Whitening and anti-inflammatory composition and preparation method thereof

Abstract

The invention discloses a whitening and anti-inflammatory composition and a preparation method thereof. The whitening and anti-inflammatory composition is prepared from the following raw materials in percentage by mass: 3 to 10 percent of sodium alginate, 2 to 8 percent of nicotinamide, 4 to 10 percent of vitamin B1, 1 to 6 percent of tranexamic acid, 1 to 3 percent of taurine and 3 to 10 percent of ceramide. By compounding the sodium alginate, the nicotinamide, the vitamin B1, the tranexamic acid, the taurine and the ceramide, the synergistic interaction among all the components is fully exerted, the antibacterial and anti-inflammatory effects can be remarkably improved, a good whitening effect can be achieved, and the whitening and anti-inflammatory composition can be used in cosmetics and has a good application prospect. The composition has the advantages of low dosage, safety, effectiveness, naturalness, low irritation and the like.

Description

Technical Field

[0001] The present invention belongs to the field of cosmetics, and particularly relates to a whitening and anti-inflammatory composition and a preparation method thereof. Background Art

[0002] The skin is the largest organ of the human body and the part where the human body directly contacts the environment. The skin is mainly divided into the epidermis, dermis and subcutaneous fat from the outside to the inside. In recent years, with the improvement of living standards, people have paid more and more attention to skin care, the use of cosmetics has become more and more frequent, and people have also paid more and more attention to skin whitening.

[0003] Raw materials with whitening effects are an indispensable type of ingredient in cosmetics. Selecting efficient and safe raw materials with whitening effects is one of the keys to the development of cosmetic formulations. However, existing raw materials with whitening effects are difficult to achieve good anti-inflammatory effects while maintaining good whitening effects. Therefore, the importance of developing a composition with both good whitening and anti-inflammatory effects has become increasingly prominent. Summary of the Invention

[0004] In view of the above deficiencies in the prior art, the present invention combines sodium alginate, niacinamide, vitamin B1, tranexamic acid, taurine and ceramide, gives full play to the synergistic effect between the components, can significantly improve the antibacterial and anti-inflammatory effects, and can achieve good whitening effects. The whitening and anti-inflammatory composition can be used in cosmetics and has the advantages of low dosage, safety, effectiveness, natural low irritation, etc.

[0005] The purpose of the present invention is to provide a whitening and anti-inflammatory composition, comprising raw materials in the following mass percentages: 3-10% of sodium alginate, 2-8% of niacinamide, 4-10% of vitamin B1, 1-6% of tranexamic acid, 1-3% of taurine and 3-10% of ceramide.

[0006] In some embodiments of the present invention, the ceramide is selected from at least one of ceramide type I, ceramide type III and ceramide type VI.

[0007] In some embodiments of the present invention, the whitening and anti-inflammatory composition further comprises 5-11% of non-crosslinked hyaluronic acid, 3-10% of vitamin B3 and 5-12% of compound amino acids.

[0008] In some embodiments of the present invention, the compound amino acids are selected from at least two of cysteine, phenylalanine, alanine, lysine acetate, methionine, proline, sodium bisulfite, glutamic acid, arginine, tyrosine, leucine, tryptophan, serine, threonine, aspartic acid, valine, isoleucine, histidine.

[0009] In some embodiments of the present invention, the whitening and anti-inflammatory composition further comprises 40-70% of a solvent.

[0010] In some embodiments of the present invention, the solvent is selected from at least one of 1,2 - propylene glycol, 1,3 - propylene glycol, 1,2 - butylene glycol, 1,3 - butylene glycol, 1,4 - butylene glycol, 1,2 - pentylene glycol, 1,5 - pentylene glycol, isopentylene glycol, isohexylene glycol, 1,2 - hexylene glycol, dipropylene glycol, water, glycerol, and methyl propylene glycol.

[0011] Another object of the present invention is to provide the application of the whitening and anti - inflammatory composition in the preparation of cosmetics. The cosmetics contain the whitening and anti - inflammatory composition, and the cosmetics include at least one of cream, foundation cream, concealer, lotion, facial cleanser, essence, toner, perfume, rouge, eyeshadow, lipstick, and blush.

[0012] Another object of the present invention is to provide the application of the whitening and anti - inflammatory composition in the preparation of cosmetics. The cosmetics contain the whitening and anti - inflammatory composition, and the cosmetics include at least one of facial mask liquid, essence, liquid foundation, toner, and makeup remover.

[0013] In some embodiments of the present invention, based on the mass percentage, the dosage of the whitening and anti - inflammatory composition is 0.5 - 5% of the cosmetics.

[0014] In some embodiments of the present invention, based on the mass percentage, the dosage of the whitening and anti - inflammatory composition is 0.5 - 5% of the cosmetics.

