Oxidized resveratrol-containing whitening composition capable of deeply fading stains and application of oxidized resveratrol-containing whitening composition

Abstract

The invention relates to a whitening composition containing oxidized resveratrol and capable of deeply fading stains and application of the whitening composition, the composition is prepared from the following components: oxidized resveratrol, VC ethyl ether, a verbascos extract and a spearmint extract, and the weight ratio of the oxidized resveratrol to the VC ethyl ether to the verbascos extract to the spearmint extract is (0.11-2): (1-5): (0.01-1.2): (0.01-2). The whitening composition provided by the invention constructs an inhibition-removal-protection-repair system for chloasma, dermis plaque, post-inflammation pigmentation and other stubborn color spots caused by basement membrane zone injury, and performs multi-target repair.

Description

Technical Field

[0001] The invention relates to the technical field of cosmetics, and in particular to a whitening composition containing oxidized resveratrol for deeply lightening spots and an application thereof. Background Art

[0002] The integrity of the basement membrane zone, as a key barrier structure between the epidermis and the dermis, directly determines the metabolic pathway of melanin. Clinical data show that more than 95% of stubborn spots such as chloasma, dermal spots, and post-inflammatory pigmentation are accompanied by basement membrane zone ruptures. This damage mechanism originates from the degradation of type IV collagen and laminin in the basement membrane zone. Ultraviolet rays activate matrix metalloproteinases (MMP-2 / MMP-9), reducing the thickness of the basement membrane zone by 40%-60%, forming a melanin permeation channel, causing epidermal melanocytes to penetrate into the dermis through the damaged area and be phagocytosed by macrophages to form melanophiles that are difficult to metabolize. These melanophils can survive in the dermis for several years, forming blue-gray patches visible to the naked eye, which is also the core reason why traditional whitening methods are difficult to eradicate stubborn spots. At the same time, the basement membrane has certain permeability and barrier functions and is an important component of the skin barrier. If the basement membrane zone is damaged, the skin barrier function is reduced, and the ability to resist external stimuli such as ultraviolet rays is weakened. This will increase the risk of skin damage due to inflammation, oxidative stress, etc., thereby indirectly affecting the synthesis and metabolism of melanin and promoting the occurrence of stubborn chloasma.

[0003] Although existing whitening ingredients such as arbutin and kojic acid can inhibit tyrosinase activity, they only act on the melanin production link in the epidermis and do not repair the basement membrane zone of the skin. Studies have shown that the recurrence rate of pigmentation treated with a single tyrosinase inhibitor is as high as 38%-65%. Its fundamental defects are: ① It cannot prevent the continuous activation of matrix metalloproteinases (MMPs) induced by ultraviolet rays, and the degradation of collagen in the basement membrane zone is not intervened; ② The basement membrane zone is not repaired, so melanin can fall into the dermis to form stubborn pigmentation; ③ Ignoring the vicious cycle of inflammatory factors (such as IL-6, TNF-α) that reversely stimulate epidermal melanocytes through damaged basement membranes. Summary of the invention

[0004] The purpose of the present invention is to overcome the shortcomings of the prior art and provide a whitening composition containing oxidized resveratrol for deeply lightening spots and its application.

[0005] To achieve the above object, the technical solution adopted by the present invention is:

[0006] In a first aspect, the present invention provides a whitening composition containing oxidized resveratrol for deeply lightening spots, comprising the following components: oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract, wherein the weight ratio of the oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract is (0.11-2):(1-5):(0.01-1.2):(0.01-2).

[0007] As a stable derivative of resveratrol, oxidized resveratrol has the core function of blocking melanin production by inhibiting tyrosinase activity. It also has antioxidant and anti-inflammatory properties, can remove free radicals and slow down the oxidative stress response caused by ultraviolet rays. This ingredient has significant effects on skin whitening and anti-aging, and is particularly suitable for improving pigmentation problems.

[0008] VC ethyl ether is a stable derivative of vitamin C. It achieves whitening and antioxidant effects by inhibiting tyrosinase activity and neutralizing free radicals, while activating the collagen synthesis pathway to improve skin elasticity. Its hydrophilic and lipophilic properties make it easier to penetrate the stratum corneum, and it performs well in anti-aging and brightening skin tone.

