An oxygenated white resveratrol-containing deep lightening spot whitening composition and use thereof

By combining oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract, the problem of stubborn pigmentation caused by basement membrane damage was solved, achieving multi-target repair and whitening effects, and enhancing the skin barrier function.

CN120093619BActive Publication Date: 2026-02-03N O D TOPIA (GUANGZHOU) BIOTECHNOLOGY CO LTD
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Patent Information

Application Number
CN202510540031.4
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2025-04-27
Publication Date
2026-02-03
Estimated Expiration
2045-04-27

AI Technical Summary

Technical Problem

Existing whitening ingredients cannot effectively prevent the activation of matrix metalloproteinases induced by ultraviolet rays, which leads to the degradation of collagen in the basement membrane and the inability to repair damage to the basement membrane, resulting in the formation and recurrence of stubborn pigmentation.

Method used

The combination of oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract enhances the skin barrier function by inhibiting tyrosinase activity, providing antioxidant and anti-inflammatory effects, and repairing the basement membrane band.

Benefits of technology

It achieves multi-target repair of stubborn pigmentation, reduces the formation of stubborn pigmentation, enhances the skin's resistance to external stimuli, and significantly fades existing stubborn pigmentation.

✦ Generated by Eureka AI based on patent content.

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Abstract

The present application relates to a kind of white composition containing oxidized white resveratrol and deep lightening spot and its application, the composition includes the following components: oxidized white resveratrol, VC ethyl ether, verbascum thapsus extract and spearmint extract, the weight ratio of the oxidized white resveratrol, VC ethyl ether, verbascum thapsus extract and spearmint extract is (0.11-2):(1-5):(0.01-1.2):(0.01-2).The white composition of the present application is aimed at stubborn spots such as chloasma caused by basement membrane zone injury, dermal spots and post-inflammatory hyperpigmentation, constructs "inhibition-removal-protection-repair" system, and carries out multi-target repair.
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Description

TECHNICAL FIELD

[0001] The present application relates to the technical field of cosmetics, in particular to a deep-fading freckle whitening composition containing oxidized white resveratrol and application thereof. BACKGROUND

[0002] As a key barrier structure between epidermis and dermis, the integrity of the basement membrane zone directly determines the melanin metabolic pathway. Clinical data shows that more than 95% of stubborn freckles such as chloasma, dermal spots and post-inflammatory hyperpigmentation are accompanied by basement membrane zone rupture. This damage mechanism is due to the degradation of collagen IV and laminin in the basement membrane zone. Ultraviolet light activates matrix metalloproteinases (MMP-2 / MMP-9), reducing the thickness of the basement membrane zone by 40%-60%, forming a melanin penetration channel, causing epidermal layer melanocytes to penetrate into the dermal layer through the damaged area, and being phagocytosed by macrophages to form melanophages that are difficult to metabolize. These melanophages can survive in the dermal layer for several years, forming visible blue-gray patches, which is the core reason why traditional whitening methods cannot eradicate stubborn freckles. At the same time, the basement membrane has certain permeability and barrier function, and is an important part of the skin barrier. If the basement membrane zone is damaged, the skin barrier function is reduced, and the resistance to external stimuli such as ultraviolet light is weakened. This increases the risk of skin damage by inflammation, oxidative stress, etc., thereby indirectly affecting the synthesis and metabolism of melanin, and promoting the production of stubborn chloasma.

[0003] Although existing whitening ingredients such as arbutin and kojic acid can inhibit tyrosinase activity, they only act on the epidermal melanin production link and do not repair the skin basement membrane zone. Studies have shown that the recurrence rate of freckles treated with a single tyrosinase inhibitor is as high as 38%-65%, and the fundamental defect is: ① unable to prevent the continuous activation of matrix metalloproteinases MMPs induced by ultraviolet light, and the degradation of basement membrane zone collagen is not intervened; ② without repairing the basement membrane zone, so that melanin can fall into the dermis to form stubborn freckles; ③ ignoring the vicious cycle of inflammation factors (such as IL-6, TNF-α) stimulating epidermal melanocytes through the damaged basement membrane. SUMMARY

[0004] The purpose of the present application is to overcome the shortcomings of the prior art and provide a deep-fading freckle whitening composition containing oxidized white resveratrol and application thereof.

