Whitening composition as well as application and cosmetic thereof

Abstract

The invention belongs to the technical field of cosmetics, and discloses a whitening composition, application thereof and cosmetics. The whitening composition is prepared from the following active ingredients in parts by mass: 16 to 24 parts of coix seed fermentation liquor, 8 to 12 parts of Chinese herbaceous peony extract combined factors, 22 to 38 parts of 4-butylresorcinol solution and 2 to 8 parts of zinc gluconate, through the synergistic effect of the four components, the activity of tyrosinase can be effectively inhibited, synthesis of cell melanin can be effectively inhibited, and the whitening effect is good.

Description

Technical Field

[0001] This invention belongs to the field of cosmetic technology and discloses a whitening composition and its uses, as well as cosmetics. Background Technology

[0002] With increasing attention to personal appearance and skin health, skin whitening has become a significant demand in the cosmetics market. Currently, the global market for skin whitening products continues to expand, and consumers are increasingly demanding safe, effective, and gentle whitening products.

[0003] Currently, most whitening products on the market achieve their whitening effect primarily through inhibiting tyrosinase activity, blocking melanin transport, and promoting melanin metabolism. However, most existing whitening products still have some problems: some whitening ingredients, such as hydroquinone, while having a significant whitening effect, have strong cytotoxicity, and long-term use may cause irreversible damage to the skin, or even trigger adverse reactions such as skin allergies and increased pigmentation; kojic acid, for example, has poor stability under high temperature and light conditions, and is easily decomposed and deteriorated, affecting the product's shelf life and whitening efficacy; niacinamide, when used at high concentrations, may cause intolerance reactions such as stinging and redness in some people with sensitive skin. Furthermore, some whitening products have relatively simple whitening ingredients, often failing to achieve the desired whitening effect.

[0004] Therefore, the technical problem that this invention needs to solve is: how to prepare a new whitening composition. Summary of the Invention

[0005] The purpose of this invention is to provide a whitening composition comprising coix seed fermentation liquid, peony extract combination factor, 4-butylresorcinol solution and zinc gluconate. When these components are used together, they have a significant synergistic effect and can exert an ultimate whitening effect.

[0006] In addition, the present invention also provides the use of a whitening composition and a cosmetic product.

[0007] To achieve the above objectives, the present invention provides the following technical solution: A whitening composition, by weight, comprises the following active ingredients in parts by weight: 16-24 parts of coix seed fermentation broth, 8-12 parts of peony extract combination factor, 22-38 parts of 4-butylresorcinol solution, and 2-8 parts of zinc gluconate.

[0008] Preferably, the whitening composition further comprises, by weight, 0.1 to 1.5 parts of decarboxylated carnosine hydrochloride and 0.05 to 2.5 parts of Polygonatum sibiricum extract combination factor.

[0009] Preferably, the whitening composition further comprises, by weight, 21-32.75 parts water, 4-6 parts butylene glycol, 0.4-0.6 parts 1,2-hexanediol, and 0.4-0.6 parts p-hydroxyacetophenone.

[0010] Preferably, the coix seed fermentation broth, based on 100% of its total mass, comprises the following components and their mass percentages: 30 wt% coix seed extract, 68 wt% glycerol, and 2 wt% 1,2-hexanediol.

[0011] Preferably, the peony extract combination factor, based on a total mass of 100%, comprises the following components and their mass percentages: 30 wt% peony root extract, 30 wt% butylene glycol, 39 wt% water, 0.5 wt% 1,2-hexanediol, and 0.5 wt% p-hydroxyacetophenone.

[0012] Preferably, the 4-butylresorcinol solution comprises, by weight 100%, the following components and their weight percentages: 10 wt% 4-butylresorcinol, 40 wt% hydroxypropyl cyclodextrin, 44 wt% water, 5 wt% 1,3-propanediol, 0.5 wt% 1,2-hexanediol, and 0.5 wt% p-hydroxyacetophenone.