[0009] Verbascum extract has the effects of photodamage protection and instant brightening. This is because the large amount of verbascoside it contains absorbs blue light / ultraviolet light through the quantum leap effect and converts it into visible light, reducing light-induced tyrosinase activation and directly inhibiting the melanin oxidation process. In addition, its rich flavonoids can promote barrier lipid synthesis, enhance the skin's resistance to external stimuli, and complement the barrier repair function of oxidized resveratrol.

[0010] The rosmarinic acid contained in spearmint extract can inhibit the formation of AGEs in the glycation reaction and reduce the dark yellow skin tone caused by the cross-linking of collagen fibers. Studies have shown that spearmint extract can reduce the accumulation of glycation products in the skin, and form a synergistic effect with the anti-glycation effect of VC ethyl ether. In addition, its antibacterial properties can relieve inflammation of sensitive skin, reduce the risk of inflammatory pigmentation, regulate the balance of skin microecology, and enhance the mildness of the formula to make it suitable for sensitive skin.

[0011] The oxidized resveratrol in the composition of the present invention has three effects. First, it inhibits the activity of human tyrosinase, directly blocks the production of melanin, and downregulates the expression of premelanosome protein (PMEL) to reduce the formation of melanosome structure; second, by inhibiting the cross-linking of advanced glycation end products (AGEs) and type IV collagen, the thickness of the basement membrane zone is increased, the true epidermal structure barrier is repaired, and melanin is blocked from penetrating into the dermis; finally, it also has a photoprotective effect to prevent melanocytes from being stimulated by ultraviolet rays to produce melanosomes. VC ethyl ether can remove free radicals to reduce the damage of oxidative stress to the basement structure, and promote the regeneration of type I and type IV collagen in the basement membrane zone, so that the density of collagen fibers is increased. At the same time, its water-oil amphiphilic properties can promote the penetration of other ingredients, so that they penetrate into the skin to repair the basement membrane zone. Mullein extract has the effect of preventing UV damage and blocking the conduction of light signals, and can also achieve an instant brightening effect by absorbing ultraviolet rays. On the one hand, the spearmint extract can cooperate with oxidized resveratrol to inhibit the formation of melanin, and on the other hand, it can cooperate with VC ethyl ether to scavenge free radicals and play an anti-glycation role. At the same time, it also has anti-inflammatory and soothing effects, can repair barrier damage, and strengthen the basement membrane zone. Therefore, the present invention uses the four ingredients of oxidized resveratrol, VC ethyl ether, verbascosa extract and spearmint extract to synergistically repair the basement membrane zone of the skin, thereby reducing the generation of stubborn spots and fading the stubborn spots that have already formed.

[0012] Preferably, the weight ratio of the oxidized resveratrol, VC ethyl ether, verbabasin extract and spearmint extract is (0.5-1.5):(1-3):(0.1-1):(0.1-1.2).

[0013] More preferably, the weight ratio of the oxidized resveratrol, VC ethyl ether, verbabasin extract and spearmint extract is (1-1.2):(1-2):(0.5-0.8):(0.1-0.8).

[0014] In a second aspect, the present invention provides use of the whitening composition for deeply lightening pigmentation spots containing oxidized resveratrol in the first aspect in the preparation of cosmetics.

[0015] Preferably, the cosmetic is a lotion, emulsion, cream, mask, essence or spray, and the added amount of the composition is 1%-3% of the total weight of the cosmetic.

[0016] In a third aspect, the present invention provides a facial cream comprising the following raw materials in weight percentage: 0.5%-5% of the whitening composition in the first aspect, 0.05%-0.3% of a thickener, 0.5%-1% of a moisturizer, 1-10% of an emulsifier, 0.5%-3% of a preservative, 0.01%-0.3% of a pH regulator and 0.01%-1% of an essence, with the remainder being deionized water.

[0017] Preferably, the thickener comprises at least one of xanthan gum, carbomer, hydroxyethyl acrylate / sodium acryloyldimethyl taurate copolymer, ammonium acryloyldimethyl taurate / VP copolymer, sclerotium gum and cetyl alcohol.

[0018] Preferably, the moisturizing agent includes at least one of allantoin, sodium polyacrylate, hydrogenated lecithin, betaine, β-glucan, trehalose, caprylyl glycol, dipropylene glycol, sodium hyaluronate, 1,2-butylene glycol, glycerin, budding pullulan and ceramide.

