A whitening and repairing composition suitable for sensitive skin and application thereof

Abstract

This invention relates to a whitening and repairing composition suitable for sensitive skin and its application, belonging to the field of cosmetic technology. The whitening and repairing composition includes Bordeaux leaf extract, thyme extract, Bletilla striata root extract, and Saussurea involucrata extract. The four components in the composition are rationally combined, exhibiting significant tyrosinase inhibitory activity, thus blocking the melanin synthesis pathway. Human efficacy tests show that the whitening and repairing composition can significantly increase ITA° and decrease skin TEWL value, indicating its whitening, pigmentation-fading, and skin-brightening effects, as well as reducing transepidermal water loss and effectively repairing the skin barrier. Simultaneously, the whitening and repairing composition can significantly improve lactic acid irritation, providing excellent soothing and calming effects on the skin.

Description

Technical Field

[0001] This invention relates to the field of cosmetic technology, and in particular to a whitening and repairing composition suitable for sensitive skin and its application. Background Technology

[0002] Skin whitening is a research hotspot in the cosmetics industry and one of the core demands of consumers. Melanin synthesis and deposition are the main factors determining skin color, and the process involves multiple biological steps: Within melanocytes, melanocyte-stimulating hormone (α-MSH) binds to the melanocortin 1 receptor (MC1R), activating adenylate cyclase, which increases the level of the second messenger cAMP, thereby upregulating the expression of tyrosinase genes and ultimately promoting melanin synthesis. The synthesized melanin is loaded into melanosomes and transported from the melanocyte cell body to the dendritic terminals via a kinesin-mediated transport mechanism, where it is then taken up by adjacent keratinocytes and finally shed with the stratum corneum or deposited on the skin surface. Therefore, inhibiting tyrosinase activity, blocking melanin transport, and interfering with upstream signal transduction pathways can all achieve skin whitening effects.

[0003] Currently, commercially available skin-whitening products mainly function through single mechanisms such as inhibiting tyrosinase (e.g., arbutin, kojic acid), blocking melanin transport (e.g., niacinamide), or providing antioxidant effects (e.g., vitamin C). These methods have the following shortcomings: First, their single mechanism of action limits their whitening effect, making it difficult to achieve synergistic inhibition across multiple pathways. Second, traditional whitening ingredients (such as nicotinic acid impurities in high-concentration arbutin and niacinamide) are highly irritating, easily causing redness, stinging, and other discomfort, making them unsuitable for sensitive skin. Third, they lack the ability to regulate the ratio of melanin types (eumelanin and pheomelanin), while glutathione, although capable of achieving this conversion, suffers from poor stability and low transdermal absorption when added directly. Therefore, developing a multi-pathway synergistic whitening composition is of great significance. Summary of the Invention

[0004] The purpose of this invention is to overcome the shortcomings of the prior art and provide a whitening and repairing composition and its application suitable for sensitive skin.

[0005] To achieve the above objectives, the technical solution adopted by the present invention is as follows: In a first aspect, the present invention provides a whitening and repairing composition comprising the following components in parts by weight: 0.01-2 parts of Bordeaux leaf extract, 0.1-5 parts of thyme extract, 0.01-2 parts of Bletilla striata root extract and 0.01-2 parts of snow lotus extract.

[0006] This invention provides a whitening and repairing composition suitable for sensitive skin. The components in the whitening and repairing composition interact with each other to achieve whitening and repairing effects on multiple levels. Alkaloids in Bordeaux leaf extract can inhibit tyrosinase activity, thereby affecting melanin synthesis. Thyme extract can inhibit the expression of melanin-carrier kinase, preventing pigmentation by inhibiting melanin transport to epidermal cells. Biphenyl compounds in Bletilla striata root extract, besides directly inhibiting tyrosinase, also have a significant binding affinity for adenylate cyclase, inhibiting its activity and thus suppressing melanin synthesis through this pathway. Chlorogenic acid and yazolide in snow lotus extract have good tyrosinase inhibitory capabilities, showing potential as skin-whitening and spot-fading skincare ingredients. Furthermore, snow lotus extract can stimulate the synthesis of antioxidants such as glutathione. Glutathione, besides directly inhibiting tyrosinase activity, can also combine with dopaquinone, an intermediate in melanin synthesis, to form cysteine-dopa, converting eumelanin synthesis into pheomelanin synthesis. Snow lotus extract can also scavenge ROS, reducing the oxidative stress on melanin production.