[0013] Furthermore, this invention discloses the use of the whitening composition described above in the preparation of cosmetics.

[0014] Finally, the present invention also discloses a cosmetic containing 1wt% to 20wt% of the above-mentioned whitening composition.

[0015] Preferably, the whitening composition contains 2.5 wt% to 20 wt% of the above-mentioned whitening composition.

[0016] Preferably, the cosmetic is one of toner, lotion, cream, serum, mask, cleanser, or shower gel.

[0017] Compared with the prior art, the beneficial effects of the present invention are: The whitening composition prepared by this invention comprises coix seed fermentation broth, peony extract combination factor, 4-butylresorcinol solution and zinc gluconate. Through the synergistic effect among the four components, it can effectively inhibit the activity of tyrosinase and effectively inhibit the synthesis of melanin in cells, thus exhibiting good whitening effects. Attached Figure Description

[0018] Figure 1 This is a bar chart showing the effect of different concentrations of the test samples in Example 1 on tyrosinase activity; Figure 2 Microscopic images showing the effect of different concentrations of the test samples in Example 1 on melanin synthesis in B16 cells; Figure 3 This is a bar chart showing the effect of different concentrations of the test samples in Example 1 on melanin synthesis in B16 cells. Detailed Implementation

[0019] The technical solution of the present invention will be clearly and completely described below with reference to the embodiments of the present invention. Obviously, the described embodiments are only some embodiments of the present invention, and not all embodiments. Based on the embodiments of the present invention, all other embodiments obtained by those skilled in the art without creative effort are within the scope of protection of the present invention. It should be noted that, where specific conditions are not specified in the embodiments, conventional conditions or conditions recommended by the manufacturer shall be followed. Reagents or instruments whose manufacturers are not specified are all conventional products that can be purchased commercially.

[0020] Material Commodity Information: Coix seed fermentation broth: purchased from Guangzhou Jikemeichuang Life Science Co., Ltd.; Peony extract combination factor: purchased from Shanghai Ruixi Industrial Co., Ltd.; 4-Butylresorcinol: purchased from Youyan Biotechnology (Huzhou) Co., Ltd.; Decarboxylated carnosine hydrochloride: purchased from Guangzhou Best Chemical Co., Ltd.; Polygonatum extract combination factors: purchased from Ruixi (Guangzhou) Trading Co., Ltd.; Zinc gluconate: purchased from Zhengzhou Ruipu Bioengineering Co., Ltd.

[0021] In this invention, unless otherwise specified, the term "Sanmuxin" refers to the trade name of the whitening composition provided in this application.

[0022] The components of the coix seed fermentation broth, peony extract combination factor, 4-butylresorcinol solution, and polygonatum extract combination factor used in the following examples are shown in Tables 1 to 4.

[0023] Table 1. Composition of Coix Seed Fermentation Broth

[0024] Table 2. Components of Peony Extract Combination Factors

[0025] Table 3. Components of 4-Butylresorcinol Solution

[0026] Table 4. Composition of Polygonatum extract combination factors

[0027] Example 1 This embodiment provides a whitening composition, which, based on a total mass of 100 parts, includes the following components and contents: 20 parts of coix seed fermentation broth, 10 parts of peony extract combination factor, 30 parts of 4-butylresorcinol solution, 5 parts of zinc gluconate, 29 parts of water, 5 parts of butylene glycol, 0.5 parts of 1,2-hexanediol, and 0.5 parts of p-hydroxyacetophenone.

[0028] Example 2

[0029] This embodiment provides a whitening composition, which, based on a total mass of 100 parts, includes the following components and contents: 16 parts of coix seed fermentation broth, 12 parts of peony extract combination factor, 38 parts of 4-butylresorcinol solution, 2 parts of zinc gluconate, 25 parts of water, 6 parts of butylene glycol, 0.4 parts of 1,2-hexanediol, and 0.6 parts of p-hydroxyacetophenone.