[0019] Preferably, the pH adjuster includes at least one of arginine, sodium hydroxide and EDTA-2Na.

[0020] Preferably, the preservative includes at least one of 1,2-propylene glycol, 1,2-hexanediol and p-hydroxyacetophenone.

[0021] Preferably, the emulsifier is at least one of dimethiconol, propylheptyl caprylate, PEG / PPG-14 / 7 dimethyl ether and polymethylsilsesquioxane.

[0022] In a fourth aspect, the present invention provides a method for preparing the facial cream in the third aspect, comprising the following steps:

[0023] S1. Mix the moisturizer, thickener and part of deionized water, homogenize at 75-85°C to obtain the aqueous phase, then add the emulsifier and stir evenly to obtain an emulsion;

[0024] S2. When the temperature of the emulsion in S1 drops to 55-65° C., add a preservative, and when the system temperature drops to 35-45° C., add the components of the whitening composition, flavor and remaining deionized water, stir evenly, and finally add a pH adjuster to adjust the pH to obtain the facial cream.

[0025] Compared with the prior art, the present invention has the following beneficial effects:

[0026] The whitening composition of the present invention comprises oxidized resveratrol, VC ethyl ether, verbabasin extract and spearmint extract. The present invention aims at stubborn pigment spots such as chloasma, dermal spots and post-inflammatory pigmentation caused by basement membrane zone damage, constructs an "inhibition-clearance-protection-repair" system, and performs multi-target repair. BRIEF DESCRIPTION OF THE DRAWINGS

[0027] Figure 1 It is a comparison chart of the inhibition of zebrafish melanin by the whitening compositions of the blank group, Example 1 and Comparative Example 1;

[0028] Figure 2 This is a comparison chart of the use of the facial cream in Application Example 1 and Comparative Application Example 5 (blank control group) at 28 days and 56 days; DETAILED DESCRIPTION

[0030] In order to better illustrate the purpose, technical solutions and advantages of the present invention, the present invention will be further described below in conjunction with specific embodiments.

[0031] The sources of the raw materials used in the following examples and comparative examples are as follows:

[0032] Oxidized resveratrol: the manufacturer is Guangzhou Bochi Biotechnology Co., Ltd.;

[0033] Mullein extract: The manufacturer is Shaanxi Sihai Biotechnology Co., Ltd.

[0034] VC ethyl ether: The manufacturer is DSM of the Netherlands;

[0035] Spearmint extract: The manufacturer is Sichuan Jiuzhouyuan Biotechnology Co., Ltd.

[0036] Unless otherwise specified, other materials, reagents, etc. used in the examples and comparative examples can be obtained from commercial sources.

[0037] Example 1

[0038] A whitening composition containing oxidized resveratrol for deeply lightening spots comprises oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract in a weight ratio of 1.1:1.5:0.7:0.5, wherein the total weight fraction of the oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract is 100 parts.

[0039] Example 2

[0040] A whitening composition containing oxidized resveratrol for deeply lightening spots comprises oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract in a weight ratio of 1:1:0.5:0.8, wherein the total weight fraction of the oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract is 100 parts.

[0041] Example 3

[0042] A whitening composition containing oxidized resveratrol for deeply lightening spots comprises oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract in a weight ratio of 1.2:1:1:0.1, wherein the total weight fraction of the oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract is 100 parts.

[0043] Example 4

[0044] A whitening composition containing oxidized resveratrol for deeply lightening spots comprises oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract in a weight ratio of 0.5:3:4:0.5, wherein the total weight fraction of the oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract is 100 parts.

[0045] Example 5

[0046] A whitening composition containing oxidized resveratrol for deeply lightening spots comprises oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract in a weight ratio of 1.5:1:0.1:1.2, wherein the total weight fraction of the oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract is 100 parts.

[0047] Example 6

[0048] A whitening composition containing oxidized resveratrol for deeply lightening spots comprises oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract in a weight ratio of 0.11:5:1.2:0.01, wherein the total weight fraction of the oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract is 100 parts.

