Whitening and repairing composition as well as preparation method and application thereof

Abstract

The invention belongs to the technical field of cosmetics, and discloses a whitening and repairing composition as well as a preparation method and application thereof. The composition disclosed by the invention is prepared from the following components: madecassoside, paeonol and adenosine. The composition starts from the dimensions of scavenging free radicals, blocking inflammation induced by ultraviolet rays and inhibiting tyrosinase activity and chromatosis, not only plays a role in a traditional whitening pathway, but also prevents skin blackening and prevents inflammation generation, and the purpose of comprehensive and efficient whitening and repairing is achieved.

Description

Technical Field

[0001] This invention belongs to the field of cosmetic technology, and specifically relates to a whitening and repairing composition, its preparation method, and its application. Background Technology

[0002] Currently, common skin-whitening ingredients on the market can be broadly categorized into three types based on their mechanisms of action: 1) Inhibiting melanin production, most of which are tyrosinase inhibitors, such as kojic acid and arbutin; 2) Inhibiting melanin transport, such as niacinamide; and 3) Promoting melanin reduction, primarily composed of strong antioxidants, such as vitamin C and its derivatives. Traditional skin-whitening products generally target tyrosinase activity and melanin, resulting in relatively singular effects. Furthermore, while some ingredients may have a certain whitening effect, they can also be highly irritating, such as rhododendron alcohol, which, if used improperly, can easily lead to adverse reactions such as skin allergies. Summary of the Invention

[0003] The present invention aims to solve at least one of the technical problems existing in the prior art. To this end, the present invention provides a whitening and repairing composition, its preparation method and application. This composition works from several dimensions, including scavenging free radicals, blocking ultraviolet-induced inflammation, inhibiting tyrosinase activity and pigmentation. It not only functions in the traditional whitening pathway, but also prevents skin darkening and inhibits the generation of inflammation, thus achieving a comprehensive and efficient whitening and repairing effect.

[0004] In a first aspect, the present invention provides a composition comprising the following components: asiaticoside, paeonol, and adenosine.

[0005] In some embodiments of the present invention, the composition comprises, by weight percentage, the following components: 1%-10% asiaticoside, 20%-30% paeonol, and 60%-70% adenosine.

[0006] Specifically, the mass percentage of the hydroxyascorbic acid glycoside can be any point value or any two-point range between 1% and 10%, such as 1%, 2%, 3%, 4%, 5%, 6%, 7%, 8%, 9%, 10%, etc.

[0007] Specifically, the mass percentage of paeonol can be any point value or any two-point range between 20% and 30%, such as 20%, 22%, 24%, 26%, 28%, 30%, etc.

[0008] Specifically, the mass percentage of adenosine can be any point value or any two-point range between 60% and 70%, such as 60%, 62.5%, 65%, 67.5%, 70%, etc.

[0009] Specifically, the hydroxyascorbic acid glycoside described in this invention has excellent anti-inflammatory and repairing effects, can inhibit the production of prostaglandins, and inhibit the expression of UVB-induced COX-2 and PAR-2, specifically by inhibiting ultraviolet-induced melanin synthesis and melanosome transfer.

[0010] Specifically, the paeonol described in this invention can, on the one hand, scavenge intracellular oxygen free radicals, and since the process of tyrosinase catalyzing the oxidation of substrates to produce pigments requires the participation of oxygen, thus blocking the melanin production chain; on the other hand, paeonol is a mixed inhibitor of tyrosinase, which can act on tyrosinase and inhibit its activity, thereby reducing melanin production.

[0011] Specifically, the adenosine described in this invention is also a component of cyclic adenosine monophosphate (cAMP). In pigmentation, cAMP acts as an intermediate second messenger to transmit external α-MSH signals, which subsequently trigger the expression of tyrosinase induced by microphthalmia-associated transcription factor (MITF) in the melanocyte nucleus.

