Composition for improving chloasma

Abstract

The invention relates to the technical field of cosmetics, in particular to a composition for improving chloasma, which is prepared from panax notoginseng saponins, tranexamic acid, palmitoyl tripeptide-5 compound, hydrolyzed pearl compound, dipotassium glycyrrhizinate and panthenol according to the mass ratio of (0.01-0.12): (0.01-3): (0.01-4): (0.001-2): (0.01-0.11): (0.05-5). The composition for improving chloasma, provided by the invention, has the effects of improving chloasma, preserving moisture, repairing, resisting inflammation, resisting oxidation and the like, plays a significant role in improving chloasma from a plurality of channels, and provides a new choice for improving chloasma.

Description

Technical Field

[0001] This invention relates to the field of cosmetic technology, and more specifically to a composition for improving melasma. Background Technology

[0002] Melasma is a common, easily diagnosed but difficult-to-treat cosmetic skin condition. Its incidence is rising annually, affecting not only appearance but also the physical and mental health of patients. Western medicine believes melasma is related to factors such as photodamage, genetic predisposition, hormonal changes, impaired skin barrier function, vascular factors, inflammatory responses, psychological factors, and oxidative stress, but the exact relationship is not fully understood. Commonly used topical medications in Western medicine include hydroquinone cream, which, while possessing some antioxidant properties, can irritate the skin and impair its barrier function.

[0003] With the continuous development of science and technology, natural plant extracts, due to their mildness, low irritation, and multiple functions, have gradually become a hot topic in cosmetic raw material research. In my country, approximately 82.64% of cosmetics contain plant extracts, and 80.17% of cosmetics use a combination of two or more plant extracts. Adding a certain amount of natural plant extracts to chemical raw materials to enhance their efficacy has become the mainstream direction of cosmetic development.

[0004] Traditional Chinese medicine believes that melasma is closely related to the liver, spleen, and kidneys, with the main pathogenesis being the inability of qi and blood to nourish the face. Panax notoginseng, a traditional Chinese medicine, has the effects of removing blood stasis, stopping bleeding, promoting blood circulation, and relieving pain. It can promote blood circulation in the skin while inhibiting acne growth. Panax notoginseng total saponins (PNS) can increase serum superoxide dismutase (SOD), reduced glutathione (GSH), and catalase (CAT) levels, exhibiting strong anti-free radical and antioxidant effects, thus playing a certain role in improving melasma. Although there are currently products using Panax notoginseng to improve melasma, the variety is limited, and the effects are generally limited to whitening and treating melasma, failing to meet the market's demand for diverse choices of products to improve melasma. Therefore, this invention provides a composition that combines the effects of improving melasma, moisturizing and repairing, and anti-inflammatory and antioxidant properties, offering a new option for improving melasma. Summary of the Invention

[0005] The purpose of this invention is to provide a composition for improving melasma that has the effects of improving melasma, moisturizing and repairing, anti-inflammatory and antioxidant properties.

[0006] To achieve the above objectives, the present invention provides the following technical solution: This invention proposes a composition for improving melasma, which consists of total saponins of Panax notoginseng, tranexamic acid, palmitoyl tripeptide-5 complex, hydrolyzed pearl compound, dipotassium glycyrrhizate, and panthenol in a mass ratio of 0.01-0.12:0.01-3:0.01-4:0.001-2:0.01-0.11:0.05-5.

[0007] Furthermore, the mass ratio of the total saponins of Panax notoginseng, tranexamic acid, palmitoyl tripeptide-5 complex, hydrolyzed pearl compound, dipotassium glycyrrhizate, and panthenol is 0.0500:2.0000:0.5000:0.1000:0.0200:0.5000.

[0008] Furthermore, the palmitoyl tripeptide-5 complex comprises palmitoyl tripeptide-5, glycerol, and water.

[0009] Furthermore, the palmitoyl tripeptide-5 complex comprises 0.1-1% palmitoyl tripeptide-5, 50-80% glycerol, and 25-50% water.

[0010] Furthermore, the hydrolyzed pearl compound includes water, hydrolyzed pearl, phenoxyethanol, propylene glycol, methylparaben, ethylparaben, and ethylhexylglycerin.