[0049] Example 7

[0050] A whitening composition containing oxidized resveratrol for deeply lightening spots comprises oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract in a weight ratio of 2:1:0.01:2, wherein the total weight fraction of the oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract is 100 parts.

[0051] Comparative Example 1

[0052] The difference between Comparative Example 1 and Example 1 is that: the composition does not add oxidized resveratrol, and VC ethyl ether, verbascosa extract and spearmint extract in a mass ratio of 1.5:0.7:0.5 are used to make up for the missing amount.

[0053] Comparative Example 2

[0054] The difference between Comparative Example 2 and Example 1 is that: VC ethyl ether is not added to the composition, and oxidized resveratrol, verbascosa extract and spearmint extract are used in a weight ratio of 1.1:0.7:0.5 to make up for the missing amount.

[0055] Comparative Example 3

[0056] The difference between Comparative Example 3 and Example 1 is that: the composition does not add the mullein extract, and uses oxidized resveratrol, VC ethyl ether and spearmint extract in a weight ratio of 1.1:1.5:0.5 to make up for the missing amount.

[0057] Comparative Example 4

[0058] The difference between Comparative Example 4 and Example 1 is that: the composition does not add spearmint extract, and uses oxidized resveratrol, VC ethyl ether and mullein extract in a weight ratio of 1.1:1.5:0.7 to make up for the missing amount. Test Example 1: Experiment on Inhibition of Collagen Degradation and Inflammatory Factor Production

[0059] This test directly verifies the repairing effect of the composition on the basement membrane zone of the epidermal junction layer by detecting the inhibition rate of the composition on the collagen degrading enzyme MMP-1 and the inflammatory factor TNF-α in dermal fibroblasts. The basement membrane zone contains a large amount of collagen. After being irradiated by UV, matrix metalloproteinases will be produced to degrade collagen. At the same time, inflammatory factors caused by UV irradiation will also cause damage to the basement membrane zone. By inhibiting collagen degradation and the production of inflammatory factors, the basement membrane zone of the skin can be prevented from being damaged and repaired, and the production of melanin and melanin particles from entering the dermis can be prevented. The specific test method is as follows:

[0060] 1. Materials and Reagents

[0061] Cell line: human skin fibroblast HSF (Jin Shaoyuan Biotechnology Co., Ltd.); culture medium: DMEM high-glucose culture medium containing 10% fetal bovine serum (Gibco).

[0062] Reagents: human matrix metalloproteinase 1 (MMP-1) ELISA kit (Shanghai ELISA Biologicals, catalog number: ml038199), human tumor necrosis factor α (TNF-α) ELISA kit (Shanghai ELISA Biologicals, catalog number: ml077385), phosphate buffered saline (PBS, pH 7.4).

[0063] Instrument: UVA irradiation lamp (irradiation dose 20mJ / cm 2 ), 96-well cell culture plates, CO 2 Incubator (37±1℃, humidity 90±5%, 5v / v%CO 2 ).

[0064] 2. Experimental Grouping

[0065] Control group: culture medium without adding test samples.

[0066] Sample group: culture medium containing 0.1 wt % of the whitening composition of Examples 1-7 and Comparative Examples 1-4, respectively.

[0067] 3. Test steps

[0068] (1) Cell culture: Human fibroblast HSF cells were revived, centrifuged and resuspended in DMEM culture medium containing 10% fetal bovine serum. The cell suspension was inoculated into a 96-well plate at a density of 2000 cells / well, and 100 μL of culture medium was added to each well. Place in a CO 2 Culture in an incubator for 24 h to ensure that the cells adhere to the wall and grow.

[0069] (2) UVA irradiation modeling: Aspirate the original culture medium and add 100 μL PBS solution to each well. Irradiate the cells with a UVA lamp at a dose of 20 mJ / cm 2 , simulating UV damage. After irradiation, PBS was immediately discarded to avoid residual residues affecting subsequent experiments.

[0070] (3) Sample treatment: Divided into a control group and a sample group, the control group: add 100 μL of fresh culture medium to each well. The sample group: add 100 μL of culture medium containing 0.1 wt% of the whitening composition to each well. The control group and the sample group are cultured for 48 hours to allow the cells to fully respond to the sample.

[0071] (4) Index detection:

[0072] ① Determination of MMP-1 content: Lyse cells according to the kit instructions, collect supernatant, detect absorbance at 450 nm by ELISA, and calculate MMP-1 concentration (pg / mL).