[0007] The rational combination of the four ingredients—Bordeaux leaf extract and snow lotus extract—directly inhibits tyrosinase, while Bletilla striata root extract indirectly inhibits tyrosinase by combining with adenylate cyclase, thus blocking melanin synthesis through dual enzyme activity inhibition. Simultaneously, snow lotus extract promotes glutathione synthesis, converting dark eumelanin into lighter pheomelanin, and scavenges ROS to reduce oxidative stress on melanin synthesis. Thyme extract blocks melanin transport to epidermal cells. These four ingredients act on melanin synthesis, signal transduction, transport, and oxidative stress, respectively, achieving a comprehensive and gentle spot-fading and repairing effect without the use of irritating whitening agents.

[0008] Furthermore, the whitening and repairing composition comprises the following components in parts by weight: 0.1-1 parts Bordeaux leaf extract, 0.5-2 parts European thyme extract, 0.05-0.5 parts Bletilla striata root extract and 0.05-1 parts Saussurea involucrata extract.

[0009] Secondly, this application provides the use of the whitening and repairing composition described in the first aspect in the preparation of cosmetics.

[0010] Furthermore, the cosmetics include any one of toners, creams, lotions, gels, and masks.

[0011] Furthermore, the amount of the whitening and repairing composition added to the cosmetic product is 1wt%-5wt%.

[0012] Thirdly, this application provides a cosmetic product containing the whitening and repairing composition described in the first aspect.

[0013] Furthermore, it also contains excipients acceptable in the cosmetics industry.

[0014] Furthermore, the excipients acceptable in the cosmetic field include at least one of solvents, humectants, pH adjusters, emollients, emulsifiers, thickeners, solubilizers, antioxidants, and fragrances.

[0015] Fourthly, this application provides a whitening and repairing emulsion containing the following components by weight percentage: 1%-5% of the whitening and repairing composition described in the first aspect, 0.05%-1.0% of a thickener, 2%-10% of a moisturizer, 0.01%-0.1% of a chelating agent, 3%-8% of a skin-moisturizing agent, 1%-5% of an emulsifier, 0.1%-4% of an antioxidant, and 0.01%-0.3% of a pH adjuster, with the balance being deionized water.

[0016] Furthermore, the preparation method of the whitening and repairing lotion includes the following steps: S1. Mix and stir a portion of the humectant, thickener, chelating agent and water, heat to 75-85℃, homogenize, and obtain phase A; S2. Mix the emollient and emulsifier, heat to 75-85℃, homogenize, and obtain phase B; S3. Mix the antioxidant and the remaining humectant, heat to 60°C to melt, and obtain phase C; S4. Add phase B to phase A, stir and mix, cool to 60℃, add phase C, stir and mix, then cool to below 45℃, add the whitening and repairing composition and continue stirring, add pH adjuster to adjust pH, discharge to obtain whitening and repairing emulsion.

[0017] Compared with the prior art, the beneficial effects of the present invention are as follows: This invention provides a whitening and repairing composition suitable for sensitive skin, comprising Bordeaux leaf extract, thyme extract, Bletilla striata root extract, and Saussurea involucrata extract. The four components in this composition are rationally combined, exhibiting significant tyrosinase inhibitory activity, thus blocking the melanin synthesis pathway. Human efficacy tests show that this whitening and repairing composition can significantly increase ITA° and decrease skin TEWL values, indicating its whitening, pigmentation-fading, and skin-brightening effects, as well as reducing transepidermal water loss and effectively repairing the skin barrier. Simultaneously, this whitening and repairing composition can significantly improve lactic acid irritation, providing excellent soothing and calming effects on the skin. Detailed Implementation

[0018] To better illustrate the purpose, technical solution, and advantages of the present invention, the present invention will be further described below in conjunction with specific embodiments.