[0011] Furthermore, the hydrolyzed pearl compound comprises 98.9% water, 0.6% hydrolyzed pearl, 0.25% phenoxyethanol, 0.075% propylene glycol, 0.075% methylparaben, 0.05% ethylparaben, and 0.05% ethylhexylglycerin.

[0012] Compared with the prior art, the present invention provides a composition for improving melasma that has the effects of improving melasma, moisturizing and repairing, anti-inflammatory and antioxidant properties. It plays a significant role in improving melasma through multiple pathways, providing a new option for improving melasma. Attached Figure Description

[0013] Figure 1 Before and after the subjects used the experimental product, the images showed a comparison.

[0014] Figure 2 Comparison of skin condition before and after subjects used the experimental product. Detailed Implementation

[0015] The technical solution of the present invention will be further described below with reference to specific embodiments. It should be understood that the following embodiments are merely illustrative and explanatory of the present invention and should not be construed as limiting the scope of protection of the present invention. All technologies implemented based on the above content of the present invention are covered within the scope of protection intended by the present invention.

[0016] The raw materials involved in the embodiments of this invention (total saponins of Panax notoginseng, tranexamic acid, palmitoyl tripeptide-5 complex, hydrolyzed pearl compound, dipotassium glycyrrhizate, panthenol) are all commercially available products.

[0017] In the following examples and comparative examples, the palmitoyl tripeptide-5 complex used was purchased from DSM Nutrition Products Co., Ltd. (batch number: UQ40152008), and the hydrolyzed pearl compound was purchased from Huzhou Huxing Daily Chemical Co., Ltd. (batch number: 20231017). Example 1:

[0018] Example composition 1 is composed of the following raw materials and their proportions: Total saponins of Panax notoginseng: Tranexamic acid: Palmitoyl tripeptide-5 complex: Hydrolyzed pearl complex: Dipotassium glycyrrhizate: Panthenol = 0.0100: 2.0256: 0.5064: 0.1013: 0.0203: 0.5064. Example 2:

[0019] Example composition 2 is composed of the following raw materials and their proportions: Panax notoginseng total saponins: tranexamic acid: palmitoyl tripeptide-5 complex: hydrolyzed pearl complex: dipotassium glycyrrhizate: panthenol = 0.0500: 2.0000: 0.5000: 0.1000: 0.0200: 0.5000. Example 3:

[0020] Example composition 3 is composed of the following raw materials and their proportions: Total saponins of Panax notoginseng: Tranexamic acid: Palmitoyl tripeptide-5 complex: Hydrolyzed pearl complex: Dipotassium glycyrrhizate: Panthenol = 0.1200: 1.9551: 0.4888: 0.0978: 0.0196: 0.4888.

[0021] Comparative Example 1 Comparative composition 1 is composed of the following raw materials and their proportions: Tranexamic acid: Palmitoyl tripeptide-5 complex: Hydrolyzed pearl complex: Dipotassium glycyrrhizate: Panthenol = 2.0000: 0.5223: 0.1045: 0.0209: 0.5223.

[0022] Comparative Example 2 Comparative composition 2 is composed of the following raw materials and their proportions: Panax notoginseng total saponins: palmitoyl tripeptide-5 complex: hydrolyzed pearl complex: dipotassium glycyrrhizate: panthenol = 0.0500: 1.3929: 0.2786: 0.0557: 1.3929.

[0023] Comparative Example 3 Comparative composition 3 is composed of the following raw materials and their proportions: Total saponins of Panax notoginseng: tranexamic acid: hydrolyzed pearl compound: dipotassium glycyrrhizate: panthenol = 0.0500: 2.0000: 0.1806: 0.0361: 0.9032.

[0024] Comparative Example 4 Comparative composition 4 is composed of the following raw materials and their proportions: Total saponins of Panax notoginseng: Tranexamic acid: Palmitoyl tripeptide-5 complex: Dipotassium glycyrrhizate: Panthenol = 0.0500: 2.0000: 0.5490: 0.0220: 0.5490.