[0073] ② TNF-α content determination: Detect TNF-α concentration (pg / mL) using the same method as above.

[0074] The MMP-1 inhibition rate and TNF-α inhibition rate were calculated according to the following calculation method. The higher the inhibition rate, the better the effect of the composition in repairing the basement membrane zone and preventing the basement membrane zone from being damaged.

[0075]

[0076] Specific data are shown in Table 1. Result judgment: The higher the inhibition rate, the more significant the protective and repairing effect of the composition on basement membrane damage. Test Example 2: Experiment on inhibiting zebrafish melanin production

[0077] The genes related to pigmentation in zebrafish are highly similar to those in humans in terms of sequence and regulatory mechanism, and are transparent throughout, making them suitable for observation under a microscope. Therefore, they are often used as a substitute for human melanin inhibition experiments. This test directly verifies the inhibitory effect of the composition on melanin production in the body by detecting the inhibition rate of the composition on melanin in zebrafish. Both dermal and epidermal spots are caused by the accumulation of melanin. Therefore, the higher the inhibition rate of the composition on melanin, the better the improvement of spots. The specific test method is as follows:

[0078] 1. Materials and Reagents

[0079] Biological materials: zebrafish embryos 6h-8h after fertilization (selection criteria: normal morphology, developed to the blastocyst stage);

[0080] Reagents: zebrafish embryo culture medium (containing methyl blue for fungal protection), phenylthiourea solution (PTU, concentration 1.5 mg / mL, used to inhibit melanocyte migration), whitening composition test samples of Examples 1-7 and Comparative Examples 1-4 (mass concentration 10 wt%, dissolved in fish embryo culture medium);

[0081] Embryo culture medium for zebrafish: weigh 2940 mg of anhydrous calcium chloride, 1233 mg of magnesium sulfate heptahydrate, 630 mg of sodium bicarbonate, 55 mg of potassium chloride, and 1 g of methyl blue and dissolve them in 10 L of water. The pH value is 6.5-8.5, and all chemicals are of analytical grade.

[0082] 2. Experimental Grouping

[0083] Blank group: 200 μL embryo culture medium;

[0084] Control group: 200 μL embryo culture medium containing 1.5 mg / mL PTU;

[0085] Sample group: 200 μL embryo culture medium containing (1.5 mg / mL PTU + 10 wt % whitening composition);

[0086] 3. Operation steps

[0087] (1) Embryo culture: Healthy zebrafish embryos were collected 6-8 hours after fertilization, washed and transferred to 24-well plates. 200 μL of the corresponding treatment solution (blank group, control group and sample group) was added to each well, with at least 12 embryos in each group. The embryos were placed in a constant temperature incubator at 28°C with a light cycle of 14 h light / 10 h dark, and cultured to 48 hpf (hours embryonic age).

[0088] (2) Sample preparation and photography:

[0089] Embryo fixation: Use forceps to gently peel off the embryo's chorion to avoid damaging the fish body.

[0090] Position adjustment: Place the embryo on a glass slide with its back facing upward and add 3% methylcellulose to cover it for fixation.

[0091] Microscopic imaging: Shot with uniform parameters using a stereo microscope.

[0092] (3) Quantitative analysis of melanin

[0093] Image import: Open the captured image with Image J and convert it to 8-bit grayscale format.

[0094] Region marking: Manually circle the embryo head and the dorsal region of the yolk (avoiding the yolk sac extension).

[0095] Intensity measurement: Calculate the average gray value of pixels in the selected area as the melanin content index (MCI).

[0096] The zebrafish melanin inhibition rate is calculated according to the following calculation method. The higher the inhibition rate, the better the effect of the composition in inhibiting melanin production and improving spots;

[0097] The calculation is as follows:

[0098] Results: The higher the inhibition rate, the stronger the ability of the composition to inhibit melanin production. See Table 1 for specific data and the comparison chart of zebrafish melanin inhibition. Figure 1 .

[0099] Table 1 Test results of whitening compositions of each group

[0100]

[0101]

[0102] Combination Figure 1 It can be seen that compared with the blank group and comparative example 1, the zebrafish melanin in Example 1 is significantly reduced, indicating that the whitening composition of Example 1 has an effect of inhibiting melanin compared with the blank group and comparative example 1.

