Composition for improving skin

Abstract

The present invention provides a cosmetic composition for improving skin, which comprises sweet bisabolol, americol, a polygonum cuspidatum extract, chrysin, quercetin, sodium mannose phosphate, kaempferol and pyruvate. The composition for improving skin according to the present invention exhibits an excellent synergistic effect on strengthening skin barrier, inhibiting pigmentation, improving wrinkles, or strengthening elasticity by means of a combination of specific components, and thus can be effectively used as a functional composition in a cosmetic or an external preparation for skin, which targets skin tissue.

Description

Technical Field

[0001] This application claims priority to Korean Patent Application No. 10-2023-0115849, filed on August 31, 2023, the entire contents of which are disclosed in the specification and drawings of that application are incorporated herein by reference.

[0002] This disclosure relates to compositions for improving skin. Background Technology

[0003] The skin acts as a barrier, protecting the body from the external environment and preventing the loss of internal moisture and oils. Furthermore, the skin is a vital organ for various physiological functions, including thermoregulation and excretion. However, various factors can lead to decreased skin cell activity and a deterioration in skin condition.

[0004] Collagen and elastin, found in the dermis of the skin, perform various functions, including maintaining the skin's mechanical strength, resisting tissue adhesion, supporting cell bonding, and influencing skin structure. Collagen decreases due to stress, aging, or photoaging caused by UV exposure. Furthermore, elastin, upon exposure to UV radiation, undergoes its three-dimensional structure disruption due to increased elastase activity. Thus, with the reduction of collagen and the decrease in elastin activity, skin tissue becomes loose and loses its elasticity.

[0005] As epidermal cell function declines and metabolism becomes less efficient, the stratum corneum (outermost layer of skin) doesn't shed easily, leading to excessive buildup. In this state, when exposed to ultraviolet radiation, skin elasticity decreases, causing wrinkles. Alternatively, if the epidermis doesn't form a sebum film, reduced moisture and sebum secretion, along with dry skin, can sometimes cause wrinkles.

[0006] When skin is exposed to ultraviolet radiation, it synthesizes melanin to protect itself. The synthesized melanin is then transferred to the skin's keratinocytes via melanosomes. These keratinocytes undergo a 28-day turnover cycle. Therefore, the melanin produced usually disappears through the keratinocytes within a 28-day cycle. However, if the skin cell cycle is not properly regulated due to stress, skin aging, or other factors, the keratinocytes cannot shed in time, leading to pigmentation issues such as sunspots, freckles, and age spots.

[0007] For skin aging caused by the aforementioned factors, ongoing research has been conducted on substances that improve skin barrier strengthening, inhibit pigmentation, and improve wrinkles or enhance elasticity by promoting collagen production, all in an effort to inhibit skin aging. However, substances with satisfactory effects in these areas are still under development, thus necessitating the development of new ingredients capable of improving these factors. Summary of the Invention

[0008] The problem that the invention aims to solve

[0009] The problem to be solved by the present invention is to provide a skin improvement composition that enhances the effects of factors such as skin barrier strengthening, pigmentation inhibition, wrinkle improvement, or elasticity enhancement.

[0010] Methods for solving problems

[0011] To address the aforementioned issues, the inventors of this invention conducted intensive research, which revealed that a composition comprising bisabolol, glutenin, Polygonum cuspidatum extract, salicumin, quercetin, sodium mannose phosphate, kaempferol, and pyruvate exhibits effects such as skin barrier strengthening, pigmentation inhibition, wrinkle improvement, and elasticity enhancement, thereby achieving excellent skin improvement results. In particular, the inventors surprisingly discovered that, compared to using these ingredients individually, combining them significantly increased the effects of skin barrier strengthening, pigmentation inhibition, wrinkle improvement, and elasticity enhancement, thus completing this invention.

[0012] Therefore, the present invention provides a cosmetic composition for skin improvement comprising bisabolol, glutenol, Polygonum cuspidatum extract, quercetin, sodium mannophosphate, kaempferol and pyruvate.