[0025] Comparative Example 5 Comparative composition 5 is composed of the following raw materials and their proportions: Panax notoginseng total saponins: tranexamic acid: palmitoyl tripeptide-5 complex: hydrolyzed pearl complex: panthenol = 0.0500: 2.0000: 0.5091: 0.1018: 0.5091.

[0026] Comparative Example 6 Comparative composition 6 is composed of the following raw materials and their proportions: Total saponins of Panax notoginseng: Tranexamic acid: Palmitoyl tripeptide-5 complex: Hydrolyzed pearl complex: Dipotassium glycyrrhizate = 0.0500: 2.0000: 0.9032: 0.1806: 0.0362.

[0027] The compositions of the above examples and comparative examples were subjected to the following evaluation experiments (whitening, anti-wrinkle, antioxidant, soothing, repairing, and human efficacy).

[0028] I. Whitening Efficacy Evaluation: Step 1: Human melanocyte plating culture; Step 2: Cell-based drug delivery; Step 3: Testing the relative expression level of melanin; The specific procedures for cell manipulation in step one include: The cultured A375 cells were digested, centrifuged, counted, and a cell concentration of 3 × 10⁶ cells was prepared. 5 Mix the sample with water at a concentration of 1 mL, add 1 mL to each well of a 12-well plate, and incubate in an incubator for 24 h ± 2 h.

[0029] The specific procedures for cell manipulation in step three include: After culturing for 24 h ± 2 h, the culture medium was discarded, the cells were washed twice with PBS, digested, and collected in 1.5 mL EP tubes. The tubes were centrifuged at 10000 rpm for 10 min, and the supernatant was discarded. 0.5 mL of 1 mol / L sodium hydroxide solution containing 10% DMSO was added to each tube. The tubes were sealed with sealing film and heated in an 80℃ water bath for 60 min. After heating, each tube was shaken to allow the cells to fully dissolve. After the temperature equilibrated to room temperature, 200 μL of the above solution was added to each well of a 96-well plate, with two replicates per EP tube. For the solvent blank group, 200 μL of sodium hydroxide solution containing 10% DMSO was added to each well (three replicates). The absorbance was measured at 405 nm using a microplate reader. The experimental results are shown in Table 1 below.

[0030] Table 1 Results of melanin synthesis inhibition by each group of compositions

[0031] II. Evaluation of anti-wrinkle and firming efficacy: Step 1: Human fibroblast plating culture; Step 2: Cell drug administration. Two hours after drug administration, administer 125 mJ / cm² to the cells. 2 UVA irradiation; Step 3: Collect cell samples and perform ELISA tests on the corresponding proteins; The specific procedures for cell manipulation in step one include: The cultured HFF-1 cells were digested, centrifuged, counted, and a cell concentration of 3 × 10⁶ cells was prepared. 5 Mix the sample with water at a concentration of 1 mL, add 1 mL to each well of a 12-well plate, and incubate in an incubator for 24 h ± 2 h.

[0032] The specific procedures for cell manipulation in step three include: After culturing for 24 h ± 2 h following drug administration, the culture medium was discarded, the cells were washed twice with PBS, digested, and collected in 1.5 mL EP tubes. The cells were centrifuged at 10000 rpm for 10 min, and the supernatant was carefully discarded. PBS containing PMSF was added, and the cells were lysed by repeated freeze-thaw cycles 2-3 times. The supernatant was collected, and the protein content was determined using a BCA assay, which was then used for subsequent ELISA experiments.

[0033] Remove the ELISA kit from the freezer 1 hour in advance and allow it to equilibrate to room temperature. Remove the collected supernatant from the -80℃ freezer beforehand, thaw it, and centrifuge at 10,000 rpm for 20 min. Set up standard wells and sample wells. Add 100 μL of each of the eight standard concentrations to the standard wells, and add 100 μL of the collected cell supernatant to each sample well. Cover with sealing film and incubate at 37℃ for 60 min. After 60 min, remove the ELISA plate, discard the liquid, add 100 μL of biotinylated antibody working solution to each well, cover with sealing film, and incubate at 37℃ for 60 min. After 60 min, remove the ELISA plate, discard the liquid, add 300 μL of prepared washing buffer to each well, let stand for 1 min, discard the washing buffer, pat dry on absorbent paper, and repeat the washing process 3 times. Add 100 μL of enzyme conjugate working solution to each well, cover with sealing film, and incubate at 37°C for 30 min. After 30 min, remove the microplate, discard the liquid, add 300 μL of prepared washing buffer to each well, let stand for 1 min, discard the washing buffer, pat dry on absorbent paper, and repeat the washing 5 times. Add 90 μL of substrate (TMB) to each well, cover with sealing film, and incubate at 37°C for 15 min. After 15 min, remove the microplate, add 50 μL of stop solution to each well, and immediately measure the OD value of each well at 450 nm.