[0103] As can be seen from Table 1, combined with the data of Example 1 and Comparative Examples 1-4, the composition of Example 1, which is a compound of four ingredients including oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract, has a significantly improved effect on the MMP inhibition rate, TNF-α inhibition rate and melanin inhibition rate compared with the compositions of Comparative Examples 1-4, which are a compound of three ingredients including oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract. This indicates that the four ingredients including oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract can synergistically inhibit collagen degradation and the production of inflammatory factors, prevent damage to the basement membrane zone of the skin and repair the basement membrane zone, and prevent the production of melanin and melanin particles from entering the dermis. This may be because oxidized resveratrol has three effects. First, it inhibits the activity of human tyrosinase, directly blocks the production of melanin, and downregulates the expression of premelanosome protein (PMEL) to reduce the formation of melanosome structure. Secondly, it inhibits the cross-linking of advanced glycation end products (AGEs) with type IV collagen, increases the thickness of the basement membrane zone, repairs the true epidermal structure barrier, and blocks the penetration of melanin into the dermis. Finally, it also has a photoprotective effect, preventing melanocytes from being stimulated by ultraviolet rays to produce melanosomes. VC ethyl ether can scavenge free radicals to reduce the damage of oxidative stress to the basement structure, and promote the regeneration of type I and type IV collagen in the basement membrane zone, increasing the density of collagen fibers. At the same time, its water-oil biphilic properties can promote the penetration of other ingredients, allowing them to penetrate deep into the skin to repair the basement membrane zone. Mullein extract has the effect of preventing UV damage and blocking the transmission of light signals, and can also achieve an instant brightening effect by absorbing ultraviolet rays. On the one hand, the extract of angelica sinensis can cooperate with oxidized resveratrol to inhibit the formation of melanin, and on the other hand, it can cooperate with VC ethyl ether to scavenge free radicals and anti-glycation. It also has anti-inflammatory and soothing effects, which can repair barrier damage and strengthen the basement membrane zone.

[0104] Combined with the data of Examples 1-7, it can be seen that when the weight ratio of oxidized resveratrol, VC ethyl ether, verbascosa extract and spearmint extract is (1-5):(1-3):(1-2):(0.1-0.3), the composition has better effects on repairing and whitening the skin.

[0105] Application Example 1-7 and Comparative Application Example 1-4

[0106] The whitening compositions of Examples 1-7 and Comparative Examples 1-4 were added to the facial cream at a concentration of 3 wt % to obtain the facial creams of Application Examples 1-7 and Comparative Application Examples 1-4. The formulas are shown in Table 2.

[0107] The preparation method of the essence of Application Examples 1-7 and Comparative Application Examples 1-4 comprises the following steps:

[0108] The preparation method of the facial cream comprises the following steps:

[0109] S1. Mix a moisturizer, a thickener and 1 / 2 amount of deionized water, homogenize at 80°C to obtain an emulsion, then add an emulsifier and stir evenly to obtain an emulsion;

[0110] S2. When the temperature of the emulsion in S1 drops to 60° C., add a preservative. When the system temperature drops to 40° C., add the components of the whitening composition, the essence and the remaining deionized water, stir evenly, and finally add a pH adjuster to adjust the pH to 6 to obtain the facial cream.

[0111] Table 2 Cream formulas of application examples 1-7 and comparative application examples 1-4

[0112]

[0113]

[0114] Comparative Application Example 5

[0115] The facial cream of comparative application example 5 does not contain the whitening composition, and uses an equal amount of deionized water to replace the composition. The preparation method is the same as that of application example 1.

[0116] Test Example 3: Efficacy test of facial cream

[0117] This test example verifies the anti-aging and barrier repair effects of the creams of Application Examples 1-7 and Comparative Application Examples 1-5. The experimental data are shown in Table 3.

[0118] Diagnostic criteria: in accordance with the clinical diagnostic criteria of "Clinical Diagnosis and Efficacy Criteria for Chloasma (2003 Revised Draft)" formulated by the Pigment Disease Group of the Dermatology and Venereology Committee of the Chinese Association of Integrated Traditional Chinese and Western Medicine: ① Light brown to dark brown patches on the face with clear boundaries, symmetrical distribution, no inflammatory reaction, and no scaling; ② No obvious subjective symptoms; ③ The condition is seasonal, with severity in summer and milder in winter; ④ Pigmentation caused by diseases such as Reye's melanosis and pigmented actinic planus is excluded.