[0012] Specifically, the whitening and repairing effects described in this invention are not achieved by simply selecting and combining a few ingredients. Instead, by studying skin whitening pathways, preventing skin darkening, and blocking inflammation mechanisms, three specific ingredients with corresponding effects—paeonol, asiaticoside, and adenosine—were selected from a large number of ingredients. After extensive research and experimentation, a scientifically reasonable compounding ratio was obtained, which synergistically enhances and complements the effects. It works from several dimensions, including scavenging free radicals, blocking UV-induced inflammation, inhibiting tyrosinase activity, and reducing pigmentation. It not only plays a role in traditional whitening pathways but also prevents skin darkening and inhibits the generation of inflammation, achieving a comprehensive and efficient whitening and repairing effect.

[0013] A second aspect of the present invention provides a method for preparing the composition described in the first aspect of the present invention, comprising the following steps:

[0014] The components are mixed to obtain the composition.

[0015] A third aspect of the present invention provides the use of the composition described in the first aspect of the present invention in the preparation of a product having whitening and repairing effects.

[0016] In some embodiments of the present invention, the product includes cosmetics or topical skin preparations.

[0017] A fourth aspect of the present invention provides a cosmetic product comprising the composition described in the first aspect of the present invention.

[0018] In some embodiments of the present invention, the composition has a mass content of 0.01%-1% in the cosmetic. The mass content of the composition can be any point value or any two points within the range of 0.01%-1%, such as 0.01%, 0.1%, 0.2%, 0.3%, 0.4%, 0.5%, 0.6%, 0.7%, 0.8%, 0.9%, 1%, etc.

[0019] In some embodiments of the present invention, the composition has a mass content of 0.01%-0.5% in cosmetics.

[0020] In some embodiments of the present invention, the dosage form of the cosmetic includes face cream, lotion, aqueous solution, gel or mask.

[0021] In some embodiments of the present invention, the cosmetic further includes at least one of emulsifier, moisturizer, thickener, chelating agent, preservative, pH adjuster and fragrance.

[0022] Compared with the prior art, the beneficial effects of the present invention are as follows:

[0023] (1) The formulation of the composition of the present invention contains hydroxyascorbic acid, paeonol and adenosine. Through such a unique formulation combination, the components produce a good synergistic effect. It works from the dimensions of clearing free radicals, blocking the inflammation induced by ultraviolet rays, inhibiting tyrosinase activity and pigmentation. It not only plays a role in the traditional whitening pathway, but also prevents skin darkening and prevents the generation of inflammation, so as to achieve the purpose of comprehensive and efficient whitening and repair.

[0024] (3) The composition of the present invention is mild and non-irritating, and its effects of inhibiting tyrosinase and scavenging free radicals are obvious. The tyrosinase activity inhibition rate is above 78%, and the hydroxyl free radical scavenging rate is above 80%. At the same time, the composition has significant repair and whitening effects in practical applications. The TEWL change rate can reach -23.15% and the melanin change rate can reach -19.25% after 4 weeks. Detailed Implementation

[0025] The present invention will be further described in detail below through specific embodiments. Unless otherwise specified, the raw materials, reagents, or apparatus used in the embodiments can be obtained from conventional commercial sources or by existing technical methods. Unless otherwise specified, the experimental or testing methods are conventional methods in the art.

[0026] Example 1

[0027] A composition comprising the following components in weight percentage: 5% asiaticoside, 30% paeonol, and 65% adenosine.

[0028] The composition of this embodiment is prepared by mixing the components.

[0029] Example 2

[0030] A composition comprising the following components in weight percentages: 10% asiaticoside, 20% paeonol, and 70% adenosine.

[0031] The composition of this embodiment is prepared by mixing the components.

[0032] Example 3

[0033] A composition comprising the following components in weight percentages: 1% asiaticoside, 29% paeonol, and 70% adenosine.

[0034] The composition of this embodiment is prepared by mixing the components.

[0035] Example 4

[0036] A composition comprising the following components in weight percentage: 5% asiaticoside, 25% paeonol and 70% adenosine.

[0037] The composition of this embodiment is prepared by mixing the components.

[0038] Comparative Example 1

[0039] The only difference from Example 1 is that adenosine is replaced with an equal amount of deionized water.

[0040] Comparative Example 2

[0041] The only difference from Example 1 is that hydroxyascorbic acid is replaced with an equal amount of deionized water.

[0042] Comparative Example 3

[0043] The only difference from Example 1 is that paeonol is replaced with an equal amount of deionized water.