[0034] The experimental results are shown in Table 2 below.

[0035] Table 2. Results of each group's composition on increasing collagen COL I and COL IV levels.

[0036] III. Antioxidant efficacy evaluation: Step 1: Human immortalized keratinocyte plating culture; Step 2: Cell drug administration. Two hours after drug administration, administer 50 mJ / cm² to the cells. 2 UVB irradiation; Step 3: Collect cell samples and perform appropriate ROS tests; The specific procedures for cell manipulation in step one include: The cultured HaCaT cells were digested, centrifuged, counted, and a cell concentration of 3 × 10⁶ cells was prepared. 5 Mix the sample with water at a concentration of 1 mL, add 1 mL to each well of a 12-well plate, and incubate in an incubator for 24 h ± 2 h.

[0037] The experimental results are shown in Table 3 below.

[0038] Table 3. Inhibition results of ROS by each group of compositions

[0039] IV. Evaluation of Soothing Efficacy: Step 1: Human immortalized keratinocyte plating culture; Step 2: Cell drug administration. Two hours after drug administration, administer 50 mJ / cm² to the cells. 2 UVB irradiation; Step 3: Collect cell samples and perform ELISA tests on the corresponding proteins; The specific procedures for cell manipulation in step one include: The cultured HaCaT cells were digested, centrifuged, counted, and a cell concentration of 3 × 10⁶ cells was prepared. 5 Mix the sample with water at a concentration of 1 mL, add 1 mL to each well of a 12-well plate, and incubate in an incubator for 24 h ± 2 h.

[0040] The specific procedures for cell manipulation in step three include: After culturing for 24 h ± 2 h following drug administration, the culture medium was collected, washed twice with PBS, digested, and the cells were collected in 1.5 mL EP tubes. The cells were centrifuged at 10000 rpm for 10 min, and the supernatant was carefully discarded. PBS containing PMSF was added, and the cells were lysed by repeated freeze-thaw cycles 2-3 times. The supernatant was collected, and the protein content was determined using a BCA assay, which was then used for subsequent ELISA experiments.

[0041] Remove the ELISA kit from the freezer 1 hour in advance and allow it to equilibrate to room temperature. Remove the collected supernatant from the -80℃ freezer beforehand, thaw it, and centrifuge at 10,000 rpm for 20 min. Set up standard wells and sample wells. Add 100 μL of each of the eight standard concentrations to the standard wells, and add 100 μL of the collected cell supernatant to each sample well. Cover with sealing film and incubate at 37℃ for 60 min. After 60 min, remove the ELISA plate, discard the liquid, add 100 μL of biotinylated antibody working solution to each well, cover with sealing film, and incubate at 37℃ for 60 min. After 60 min, remove the ELISA plate, discard the liquid, add 300 μL of prepared washing buffer to each well, let stand for 1 min, discard the washing buffer, pat dry on absorbent paper, and repeat the washing process 3 times. Add 100 μL of enzyme conjugate working solution to each well, cover with sealing film, and incubate at 37℃ for 30 min. After 30 min, remove the microplate, discard the liquid, add 300 μL of prepared washing buffer to each well, let stand for 1 min, discard the washing buffer, pat dry on absorbent paper, and repeat the washing 5 times. Add 90 μL of substrate (TMB) to each well, cover with sealing film, and incubate at 37℃ for 15 min. After 15 min, remove the microplate, add 50 μL of stop solution to each well, and immediately measure the OD value of each well at 450 nm. The experimental results are shown in Table 4 below.