[0013] The bisabolol used in this invention, under the IUPAC name (2S)-6-methyl-2-[(1S)-4-methylcyclohex-3-en-1-yl]hept-5-en-2-ol, also known as α-bisabolol or levomenol, is a natural monocyclic sesquiterpenes alcohol. The bisabolol used in this invention can be obtained by purchase or synthesis. The composition may contain 0.00001 to 50% by weight of the above-mentioned bisabolol, preferably 0.0001 to 5% by weight.

[0014] The oryzanol used in this invention, also known as gammaoryzanol (γ-oryzanol), is a mixture of lipids extracted from rice (Oryza sativa). γ-oryzanol is primarily produced during the fat fractionation of rice sugar and rice sugar oil, and is a mixture of ferulic acid esters of phytosterols and triterpenoids, particularly a mixture of cycloartenyl ferulate, 24-methylenecycloartanyl ferulate, and campesteryl ferulate, which constitute 80% of γ-oryzanol. The oryzanol used in this invention can be obtained from rice or is commercially available. The composition contains 0.00001 to 5% by weight of the above-mentioned oryzanol, preferably 0.0001 to 1% by weight.

[0015] The Polygonum cuspidatum extract used in this invention refers to a substance extracted from Polygonum cuspidatum. Polygonum cuspidatum (also known as Fallopia japonica and Polygonum cuspidatum) is a perennial herb belonging to the Polygonaceae family of the order Polygonales. It grows in mountains and fields throughout my country. Its stem is hollow, and the stems of seedlings are scattered with purplish-red spots. The Polygonum cuspidatum used in this invention can be obtained by purchasing or direct harvesting. The composition may contain 0.00001 to 5% by weight of the above-mentioned Polygonum cuspidatum extract, preferably 0.0001 to 1% by weight.

[0016] The Polygonum cuspidatum extract used in this invention comprises an extract obtained by extracting Polygonum cuspidatum, a diluted or concentrated extract of the extract, a dried product obtained by drying the extract, a formulation or tablet of the extract, or a mixture or fraction thereof, as well as the extract itself and all dosage forms that can be formed using the extract. The Polygonum cuspidatum extract used in this invention is also commercially available.

[0017] The type of extraction solvent used when extracting Polygonum cuspidatum is not particularly limited, and any solvent known in the art can be used. Examples of extraction solvents include C1 to C4 lower alcohols such as water, methanol, ethanol, propanol or butanol, polyols such as glycerol, butenediol or propylene glycol, and hydrocarbon solvents such as methyl acetate, ethyl acetate, acetone, benzene, hexane, diethyl ether or dichloromethane, or mixtures thereof, but not limited thereto. Preferably, water, lower alcohols, 1,3-butenediol, and ethyl acetate are used alone or in combination of two or more.

[0018] In one embodiment of the present invention, the above-mentioned Polygonum cuspidatum extract is filtered to remove floating solid particles, for example, by filtering the particles with nylon or by using a freeze-drying method, and then used directly, or by drying it using freeze-drying, hot air drying, spray drying, etc.

[0019] The chrysin used in this invention, also known as 5,7-dihydroxyflavone, is a flavonoid extracted from plants. The chrysin used in this invention can be obtained by purchase or synthesis. The composition may contain 0.00001 to 5% by weight of the above-mentioned chrysin, preferably 0.0001 to 1% by weight, relative to the total weight of the composition.

[0020] The quercetin used in this invention, also known as 3,3',4',5,7-pentahydroxyflavone, is a plant flavonol belonging to the flavonoid group of polyphenols. The quercetin used in this invention can be obtained by purchase or synthesis. The composition contains 0.00001 to 5% by weight of the above-mentioned quercetin, preferably 0.0001 to 1% by weight, relative to the total weight of the composition.

[0021] The sodium mannose phosphate used in this invention has the chemical formula C6H. 12 O9PNa can be obtained by purchase or synthesis. The composition contains 0.00001 to 1% by weight of the above-mentioned sodium mannose phosphate, preferably 0.0001 to 0.5% by weight of the above-mentioned sodium mannose phosphate, relative to the total weight of the composition.

[0022] The kaempferol used in this invention, also known as 3,4',5,7-tetrahydroxyflavone, is a natural flavonoid. The kaempferol used in this invention can be obtained by purchase or synthesis. The composition may contain 0.00001 to 1% by weight of the above-mentioned kaempferol, preferably 0.0001 to 0.5% by weight.