[0044] Comparative Example 4

[0045] The only difference from Example 1 is that paeonol and adenosine are replaced with deionized water in equal amounts.

[0046] Comparative Example 5

[0047] The only difference from Example 1 is that hydroxyascorbic acid and adenosine are replaced with deionized water in equal amounts.

[0048] Comparative Example 6

[0049] The only difference from Example 1 is that hydroxyascorbic acid and paeonol are replaced with deionized water in equal amounts.

[0050] Comparative Example 7

[0051] The only difference from Example 1 is that asiaticoside is replaced in equal amounts with a centella asiatica extract, which has similar effects to asiaticoside.

[0052] Comparative Example 8

[0053] The only difference from Example 1 is that paeonol is replaced in equal amounts with peony root extract, which has similar effects to paeonol.

[0054] Comparative Example 9

[0055] The only difference from Example 1 is that adenosine is replaced in equal amounts with caffeine, which has a similar effect to adenosine.

[0056] Application Example 1

[0057] The composition of Example 1 was used to prepare a whitening and repairing toner, and the specific formula is shown in Table 1.

[0058] Table 1

[0059]

[0060] The method for preparing the toner according to Example 1 includes the following steps:

[0061] (1) Add phase A raw material to a mixing pot, heat to 60°C, and stir homogenously until dissolved;

[0062] (2) Heat the B phase raw material to 60°C until it melts and becomes transparent, then add it to a mixing pot and disperse it evenly, and then cool it down to 40°C;

[0063] (3) Add the C phase raw material to the mixing pot and stir to disperse it evenly;

[0064] (4) After the raw material of phase D is evenly dispersed, it is added to the mixing pot and evenly dispersed. The temperature is then reduced to below 37°C to obtain whitening and repairing lotion.

[0065] Application Example 2

[0066] The composition of Example 1 was used to prepare a whitening and repairing facial mask, and the specific formula is shown in Table 2.

[0067] Table 2

[0068]

[0069] The method for preparing the face mask according to Example 2 includes the following steps:

[0070] (1) Add phase A raw material to a mixing pot, heat to 60°C, and stir homogenously until dissolved;

[0071] (2) Add phase B raw material to the mixing pot and disperse it evenly;

[0072] (3) After heating the C phase raw material to 60°C until it melts and becomes transparent, add it to a mixing pot and disperse it evenly, then cool it down to 40°C;

[0073] (4) Add the D phase raw material to the mixing pot and stir to disperse it evenly;

[0074] (5) After the E phase raw material is evenly dispersed, it is added to the mixing pot and evenly dispersed. The temperature is then reduced to below 37°C to obtain the whitening and repairing mask.

[0075] Application Example 3

[0076] The composition of Example 1 was used to prepare a whitening and repairing lotion, and the specific formula is shown in Table 3.

[0077] Table 3

[0078]

[0079] The method for preparing the emulsion according to Example 3 includes the following steps:

[0080] (1) Add phase A raw material to the emulsification pot, heat to 80°C, and stir homogenously to dissolve evenly.

[0081] (2) Mix the B phase raw materials and heat them to 80°C. Stir and disperse them evenly, then add them to the emulsification pot, homogenize and emulsify them, stir evenly, and then cool them down to 60°C.

[0082] (3) After heating the C phase raw material to 60°C until it melts and becomes transparent, add it to the emulsification pot and disperse it evenly, and then cool it down to 40°C;

[0083] (4) After the raw material of phase D is evenly dispersed, it is added to the emulsification pot and evenly dispersed. The temperature is then reduced to below 37°C to obtain the whitening and repairing emulsion.

[0084] Application Example 4

[0085] The composition of Example 1 was used to prepare a whitening and repairing face cream, and the specific formula is shown in Table 4.

[0086] Table 4

[0087]

[0088]

[0089] The method for preparing the face cream according to Example 4 includes the following steps:

[0090] (1) Add phase A raw material to the emulsification pot, heat to 80°C, and stir homogenously to dissolve evenly.

[0091] (2) Mix the B phase raw materials and heat them to 80°C. Stir and disperse them evenly, then add them to the emulsification pot, homogenize and emulsify them, stir evenly, and then cool them down to 60°C.