[0119] Inclusion criteria: According to the "Technical Specifications for Safety of Cosmetics" (2015), 60 women aged 50-65 years diagnosed with symmetrical facial melasma by dermatologists were selected and randomly divided into 12 groups, 5 people in each group. Under normal circumstances, volunteers use the product on their entire face. Each volunteer takes 1g of cream and applies it to the face twice a day, massaging it for absorption. Volunteers used instruments to quantify the improvement of facial indicators in an air-conditioned room with a temperature of 21±1℃ and a humidity of 50±10%, and used VISIA-CR to take high-definition facial images. The test time was before use, 28 days after use, and 56 days after use:

[0120] Melasma severity (MASI): Quantitative assessment is performed based on the area (A), color depth (D), and color uniformity (H) of melasma. Forehead (F) 30%, right cheek (MR) 30%, left cheek (ML) 30%, and mandible (C) 10%. The severity and area of ​​melasma are assessed based on the proportion of pigment in these four areas.

[0121] Color depth rating: 0 none, 1 slight, 2 mild, 3 moderate, 4 severe;

[0122] The homogeneity score was: 0 none, 1 slight, 2 mild, 3 significant, 4 maximum;

[0123] Melasma area scoring: 0% is 0; <10% is 1; 10%-29% is 2; 30%-49% is 3; 50%-69% is 4; 70%-89% is 5; >90% is 6.

[0124] Forehead score = 0.3 × (D + H) × A;

[0125] Right cheek score = 0.3 × (D + H) × A;

[0126] Left cheek score = 0.3 × (D + H) × A;

[0127] Mandibular score = 0.1 × (D + H) × A;

[0128] MASI total score = the sum of the above scores.

[0129] Melasma color: Use the Mexameter MX 18 probe to randomly measure 3 points at the center and edge of the spot and record the melanin data;

[0130] Skin barrier: Tewameter TM Hex transepidermal water loss instrument was used to measure the transepidermal water loss TEWL value at the zygomatic position.

[0131] The calculation formula is as follows:

[0132] Melasma improvement rate = (MASI 使用前 -MASI 使用后 ) / MASI 使用前 ×100%;

[0133] Chloasma color improvement rate = (chloasma color area 使用前 - Melasma color area 使用后 ) / Chloasma color area 使用前 ×100%;

[0134] TEWL value improvement rate = (TEWL value 使用后 -TEWL value 使用前 ) / TEWL value使用前 ×100%; the calculation results are shown in Table 2, and the comparison chart of the subjects is shown in Figure 2 .

[0135] Table 2 Human test results of each group of facial creams

[0136]

[0137]

[0138] The whitening effect of the application example is expressed by the improvement rate of MASI of melasma severity and the improvement rate of melasma color, and the repair effect on barrier damage is expressed by the improvement rate of TEWL value.

[0139] Depend on Figure 2 It can be seen that after 28 days of use, the facial cream of Application Example 1 has a significantly improved effect on fading chloasma under the eyes of the test subjects' foreheads compared with that of Comparative Application Example 5, indicating that the facial cream with the whitening composition added has good whitening, freckle removal and repairing effects.

[0140] It can be seen from the data of Application Example 1 and Comparative Application Examples 1-5 in Table 2 that the composition of Example 1, which is a compound of four ingredients including oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract, has significantly improved effects on whitening and freckle removal and barrier repair than the compositions of Comparative Examples 1-5, indicating that the four ingredients, oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract, can synergistically repair the basement membrane zone, improve the skin's resistance to external stimuli such as ultraviolet rays, avoid the risk of skin damage such as inflammation and oxidative stress, and can also affect the synthesis and metabolism of melanin, reduce the formation of stubborn spots and fade the stubborn spots that have already formed.

[0141] Combined with the data of Application Examples 1-7, it can be seen that when the weight ratio of oxidized resveratrol, VC ethyl ether, verbascosa extract and spearmint extract is (1-1.2):(1-2):(0.5-0.8):(0.1-0.8), the barrier repair and anti-aging effects of the composition are better.