[0019] The ingredients used in the following embodiments are from the following sources: Bordeaux leaf extract was purchased from BASF under the product name BETAPUR® A00067. The thyme extract was purchased from Changsha Xiangbairui Biotechnology Co., Ltd., and its product name is thyme extract. Bletilla striata root extract was purchased from Shaanxi Zelang Biotechnology Co., Ltd., and its product name is Bletilla striata root extract. The snow lotus extract was purchased from Shaanxi Baichuan Biotechnology Co., Ltd., and its product name is Snow Lotus Extract.

[0020] Unless otherwise specified, all other materials and reagents used in the examples are commercially available.

[0021] Examples 1-5 The whitening and repairing compositions of Examples 1-5 were prepared according to the formula shown in Table 1. The preparation method of the whitening and repairing compositions is to weigh the corresponding weight parts of the components and mix them evenly to obtain the whitening and repairing compositions.

[0022] Table 1. Components and Dosage of the Whitening and Repairing Composition

[0023] Note: "-" indicates no addition; the total weight of the compositions prepared in Examples 1-5, Comparative Examples 1-4 and the following comparative examples is the same.

[0024] Comparative Example 5 This comparative example provides a whitening and repairing composition, which differs from Example 1 only in that Bordeaux leaf extract is not added to the composition, but an equal amount of olive leaf extract is used to make up for the missing amount, and the other parameters are the same as those in Example 1.

[0025] Comparative Example 6 This comparative example provides a whitening and repairing composition, which differs from Example 1 only in that the composition does not contain thyme extract, but instead uses an equal amount of oregano extract to make up for its deficiency. All other parameters are the same as in Example 1.

[0026] Comparative Example 7 This comparative example provides a whitening and repairing composition, which differs from Example 1 only in that the composition does not contain Bletilla striata root extract, but instead uses an equal amount of Ampelopsis japonica root extract to make up for the missing amount. All other parameters are the same as in Example 1.

[0027] Comparative Example 8 This comparative example provides a whitening and repairing composition, which differs from Example 1 only in that the composition does not contain snow lotus extract, but instead uses an equal amount of edelweiss extract to make up for the missing amount. All other parameters are the same as in Example 1.

[0028] Comparative Example 9 This comparative example provides a whitening and repairing composition, which differs from Example 1 only in that the composition includes the following components in parts by weight: 3 parts Bordeaux leaf extract, 0.05 parts European thyme extract, 4.5 parts Bletilla striata root extract, and 3 parts Saussurea involucrata extract.

[0029] Application Examples 1-5 and Comparative Application Examples 1-9 The whitening and repairing compositions of Examples 1-5 and Comparative Examples 1-9 were added to the whitening and repairing lotion at a concentration of 2.5 wt% to obtain the whitening and repairing lotion of Application Examples 1-5 and Comparative Application Examples 1-9. The formulations are shown in Table 2.

[0030] Table 2. Component composition and dosage of the emulsion

[0031] The preparation method of the whitening and repairing lotion includes the following steps: S1. Mix each component of phase A with water and stir. Heat to 80°C and homogenize at 1200 r / min for 5 min. After homogenization, keep warm for later use to obtain phase A. S2. Mix the components of phase B, heat to 80°C, homogenize at 1200 r / min for 5 min, and keep warm after homogenization to obtain phase B; S3. Mix the components of phase C and heat to 60°C to melt them to obtain phase C; S4. Add phase B to phase A at 300 r / min and stir to mix. Then, cool down to 60°C and add phase C at 300 r / min and stir to mix. Then, cool down to below 45°C, add the corresponding whitening and repairing composition, and continue stirring for 5 minutes. Finally, add arginine to adjust the pH, then stop stirring, discharge the product, and obtain the whitening and repairing emulsion.

[0032] The present invention also provides a blank application example emulsion, which differs from application example 1 only in that the whitening and repairing composition is not added, and the missing amount is made up with an equal amount of deionized water. The remaining steps and parameters are the same as those in application example 1, and the blank application example emulsion is prepared.

