Dermatological composition for external application

Abstract

The present invention relates to a dermatological composition for external application, containing, as an active ingredient, a complex ingredient comprising betulin, a ceramide, a soybean extract, and a green tea seed extract. The dermatological composition for external application has the effects of improving the skin barrier by activating keratinocyte proliferation, enhancing the moisture retention of the skin by reducing transepidermal water loss, and improving acne by inhibiting the lipase activity of Cutibacterium acnes.

Description

External skin preparation composition

[0001] Cross-citation with related applications

[0002] This application claims the benefit of priority based on Korean Patent Application No. 10-2024-0150646 dated October 30, 2024, and all contents disclosed in the document of said Korean Patent Application are incorporated herein as part of this specification.

[0003] Technology field

[0004] The present invention relates to a composition for external use on the skin.

[0005] The skin, the outermost organ of the human body, consists of the epidermis and dermis; among these, the stratum corneum, which is the outermost layer in contact with the outside environment, plays the role of maintaining skin moisture and protecting the skin from various external stimuli.

[0006] The stratum corneum, the outermost layer of the epidermis, is formed from keratinocytes and consists of fully differentiated keratinocytes and a surrounding lipid layer. Keratinocytes are characteristic cells that ascend to the skin surface after undergoing stepwise changes in form and function from basal cells, which continuously proliferate in the lowest layer of the epidermis. After a certain period, old keratinocytes slough off from the skin, and new keratinocytes take over their functions; this repetitive series of changes is called epidermal cell differentiation or keratinization. Furthermore, during the keratinization process, keratinocytes produce Natural Moisturizing Factors (NMF) and intercellular lipids (ceramides, cholesterol, fatty acids) to form the stratum corneum. This process gives the stratum corneum firmness and flexibility, enabling it to function as a skin barrier.

[0007] The function of this stratum corneum can easily be lost due to lifestyle factors such as excessive washing or bathing, environmental factors like dry air pollutants, and endogenous conditions such as atopic or senile skin. In fact, due to the increasing variety of factors in modern times, there has been a recent trend of increasing complaints regarding dry skin symptoms and related disorders. Furthermore, changes in the external environment and the progression of aging cause various internal changes in the skin, leading to damage to the skin barrier. Consequently, this can result in skin inflammation, dryness, and itching. This decline in skin barrier function leads to increased influx of allergens, increased moisture loss, changes in the skin microbial community, and alterations in skin lipid composition, which exacerbate skin inflammation and become a cause of skin diseases. While steroids are primarily used to treat inflammatory skin conditions, they have the disadvantage of causing resistance with use and weakening the skin barrier, making long-term treatment difficult.

[0008] Therefore, there is a growing need for compositions that effectively strengthen skin barrier function while being safe and free from side effects.

[0009] <Prior Art Literature>

[0010] Republic of Korea Published Patent Application No. 10-2003-0067545

[0011] The present invention aims to provide a topical skin composition with excellent efficacy in improving the skin barrier, improving skin hydration, and improving acne.

[0012] The present invention, for solving the problems described above, provides a topical skin composition containing a complex ingredient as an active ingredient comprising betulin; ceramide; soybean extract; and green tea seed extract.

[0013] The above ceramide may be one or more selected from the group consisting of natural ceramides including ceramide EOP, ceramide NS, ceramide ENG, ceramide NP, ceramide AP, and ceramide AS; synthetic ceramides; and pseudo-ceramides.

[0014] The content of the above composite component may be 0.001% to 20% by weight based on the total weight of the above topical skin composition.

[0015] The above external skin composition may comprise, based on the total weight of the above complex components, 1 to 80 weight% of the betulin, 0.1 to 50 weight% of the ceramide, 0.1 to 60 weight% of the soybean extract, and 0.1 to 50 weight% of the green tea seed extract.

[0016] The above betulin and the above ceramide may be included in a weight ratio of 1:0.01 to 20.

[0017] The above soybean extract and the above green tea seed extract may be included in a weight ratio of 1:0.01 to 20.

[0018] The above soybean extract and the above green tea seed extract can each be extracted using one or more selected from the group consisting of water and organic solvents.

[0019] The above organic solvent may be an alcohol having 1 to 10 carbon atoms.

[0020] The above soybean extract and green tea seed extract can be obtained through cold extraction.

[0021] The above topical skin composition may be for improving the skin barrier, improving skin hydration, or improving acne.