[0023] The pyruvate used in this invention refers to the negatively charged form of pyruvic acid (C3H4O3) (C3H3O3-). The cation forming the salt with the negatively charged pyruvate is selected from, but is not limited to, the group consisting of sodium, potassium, calcium, magnesium, barium, aluminum, and mixtures thereof. The pyruvate used in this invention can be obtained by purchase or synthesis. The composition contains 0.00001 to 1% by weight of the above-mentioned pyruvate, preferably 0.0001 to 0.5% by weight.

[0024] In one embodiment, the mixture comprises 0.0001 to 50% by weight of the above-mentioned active ingredients relative to the total weight of the composition, preferably 0.001 to 10% by weight of the above-mentioned active ingredients. The effect is more superior when the content of the above-mentioned active ingredient mixture is within the above range.

[0025] In one embodiment, when mixing the above-mentioned active ingredients, the weight ratio of bisabolol: glutenol: Polygonum cuspidatum extract: salicumin: quercetin: sodium mannophosphate: kaempferol: pyruvate is 1:0.05~0.5:0.01~0.1:0.005~0.05:0.005~0.05:0.001~0.01:0.0005~0.005:0.00005~0.0005, preferably 1:0.05~0.3:0.04~0.08:0.01~0.04:0.01~0.04:0.004~0.008:0.0005~0.003:0.0001~0.0004.

[0026] In one embodiment, the above-described cosmetic composition comprises, as a solvent, one of the following groups: water, lower alcohols of C1 to C4, polyols, and mixtures thereof.

[0027] In one embodiment, the aforementioned skin improvement is selected from the group consisting of skin barrier strengthening, pigmentation inhibition, wrinkle improvement, or elasticity enhancement, and a combination thereof.

[0028] The term "skin barrier" as used in this instruction manual refers to the physical, chemical, or physiological barrier formed by the skin to prevent the invasion of external substances such as pathogens and the outflow of substances, while also preventing chemical or physical damage and the loss of moisture or minerals. Furthermore, the term "skin barrier strengthening / improvement" refers to the chemical or biological restoration of a damaged skin barrier, improving its function as a barrier to effectively prevent the invasion of external substances or the outflow of substances. This differs from simply directly filling the skin with moisture or physically preventing moisture loss through skin moisturizing.

[0029] Regarding skin barrier strengthening, in the binding between cells, there is a tight junction protein called Zonulaoccludens-1 (ZO-1). ZO-1 is a 220kD terminal membrane protein encrypted through the human TJP1 gene and belongs to the tight junction-related protein series, namely ZO-1, ZO-2, and ZO-3. ZO-1 is responsible for strengthening the binding between epidermal cells. Decreased expression of ZO-1 is observed in skin with weakened skin barriers, such as those caused by allergies or psoriasis.

[0030] Regarding pigmentation, the regulation of skin pigmentation is achieved through a complex melanogenic paracrine network between mesothelial cells and epithelial cells, thereby regulating the survival, proliferation, and melanin production of melanocytes. KITLG, a melanocyte-derived growth factor, and its container c-Kit, play a crucial role in regulating physiological and pathological skin pigmentation by triggering the Ras / MAPK signaling pathway. Specifically, KITLG, a factor secreted by keratinocytes, acts as a c-Kit ligand to activate the c-Kit melanin synthesis pathway; therefore, KITLG inhibitors have pigmentation-inhibiting effects.

[0031] The term "skin elasticity enhancement" as used in this specification refers to increasing skin elasticity by inhibiting collagen-degrading enzymes and promoting collagen production, thereby inhibiting or preventing the loss of skin elasticity or alleviating already reduced elasticity. This "skin elasticity enhancement" is achieved by increasing the production of fibronectin and collagen, thus forming a strong skeleton of skin cells. Additionally, MMP9 (matrix metalloproteinase-9), as an ECM (extracellular matrix) degradase secreted in the epidermis, has the function of breaking down collagen in the dermis; therefore, inhibiting MMP9 promotes collagen production.