[0033] Test Example 1: Tyrosinase Inhibition Test Sample solution: The whitening and repairing compositions prepared in Examples 1-5 and Comparative Examples 1-9 were diluted with PBS buffer to a 5wt% sample solution; Solution preparation: L-DOPA solution: Accurately weigh 0.0125 g of levodopa, place it in a 25 mL brown volumetric flask, dilute to the mark with PBS buffer, and prepare for later use; 100 U / mL tyrosinase solution: Dilute 25 KU tyrosinase to a 25 mL brown volumetric flask with PBS buffer, and bring the volume up to the mark to obtain a 1000 U / mL tyrosinase solution. Aliquot the solution, and when using, take 1 mL of the 1000 U tyrosinase solution and dilute it 10 times to obtain a 100 U tyrosinase solution. Prepare test tubes A, B, C, and D for each test sample according to the following specifications: Tube A: 3 mL PBS buffer and 0.5 mL tyrosinase solution; Tube B: 3.5 mL PBS buffer; Tube C: 1 mL sample solution, 2 mL PBS buffer, and 0.5 mL tyrosinase solution; Tube D: 1 mL sample solution and 2.5 mL PBS buffer; Zeroing tube: PBS buffer; After preparation, 0.5 mL of L-DOPA solution was added to tubes A, B, C, and D respectively, and the reaction was carried out at 37℃ for 30 min. The absorbance of tubes A, B, C, and D at 475 nm was measured using a zeroing tube. Each sample was tested three times. The tyrosinase inhibition rate of the test sample was calculated using the following formula: Tyrosinase inhibition rate (%) = 1 - (CD) / (AB) × 100%; Where A is the absorbance value of tube A, B is the absorbance value of tube B, C is the absorbance value of tube C, and D is the absorbance value of tube D. The results are shown in Table 3.

[0034] As shown in Table 3, the whitening and repairing composition provided by this invention has a significant tyrosinase inhibition rate, indicating that the whitening and repairing composition can inhibit melanin production from the source, thereby achieving the effects of whitening and brightening, and improving pigmentation. Comparing the data of Comparative Examples 1-9 with Example 1, the tyrosinase inhibition ability of the whitening and repairing compositions of Comparative Examples 1-9 is much lower than that of Example 1. The difference between Comparative Examples 1-9 and Example 1 is that the whitening and repairing compositions lack one of Bordeaux leaf extract, thyme extract, Bletilla striata root extract, and Saussurea involucrata extract; one of the components of the composition is replaced with an active ingredient with a similar function; or the dosage ratio of the four components is not within the scope of this invention. This indicates that the Bordeaux leaf extract, thyme extract, Bletilla striata root extract, and Saussurea involucrata extract in the composition provided by this invention can synergistically improve the tyrosinase inhibition ability of the composition within a specific dosage ratio range.

[0035] Table 3 Results of Tyrosinase Inhibition Test Example 1 83.5 Example 2 76.1 Example 3 78.4 Example 4 79.9 Example 5 81.2 Comparative Example 1 57.7 Comparative Example 2 54.6 Comparative Example 3 51.9 Comparative Example 4 52.3 Comparative Example 5 62.8 Comparative Example 6 64.1 Comparative Example 7 60.5 Comparative Example 8 61.7 Comparative Example 9 65.0 Test Example 2: Whitening and Repairing Effect Test Asian subjects aged 18-45 were selected to participate in the test. The subjects were randomly divided into 15 groups of 5 people each. The whitening and repairing lotion of application examples 1-5, the control application examples 1-9, and the blank application example were used on the whole face. They were used once in the morning and once in the evening. The method of use was to take 1 mL of the sample and apply it evenly to the whole face after cleansing and moisturizing in the morning and evening, and gently massage until fully absorbed. Various indicators were tested before use and after 28 days of use.

[0036] Test method: After cleansing their face with facial cleanser, the subjects patted their face dry with lint-free absorbent paper towels and then sat quietly for at least 30 minutes until their skin condition stabilized. The skin ITA° value and TEWL value were measured using a Colorimeter CL400 color probe and a Tewameter®™ Hex transepidermal water loss probe, respectively.