[0022] The topical skin composition according to the present invention contains a complex component comprising betulin; ceramide; soybean extract; and green tea seed extract as an active ingredient, thereby having efficacy in improving the skin barrier through keratinocyte proliferation activity, efficacy in improving skin hydration through reduction of transepidermal water loss, and efficacy in improving acne through inhibition of lipase activity of Cutibacterium acnes.

[0023] The effects of the present invention are not limited to those mentioned above, and other unmentioned effects will be clearly understood by a person skilled in the art from the description below.

[0024] The advantages and features of the present invention and the methods for achieving them will become clear by referring to the embodiments described in detail below. However, the present invention is not limited to the embodiments disclosed below but can be implemented in various different forms. These embodiments are provided merely to ensure that the disclosure of the present invention is complete and to fully inform those skilled in the art of the scope of the present invention, and the present invention is defined only by the scope of the claims.

[0025] The terms used in this specification are for describing the embodiments and are not intended to limit the invention. In this specification, the singular form includes the plural form unless specifically stated otherwise in the text. The terms "comprises" and / or "comprising" as used in this specification do not exclude the presence or addition of one or more other components in addition to the components mentioned. Throughout the specification, "and / or" includes each of the mentioned components and all combinations of one or more. Although terms such as "first," "second," etc., are used to describe various components, these components are not limited by these terms. These terms are used merely to distinguish one component from another. Therefore, the first component mentioned below may be the second component within the technical scope of the invention.

[0026] Unless otherwise defined, all terms used herein (including technical and scientific terms) may be used in a meaning commonly understood by those skilled in the art to which the present invention pertains. Additionally, terms defined in commonly used dictionaries are not to be interpreted ideally or excessively unless explicitly and specifically defined otherwise.

[0027] In this specification, the term "skin" refers to tissue covering the surface of an animal's body, and is a broad concept that includes not only tissue covering the surface of the body such as the face or body, but also the scalp and hair.

[0028] In this specification, the term "extract" includes all substances obtained by extracting components from natural products, regardless of the extraction method or the type of component. For example, it is a broad concept that includes substances obtained by extracting solvent-soluble components from natural products using water or organic solvents, and substances obtained by extracting only specific components of natural products, such as oils.

[0029] Units used in the specification of the present invention without special mention are based on weight, and for example, units of % or ratio mean weight % or weight ratio.

[0030]

[0031] The present invention will be described in detail below.

[0032] The present invention provides a topical skin composition containing a complex ingredient comprising betulin; ceramide; soybean extract; and green tea seed extract as an active ingredient.

[0033] In the case of a topical skin composition composed of the above ingredients, it may exhibit excellent efficacy in improving the skin barrier through keratinocyte proliferation activity, efficacy in improving skin hydration through reduction of transepidermal water loss, and efficacy in improving acne through inhibition of lipase activity of Cutibacterium acnes.

[0034] In one embodiment, Betulin included in the topical skin composition is a type of triterpene found in nature, which is mainly isolated from birch bark. It is a naturally derived substance known to have anticancer activity in recent studies, and is currently being studied for its antiviral and antibacterial functions.

[0035] The content of the above betulin may be 1 to 80 weight%, 10 to 85 weight%, 15 to 80 weight%, or 30 to 50 weight% based on the total weight of the above composite components. If betulin is included in an amount less than the aforementioned range, it may not produce an effective effect, and if betulin is included in an amount greater than the aforementioned range, the efficacy may be significantly lower than that exhibited within the above range.

[0036] In one embodiment, the ceramide included in the above-mentioned topical skin composition is a major lipid component constituting the stratum corneum and plays an important role in the formation of the skin's moisturizing ability and the occurrence of skin barrier disorders. Ceramide accounts for about 40 to 50% or more of the intercellular lipids constituting the stratum corneum of the skin and is an essential component that exhibits the structure formation or function of the stratum corneum. It functions as a lipid barrier that inhibits moisture evaporation from the stratum corneum and maintains the orderly structure of the stratum corneum.

[0037] The above ceramides are given backbone names S, P, and H respectively depending on the type of basic structure, sphingosine, phytosphingosine, and 6-OH-sphingosine, and can be further classified into EOS, EOP, EOH, NS, NP, NH, AS, AP, and AH depending on the bonding form of the fatty acids.

[0038] The above ceramides each have different polarities and can be classified into ceramide EOP, ceramide NS, ceramide ENG, ceramide NP, ceramide AS, and ceramide AP depending on the degree of polarity; due to their respective characteristic structures and physicochemical properties, ceramides play a role in forming an optimal permeability barrier.