[0015] Compared with the prior art, the present invention has the following beneficial effects: By compounding sodium alginate, niacinamide, vitamin B1, tranexamic acid, taurine, and ceramide, the present invention gives full play to the synergistic effect between the components, can significantly improve the antibacterial and anti - inflammatory effects, and can achieve good whitening efficacy. The whitening and anti - inflammatory composition can be used in cosmetics and has the advantages of low dosage, safety and effectiveness, and natural low irritation. Specific Embodiments

[0016] In order to enable those skilled in the art to better understand the technical solutions in the present invention, the technical solutions of the present invention will be clearly and completely described below in conjunction with the embodiments of the present invention. Obviously, the described embodiments are only a part of the embodiments of the present invention, rather than all the embodiments. Based on the embodiments of the present invention, all other embodiments obtained by those of ordinary skill in the art without creative work shall fall within the protection scope of the present invention.

[0017] Preparation of the whitening and anti - inflammatory composition: Table 1. Raw material composition of the whitening and anti - inflammatory composition.

[0018]

[0019] According to the raw materials and mass percentages in Table 1, add the above raw materials into a 250 mL flask equipped with a thermometer and a stirrer, heat up to 40 °C, stir for 30 - 50 min until completely mixed evenly, and after cooling to room temperature, filter to remove insoluble impurities to obtain the whitening and anti-inflammatory composition.

[0020] Minimum inhibitory concentration test: Test strains: The bacteria used in this experiment are Staphylococcus aureus ATCC6538, Escherichia coli ATCC8739, and Pseudomonas aeruginosa ATCC9027; the fungus is Aspergillus niger ATCC16404, all of which are sourced from the Guangdong Microbial Culture Collection Center.

[0021] Test media: Malt extract broth medium, nutrient broth medium.

[0022] Preparation of bacterial suspension: (1) Preparation of bacterial suspension: Add sterile 0.9% sodium chloride aqueous solution to the bacterial strain slant, wash out a certain amount of bacteria, add the washed bacteria to a sterile container with the same size as the No. 2 turbidity standard tube, and then add sterile 0.9% sodium chloride aqueous solution to the sterile container to dilute the bacteria until the turbidity is the same as that of the No. 2 turbidity standard tube (corresponding approximate bacterial concentration: 6×10 8 cfu / ml).

[0023] (2) Preparation of Aspergillus niger suspension: Use sterile 0.9% sodium chloride aqueous solution containing 0.05% Tween - 80 to elute Aspergillus niger spores to prepare an Aspergillus niger spore suspension, filter the Aspergillus niger spore suspension to remove mycelia, and make the Aspergillus niger spore suspension contain about 10 8 cfu / ml, for standby.

[0024] Test operation steps: S1. Prepare test solutions with different concentrations from the whitening and anti - inflammatory compositions of Examples 1 - 5 and Comparative Examples 1 - 8 respectively using distilled water. Take 2.5 ml of each diluted test solution and add it to a test tube containing 2.5 ml of double - concentration nutrient broth.

[0025] S2. Take 0.1 ml of bacterial suspension with a bacterial content of about 10 8 cfu / ml and inoculate it into test tubes containing the whitening and anti - inflammatory composition solutions of Examples 1 - 5 and Comparative Examples 1 - 8 in nutrient broth respectively as test group samples.

[0026] S3. Inoculate test tubes containing nutrient broth without the whitening and anti - inflammatory composition in the same way as a positive control group sample.

[0027] S4. Take 2 test tubes containing nutrient broth as samples for the negative control group.

[0028] S5. Place the test group samples, positive control group samples, and negative control group samples in an incubator at 37 °C and incubate for 48 h, then observe the results.

[0029] S6. During the experiment, the test bacterial suspension should be subjected to viable bacteria culture counting, and its working concentration should be 5×10 5 cfu / ml to 5×10 6 cfu / ml.

[0030] Judgment criteria: When there is bacterial growth (turbidity) in the positive control tube, no bacterial growth (transparent) in the negative control tube, and the working concentration of the test bacterial suspension is 5×10 5 cfu / ml to 5×10 6 cfu / ml, the antibacterial (or inhibitory) agent concentration corresponding to the highest dilution at which there is no bacterial growth in the test group is the minimum inhibitory concentration of the sample against the test bacteria.

[0031] Table 2. Results of minimum inhibitory concentration determination.

[0032]

[0033] As can be seen from Table 2, there is an obvious synergistic antibacterial effect among sodium alginate, niacinamide, vitamin B1, tranexamic acid, taurine, and ceramide.

[0034] Anti-inflammatory efficacy test: Test method: Refer to the test method for measuring the content of in vitro IL-1β inflammatory factor in the anti-inflammatory efficacy test of cosmetics - lipopolysaccharide-induced macrophage cell line inflammatory cell model in T / SHRH 033-2020.