[0030] Example 3

[0031] This embodiment provides a whitening composition, which, based on a total mass of 100 parts, includes the following components and contents: 24 parts of coix seed fermentation broth, 8 parts of peony extract combination factor, 22 parts of 4-butylresorcinol solution, 8 parts of zinc gluconate, 33 parts of water, 4 parts of butylene glycol, 0.6 parts of 1,2-hexanediol, and 0.4 parts of p-hydroxyacetophenone.

[0032] Example 4

[0033] This embodiment provides a whitening composition, which, based on a total mass of 100 parts, includes the following components and contents: 22 parts of coix seed fermentation broth, 11 parts of peony extract combination factor, 25 parts of 4-butylresorcinol solution, 4 parts of zinc gluconate, 31 parts of water, 6 parts of butylene glycol, 0.6 parts of 1,2-hexanediol, and 0.4 parts of p-hydroxyacetophenone.

[0034] Example 5

[0035] This embodiment provides a whitening composition, which, based on a total mass of 100 parts, includes the following components and contents: 20 parts of coix seed fermentation broth, 10 parts of peony extract combination factor, 30 parts of 4-butylresorcinol solution, 1.5 parts of decarboxylated carnosine hydrochloride, 5 parts of zinc gluconate, 27.5 parts of water, 5 parts of butylene glycol, 0.5 parts of 1,2-hexanediol, and 0.5 parts of p-hydroxyacetophenone.

[0036] Example 6

[0037] This embodiment provides a whitening composition, which, based on a total mass of 100 parts, includes the following components and contents: 20 parts of coix seed fermentation broth, 10 parts of peony extract combination factor, 30 parts of 4-butylresorcinol solution, 1.5 parts of polygonatum extract combination factor, 5 parts of zinc gluconate, 27.5 parts of water, 5 parts of butylene glycol, 0.5 parts of 1,2-hexanediol, and 0.5 parts of p-hydroxyacetophenone.

[0038] Example 7

[0039] This embodiment provides a whitening composition, which, based on a total mass of 100 parts, includes the following components and contents: 20 parts of coix seed fermentation broth, 10 parts of peony extract combination factor, 30 parts of 4-butylresorcinol solution, 0.75 parts of decarboxylated carnosine hydrochloride, 0.75 parts of polygonatum extract combination factor, 5 parts of zinc gluconate, 27.5 parts of water, 5 parts of butylene glycol, 0.5 parts of 1,2-hexanediol, and 0.5 parts of p-hydroxyacetophenone.

[0040] Comparative Examples 1-4 Comparative Examples 1-4 provide a whitening composition comprising the components and parts by mass as shown in Table 5.

[0041] Table 5 Component Table Job's tears fermentation liquid Peony extract combination factor 4-Butylresorcinol solution Zinc gluconate water Butylene glycol 1,2-Hexanediol p-Hydroxyacetophenone Total number of copies Comparative Example 1 0 15 45 5 29 5 0.5 0.5 100 Comparative Example 2 23 0 37 5 29 5 0.5 0.5 100 Comparative Example 3 40 20 0 5 29 5 0.5 0.5 100 Comparative Example 4 20 10 30 0 34 5 0.5 0.5 100 The preparation methods of the whitening compositions in each embodiment and comparative example are as follows: Add each component to water in the specified proportions, dissolve at 25°C, and mix thoroughly to obtain the whitening composition.

[0042] Performance testing 1. Experimental Principle In the biosynthesis of melanin in the skin, tyrosinase is a key enzyme that acts on tyrosine, which spontaneously undergoes a series of reactions to ultimately form melanin. Tyrosinase catalyzes the production of melanin from tyrosine in a pH 6.8 buffer solution, and its absorbance can be measured at 450 nm. Raw materials that inhibit tyrosinase activity can reduce the catalytic effect of tyrosinase, thereby lowering the absorbance. The inhibitory effect of the sample on tyrosinase activity can be assessed based on changes in absorbance. Melanin production by melanocytes in the skin is the main cause of skin darkening and pigmentation. Therefore, this experiment uses tyrosinase and melanocytes as testing tools, and evaluates the skin-whitening efficacy of the samples by measuring changes in tyrosinase activity and melanin content after drug treatment.