[0039] The aforementioned Ceramide EOP is primarily used to improve dry and itchy skin conditions. Additionally, Ceramide NP is a complex active ingredient that serves as the most important substance among the lipids contained in the skin's keratin, providing particularly excellent skin moisturization. It plays a key role in strengthening the skin's lipid barrier and forming a protective film against the external environment.

[0040] The above ceramide may be one or more selected from the group including, for example, natural ceramides including ceramide EOP, ceramide NS, ceramide NG, ceramide NP, ceramide AP, and ceramide AS; synthetic ceramides; and pseudo-ceramides. As a specific example, the above ceramide may be natural ceramide, and as a more specific example, the above ceramide may be ceramide NP. Here, synthetic ceramide may refer to ceramide that has been artificially synthesized, and pseudo-ceramide may refer to a component having a chemical structure and efficacy similar to natural ceramide.

[0041] The content of the ceramide may be 0.1 to 50 weight%, 1 to 45 weight%, 5 to 40 weight%, or 5 to 18 weight% based on the total weight of the composite component. If the ceramide is included in an amount less than the aforementioned range, it may not produce an effective effect, and if the ceramide is included in an amount greater than the aforementioned range, the efficacy may be significantly lower than that exhibited within the aforementioned range.

[0042] In one embodiment, the betulin and the ceramide may be included in a weight ratio of 1:0.001 to 20, 1:0.01 to 10, or 1:0.05 to 5. When the content of betulin and ceramide is controlled within the aforementioned weight ratios, skin keratinocyte proliferation and skin moisturizing activity are superior, and the effect of inhibiting lipase activity of acne bacteria that cause acne may be superior.

[0043] In one embodiment, regarding the soybean extract included in the above-described topical skin composition, the soybean may be soybean, black soybean (Seoritae), yellow soybean (Baektae), kidney bean, lentil, chickpea, chestnut bean, ginseng bean, or cowpea, but is not limited thereto. The isoflavones of soybeans improve damaged skin and revitalize skin elasticity by firming the skin. Containing abundant protein and vitamin components, they enhance the skin's defense ability to protect itself from external stimuli and form a natural protective barrier on the skin. The main component of the soybean extract used as an emulsifier is lysophospholipid. Lysophospholipid is one of the phospholipid components of soybeans and is extracted from components containing lecithin, hypoxy, etc. As a specific example, the soybean may be glycine soja.

[0044] The content of the above soybean extract may be 0.1 to 60 weight%, 1 to 55 weight%, 5 to 50 weight%, or 30 to 45 weight% based on the total weight of the above composite components. If the soybean extract is included in an amount less than the aforementioned range, it may not produce an effective effect, and if the soybean extract is included in an amount greater than the aforementioned range, the efficacy may be significantly lower than that exhibited within the above range.

[0045] In one embodiment, regarding the green tea seed extract included in the above-mentioned topical skin composition, the green tea is a perennial evergreen plant belonging to the family Theaceae and has been consumed since the Three Kingdoms period. Recently, as the functionality of various components contained in green tea is gradually being revealed, its value is being re-recognized. Green tea contains a large amount of beneficial components such as polyphenols, caffeine, amino acids, and vitamin C, and has been found to be highly effective for hangover relief, nicotine detoxification, fatigue recovery, cardiotonic effects, and skin beauty. In particular, the functionality of polyphenols, which are most abundant in green tea, is receiving significant attention as their effects such as antioxidant, anti-cholesterol, blood sugar lowering, anti-tumor, and platelet aggregation inhibition have been proven. Catechin is a type of polyphenol that softens the skin and strengthens the skin barrier, thereby maintaining healthy skin.

[0046] The main emulsifying component among the above green tea seed extracts is triterpene saponin. Triterpene saponin refers to a compound that has a triterpene as a sapogenin (aglycone) and forms a glycosidic or ester bond with a sugar. Triterpene saponins are distinguished according to the type of sapogenin, and representative examples include saponins having a pentacyclic triterpene as a sapogenin, such as oleanane, ursane, lupane, hopane, and taraxerane. In addition, saponins are distinguished according to their binding positions with sugar chains. Taking oleanolic acid as an example, those bound to a sugar chain at either the C-3 or C-28 position are called monodesmosides, while those bound to a sugar chain at both the C-3 and C-28 positions are classified as bisdesmosides. At the C-3 position, binding to the sugar chain is primarily achieved through glycosidic bonds, while at the C-28 position, binding is primarily achieved through ester bonds. The sugars that primarily bind to saponins include glucose, galactose, rhamnose, xylos, arabinose, and glucuronic acid.