[0035] Table 3. Test substance working solution.

[0036]

[0037] After the test substance working solution is prepared, it is placed in an incubator at 37 °C ± 1 °C with a CO2 concentration of 5% ± 1% for 24 h, then a sufficient amount of cell supernatant is collected, and the content of the inflammatory factor is measured according to the instructions of the ELISA kit (Elisa Kit CUSABIO).

[0038] The test is valid if the inflammatory factor in the positive control group is ≥ 25%.

[0039] Calculate the inhibition rate according to formula (1): Inhibition rate (%) = (1 - T / C) × 100% Formula (1) Where: T—the average value of the inflammatory factor content of the test substance; C—the average content of inflammatory factors in the negative control

[0040] Table 4. Test results of anti-inflammatory ability

[0041]

[0042] As can be seen from the results in Table 4, the whitening and anti-inflammatory composition of the present invention has the effect of synergistically inhibiting IL-1β

[0043] Test of the inhibition rate of tyrosinase activity Test method: Refer to the test method for the inhibition of tyrosinase activity by cosmetic raw materials (in vitro method) in T / GDCA 006-2021

[0044] Preparation of solutions (1) Preparation of tyrosinase solution: Dissolve tyrosinase with PBS buffer to 500 U / ml, dispense, and store at -20°C to avoid secondary freezing and thawing

[0045] (2) Preparation of L-tyrosine solution: Dissolve 0.025 g of L-tyrosine with an appropriate amount of PBS buffer solution, sonicate to fully dissolve it, and then make up the volume to 50 mL with PBS buffer solution to prepare a 0.5 g / L L-tyrosine solution for immediate use

[0046] (3) Preparation of positive control solution: Dilute kojic acid with ultrapure water to a series of mass concentration gradient solutions of 0.040 g / L, 0.020 g / L, 0.010 g / L, 0.008 g / L, 0.005 g / L, 0.002 g / L, and 0.001 g / L

[0047] (4) Preparation of sample solution: Use PBS buffer to prepare the whitening and anti-inflammatory compositions of Examples 1-3 and Comparative Examples 9-12 into a 1% concentration to be tested

[0048] Test grouping In the test, it is divided into a solvent background group (T a ), a solvent reaction well group (T b ), a sample background group (T c ), and a sample reaction group (T d )). The solvent background group (T a ) is composed of solvent, PBS buffer solution, and tyrosinase solution; the solvent reaction well group (T b ) is composed of L-tyrosine solution, solvent, PBS buffer solution, and tyrosinase solution; the sample background group (T c ) is composed of sample solution, PBS buffer solution, and tyrosinase solution; the sample reaction group (T dwere L-tyrosine solution, sample solution, PBS buffer solution, and tyrosinase solution. There were three replicate wells in each group.

[0049] Test procedure: According to the reagent addition amounts in Table 5, add L-tyrosine solution, sample solution / solvent, and PBS buffer solution to each well in sequence. Incubate with constant shaking in a full-wavelength microplate reader at 37 °C for 5 min, and continue to incubate for 7 min. That is, after sample addition, incubate for a total of 12 min under the constant temperature condition of 37 °C. At the end of the incubation, add 20 μL of tyrosinase solution to each well in sequence, mix well at 37 °C and react for 5 min ± 5 s, then take readings and measure at a wavelength of 475 nm.

[0050] Table 5. Reagent addition table for the inhibitory ability of tyrosinase activity

[0051] Data processing: Calculation of the inhibition rate of tyrosinase activity:

[0052] In the above formula: A a ——Average absorbance of the solvent blank well; A b ——Absorbance of the solvent reaction well; A c ——Average absorbance of the sample blank well; A d ——Absorbance of the sample reaction well.

[0053] Half maximal inhibitory concentration (IC 50 value) of the positive control: Using the positive control concentration as the abscissa and the corresponding inhibition rate of tyrosinase activity as the ordinate, plot a curve graph, fit a linear regression equation, (R 2 ≥0.900) and calculate the positive control concentration corresponding to an inhibition rate of tyrosinase activity of 50% according to the equation. The IC 50 of the positive control kojic acid should be in the range of 0.005 g / L to 0.01 g / L, then this test is considered valid.

[0054] Table 6. Test results of the inhibition rate of tyrosinase activity.

[0055]

[0056] From the results in Table 6, it can be seen that there is a synergistic effect in inhibiting the activity of tyrosinase among non-crosslinked hyaluronic acid, vitamin B3, niacinamide, and tranexamic acid.

