that may have not only a cosmetic function but also a medical function in addition to the cosmetic function.

[0038] The dosage form of the cosmetic composition is not particularly limited and can be appropriately selected depending on the purpose.

[0039] For example, the cosmetic composition may be formulated into a solution, suspension, emulsion, paste, gel, cream, lotion, powder, soap, surfactant-containing cleansing, oil, powder foundation, emulsion foundation, wax foundation, spray, etc., but is not limited thereto. More specifically, cosmetic compositions such as cleansers, tonics, hair styling products, nourishing lotions, essences, serums, treatments, conditioners, shampoos, lotions, hair care products or hair dyes, oil-in-water (O / W) and water-in-oil (O / W) types, W / O The composition may be formulated into a basic cosmetic product such as a skin lotion, skin toner, astringent, lotion, milk lotion, moisturizing lotion, nourishing lotion, massage cream, nourishing cream, moisturizing cream, hand cream, ointment, foundation, essence, nourishing essence, pack, soap, cleansing foam, cleansing lotion, cleansing cream, body lotion, body cleanser, lotion, ointment, gel, cream, patch, and spray. In addition to the essential ingredients, the composition may contain other ingredients in each formulation, as easily selected by those skilled in the art depending on the type of topical agent or intended use. For example, the composition may further contain a UV protection agent, a hair conditioning agent, a fragrance, etc.

[0040] The cosmetic composition may contain a cosmetically acceptable medium or base, which may be provided in any formulation suitable for topical application, such as a solution, a gel, a solid or pasty anhydrous product, an emulsion obtained by dispersing an oily phase in an aqueous phase, a suspension, a microemulsion, a microcapsule, a microgranule or an ionic (liposome) and / or non-ionic vesicular dispersion, or in the form of a cream, a skin, a lotion, a powder, an ointment, a spray or a concealer stick. These compositions may be prepared by conventional methods known in the art.

[0041] When the dosage form of the present invention is a solution or emulsion, a solvent, solubilizer or emulsifier is used as a carrier component, such as water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl alcohol, benzyl benzoate, propylene glycol, 1,3-butyl glycol oil, glycerol aliphatic esters, polyethylene glycol or fatty acid esters of sorbitan.

[0042] When the dosage form of the present invention is a suspension, the carrier component may be a liquid diluent such as water, ethanol or propylene glycol, a suspending agent such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester and polyoxyethylene sorbitan ester, microcrystalline cellulose, aluminum metahydroxide, bentonite, agar or tracant.

[0043] When the dosage form of the present invention is a paste, cream or gel, the carrier component may be animal oil, vegetable oil, wax, paraffin, starch, tragacanth, cellulose derivatives, polyethylene glycol, silicone, bentonite, silica, talc or zinc oxide.

[0044] When the dosage form of the present invention is a powder or spray, lactose, talc, silica, aluminum hydroxide, calcium silicate, or polyamide powder can be used as a carrier component, and particularly when it is a spray, it can additionally contain a propellant such as chlorofluorohydrocarbon, propane / butane, or dimethyl ether.

[0045] In one embodiment of the present invention, the cosmetic composition may additionally contain a thickener. The thickener contained in the cosmetic composition of the present invention may be methyl cellulose, carboxymethyl cellulose, carboxymethyl hydroxyguanine, hydroxymethyl cellulose, hydroxyethyl cellulose, carboxyvinyl polymer, polyquaternium, cetearyl alcohol, stearic acid, carrageenan, etc., preferably one or more of carboxymethyl cellulose, carboxyvinyl polymer, and polyquaternium, and most preferably carboxyvinyl polymer.

[0046] In one embodiment of the present invention, the cosmetic composition may contain various suitable bases and additives as needed, and the types and amounts of these components can be easily selected by the inventor. If necessary, acceptable additives may be included, such as preservatives, colorants, additives, and other components commonly used in the art.

[0047] Specifically, the preservative may be phenoxyethanol or 1,2-hexanediol, and the fragrance may be an artificial fragrance.

[0048] In one embodiment of the present invention, the cosmetic composition may contain a composition selected from the group consisting of water-soluble vitamins, oil-soluble vitamins, polymeric peptides, polymeric polysaccharides, sphingolipids, and seaweed extracts. Other ingredients that may be added include oils and fats, moisturizers, emollients, surfactants, organic and inorganic pigments, organic powders, UV absorbers, preservatives, disinfectants, antioxidants, plant extracts, pH adjusters, alcohols, colorants, fragrances, blood circulation enhancers, cooling agents, antiperspirants, purified water, etc.