[0047] The content of the green tea seed extract may be 0.1 to 50 weight%, 1 to 45 weight%, 5 to 40 weight%, or 5 to 20 weight% based on the total weight of the complex components. If the green tea seed extract is included in an amount less than the aforementioned range, it may not produce an effective effect, and if the green tea seed extract is included in an amount greater than the aforementioned range, the efficacy may be significantly lower than that exhibited within the aforementioned range.

[0048] In one embodiment, the soybean extract and the green tea seed extract may be included in a weight ratio of 1:0.001 to 20, 1:0.01 to 10, or 1:0.05 to 5. When the content of the soybean extract and the green tea seed extract is controlled within the aforementioned weight ratios, the skin keratinocyte proliferation and skin moisturizing activity are superior, and the effect of inhibiting the lipase activity of acne bacteria that cause acne may be superior.

[0049] In one embodiment, the soybean extract and the green tea seed extract may each be extracted using one or more selected from the group consisting of water and organic solvents.

[0050] The above organic solvent may be an alcohol having 1 to 10 carbon atoms, C1 to C6, or a lower alcohol having C1 to C4, such as methanol, ethanol, propanol, and butanol.

[0051] The extraction methods for the above soybean extract and green tea seed extract are not particularly limited and include, for example, cold extraction, ultrasonic extraction, reflux extraction, hot water extraction, etc., and as a specific example, the cold extraction method may be used.

[0052] In the case of the above cold extraction, the extraction raw material and an aqueous alcohol solution can be mixed and cold extraction can be performed at a temperature of 15°C to 25°C for 36 to 60 hours or 36 to 48 hours. Under the aforementioned conditions, active ingredients can be extracted with high efficiency while minimizing the loss of active ingredients due to the temperature of the cold extraction.

[0053] The above cold-extracted extract may undergo a filtration step. In the filtration step, filter paper with a pore size of 2 μm to 10 μm or 6 μm to 10 μm may be used. When filtered under the aforementioned conditions, the filtrate of the extract can be effectively collected, and the residue remaining from the filtration process may undergo an extraction process again, and this process may be repeated multiple times.

[0054] The extract obtained from the above filtration step can be prepared in the form of a dried powder by concentrating under reduced pressure at a temperature of 45°C or lower, or between 20°C and 45°C. When concentrating under reduced pressure under the aforementioned conditions, the extract can be prevented from boiling over.

[0055] The above soybean extract and green tea seed extract can be obtained in a dried, cut form or in the form of a powder.

[0056] In one embodiment, the content of the composite component may be 0.001% to 20% by weight, 0.001% to 10% by weight, or 0.01% to 5% by weight with respect to the total weight of the topical skin composition. A topical skin composition containing the composite component as an active ingredient within the aforementioned range may have excellent efficacy in improving the skin barrier, improving skin hydration, and improving acne.

[0057] In one embodiment, the topical skin composition may be for improving the skin barrier, improving skin hydration, or improving acne. Specifically, the topical skin composition has an effect of improving the skin barrier through keratinocyte proliferation activity, an effect of improving skin hydration through a reduction in transepidermal water loss, and an effect of improving acne by inhibiting the lipase activity of Cutibacterium acnes, an acne-causing bacterium. Here, Cutibacterium acnes induces the expression of inflammatory cytokines IL-1β, IL-6, IL-8, and TNF-α. Additionally, by secreting lipase, it produces linoleic acid and oleic acid, which are skin-irritating unsaturated fatty acids.

[0058] In one embodiment, the external skin composition has a formulation selected from the group consisting of a suspension, an ointment, a lotion, and a spray. For example, the external skin composition may have a formulation selected from the group consisting of a skin lotion, a skin softener, a skin toner, a softening lotion, a nourishing lotion, a massage cream, a nourishing cream, a moisture cream, a hand cream, a foundation, an essence, a nourishing essence, a cream, a soap, a cleansing foam, a cleansing lotion, a cleansing cream, a body lotion, a body cream, and a pack.

[0059] In one embodiment, the external skin composition may further include a moisturizer, an emollient, a surfactant, a UV absorber, a preservative, a disinfectant, an antioxidant, a pH adjuster, organic and inorganic pigments, and a fragrance.

[0060] The above-mentioned topical skin composition may further include, in addition to the above components, conventional additives used in the art within a range that does not impede the purpose of the present invention, and the types and amounts thereof may be appropriately selected and adjusted by a person skilled in the art.