[0037] The skin improvement of each volunteer was analyzed after 28 days of using the whitening and repairing lotion. The improvement was expressed as an improvement rate, calculated as follows: ITA° value improvement rate (%) = (ITA° value) 使用28天后- ITA° value 使用前 ) / ITA° value 使用前 ×100%; TEWL value improvement rate (%) = (TEWL value) 使用前- TEWL value 使用28天后 ) / TEWL value 使用前 ×100%; The higher the improvement rate (%) relative to the initial value, the stronger the efficacy. The calculation results are shown in Table 4.

[0038] As shown in Table 4, compared with the blank application examples, the whitening and repairing lotions of Application Examples 1-5 provided by this invention have higher ITA° value improvement rates and TEWL value improvement rates, indicating that the whitening and repairing lotion and whitening and repairing composition provided by this invention can reduce melanin production, brighten skin tone, and achieve a whitening effect. Simultaneously, they can repair the skin barrier and reduce moisture loss, thus possessing both whitening and barrier repair functions. Comparing the data of Application Examples 1-9 with Application Example 1 shows that the combination of Bordeaux leaf extract, thyme extract, Bletilla striata root extract, and Saussurea involucrata extract within a specific range can synergistically improve the whitening, brightening, and skin barrier repair effects of the obtained whitening and repairing composition and its lotion.

[0039] Table 4. Whitening and Repairing Effect Test Results Application Example 1 24.8 30.1 Application Example 2 21.6 25.4 Application Example 3 22.9 26.8 Application Example 4 23.4 28.5 Application Example 5 24.1 29.3 Comparative Application Example 1 11.7 13.9 Comparative Application Example 2 10.5 13.2 Comparative Application Example 3 9.2 12.7 Comparative Application Example 4 9.8 11.5 Comparative Application Example 5 14.3 15.1 Comparative Application Example 6 15.5 16.4 Comparative Application Example 7 13.0 17.2 Comparative Application Example 8 13.6 17.9 Comparative Application Example 9 16.1 18.5 Blank application example 2.2 7.3 Test Example 3: Sensitive Skin Suitability Test Using the whitening and repairing lotion from Application Examples 1-5, the control application examples 1-9, and the lotion from the blank application example as test samples, the suitability of the product for sensitive skin was determined by judging the improvement rate of lactic acid stinging before and after use by people with sensitive skin.

[0040] Volunteer selection: 75 people with sensitive skin were selected as volunteers, with 5 people in each group.

[0041] Test procedure: The test was conducted on the nasolabial folds of volunteers. 50 μL of 10wt% lactic acid solution was dropped onto a single layer of filter paper with a diameter of 0.8 cm. The subjects were asked about their stinging sensation at 0.5 min and 2.5 min. The subjects were scored on a 4-point scale (0 points for no stinging, 1 point for mild stinging, 2 points for moderate stinging, and 3 points for severe stinging. The median score can be used to describe the degree of sensation, such as 0.5 or its median value).

[0042] Sample usage: Volunteers in the sample group applied the samples from Application Examples 1-5 or the control samples 1-9 to their entire face, while volunteers in the blank control group used the lotion from the blank application examples. Volunteers applied the product twice daily, morning and evening, applying 1 mL of lotion each time, for two consecutive weeks. After two weeks of use, the above test steps were repeated.

[0043] Record the lactic acid stinging scores of volunteers before and after 2 weeks of use, and calculate the improvement rate of lactic acid stinging in volunteers.

[0044] The improvement rate of lactic acid stinging (%) was calculated as follows: (sum of lactic acid stinging scores before use - sum of lactic acid stinging scores after 2 weeks of use) / sum of lactic acid stinging scores before use × 100%. The sum of lactic acid stinging scores = the average lactic acid stinging score over 0.5 minutes + the average stinging score over 2.5 minutes.

[0045] The higher the improvement rate of lactic acid stinging, the better the repair effect of the sample, and the more suitable the product is for people with sensitive skin.