[0092] (3) Add the C phase raw material to the emulsifying pot and homogenize and disperse it evenly;

[0093] (4) After heating the D phase raw material to 60°C until it melts and becomes transparent, add it to the emulsification pot and disperse it evenly, and then cool it down to 40°C;

[0094] (5) After the E phase raw materials are evenly dispersed, they are added to the emulsification pot and evenly dispersed. The temperature is then reduced to below 37°C to obtain the whitening and repairing face cream.

[0095] Application Comparative Example 1

[0096] The only difference from Application Example 4 is that the composition of Example 1 is replaced with an equal amount of deionized water, while the other components, proportions and preparation methods remain the same as in Application Example 4.

[0097] Application Comparative Example 2-10

[0098] The only difference from Application Example 4 is that the composition of Example 1 is replaced in equal amounts with the compositions of Comparative Examples 1-9, while the other components, proportions and preparation methods remain the same as in Application Example 4.

[0099] Experimental Example 1: Red Blood Cell Hemolysis Test

[0100] The red blood cell hemolysis test (RBC) is an alternative to the rabbit eye irritation test (Draize test). Its basic principle is to evaluate the damage of chemicals to eye tissue cells by measuring the amount of hemoglobin dissolved and the degree of denaturation. Internationally, the RBC test is mainly used to evaluate the eye irritation of chemicals in cosmetics and raw materials.

[0101] The compositions of Examples 1-4 and the compositions of Comparative Examples 1-9 were subjected to erythrocyte hemolysis tests in accordance with the European Centre for Validation of Alternative Methods (ECVAM) erythrocyte hemolysis test methods and grading standards.

[0102] The ECVAM RBC irritation grading standards for cosmetic products are shown in Table 5. In this table, L / D is the ratio of HD50 to DI, where HD50 is the sample concentration at which 50% of red blood cells undergo hemolysis, and DI is the protein denaturation index.

[0103] Table 5

[0104] L / D Classification ﹥100 Non-irritating 10 < L / D ≤ ​​100 Mild irritation 1 < L / D ≤ ​​10 Mild irritation 0.1 < L / D ≤ ​​1 moderate irritation L / D≤0.1 Severe irritation

[0105] The results of the red blood cell hemolysis experiment are shown in Table 6.

[0106] Table 6

[0107] sample evaluate Example 1 Non-irritating Example 2 Non-irritating Example 3 Non-irritating Example 4 Non-irritating Comparative Example 1 Non-irritating Comparative Example 2 Non-irritating Comparative Example 3 Non-irritating Comparative Example 4 Non-irritating Comparative Example 5 Non-irritating Comparative Example 6 Non-irritating Comparative Example 7 Non-irritating Comparative Example 8 Non-irritating Comparative Example 9 Non-irritating

[0108] As shown in Table 6, the hemolysis test results of red blood cells indicate that the compositions of Examples 1-4 and Comparative Examples 1-9 are all non-irritating. This demonstrates that the compositions of the present invention are mild and non-irritating.

[0109] Experimental Example 2: Test for Inhibition of Tyrosinase Activity

[0110] An in vitro tyrosinase activity inhibition experiment was conducted. Four test tubes were filled with 0.1 mol / L phosphate buffered saline (PBS) at pH 6.8, the sample solution, and 0.5 g / L L-tyrosine solution, respectively. The tubes were incubated at 37°C for 10 min, then 100 U / mL tyrosinase solution was added, and the reaction was continued at 37°C for another 10 min. The absorbance (A) was measured at 475 nm. The experimental design is shown in Table 7; where C1 is the blank control, C2 is used for blank zeroing, T1 is the sample group, and T2 is used for sample zeroing.

[0111] Table 7

[0112] <![CDATA[C1 / mL]]> <![CDATA[C2 / mL]]> <![CDATA[T1 / mL]]> <![CDATA[T2 / mL]]> sample -- -- 0.8 0.8 PBS (pH=6.8) 1.8 1.4 1.0 0.6 L-tyrosine 0.8 0.8 0.8 0.8 Tyrosinase -- 0.4 -- 0.4 Total 2.6 2.6 2.6 2.6

[0113] Calculation formula: Tyrosinase activity inhibition rate = [1-A] T / A C ]×100%;

[0114] Among them, A C The absorbance value for the blank control is Ac = Ac1 - Ac2;

[0115] A T Let At be the absorbance value of the sample, where At = At1 - At2.