[0049] In addition, the ingredients that may be added other than these are not limited to those mentioned above, and any of the ingredients mentioned above can be added within a range that does not impair the purpose and effects of the present invention.

[0050] Furthermore, the cosmetic composition according to one embodiment can be used not only as a pharmaceutical composition as described above but also as a functional health food, for example, as a main ingredient, auxiliary ingredient, food additive, functional food, or beverage.

[0051] The term "food" refers to a natural or processed product containing one or more nutrients, preferably a product that has undergone some processing step to be ready for direct consumption, and in its usual sense includes all foods, food additives, functional foods, and beverages.

[0052] Examples of foods to which the food composition can be added include various foods, beverages, gum, tea, vitamin complexes, and functional foods. Additional examples include, but are not limited to, special nutritional foods (e.g., infant formula, infant foods, etc.), processed meat products, fish products, tofu, jelly, noodles (e.g., ramen, soba, etc.), bread, health supplements, seasonings (e.g., soy sauce, soybean paste, gochujang, mixed sauce, etc.), sauces, confectioneries (e.g., snacks), candies, chocolates, gum, ice cream, dairy products (e.g., fermented milk, cheese, etc.), other processed foods, kimchi, salted foods (various types of kimchi, jangachi, etc.), beverages (e.g., fruit drinks, vegetable drinks, soy milk, fermented drinks, etc.), and natural seasonings (e.g., ramen soup, etc.). The above foods, beverages, and food additives can be prepared by conventional methods.

[0053] Furthermore, the term "functional food" or "healthy functional food" refers to a food group that has been given added value using physical, biochemical, or biotechnological techniques to act and express the function of the food for a specific purpose, or a food that has been designed and processed to fully express in the body the biological regulatory functions of the food composition related to regulating the body's defense rhythm, preventing and recovering from diseases, etc., and specifically refers to a health functional food. The functional food may contain a food-technically acceptable food supplement additive, and may further contain appropriate carriers, excipients, and diluents that are commonly used in the manufacture of functional foods.

[0054] The dietary supplement may be in the form of, but is not limited to, powder, granules, tablets, capsules or drinks.

[0055] According to another embodiment, there is provided a method for strengthening the skin barrier by applying to the skin a composition containing an effective amount of the compound represented by Chemical Formula 1 as an active ingredient.

[0056] The advantages and features of the present invention, and the methods for achieving them, will become clearer with reference to the following detailed examples. The present invention will be described in detail below with reference to the following examples. However, these examples are for the purpose of specifically explaining the present invention, and the scope of the present invention is not limited to these examples.

[0057] (Example) Test example: Confirmation of the expression level of keratinocyte differentiation markers (KRT1, KRT10) and desmosome component factor (DSC1) Normal human epidermal keratinocytes (NHEK) were cultured in a 6-well plate incubator. After 24 hours, the medium was replaced with phosphate-buffered saline (PBS) and UVB (25 mJ / cm ) was applied. 2 ) and cultured in NHEK culture medium supplemented with 10 nM of a compound represented by the following formula 1-1 (Cayman Chemical). On the fourth day of culture, the cells were harvested, RNA was isolated, and cDNA was synthesized by reverse transcriptional polymerase chain reaction (RT-PCR). Taqman real-time PCR was then performed using the synthesized cDNA to measure the gene expression levels of keratinocyte differentiation markers KRT1 and KRT10 and desmosome component DSC1. The results are shown in Figures 1 to 3 below. As shown in Figures 1 to 3, the gene expression levels of keratin 1 (KRT1), keratin 10 (KRT10), and DSC1 decreased after UV irradiation, but increased again after treatment with the compound represented by the following formula 1-1. This indicates that the compound represented by the following formula 1-1 improves the skin barrier damaged by UV rays.

[0058] [ka]

[0059] Although the preferred embodiments of the present invention have been described in detail above, the scope of the present invention is not limited thereto, and various modifications and improvements made by those skilled in the art using the basic concept of the present invention defined in the following claims also fall within the scope of the present invention.

Claims

1. A cosmetic composition for strengthening the skin barrier, which contains a compound represented by the following chemical formula 1-1 as an active ingredient, reduces moisture loss from the skin and improves skin moisturizing power. 【Chemical 1】

2. The cosmetic composition for reinforcing skin barrier according to claim 1, wherein the compound represented by Chemical Formula 1-1 is contained in a concentration range of 0.01 μM to 100 μM.

3. The cosmetic composition for strengthening the skin barrier according to claim 1, wherein the composition strengthens the skin barrier damaged by ultraviolet rays.

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