[0061]

[0062] The present invention provides a use for a complex ingredient comprising betulin; ceramide; soybean extract; and green tea seed extract to be used as a topical skin composition.

[0063] The present invention provides a use for a topical skin composition containing a complex ingredient comprising betulin; ceramide; soybean extract; and green tea seed extract as an active ingredient to activate the proliferation of skin keratinocytes.

[0064] The present invention provides a use for a topical skin composition containing a complex ingredient comprising betulin; ceramide; soybean extract; and green tea seed extract as an active ingredient to reduce transepidermal water loss.

[0065] The present invention provides a use for a topical skin composition containing a complex ingredient comprising betulin; ceramide; soybean extract; and green tea seed extract as an active ingredient to inhibit the lipase activity of Cutibacterium acnes.

[0066] The present invention provides a use for a topical skin composition containing a complex ingredient comprising betulin; ceramide; soybean extract; and green tea seed extract as an active ingredient, for improving the skin barrier, improving skin hydration, or improving acne.

[0067]

[0068] The present invention provides a method for activating skin keratinocyte proliferation by applying a topical skin composition containing a complex ingredient comprising betulin; ceramide; soybean extract; and green tea seed extract as an active ingredient to the skin of an animal.

[0069] The present invention provides a method for reducing transepidermal water loss by applying a topical skin composition containing a complex ingredient comprising betulin; ceramide; soybean extract; and green tea seed extract as an active ingredient to the skin of an animal.

[0070] The present invention provides a method for inhibiting the lipase activity of Cutibacterium acnes by applying a topical skin composition containing a complex ingredient comprising betulin; ceramide; soybean extract; and green tea seed extract as an active ingredient to the skin of an animal.

[0071] The present invention provides a method for improving the skin barrier, improving skin hydration, or improving acne by applying a topical skin composition containing a complex ingredient comprising betulin; ceramide; soybean extract; and green tea seed extract as an active ingredient to the skin of an animal.

[0072] The complex component comprising the above betulin; ceramide; soybean extract; and green tea seed extract is as described above.

[0073] The above animal could be a human.

[0074]

[0075] Specific embodiments of the present invention are presented below. However, the embodiments described below are merely intended to specifically illustrate or explain the present invention and should not be limited thereto. Furthermore, details not described herein can be sufficiently technically inferred by a person skilled in the art, so their description is omitted.

[0076]

[0077] [Preparation Example]

[0078] Preparation Example 1: Preparation of Soybean Extract

[0079] 100 g of soybeans (source: Cheongju) were collected, 1 L of 70% ethanol aqueous solution was added, and the mixture was cold-boiled at a temperature of 15 to 25 ℃ for 48 hours, after which it was filtered using Whatman No. 2. The filtered extract was concentrated under reduced pressure at 45 ℃ or lower to produce dried soybean extract powder.

[0080]

[0081] Preparation Example 2: Preparation of green tea seed extract

[0082] 100 g of green tea seeds (source: Boseong) were collected, 1 L of 70% ethanol aqueous solution was added, and the mixture was cold-infused at a temperature of 15 to 25 ℃ for 48 hours, after which it was filtered using Whatman No. 2. The filtered extract was concentrated under reduced pressure at 45 ℃ or lower to produce a dried green tea seed extract powder.

[0083]

[0084] [Examples and Comparative Examples]

[0085] A complex composition was formulated by mixing betulin, ceramide NP, the soybean extract of Preparation Example 1, and the green tea seed extract of Preparation Example 2 in the weight ratios shown in Table 1 below. For comparative experiments, Comparative Examples 1 to 7 were formulated by excluding one or more of betulin, ceramide NP, soybean extract, and green tea seed extract.

[0086] Here, betulin is represented by the chemical formula 1 below, and ceramide NP is represented by the chemical formula 2 below.

[0087] [Chemical Formula 1]

[0088]

[0089] CAS number: 473-98-3

[0090] Purchased from: Sigma-aldrich

[0091] [Chemical Formula 2]

[0092]

[0093] CAS number: 100403-19-8

[0094]

[0095] Classification Betulin Ceramide NPidoll Soybean Extract Green Tea Seed Extract Example 1 1 1 1 1 Example 2 2 1 1 1 Example 3 4 1 1 1 Example 4 8 1 1 1 Example 5 2 1 2 1 Example 6 4 1 4 1 Example 7 8 1 8 1 Comparative Example 1 1 1 2 1 3 1 4 1 Comparative Example 3 1 4 1 Comparative Example 5 1 1 6 1 1 7 Comparative Example 7 1 1 1