[0043] 2. Equipment and materials 2.1 Equipment: 37℃ constant temperature incubator, multi-functional microplate reader (TECAN, SPARK), microscope (Olympus); 2.2 Cell line: B16 (mouse melanoma cells); 2.3 Reagents: Tyrosinase (Merck), L-tyrosine (Merck), kojic acid (purity ≥98.5%, source leaf), melanin staining kit (ferrous sulfate method) (Solepro), DMEM high glucose medium containing 10% FBS (complete medium).

[0044] 3. Sample processing Test sample group: The whitening composition samples prepared in Examples 1 to 7 and Comparative Examples 1 to 4 were filtered through a 0.22um filter membrane, and the filtrate was collected as the test sample mother liquor and diluted with purified water to a volume concentration of 1.0%, 1.5%, 2.5%, 5.0%, 7.5%, and 10.0%.

[0045] Blank control group: pure water; Positive control group: kojic acid (100 μg / mL).

[0046] 4. Test Methods 4.1 Inhibition of tyrosinase activity Add 50 μL of different concentrations of test sample diluent and 20 μL of 200 U / mL tyrosinase solution to a 96-well plate, vortex to mix, and incubate at 37 °C for 10 min. Then add 130 μL of L-tyrosine solution, vortex to mix, and incubate at 37 °C for 15 min. Measure the OD450 nm value and calculate the tyrosinase inhibition rate according to Formula 1.

[0047] Formula 1:

[0048] In the formula: T: Absorbance of the sample tube, i.e., the absorbance of the solution after the sample reacts with tyrosinase; T0: Sample background absorbance; C: The average of three absorbance readings from the enzyme reaction tube, i.e., the absorbance of the tyrosinase and dopa reaction without the addition of sample; C0: Solvent background absorbance.

[0049] 4.1.1 Test Results The results of tyrosinase inhibition rate are as follows: Figure 1 As shown in Tables 6 and 7.

[0050] Table 6 Tyrosinase Inhibition Rate

[0051] pass Figure 1As shown in Table 6, the inhibition rates of tyrosinase activity by using 1.0%, 1.5%, 2.5%, 5.0%, 7.5%, and 10.0% of the Sanmu core (Example 1) were 8.23%, 11.36%, 30.22%, 45.76%, 78.27%, and 83.41%, respectively, which were significantly different from the blank control group, indicating that the Sanmu core (Example 1) has a significant inhibitory effect on tyrosinase activity.

[0052] Similarly, it can be seen that the whitening composition provided in Example 1 has the highest tyrosinase inhibition rate when its content is 10.0%. Therefore, the tyrosinase activity inhibition test was performed on the compositions provided in Examples 2-7 and Comparative Examples 1-4 with a volume concentration of 10.0%, and the tyrosinase inhibition rates are shown in Table 7.

[0053] Table 7. Tyrosinase Inhibition Rate Data sample Tyrosinase inhibition rate (%) Example 2 82.65 Example 3 84.17 Example 4 83.42 Example 5 85.67 Example 6 85.24 Example 7 89.49 Comparative Example 1 60.38 Comparative Example 2 71.94 Comparative Example 3 68.75 Comparative Example 4 58.96 As can be seen from the data in Tables 6 and 7, the Sanmu core has a significant inhibitory effect on tyrosinase activity, especially in Example 7, which has an excellent whitening effect.