[0042] Table 4 Results of PGE2 inhibition by each group of compositions

[0043] V. Evaluation of Repair Efficacy: Step 1: Human immortalized keratinocyte plating culture; Step 2: Cell-based drug delivery; Step 3: Collect cell samples and perform ELISA tests on the corresponding proteins; The specific procedures for cell manipulation in step one include: The cultured HaCaT cells were digested, centrifuged, counted, and a cell concentration of 3 × 10⁶ cells was prepared. 5 Mix the sample with water at a concentration of 1 mL, add 1 mL to each well of a 12-well plate, and incubate in an incubator for 24 h ± 2 h.

[0044] The specific procedures for cell manipulation in step three include: After culturing for 24 h ± 2 h following drug administration, the culture medium was discarded, the cells were washed twice with PBS, digested, and collected in 1.5 mL EP tubes. The cells were centrifuged at 10000 rpm for 10 min, and the supernatant was carefully discarded. PBS containing PMSF was added, and the cells were lysed by repeated freeze-thaw cycles 2-3 times. The supernatant was collected, and the protein content was determined using a BCA assay, which was then used for subsequent ELISA experiments.

[0045] Remove the ELISA kit from the freezer 1 hour in advance and allow it to equilibrate to room temperature. Remove the collected supernatant from the -80℃ freezer beforehand, thaw it, and centrifuge at 10,000 rpm for 20 min. Set up standard wells and sample wells. Add 100 μL of each of the eight standard concentrations to the standard wells, and add 100 μL of the collected cell supernatant to each sample well. Cover with sealing film and incubate at 37℃ for 60 min. After 60 min, remove the ELISA plate, discard the liquid, add 100 μL of biotinylated antibody working solution to each well, cover with sealing film, and incubate at 37℃ for 60 min. After 60 min, remove the ELISA plate, discard the liquid, add 300 μL of prepared washing buffer to each well, let stand for 1 min, discard the washing buffer, pat dry on absorbent paper, and repeat the washing process 3 times. Add 100 μL of enzyme conjugate working solution to each well, cover with sealing film, and incubate at 37°C for 30 min. After 30 min, remove the microplate, discard the liquid, add 300 μL of prepared washing buffer to each well, let stand for 1 min, discard the washing buffer, pat dry on absorbent paper, and repeat the washing 5 times. Add 90 μL of substrate (TMB) to each well, cover with sealing film, and incubate at 37°C for 15 min. After 15 min, remove the microplate, add 50 μL of stop solution to each well, and immediately measure the OD value of each well at 450 nm. The experimental results are shown in Table 5 below.

[0046] Table 5 Results of ZO-1 enhancement for each group of compositions

[0047] VI. Human Efficacy Assessment: Qualified subjects were selected according to the inclusion and exclusion criteria and divided into experimental and control groups. When grouping, factors that may affect the results, such as the severity of melasma, were considered and the subjects were evenly distributed to ensure comparability between groups. In cases where the pigmentation on the left and right sides of the test site is symmetrical, the subjects can be divided into experimental product side and control product side to ensure that the final number of valid cases is not less than 30 people / group (side).

[0048] (1) Selection criteria Applicants must be healthy women or men aged 18-60; have at least one prominent pigmented spot at the test site with an ITA° difference greater than 10° from the surrounding skin, and a diameter of not less than 3 mm (not freckles, moles, etc., that are difficult to improve with topical preparations in clinical practice); have no allergic diseases or history of allergies to cosmetics or other topical preparations; have no history of photosensitivity diseases and have not used any drugs that affect photosensitivity recently; the skin at the test site should be free of birthmarks, inflammation, scars, hirsutism, etc.; be able to understand the test process, voluntarily participate in the test, and sign a written informed consent form.