[0096]

[0097] [Experimental Example]

[0098] Experimental Example 1: Evaluation of Skin Keratinocyte Proliferation Activity

[0099] To measure the proliferative activity of skin keratinocytes, 1 x 10⁶ HaCaT keratinocytes 4After dispensing the samples into a 96-well plate at a cell / well concentration, the cells were cultured for 24 hours under conditions of 37°C, 5% CO2. After removing the culture medium, the samples of Examples 1 to 7 and Comparative Examples 1 to 7 were dissolved in serum-free DMEM medium at a concentration of 0.2 ppm and treated with HaCaT keratinocytes, followed by additional culture for 24 hours. To confirm cell viability after culture, the culture medium was removed, and 200 µl of MTT solution at a concentration of 0.5 mg / ml was dissolved in each well. The absorbance was measured at a wavelength of 540 nm using a micro-plate reader. As a normal control, the cell viability of the wells not treated with the extract was set to 100%. The cell viability of the sample treatment groups of Examples 1 to 7 and Comparative Examples 1 to 7 was calculated according to Equation 1, and the results are shown in Table 2.

[0100] [Mathematical Formula 1]

[0101] Skin keratinocyte survival rate (%) = (A / B) x 100

[0102] A: Absorbance of the test group treated with the sample

[0103] B: Absorbance of the control group that was not treated with the sample

[0104] Separation Cell Viability (%) Example 1 106.21 Example 2 107.31 Example 3 109.40 Example 4 107.76 Example 5 121.42 Example 6 123.83 Example 7 120.44 Comparative Example 194.99 Comparative Example 246.63 Comparative Example 3 101.09 Comparative Example 4 101.32 Comparative Example 576.83 Comparative Example 695.65 Comparative Example 797.00

[0105] Looking at Table 2 above, the skin keratinocyte proliferation activity was found to be higher when the samples of Examples 1 to 7 according to the present invention were treated compared to Comparative Examples 1 to 7. In particular, when the samples of Examples 5 to 7 were used, a high proliferation activity of 20% or more was confirmed. Through this, it can be seen that the examples according to the present invention enhance the activity of keratinocytes and have excellent efficacy in improving the skin barrier.

[0106]

[0107] Experimental Example 2: Evaluation of Skin Moisturizing Activity

[0108] To measure the skin moisturizing effect, a transepidermal water loss (TEWL) verification experiment was performed using samples from Examples 1 to 7 and Comparative Examples 1 to 7.

[0109] For 10 adults aged 30 to 45 years, samples of Examples 1 to 7 and Comparative Examples 1 to 7 were diluted to 1% in squalane and applied to the test site (arm) for one week, after which the transepidermal water loss of each test site was measured using a water evaporation meter (Vapometer, Delfin Technologies, Finland). Here, the application was performed once daily with an application amount of 0.1 g on a 1.5 cm x 1.5 cm application area of ​​the arm. The measured changes in transepidermal water loss are shown in Table 3.

[0110] Sample 1% (10,000 ppm) Reduction Rate of Transepidermal Water Loss (%) (Compared to Control Group) Untreated Control Group 0 Example 1 19.25 Example 2 24.08 Example 3 25.59 Example 4 24.37 Example 5 31.36 Example 6 29.86 Example 7 30.23 Comparative Example 110.53 Comparative Example 2 13.35 Comparative Example 36.6 Comparative Example 48.12 Comparative Example 5 13.61 Comparative Example 6 15.81 Comparative Example 7 15.37

[0111] Looking at Table 3 above, compared to Comparative Examples 1 to 7, the skin moisturizing effect through the reduction of transepidermal water loss was high when the samples of Examples 1 to 7 according to the present invention were treated. In particular, the most excellent skin moisturizing activity was confirmed when the samples of Examples 5 to 7 were treated.

[0112]

[0113] Experimental Example 3: Safety evaluation for the skin

[0114] To confirm the skin safety of the topical skin composition of the present invention, a patch test was conducted on 20 adult men and women by applying samples of Examples 1 to 7 and Comparative Examples 1 to 7 diluted in squalane to 5% (50,000 ppm) to evaluate skin safety. Here, the patch site was the back of the subject, and a patch containing 0.1 g of the diluted sample was applied to an area of ​​1.5 cm x 1.5 cm. A first reading was performed 1 hour after the patch was removed, and a second reading was performed 24 hours after the patch was removed. To determine the intensity of skin irritation, the skin irritation of the extract samples was visually judged by calculating the average skin reaction score by assigning weights according to the degree of positive skin reaction, and the results are shown in Table 4 below.