[0032] In one embodiment of the present invention, the above-mentioned cosmetic composition includes auxiliary agents commonly used in the field of cosmetics, such as fatty substances, organic solvents, solvents, concentrates, gelling agents, softeners, antioxidants, suspending agents, stabilizers, foaming agents, fragrances, surfactants, water, ionic or nonionic emulsifiers, fillers, metal ion sealants, chelating agents, preservatives, vitamins, blocking agents, wetting agents, essential oils, dyes, pigments, hydrophilic or lipophilic active agents or liposomes, etc., and may also include any other ingredients commonly used in cosmetics.

[0033] In one embodiment of the present invention, the dosage form of the above-mentioned cosmetic composition is, for example, manufactured as a solution, emulsion, suspension, ointment, face cream, face lotion, gel, powder, gel water, facial cleanser containing surfactant, oil, soap, liquid cleansing material, bath additive, foundation cream, foundation, serum, toner, foam, face mask, softening lotion, sunscreen or sunscreen oil, etc. Preferably, the dosage form of the above-mentioned cosmetic composition is manufactured as a topical ointment, softening toner, nourishing toner, nourishing cream, massage cream, serum, face mask, lotion or oil gel, etc.

[0034] The present invention also provides a topical skin composition comprising bisabolol, rice glutenol, Polygonum cuspidatum extract, guarin, quercetin, sodium mannose phosphate, kaempferol and pyruvate.

[0035] In one embodiment, the aforementioned topical skin composition refers to a solid, semi-solid, or liquid topical agent formed by mixing active ingredients in various mechanisms such as oils, petroleum ethers, lanolin, or glycerin to create a form that is easy to apply. The dosage form is not particularly limited and can be a powder, gel, ointment, cream, liquid, or aerosol.

[0036] In one embodiment of the present invention, the above-described topical skin composition is applied to the face or other body parts via transdermal administration, such as direct application or spraying onto the skin. The terms "administration" or "application" refer to the delivery of the disclosed composition to the skin by any suitable method. The composition can be administered via any common route, as long as it reaches the target tissue; it can be transdermal, preferably topical application. The frequency of administration or application of the composition can be appropriately determined according to the user's needs. The dosage of the composition can be appropriately adjusted according to individual differences such as age or skin condition, or the dosage form; typically, an appropriate amount can be applied to the skin once or several times a day for use for one week or several months.

[0037] The present invention also provides the skin-improving uses of compositions comprising bisabolol, rice glutenol, Polygonum cuspidatum extract, guarin, quercetin, sodium mannose phosphate, kaempferol and pyruvate.

[0038] The present invention also provides a method for manufacturing a cosmetic composition for skin improvement, the method comprising the step of mixing bisabolol, rice glutenol, Polygonum cuspidatum extract, guarin, quercetin, sodium mannophosphate, kaempferol and pyruvate.

[0039] The present invention also provides a method for improving skin, the method comprising applying a composition comprising bisabolol, rice glutenol, Polygonum cuspidatum extract, guarin, quercetin, sodium mannophosphate, kaempferol and pyruvate to the skin.

[0040] In one embodiment of the present invention, in the above-described skin improvement method, the composition is applied to the skin at an dosage of 1 to 1000 mg / L, preferably 10 to 500 mg / L, of the active ingredient in the composition. Furthermore, in the above method, the composition can be applied to the skin for more than one week, for example, from one day to six months, preferably from one week to four months; the longest application time is not limited. Additionally, in the above method, the composition can be applied to the skin once to six times a day, preferably once to three times, for example, twice a day, once in the morning and once in the evening.

[0041] Preferably, all ingredients described in this disclosure do not exceed the maximum usage limits specified in the relevant regulations and standards of Korea, China, the United States, Europe, Japan, etc. (e.g., regulations on cosmetic safety standards (Korea) or cosmetic safety technical specifications (China)). That is, preferably, the cosmetic or topical skin composition of this disclosure contains the ingredients of this disclosure within the content limits permitted by the relevant regulations and standards of each country.

[0042] Invention Effects

[0043] The skin-improving compositions of the present invention exhibit excellent synergistic effects on skin barrier strengthening, pigmentation inhibition, wrinkle improvement, and elasticity enhancement through the combination of specific ingredients. Therefore, the skin-improving compositions of the present invention can be effectively used as functional compositions in cosmetics or topical skin agents targeting skin tissue. Attached Figure Description

[0044] Figure 1 The results show the ZO-1 expression levels of individual substances and mixtures containing bisabolol, glutenol, Polygonum cuspidatum extract, guarin, quercetin, sodium mannose phosphate, kaempferol, and pyruvate.