[0057] Human skin patch test: The whitening and anti-inflammatory compositions prepared in Examples 1-5 were respectively used to prepare facial mask liquids according to the formulation in Table 7, and the facial mask liquids of Examples 6-10 were obtained. The irritancy and safety of the facial mask liquids of Examples 6-10 were detected. The formulation and production process of the facial mask liquids are shown in Table 7.

[0058] Table 7. Composition table and production process of the facial mask liquid.

[0059]

[0060] Test method: Refer to Section 2, Article 6.1 of Chapter 7 of the "Technical Specifications for Cosmetics Safety" (2015 Edition), Skin Closed Patch Test.

[0061] Weigh 0.02 mL of the facial mask liquids of Examples 6-10 into the patch test device respectively. At the same time, set up a blank control group, and the control is the diluent of this cosmetic. Select 250 healthy volunteers and divide them into 5 groups, with 50 volunteers in each group, aged 18-24 years old and without a history of allergies. After cleaning the inner side of the forearm of the subjects, take 0.02 mL of the facial mask liquid and add it to the filter paper attached to the patch test device. Apply the patch test device to the inner side of the forearm of the subjects with non-irritating tape. After pasting, gently press it with your finger to make it evenly adhere to the skin and keep it for 24 h. The subjects should keep the patch area dry within 24 h and avoid strenuous exercise, scratching the patch area, long-term sunlight exposure, etc. After 24 h, remove the test device and make marks. Observe the skin reactions according to the criteria in Table 8 at 30 min, 24 h and 48 h after removing the test device of the test substance, and record the observation results.

[0062] Table 8. Grading criteria for skin reactions in the skin closed patch test

[0063] Table 9. Results of the skin patch test

[0064] As can be seen from Table 9, the facial mask liquids of Examples 6-10 of the present invention have low irritancy and high safety.

[0065] Finally, it should be noted that the above examples are only used to illustrate the technical solutions of the present invention and not to limit it. Although the present invention has been described in detail with reference to the above examples, those of ordinary skill in the art should understand that after reading the specification of this application, they can still modify the specific implementation manners of the present invention or make equivalent replacements, but these modifications or changes are all within the scope of protection of the pending claims of this invention application.

Claims

1. A whitening and anti-inflammatory composition, characterized in that: The invention comprises the following raw materials in percentage by weight: 3-10% sodium alginate, 2-8% nicotinamide, 4-10% vitamin B1, 1-6% tranexamic acid, 1-3% taurine and 3-10% ceramide.

2. The whitening and anti-inflammatory composition according to claim 1, characterized in that: The ceramide is selected from at least one of type I ceramide, type III ceramide and type VI ceramide.

3. The whitening and anti-inflammatory composition according to claim 1, characterized in that: The whitening and anti-inflammatory composition further comprises 5-11% of non-cross-linked hyaluronic acid, 3-10% of vitamin B3 and 5-12% of complex amino acids.

4. The whitening and anti-inflammatory composition according to claim 3, characterized in that: The composite amino acids are selected from at least two of cysteine, phenylalanine, alanine, lysine acetate, methionine, proline, sodium bisulfite, glutamic acid, arginine, tyrosine, leucine, tryptophan, serine, threonine, aspartic acid, valine, isoleucine, and histidine.

5. The whitening and anti-inflammatory composition according to claim 1, characterized in that: The whitening and anti-inflammatory composition further comprises 40-70% of a solvent.

6. The whitening and anti-inflammatory composition according to claim 1, characterized in that: The solvent is selected from at least one of 1,2-propylene glycol, 1,3-propylene glycol, 1,2-butylene glycol, 1,3-butylene glycol, 1,4-butylene glycol, 1,2-pentanediol, 1,5-pentanediol, isopentyl glycol, isohexylene glycol, 1,2-hexanediol, dipropylene glycol, water, glycerol, and methylpropylene glycol.

7. Use of the whitening and anti-inflammatory composition according to any one of claims 1 to 6 in the preparation of cosmetics, characterized in that: The cosmetics contain the whitening and anti-inflammatory composition, and the cosmetics include at least one of cream, foundation cream, concealer cream, lotion, cleanser, stock solution, toner, perfume, rouge, eye shadow, lipstick, and blush.

8. Use of the whitening and anti-inflammatory composition according to any one of claims 1 to 6 in the preparation of cosmetics, characterized in that: The cosmetic contains the whitening and anti-inflammatory composition, and the cosmetic comprises at least one of a facial mask liquid, an essence liquid, a foundation liquid, a toner, and a makeup remover.

9. The use according to claim 7, characterized in that Calculated by mass percentage, the amount of the whitening and anti-inflammatory composition is 0.5-5% of the cosmetics.

10. The use according to claim 8, characterized in that Calculated by mass percentage, the amount of the whitening and anti-inflammatory composition is 0.5-5% of the cosmetics.

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