[0115] Sample 5% (50,000 ppm) 1 hour after 24 hours after Determination of average skin reaction score Skin positive reaction degree weight 0.5 1 2 3 0.5 1 2 3 Example 1 50,000 ppm Relevant persons (persons) 000000000 Non-irritating Example 2 250,000 ppm Relevant persons (persons) 000000000 Non-irritating Example 350,000 ppm Relevant persons (persons) 000000000 Non-irritating Example 450,000 ppm Relevant persons (persons) 0000000000 Non-irritating Example 550,000 ppm Relevant persons (persons) 0000000000 Non-irritating Example 650,000 ppm Relevant persons (persons) 000000000 Non-irritating Example 750,000 ppm Relevant Persons (Persons) 000000000 Non-irritating Comparative Example 150,000 ppm Relevant Persons (Persons) 000000000 Non-irritating Comparative Example 250,000 ppm Relevant Persons (Persons) 000000000 Non-irritating Comparative Example 350,000 ppm Relevant Persons (Persons) 000000000 Non-irritating Comparative Example 450,000 ppm Relevant Persons (Persons) 000000000 Non-irritating Comparative Example 550,000 ppm Relevant Persons (Persons) 000000000 Non-irritating Comparative Example 650,000 ppm Relevant Persons (Persons) 000000000 Non-irritating Comparative Example 750,000 ppm Relevant Persons (Persons) 000000000 Non-irritating

[0116] Looking at Table 4 above, no one showed a positive skin reaction corresponding to a weight of 0.5 to 3 during the first and second readings after removing a patch applied with 5% of the samples of Examples 1 to 7, and through this, it can be confirmed that there is no skin irritation when the samples of Examples 1 to 7 at 5% or less are applied to the skin. In other words, it can be seen that there is no skin irritation in the case of the external skin composition containing the samples of Examples 1 to 7 according to the present invention.

[0117]

[0118] Experimental Example 4: Evaluation of Lipase Activity Inhibition of Cutibacterium acnes (C. acnes)

[0119] Lipase secreted by Cutibacterium acnes breaks down triglycerides and esters, which are components of sebum, to produce linoleic acid and oleic acid, which are skin-irritating unsaturated fatty acids. To evaluate the lipase activity inhibitory effect of the samples of Examples 1 to 7 and Comparative Examples 1 to 7, the following process was performed.

[0120] An enzyme buffer was prepared by adding 30 μl of 90 mM citrate buffer, 30 μl of 10 mM 4-nitrophenyl dodecanoate (p-NPD), 30 μl of 5% Triton X-100, and 610 μl of Tris-HCl buffer (pH 8.0) to 200 μl of Cutibacterium acnes culture medium. Samples of Examples 1 to 7 and Comparative Examples 1 to 7, diluted with Phosphate Buffered Saline (PBS) to a concentration of 500 ppm, were added to the enzyme buffer and reacted at 30°C for 1 hour. A group in which the Cutibacterium acnes culture medium was not treated with the samples was used as a control. Then, the degree of hydrolysis of 4-nitrophenyl dodecanoate (p-NPD) into 4-nitrophenol (p-nitrophenol) was measured by absorbance at a wavelength of 405 nm. The lipase activity rate (%) was expressed as a relative value of the lipase activity when treated with the samples of Examples 1 to 7 and Comparative Examples 1 to 7, with the lipase activity of the control group (not treated) set to 100. The lipase activity rate was calculated using the following Equation 2, and the results are shown in Table 5 below.

[0121] [Mathematical Formula 2]

[0122] Lipase activity rate (%) = (B / A) X 100

[0123] A: Absorbance of the control group that was not treated with the sample

[0124] B: Absorbance of the experimental group treated with the sample

[0125] Sample 0.1% (1,000 ppm) Lipase Activity Rate (%) Control Group 100 Example 185.51 Example 284.11 Example 376.5 Example 477.3 Example 560.43 Example 653.46 Example 755.9 Comparative Example 199.74 Comparative Example 292.97 Comparative Example 392.62 Comparative Example 493.77 Comparative Example 590.17 Comparative Example 689.14 Comparative Example 789.35

[0126] Looking at Table 5, it was confirmed that the samples of Examples 1 to 7 effectively inhibited the lipase activity secreted by Cutibacterium acnes. In other words, it was found that the composition according to the present invention is effective in inhibiting the lipase activity of acne bacteria that cause acne.