[0116] The compositions of Examples 1-4 and Comparative Examples 1-9 were dissolved in 30 wt% 1,3-propanediol aqueous solution to prepare sample solutions, which were used to determine the inhibition rate of tyrosinase activity. The results are shown in Table 8.

[0117] Table 8

[0118]

[0119]

[0120] As can be seen from the data in Table 8, the tyrosinase activity inhibition rate of the compositions in Examples 1-4 is all above 78%, indicating that they have a very good tyrosinase activity inhibition rate. In contrast, in Comparative Examples 1-9, due to the lack of components or the use of non-inventory combination formulations, the tyrosinase activity inhibition rate is kept at a low level, all less than 61%. This shows that the combination of asiaticoside, paeonol and adenosine in this invention, as well as their ratio, is scientifically reasonable, and the components in the composition have a synergistic effect.

[0121] Experimental Example 3: Hydroxyl Radical Scavenging Test

[0122] The amounts of each solution added were as shown in Table 9. In the colorimetric tube, 9 mmol / L FeSO4, 9 mmol / L ethanol-salicylic acid, a suitable amount of deionized water, and finally 8.8 mmol / L H2O2 were added and shaken well. The tube was then heated in a 37°C water bath for 15 minutes and the absorbance A0 was measured. For A0 determination, the reference solution was a system without hydrogen peroxide. The absorbance A was measured by adding the solutions shown in Table 9 according to the above method. X A X0 A X A X0 During the measurement, the reference solution was deionized water.

[0123] Table 9

[0124]

[0125]

[0126] Calculation formula: Hydroxyl radical scavenging rate (%) = [A0 - ( ... X -A X0 [) / A0]×100%, where A0 is the absorbance value of the blank control; A X To add the absorbance value of the sample; A X0 The background absorbance is the value without the addition of the colorimetric reagent H2O2.

[0127] The compositions of Examples 1-4 and Comparative Examples 1-9 were used to determine the scavenging rate of hydroxyl radicals, and the results are shown in Table 10.

[0128] Table 10

[0129] sample Hydroxyl radical scavenging rate / % Example 1 89.53 Example 2 82.46 Example 3 86.49 Example 4 80.63 Comparative Example 1 59.26 Comparative Example 2 62.13 Comparative Example 3 63.57 Comparative Example 4 45.98 Comparative Example 5 56.74 Comparative Example 6 53.15 Comparative Example 7 60.84 Comparative Example 8 72.16 Comparative Example 9 64.36

[0130] As can be seen from the data in Table 10, the hydroxyl radical scavenging rates of the compositions in Examples 1-4 are all above 80%, indicating that they have a very good hydroxyl radical scavenging rate. In contrast, the hydroxyl radical scavenging rates of Comparative Examples 1-9 are significantly lower than those of the Examples, indicating that the compositions prepared in the Examples of the present invention have synergistic and complementary effects among their components, thus achieving better results.

[0131] Experimental Example 4: Human Transdermal Water Loss Test

[0132] Fifty-five healthy subjects were randomly divided into 11 groups of five each. The face creams prepared using Application Example 4 and Comparative Examples 1-10 were used as test samples. Subjects applied the samples to their faces twice daily, morning and evening. Using a Corneometer CM825 skin moisture meter and an AF200 skin moisture loss meter, facial moisture content and transepidermal water loss (TEWL) were measured before use (D0) and on day 28 (D28) under conditions of 21±1℃ and 50±10% humidity. After cleansing the face and waiting 20 minutes, the corresponding change rates were calculated to comprehensively evaluate the product's moisturizing and repairing effects on human skin. The experimental results are shown in Table 11.