[0045] Figure 2 The results show the KITLG inhibitory effects of individual substances of bisabolol, glutenol, Polygonum cuspidatum extract, salicumin, quercetin, sodium mannose phosphate, kaempferol and pyruvate, and mixtures containing these substances.

[0046] Figure 3 The results show the MMP9 inhibitory effects of individual substances of bisabolol, glutenol, Polygonum cuspidatum extract, salicumin, quercetin, sodium mannose phosphate, kaempferol and pyruvate, and mixtures containing these substances. Detailed Implementation

[0047] The present invention will now be described in detail through embodiments, etc., to aid in understanding. However, the embodiments of the present invention can be modified into various different forms, and the scope of the present invention is not limited to the embodiments described below. The embodiments of the present invention are provided to illustrate the present invention more completely to those skilled in the art.

[0048] Example 1. Manufacturing a composition for skin improvement

[0049] A skin lotion composition was manufactured using bisabolol, glutenin, Polygonum cuspidatum extract, eugenol, quercetin, sodium mannose phosphate, kaempferol, and pyruvate, according to the formulations listed in Table 1 below, by a conventional method.

[0050] Table 1

[0051] Experimental Example 1. Skin Barrier Strengthening

[0052] Immunocytochemistry was performed to detect the expression level of ZO-1, a key protein constituting the cell barrier. HaCaT cells were seeded in 24-well plates and cultured at 37°C in 5% CO2 for 24 hours. The sample was dissolved in 1 mL of culture medium and applied to the cells, followed by further culture at 37°C in 5% CO2 for 24 hours. After washing with PBS, the cells were fixed at room temperature with 4% paraformaldehyde for 10 minutes. The cells were then permeabilized with PBS containing 0.1% Triton X-100 and blocked with PBS containing 5% FBS and 1% BSA. ZO-1 primary antibody (Abcam, Cambridge, UK) was applied at 4°C for 12 hours, followed by secondary antibody (Thermo Fisher Scientific, MA, USA) at room temperature for 1 hour before staining. Using a fully automated live-cell imaging system (EVOS) TMHigh-resolution fluorescence images were captured using the FLAuto2 Imaging System (ThermoFisher Scientific, MA, USA), and quantitative analysis of fluorescence intensity was performed using Celleste image analysis software (ThermoFisher Scientific, MA, USA).

[0053] Regarding the experimental substances, bisabolol, rice glutenin, Polygonum cuspidatum extract, guarin, quercetin, sodium mannose phosphate, kaempferol, and pyruvate, as well as mixtures containing these substances, were prepared to a concentration of 1 μg / ml as shown in Table 2 below. The detected ZO-1 expression levels are as follows: Figure 1 As shown.

[0054] Table 2

[0055] like Figure 1 As shown, bisabolol, glutenol, Polygonum cuspidatum extract, salicumin, quercetin, sodium mannose phosphate, kaempferol, and pyruvate each showed a ZO-1 expression effect of approximately 0.5 to 2.5 times compared to the control group. When these mixtures were treated, the ZO-1 expression level increased by approximately 8 times, thus demonstrating an excellent synergistic effect.

[0056] Example 2-3. Evaluation of inhibition of pigmentation and promotion of collagen production

[0057] mRNA expression analysis was performed to evaluate the inhibitory efficacy of KITLG and MMP9 expression. HaCaT cells were seeded in 24-well plates and cultured at 37°C in 5% CO2 for 24 hours. After dissolving the experimental material in 1 mL of culture medium and treating the cells, they were further cultured at 37°C in 5% CO2 for 24 hours. RNA prep was performed on the AccuPrep® Universal RNA Extraction Kit (BIONEER; cat#K-3140) stage to extract RNA from these cultured cells. cDNA was fabricated based on the extracted RNA using AccuPower® RocketScript™ Cycle RT PreMix(dT20) (BIONEER; cat#K-2202). Real-time quantitative polymerase chain reaction (PCR) was then performed using the fabricated cDNA. Taqman Universal Master Mix II (containing UNG) (ABI; cat #4440045, USA) was used as a probe. Taqman™ probes GAPDH (reference gene), KITLG, and MMP9 were used as probes. PCR reactions were performed according to the ABI 7500 Real-Time PCR system protocol, and data were obtained using ABI software (delta-Ct method).