[0005] To achieve the above-mentioned purpose, the technical scheme adopted by the present application is:

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

[0007] Oxidized resveratrol, a stable derivative of resveratrol, functions primarily by inhibiting tyrosinase activity to block melanin production. It also possesses antioxidant and anti-inflammatory properties, scavenging free radicals and mitigating UV-induced oxidative stress. 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 simultaneously activating collagen synthesis pathways to improve skin elasticity. Its hydrophilic and lipophilic properties make it easier to penetrate the stratum corneum, resulting in excellent performance in anti-aging and skin brightening.

[0009] Verbena extract offers protection against photodamage and immediate brightening effects. This is because its high content of verbascoside absorbs blue / ultraviolet light and converts it into visible light through quantum leaps, reducing photo-induced tyrosinase activation and directly inhibiting melanin oxidation. Furthermore, its rich flavonoid content promotes barrier lipid synthesis, enhancing the skin's resistance to external stimuli, complementing the barrier repair function of oxidized resveratrol.

[0010] Spearmint extract contains rosmarinic acid, which can inhibit the formation of AGEs during glycation and reduce dullness caused by collagen fiber cross-linking. Studies show that spearmint extract can reduce the accumulation of skin glycation products, synergistically working with the anti-glycation effect of VC ethyl ether. Furthermore, its antibacterial properties can alleviate inflammation in sensitive skin, reduce the risk of inflammatory hyperpigmentation, and regulate the skin's microecological balance, enhancing the gentleness of the formula and making it suitable for sensitive skin.

[0011] The oxidized resveratrol in the composition of this invention has three main effects: First, it inhibits human tyrosinase activity, directly blocking melanin production, and simultaneously downregulates premelanosome protein (PMEL) expression, reducing melanosome structure formation; second, it increases the thickness of the basement membrane by inhibiting the cross-linking of advanced glycation end products (AGEs) with type IV collagen, repairing the dermal-epidermal barrier structure and blocking melanin penetration into the dermis; finally, it also has a photoprotective effect, preventing melanocytes from producing melanosomes under ultraviolet stimulation. VC ethyl ether can scavenge free radicals to reduce oxidative stress damage to the basement membrane structure and promote the regeneration of type I and type IV collagen in the basement membrane, increasing collagen fiber density. Its amphiphilic properties also promote the penetration of other ingredients, allowing them to deeply repair the basement membrane. Verbena officinalis extract has the effect of preventing UV damage and blocking light signal transmission, and can also achieve an immediate brightening effect by absorbing ultraviolet light. Spearmint extract can synergistically inhibit melanin formation with resveratrol, and also scavenge free radicals and exert anti-glycation effects with VC ethyl ether. It also possesses anti-inflammatory and soothing properties, repairing barrier damage and strengthening the basement membrane. Therefore, this invention utilizes four ingredients—resveratrol, VC ethyl ether, mullein extract, and spearmint extract—to synergistically repair the skin's basement membrane, thereby reducing the formation of stubborn pigmentation and fading existing stubborn pigmentation.

[0012] Preferably, the weight ratio of oxidized resveratrol, VC ethyl ether, mullein 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 oxidized resveratrol, VC ethyl ether, mullein 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 the application of the whitening composition containing oxidized resveratrol for deep fading of pigmentation in the first aspect in the preparation of cosmetics.

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

[0016] Thirdly, the present invention provides a face cream comprising the following ingredients by weight percentage: 0.5%-5% of the whitening composition of 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 adjuster, and 0.01%-1% of a fragrance, with the balance 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 moisturizer comprises at least one of allantoin, sodium polyacrylate, hydrogenated lecithin, betaine, β-glucan, trehalose, caprylyl glycol, dipropylene glycol, sodium hyaluronate, 1,2-butanediol, glycerin, budding stalk polysaccharide, 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 polydimethylsiloxane alcohol, propyl heptyl octanoate, PEG / PPG-14 / 7 dimethyl ether, and polymethylsilsesquioxane.

[0022] Fourthly, the present invention provides a method for preparing the face cream of the third aspect, comprising the following steps:

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

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

[0025] Compared with the prior art, the beneficial effects of the present invention are as follows:

[0026] The whitening composition of the present invention comprises oxidized resveratrol, VC ethyl ether, mullein extract, and spearmint extract. The present invention constructs an "inhibition-clearance-protection-repair" system for multi-target repair targeting stubborn pigmentation such as melasma, dermal melasma, and post-inflammatory hyperpigmentation caused by basement membrane damage. Attached Figure Description

[0027] Figure 1 Comparative graph showing the inhibition of melanin in zebrafish by the whitening compositions of the blank group, Example 1, and Comparative Example 1.