[0049] (2) Exclusion criteria Pregnant or breastfeeding women, or those planning to conceive in the near future; those with a history of skin diseases such as psoriasis, eczema, atopic dermatitis, or severe acne; those with other chronic systemic diseases; those who have taken orally or used topical anti-inflammatory drugs such as corticosteroids within the past month; those who have used any products or drugs that affect skin color (such as hydroquinone preparations) such as glycolic acid or salicylic acid within the past two months; those who have used retinoid preparations or undergone cosmetic treatments such as chemical peels, lasers, or pulsed light on the test site within the past three months; those who have unavoidable prolonged sun exposure; those who have participated in other clinical trials within the past two months; and other individuals deemed unsuitable for participation in the trial based on clinical evaluation.

[0050] (3) Subject restrictions During the test, the test site must use the test product or control product provided by the testing institution. No other products with whitening or spot-removing effects or that may affect the test results may be used. There should be no sun exposure during the test, and the test site should be protected from the sun.

[0051] (4) Test substance Test product: An aqueous solution containing the composition of Example 2 (total saponins of Panax notoginseng: tranexamic acid: palmitoyl tripeptide-5 complex: hydrolyzed pearl complex: dipotassium glycyrrhizate: panthenol = 0.0500: 2.0000: 0.5000: 0.1000: 0.0200: 0.5000).

[0052] Control product: Aqueous solution of Example 2 composition without additional addition.

[0053] Instructions for use: Staff will distribute the test product and control product and provide usage guidance to the subjects according to the instructions, ensuring that the subjects use the product correctly and continuously for 2 weeks. Subjects are required to record the usage time and any discomfort or adverse reactions during use.

[0054] (5) Instruments and equipment Standard image capturing equipment: A capturing system capable of capturing images of the front, left, and right sides of the face or other test sites, equipped with visible light / polarized light filters.

[0055] (6) Environmental conditions The results of the test should be observed in a constant environment with a temperature of 21±1°C and a relative humidity of 50±10% RH. The visual assessment should also be conducted under constant lighting conditions (fluorescent tubes or LED lights with a color temperature of 5500~6500K). All subjects should be allowed to adapt to this environment for at least 30 minutes before assessment and testing can be performed.

[0056] (7) Test Procedure Before product use, eligible subjects underwent baseline skin value assessment and testing, including visual assessment, instrument testing, and standard image capture, and the results were recorded. The same assessment and testing were repeated two weeks after product use.

[0057] (8) Image acquisition and analysis Standard images were captured using a skin imaging system at each visit time. Image analysis software was used to analyze and record relevant parameters (mean optical density of pigmented spots, percentage of pigmented spot area) at different visit times for the tested areas; the smaller the mean optical density of pigmented spots in the images of the tested areas, the lighter the skin tone.

[0058] The experimental results are shown in Table 6 below; a comparison chart of the before and after use of the test product can be found in the table. Figure 1 and Figure 2 As shown.

[0059] Table 6. Results of relevant parameters (mean ± standard deviation) after using the composition for improving melasma.

[0060] Note: Compared with the control product group, * p＜0.05。

[0061] While specific embodiments of the present invention have been described above, those skilled in the art should understand that the specific embodiments described are merely illustrative and not intended to limit the scope of the invention. Modifications and variations made by those skilled in the art in accordance with the spirit of the invention should be covered within the scope of protection of the claims of the present invention.

Claims

1. A composition for improving melasma, characterized in that: It is composed of total saponins of Panax notoginseng, tranexamic acid, palmitoyl tripeptide-5 complex, hydrolyzed pearl compound, dipotassium glycyrrhizate, and panthenol in a mass ratio of 0.01-0.12:0.01-3:0.01-4:0.001-2:0.01-0.11:0.05-5.

2. The composition for improving melasma according to claim 1, characterized in that: The mass ratio of the total saponins of Panax notoginseng, tranexamic acid, palmitoyl tripeptide-5 complex, hydrolyzed pearl compound, dipotassium glycyrrhizate, and panthenol is 0.0500:2.0000:0.5000:0.1000:0.0200:0.5000.

3. The composition for improving melasma according to claim 1, characterized in that: The palmitoyl tripeptide-5 complex comprises palmitoyl tripeptide-5, glycerol, and water.

4. The composition for improving melasma according to claim 1, characterized in that: The hydrolyzed pearl compound includes water, hydrolyzed pearl, phenoxyethanol, propylene glycol, methylparaben, ethylparaben, and ethylhexylglycerin.

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