[0142] In summary, the whitening composition of the present invention can prevent damage to the basement membrane zone of the skin and repair the basement membrane zone by the synergistic effect of the four ingredients of oxidized resveratrol, VC ethyl ether, verbascosa extract and spearmint extract, by inhibiting collagen degradation and the production of inflammatory factors, and prevent the production of melanin and melanin particles from entering the dermis, thereby achieving a synergistic repair and whitening and freckle removal effect.

[0143] Finally, it should be noted that the above embodiments are only used to illustrate the technical solution of the present invention rather than to limit the scope of protection of the present invention. Although the present invention has been described in detail with reference to the preferred embodiments, those skilled in the art should understand that the technical solution of the present invention can be modified or replaced by equivalents without departing from the essence and scope of the technical solution of the present invention.

Claims

1. A whitening composition containing oxidized resveratrol for deep lightening of pigmentation, characterized in that: The invention comprises the following components: oxidized resveratrol, VC ethyl ether, verbabasin extract and spearmint extract, wherein the weight ratio of the oxidized resveratrol, VC ethyl ether, verbabasin extract and spearmint extract is (0.11-2):(1-5):(0.01-1.2):(0.01-2).

2. The whitening composition for deeply lightening spots containing oxidized resveratrol according to claim 1, characterized in that: The weight ratio of the oxidized resveratrol, VC ethyl ether, verbabasin extract and spearmint extract is (0.5-1.5):(1-3):(0.1-1):(0.1-1.2).

3. The whitening composition for deeply lightening pigmentation spots containing oxidized resveratrol according to claim 1, characterized in that: The weight ratio of the oxidized resveratrol, VC ethyl ether, verbabasin extract and spearmint extract is (1-1.2):(1-2):(0.5-0.8):(0.1-0.8).

4. Use of the whitening composition for deeply lightening spots containing oxidized resveratrol according to any one of claims 1 to 3 in the preparation of cosmetics.

5. Use of the whitening composition for deeply lightening spots containing oxidized resveratrol as claimed in claim 4 in the preparation of cosmetics, characterized in that: The cosmetics are lotions, emulsions, creams, facial masks, essences or sprays, and the added amount of the composition is 1%-3% of the total weight of the cosmetics.

6. A facial cream, characterized in that: The invention comprises the following raw materials in weight percentage: 0.5%-5% of the whitening composition according to any one of claims 1 to 3, 0.05%-0.3% of a thickener, 0.5%-1% of a moisturizer, 1-10% of an emulsifier, 0.5%-3% of a preservative, 0.01%-0.3% of a pH regulator and 0.01%-1% of an essence, and the balance is deionized water.

7. The facial cream according to claim 6, characterized in that The raw material is selected from at least one of (a) to (e): (a) the thickener comprises at least one of xanthan gum, carbomer, hydroxyethyl acrylate / sodium acryloyldimethyl taurate copolymer, ammonium acryloyldimethyl taurate / VP copolymer, sclerotium gum and cetyl alcohol; (b) the moisturizing agent comprises at least one of allantoin, sodium polyacrylate, hydrogenated lecithin, betaine, β-glucan, trehalose, caprylyl glycol, dipropylene glycol, sodium hyaluronate, 1,2-butylene glycol, glycerol, budding pullulan polysaccharide and ceramide; (c) the pH adjusting agent comprises at least one of arginine, sodium hydroxide and EDTA-2Na; (d) the preservative comprises at least one of 1,2-propylene glycol, 1,2-hexanediol and p-hydroxyacetophenone; (e) The emulsifier is at least one of dimethiconol, propylheptyl octanoate, PEG / PPG-14 / 7 dimethyl ether and polymethylsilsesquioxane.

8. The method for preparing the facial cream according to claim 7, characterized in that: The following steps are involved: S1. Mix the moisturizer, thickener and part of deionized water, homogenize at 75-85°C to obtain the aqueous phase, then add the emulsifier and stir evenly to obtain an emulsion; S2. When the temperature of the emulsion in S1 drops to 55-65° C., add a preservative, and when the system temperature drops to 35-45° C., add the components of the whitening composition, flavor and remaining deionized water, stir evenly, and finally add a pH adjuster to adjust the pH to obtain the facial cream.

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