[0046] As shown in Table 5, compared with the blank application example, the whitening and repairing lotion of Application Examples 1-5 provided by the present invention achieved a lactic acid stinging improvement rate of 65.71%-70.73%, indicating that the whitening and repairing lotion provided by the present invention can effectively improve skin sensitivity and increase skin tolerance, making it suitable for people with sensitive skin. Furthermore, comparing the data of Application Examples 1-9 with Application Example 1 shows that the Bordeaux leaf extract, thyme extract, Bletilla striata root extract, and Saussurea involucrata extract in the whitening and repairing composition provided by the present invention produce a synergistic effect within a specific range, significantly improving the skin repair effect of the whitening and repairing composition, making it more suitable for people with sensitive skin.

[0047] Table 5 Results of the test for suitability for sensitive skin Application Example 1 70.59 Application Example 2 64.71 Application Example 3 66.67 Application Example 4 68.42 Application Example 5 70.59 Comparative Application Example 1 47.05 Comparative Application Example 2 46.67 Comparative Application Example 3 46.67 Comparative Application Example 4 42.11 Comparative Application Example 5 50.00 Comparative Application Example 6 50.00 Comparative Application Example 7 52.63 Comparative Application Example 8 55.00 Comparative Application Example 9 57.14 Blank application example 15.79 Finally, it should be noted that the above embodiments are only used to illustrate the technical solutions of the present invention and are not intended to limit the scope of protection of the present invention. Although the present invention has been described in detail with reference to preferred embodiments, those skilled in the art should understand that modifications or equivalent substitutions can be made to the technical solutions of the present invention without departing from the essence and scope of the technical solutions of the present invention.

Claims

1. A whitening and repairing composition, characterized in that, It includes the following components in parts by weight: 0.01-2 parts Bordeaux leaf extract, 0.1-5 parts European thyme extract, 0.01-2 parts Bletilla striata root extract and 0.01-2 parts Saussurea involucrata extract.

2. The whitening and repairing composition as described in claim 1, characterized in that, It includes the following components in parts by weight: 0.1-1 part Bordeaux leaf extract, 0.5-2 parts European thyme extract, 0.05-0.5 parts Bletilla striata root extract and 0.05-1 part Saussurea involucrata extract.

3. The use of the whitening and repairing composition according to claim 1 or 2 in the preparation of cosmetics.

4. The application as described in claim 3, characterized in that, The cosmetics include any one of the following: toner, cream, lotion, gel, and mask.

5. The application as described in claim 3, characterized in that, The amount of the whitening and repairing composition added to the cosmetic product is 1wt%-5wt%.

6. A cosmetic product, characterized in that, Contains the whitening and repairing composition as described in claim 1 or 2.

7. The cosmetic product as described in claim 6, characterized in that, It also contains excipients acceptable in the cosmetics industry.

8. The cosmetic product as described in claim 7, characterized in that, The excipients acceptable in the cosmetics field include at least one of solvents, humectants, pH adjusters, emollients, emulsifiers, thickeners, solubilizers, antioxidants, and fragrances.

9. A whitening and repairing lotion, characterized in that, It contains the following components by weight percentage: The whitening and repairing composition according to claim 1 or 2 comprises 1%-5% thickener, 0.05%-1.0% moisturizer, 2%-10% chelating agent, 0.01%-0.1% emollient, 3%-8% skin moisturizer, 1%-5% emulsifier, 0.1%-4% antioxidant and 0.01%-0.3% pH adjuster, with the balance being deionized water.

10. The whitening and repairing lotion as described in claim 9, characterized in that, The preparation method of the whitening and repairing lotion includes the following steps: S1. Mix and stir a portion of the humectant, thickener, chelating agent and water, heat to 75-85℃, homogenize, and obtain phase A; S2. Mix the emollient and emulsifier, heat to 75-85℃, homogenize, and obtain phase B; S3. Mix the antioxidant and the remaining humectant, heat to 60°C to melt, and obtain phase C; S4. Add phase B to phase A, stir and mix, cool to 60℃, add phase C, stir and mix, then cool to below 45℃, add the whitening and repairing composition and continue stirring, add pH adjuster to adjust pH, discharge to obtain whitening and repairing emulsion.

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