[0058] Delta Ct: Ct(target gene) - Ct(GAPDH)

[0059] Delta delta Ct: delta Ct (experimental treatment group) - delta Ct (control group)

[0060] The delta Ct value obtained by the above calculation formula can be regarded as the increase in the number of genes in the treatment group relative to the control group. The number of genes increases by a power of 2, and the expression level is calculated as 2^(-delta Ct). When the expression level in the treatment group is low relative to the control group, it is judged to have the effect of inhibiting the expression of the gene.

[0061] For the control group, a culture medium without experimental substances was used. For the experimental substances, the following were used as listed in Table 2 above: bisabolol, rice glutenin, Polygonum cuspidatum extract, salicylic acid, quercetin, sodium mannose phosphate, kaempferol, and pyruvate, each mixed with these substances, to a final concentration of 1 μg / ml. The degree of KITLG expression inhibition was detected as follows: Figure 2 As shown, the degree of MMP9 expression inhibition is as follows: Figure 3 As shown.

[0062] like Figure 2 As shown, each of the following substances—bisabolol, glutenol, Polygonum cuspidatum extract, salicumin, quercetin, sodium mannose phosphate, kaempferol, and pyruvate—showed approximately 40% to 80% KITLG expression values ​​or even increased KITLG expression compared to the control group. In the case of treating these mixtures, the KITLG expression values ​​showed a low value of approximately 20%, thus demonstrating excellent synergistic effects.

[0063] In addition, such as Figure 3 As shown, bisabolol, glutenol, Polygonum cuspidatum extract, salicumin, quercetin, sodium mannose phosphate, kaempferol, and pyruvate each showed approximately 50% to 90% MMP9 expression values ​​or even increased MMP9 expression compared to the control group. In the case of treating these mixtures, MMP9 expression showed a small value of less than 20%, thus demonstrating excellent synergistic effects.

Claims

1. A cosmetic composition for skin improvement, characterized in that, The above-mentioned cosmetic composition for skin improvement contains bisabolol, glutenol, Polygonum cuspidatum extract, quercetin, sodium mannophosphate, kaempferol and pyruvate.

2. The skin-improving cosmetic composition according to claim 1, characterized in that, The weight ratio of bisabolol, glutenol, Polygonum cuspidatum extract, salicumin, quercetin, sodium mannophosphate, kaempferol, and pyruvate is 1:0.05~0.5:0.01~0.1:0.005~0.05:0.005~0.05:0.001~0.01:0.0005~0.005:0.00005~0.0005.

3. The cosmetic composition according to claim 1, characterized in that, The cosmetic composition described above, as a solvent, comprises one of the group consisting of water, lower alcohols from C1 to C4, polyols, and mixtures thereof.

4. The cosmetic composition according to claim 1, characterized in that, The aforementioned skin improvements are selected from one or more groups consisting of skin barrier strengthening, pigmentation inhibition, wrinkle improvement, and elasticity enhancement.

5. A skin-improving topical skin agent composition, characterized in that, The above-mentioned skin-improving topical skin agent composition contains bisabolol, rice glutenol, Polygonum cuspidatum extract, guarin, quercetin, sodium mannose phosphate, kaempferol, and pyruvate.

6. The topical skin composition according to claim 5, characterized in that, The weight ratio of bisabolol, glutenol, Polygonum cuspidatum extract, salicumin, quercetin, sodium mannophosphate, kaempferol, and pyruvate is 1:0.05~0.5:0.01~0.1:0.005~0.05:0.005~0.05:0.001~0.01:0.0005~0.005:0.00005~0.0005.

7. The topical skin composition according to claim 5, characterized in that, The above-mentioned topical skin composition comprises, as a solvent, one of the groups consisting of water, lower alcohols selected from C1 to C4, polyols, and mixtures thereof.

8. The topical skin composition according to claim 5, characterized in that, The aforementioned skin improvements are selected from one or more groups consisting of skin barrier strengthening, pigmentation inhibition, wrinkle improvement, and elasticity enhancement.

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