[0133] Table 11

[0134] sample 28-day moisture content change rate / % 28-day TEWL change rate / % Application Example 4 35.48 -23.15 Application Comparative Example 1 20.74 -5.64 Application Comparative Example 2 26.54 -15.40 Application Comparative Example 3 23.74 -13.84 Application Comparative Example 4 27.96 -16.23 Application Comparative Example 5 20.13 -9.10 Application Comparative Example 6 21.46 -12.47 Application Comparative Example 7 18.62 -8.29 Application Comparative Example 8 28.45 -15.68 Application Comparison Example 9 23.87 -13.74 Application Comparison Example 10 26.41 -20.05

[0135] A higher rate of change in water content indicates better moisturizing ability, and a greater decrease in the rate of change in transepidermal water loss indicates better repair ability. As can be seen from the results in Table 11, the cream prepared using Example 4 showed better results in both water content and transepidermal water loss, indicating that the cream containing the composition of this invention has better moisturizing and repairing effects. The scientific combination of asiaticoside, paeonol, and adenosine in the composition demonstrates a synergistic effect among the components.

[0136] Experiment 5: Human Skin Whitening Experiment

[0137] Fifty-five healthy subjects were randomly divided into 11 groups of five each. The face creams prepared using Application Example 4 and Comparative Examples 1-10 were used as test samples. Subjects applied the samples to their faces twice daily, morning and evening, for four consecutive weeks, avoiding washing them off with water after application. Melanin content in the skin was measured using a skin melanin analyzer before use and every week thereafter, and the rate of melanin change was calculated. The results are shown in Table 12.

[0138] Table 12

[0139]

[0140] As shown in Table 12, the face cream prepared using Example 4 exhibits superior pigmentation reduction ability, with a reduction of approximately 20% in facial melanin after four weeks of use. In contrast, under the same conditions, the face cream used in Comparative Example 1 (without the composition of this invention) showed a melanin reduction rate of only 6.48%, indicating minimal change. Furthermore, while the face creams prepared using Comparative Examples 2-10 also demonstrated some melanin-reducing ability, their melanin reduction rates were all lower than those of the face cream prepared using Example 4. This indicates that the face cream containing the composition of this invention has a significant effect in reducing pigmentation. The scientific combination of asiaticoside, paeonol, and adenosine results in a synergistic effect among the components of the composition.

[0141] In summary, the whitening and repairing composition provided by this invention, through its scientifically and rationally combined components, exhibits synergistic and complementary effects. The composition of this invention is mild and non-irritating, and its tyrosinase inhibition and hydroxyl radical scavenging effects are significantly superior to compositions lacking any components or with combinations different from those of this invention. When the composition of this invention was added to a face cream base for testing its body repair and whitening effects, the results showed that, compared to a blank face cream, it had excellent repairing and pigmentation reduction capabilities.

[0142] The preferred embodiments of the present invention have been described in detail above, but the present invention is not limited to the embodiments described. Those skilled in the art can make various equivalent modifications or substitutions without departing from the spirit of the present invention, and these equivalent modifications or substitutions are all included within the scope defined by the claims of this application.

Claims

1. A composition, characterized in that, The composition comprises the following components: asiaticoside, paeonol, and adenosine.

2. The composition according to claim 1, characterized in that, The composition comprises, by weight percentage, the following components: 1%-10% asiaticoside, 20%-30% paeonol, and 60%-70% adenosine.

3. A method for preparing the composition according to claim 1 or 2, characterized in that, Includes the following steps: The components are mixed to obtain the composition.

4. The use of the composition according to claim 1 or 2 in the preparation of products with whitening and repairing effects.

5. The application according to claim 4, characterized in that, The products include cosmetics or topical skin preparations.

6. A cosmetic product, characterized in that, The cosmetic product includes the composition according to claim 1 or 2.

7. The cosmetic product according to claim 6, characterized in that, The composition has a mass content of 0.01%-1% in cosmetics.

8. The cosmetic product according to claim 7, characterized in that, The composition has a mass content of 0.01%-0.5% in cosmetics.

9. The cosmetic product according to claim 6, characterized in that, The dosage forms of the cosmetics include face creams, lotions, liquids, gels, or masks.

10. The cosmetic product according to claim 6, characterized in that, The cosmetics also include at least one of the following: emulsifiers, moisturizers, thickeners, chelating agents, preservatives, pH adjusters, and fragrances.

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