[0054] 4.2 B16 cell melanin synthesis inhibition assay 4.2.1 Cell Preparation B16 cells were cultured in a complete culture at 37°C with 5% CO2. 2 Cultured cells, maintaining a concentration of 1.0 × 10⁶ cells per mL. 5 ~5.0×10 6 Individual samples were passaged and used for biological activity assays 24–36 hours later.

[0055] 4.2.2 Screening for safe concentrations of test substances Cells were seeded at 3500 cells / well in 96-well cell culture plates and cultured adherently for 24 h. The old culture medium was removed, and complete culture medium containing different concentrations of the test substance was added and incubated for 24 h. 0.5% MTT was added and the plates were incubated at 37°C with 5% CO2. 2 Incubate for 4 hours. Discard the culture plate liquid, add DMSO (dimethyl sulfoxide), and measure the absorbance at a wavelength of 490 nm using a microplate reader. Record the measurement results.

[0056] 4.2.3 Efficacy Testing Cell plating: Cells were resuspended in fresh complete culture medium and seeded at 2500 cells / well into 6-well cell culture plates and cultured adherently for 24 hours.

[0057] Sample preparation: Select a safe concentration of the test substance that is non-toxic to cells, and set up a blank control group, a test sample group, and a positive control group as follows: Blank control group: pure water; Test sample group: The whitening composition samples prepared in Examples 1-7 and Comparative Examples 1-4 were filtered through a 0.22 μm filter membrane, and the filtrate was collected as the mother liquor of the test sample. The mother liquor was then diluted with purified water to a volume concentration of 0.005%, 0.01%, 0.02%, and 0.03%, respectively. Positive control group: kojic acid (50 μg / mL).

[0058] First medium change: Discard the old culture medium, add the prepared solutions of each group to a 6-well cell culture plate, and continue culturing.

[0059] Second medium change: 48 hours after the first medium change, the cell culture medium was replaced with one containing the blank control group, the test sample group (0.005%, 0.01%, 0.02%, 0.03%), and the positive control group, and culture continued.

[0060] Third medium change: 72 hours after the second medium change, replace with new cell culture medium and continue culturing for 48-72 hours (until the cell fusion rate reaches over 90%).

[0061] Melanin content detection: Staining was performed according to the instructions of the melanin staining kit (ferrous sulfate method). Observation and photography were conducted under a microscope. Figure 2 As shown, statistical analysis was then performed.

[0062] 4.2.4 Test Results B16 cell melanin synthesis inhibition rate as follows Figure 3 As shown in Tables 8 and 9.

[0063] Table 8. Inhibition rate of melanin synthesis in B16 cells

[0064] pass Figure 2 , Figure 3 As shown in Table 8, compared with the blank control group, the melanin content and melanin synthesis inhibition of B16 cells were significantly reduced after treatment with 50 μg / mL kojic acid (positive control group), proving that the experimental system was valid.

[0065] Melanin staining showed that treatment with 0.005%, 0.01%, 0.02%, and 0.03% of the three-component micrograft (Example 1) significantly reduced the melanin content of B16 cells. Using 0.005%, 0.01%, 0.02%, and 0.03% of the Sanmu core (Example 1), the inhibition rates of melanin synthesis in B16 cells were 65.46%, 75.85%, 76.51%, and 79.98%, respectively, which were significantly different from the blank control group (p < 0.01), indicating that the Sanmu core (Example 1) has a significant inhibitory effect on melanin synthesis in B16 cells.

[0066] Similarly, it can be seen that when the whitening composition provided in Example 1 has a content of 0.03%, its B16 cell melanin synthesis inhibition rate is the highest. Therefore, the compositions provided in Examples 2-7 and Comparative Examples 1-4 with a volume concentration of 0.03% were tested for B16 cell melanin synthesis inhibition, and their B16 cell melanin synthesis inhibition rates are shown in Table 9.