[0127]

[0128] [Formulation Example]

[0129] Formulation Example 1: Toner

[0130] Ingredients (Weight %) Formulation Example 1: Toner 1-11-21-31-41-51-61-7 Example 1 1.0------Example 2 1.0-----Example 3 1.0----Example 4 1.0---Example 5 1.0--Example 6 1.0-Example 7 1.0 Trehalose 2222222 Glycerin 5555555 1,2-Hexanediol 2222222 EDTA-2Na 0.02 0.02 0.02 0.02 0.02 0.02 0.02 2 Purified Water Remaining Remaining Remaining Remaining Remaining Remaining Remaining

[0131] Formulation Example 2: Essence

[0132] Ingredients (Weight %) Formulation Example 2: Essence 1-11-21-31-41-51-61-7 Example 1 1.0------Example 2 1.0-----Example 3 1.0----Example 4 1.0---Example 5 1.0--Example 6 1.0-Example 7------1.0 Trehalose 2222222 Glycerin 101010101010101010101010101,2-Hexanediol 22222222 Carbomer 0.150.150.150.150.150.150.15 Tromethamine 0.10.10.10.10.10.10.10.1 EDTA-2Na 0.020.020.020.020.020.020.020.02 Purified Water Remaining Remaining Remaining Remaining Remaining Remaining Remaining Remaining

[0133] Formulation Example 3: Cream

[0134] Ingredients (Weight %) Formulation Example 3: Cream 1-11-21-31-41-51-61-7 Example 1 1.0------Example 2 1.0-----Example 3 1.0----Example 4 1.0---Example 5 1.0--Example 6 1.0-Example 7 1.0 Sunflower Seed Oil 3333333 Ethylhexyl Palmitate 7777777 PEG-100 Stearate, Glyceryl Stearate 2222222 Polysorbate 601111111 Sorbitan Stearate 0.50.50.50.50.50.50.5 Trehalose 2222222 Glycerin 1010101010101010 1,2-Hexanediol 2222222 Carbomer 0.30.30.30.30.30.30.30.3 Tromethamine 0.20.20.20.20.20.20.20.2 EDTA-2Na 0.020.020.020.020.020.020.02 Purified Water Remaining Amount Remaining Amount Remaining Amount Remaining Amount Remaining Amount Remaining Amount

[0135] As shown in Tables 6 to 8 above, it was possible to prepare topical skin preparations with various formulations using other composite components of the present invention, and to exhibit efficacy in improving the skin barrier through keratinocyte proliferation activity, efficacy in improving skin hydration through reduction of transepidermal water loss, and efficacy in improving acne through inhibition of lipase activity of Cutibacterium acnes.

[0136] Although embodiments of the present invention have been described above, those skilled in the art will understand that the present invention may be implemented in other specific forms without altering its technical concept or essential features. Therefore, the embodiments described above should be understood as illustrative in all respects and not restrictive.

Claims

Betulin; Ceramide; Soybean extract; and A topical skin composition containing a complex ingredient including green tea seed extract as an active ingredient. In paragraph 1, The above ceramide is a topical skin composition comprising one or more selected from the group consisting of natural ceramides including ceramide EOP, ceramide NS, ceramide NG, ceramide NP, ceramide AP, and ceramide AS; synthetic ceramides; and pseudo-ceramides. In paragraph 1, A topical skin composition in which the content of the above-mentioned composite component is 0.001% to 20% by weight based on the total weight of the topical skin composition. In paragraph 1, A topical skin composition comprising, based on the total weight of the above composite components, 1 to 80 weight% of the betulin, 0.1 to 50 weight% of the ceramide, 0.1 to 60 weight% of the soybean extract, and 0.1 to 50 weight% of the green tea seed extract. In paragraph 1, A topical skin composition comprising the above betulin and the above ceramide in a weight ratio of 1:0.01 to 20. In paragraph 1, A topical skin composition comprising the above soybean extract and the above green tea seed extract in a weight ratio of 1:0.01 to 20. In paragraph 1, A skin external preparation composition in which the above soybean extract and the above green tea seed extract are each extracted using one or more selected from the group consisting of water and organic solvents. In Paragraph 7, The above organic solvent is an alcohol having 1 to 10 carbon atoms, in a skin external preparation composition. In paragraph 1, The above soybean extract and green tea seed extract are a topical skin composition obtained through cold extraction. In paragraph 1, The above-mentioned topical skin composition is a topical skin composition for improving the skin barrier, improving skin hydration, or improving acne.

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