[0067] Table 9. Data on Melanin Synthesis Inhibition Rate sample Melanin synthesis inhibition rate (%) Example 2 79.98 Example 3 81.64 Example 4 80.93 Example 5 83.15 Example 6 84.23 Example 7 88.36 Comparative Example 1 63.53 Comparative Example 2 66.17 Comparative Example 3 63.96 Comparative Example 4 61.22 In summary, the three-mu core has a significant inhibitory effect on melanin synthesis in B16 cells.

[0068] Application Example 1 This embodiment provides a toner composed of 1 wt% of the whitening composition described in Example 1 and 99 wt% of a conventional toner base.

[0069] Application Example 2 This embodiment provides an emulsion consisting of 6 wt% of the antioxidant repair composition described in Example 2 and 94 wt% of a conventional emulsion matrix.

[0070] Application Example 3 This embodiment provides a serum composed of 20 wt% of the antioxidant repair composition described in Example 3 and 80 wt% of a conventional serum base.

[0071] Application Example 4 This embodiment provides a face mask consisting of 3.5 wt% of the antioxidant repair composition described in Example 4 and 96.5 wt% of a conventional face mask base.

[0072] It will be apparent to those skilled in the art that the present invention is not limited to the details of the exemplary embodiments described above, and that the invention can be implemented in other specific forms without departing from its spirit or essential characteristics. Therefore, the embodiments should be considered in all respects as exemplary and non-limiting, and the scope of the invention is defined by the appended claims rather than the foregoing description. Thus, all variations falling within the meaning and scope of equivalents of the claims are intended to be included within the present invention. No reference numerals in the claims should be construed as limiting the scope of the claims.

Claims

1. A whitening composition, characterized in that, Based on mass parts, it contains the following active components: 16-24 parts of coix seed fermentation broth, 8-12 parts of peony extract combination factor, 22-38 parts of 4-butylresorcinol solution, and 2-8 parts of zinc gluconate.

2. The whitening composition according to claim 1, characterized in that, The whitening composition further comprises, by weight, 0.1 to 1.5 parts of decarboxylated carnosine hydrochloride and 0.05 to 2.5 parts of Polygonatum sibiricum extract combination factor.

3. The whitening composition according to claim 1, characterized in that, The whitening composition, by weight, also includes 21-32.75 parts water, 4-6 parts butylene glycol, 0.4-0.6 parts 1,2-hexanediol, and 0.4-0.6 parts p-hydroxyacetophenone.

4. The whitening composition according to claim 1, characterized in that, The coix seed fermentation broth, based on a total mass of 100%, comprises the following components and their mass percentages: 30 wt% coix seed extract, 68 wt% glycerol, and 2 wt% 1,2-hexanediol.

5. The whitening composition according to claim 1, characterized in that, The peony extract combination factor, based on a total mass of 100%, includes the following components and their mass percentages: 30 wt% peony root extract, 30 wt% butylene glycol, 39 wt% water, 0.5 wt% 1,2-hexanediol, and 0.5 wt% p-hydroxyacetophenone.

6. The whitening composition according to claim 1, characterized in that, The 4-butylresorcinol solution, by total mass of 100%, comprises the following components and their mass percentages: 10 wt% 4-butylresorcinol, 40 wt% hydroxypropyl cyclodextrin, 44 wt% water, 5 wt% 1,3-propanediol, 0.5 wt% 1,2-hexanediol, and 0.5 wt% p-hydroxyacetophenone.

7. Use of the whitening composition according to any one of claims 1 to 6 in the preparation of cosmetics.

8. A cosmetic product, characterized in that, Containing 1wt% to 20wt% of the whitening composition as described in any one of claims 1 to 6.

9. The cosmetic product according to claim 8, characterized in that, Contains 3.5wt% to 20wt% of the whitening composition as described in any one of claims 1 to 6.

10. The cosmetic product according to claim 8, characterized in that, The cosmetic product is one of the following: toner, lotion, face cream, serum, face mask, facial cleanser, or shower gel.

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