[0028] Figure 2 The graph shows the comparison of face cream usage over 28 and 56 days in Application Example 1 and Comparative Application Example 5 (blank control group). Detailed Implementation

[0029] 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.

[0030] The sources of the raw materials used in the following examples and comparative examples are as follows:

[0031] Oxidized resveratrol: Manufacturer: Guangzhou Bochi Biotechnology Co., Ltd.

[0032] Verbena officinalis extract: manufactured by Shaanxi Sihai Biotechnology Co., Ltd.

[0033] VC ethyl ether: manufactured by DSM, Netherlands;

[0034] Spearmint extract: manufactured by Sichuan Jiuzhouyuan Biotechnology Co., Ltd.

[0035] Unless otherwise specified, all other materials, reagents, etc. used in the examples and comparative examples are commercially available.

[0036] Example 1

[0037] A whitening composition for deep fading of pigmentation containing oxidized resveratrol, comprising 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 mass fraction of oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract is 100 parts.

[0038] Example 2

[0039] A whitening composition for deep fading of pigmentation containing oxidized resveratrol, comprising oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract in a weight ratio of 1:1:0.5:0.8, wherein the total mass fraction of oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract is 100 parts.

[0040] Example 3

[0041] A whitening composition for deep fading of pigmentation containing oxidized resveratrol, comprising oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract in a weight ratio of 1.2:1:1:0.1, wherein the total mass fraction of oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract is 100 parts.

[0042] Example 4

[0043] A whitening composition for deep fading of pigmentation containing oxidized resveratrol, comprising oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract in a weight ratio of 0.5:3:4:0.5, wherein the total mass fraction of oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract is 100 parts.

[0044] Example 5

[0045] A whitening composition for deep fading of pigmentation containing oxidized resveratrol, comprising 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 mass fraction of oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract is 100 parts.

[0046] Example 6

[0047] A whitening composition for deep fading of pigmentation containing oxidized resveratrol, comprising 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 mass fraction of oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract is 100 parts.

[0048] Example 7

[0049] A whitening composition for deep fading of pigmentation containing oxidized resveratrol, comprising oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract in a weight ratio of 2:1:0.01:2, wherein the total mass fraction of oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract is 100 parts.

[0050] Comparative Example 1

[0051] The difference between Comparative Example 1 and Example 1 is that: no oxidized resveratrol was added to the composition, and the missing amount was made up by VC ethyl ether, mullein extract and spearmint extract in a mass ratio of 1.5:0.7:0.5.

[0052] Comparative Example 2

[0053] The difference between Comparative Example 2 and Example 1 is that the composition does not contain VC ethyl ether, and the missing amount is made up by oxidized resveratrol, mullein extract and spearmint extract in a weight ratio of 1.1:0.7:0.5.

[0054] Comparative Example 3

[0055] The difference between Comparative Example 3 and Example 1 is that the composition does not contain mullein extract, and the missing amount is made up by oxidized resveratrol, VC ethyl ether and spearmint extract in a weight ratio of 1.1:1.5:0.5.

[0056] Comparative Example 4

[0057] The difference between Comparative Example 4 and Example 1 is that: no spearmint extract was added to the composition, and the missing amount was made up by oxidized resveratrol, VC ethyl ether and mullein extract in a weight ratio of 1.1:1.5:0.7.

[0058] Test Example 1: Experiment on Inhibiting Collagen Degradation and Inflammatory Factor Production

[0059] This test directly verifies the repair effect of the composition on the basement membrane of the dermal-epidermal junction by detecting the inhibition rates of the composition on the collagen-degrading enzyme MMP-1 and the inflammatory factor TNF-α in dermal fibroblasts. The basement membrane contains a large amount of collagen, which is degraded by matrix metalloproteinases after UV irradiation. Simultaneously, inflammatory factors induced by UV irradiation also damage the basement membrane. By inhibiting collagen degradation and the production of inflammatory factors, damage to the skin's basement membrane can be prevented and repaired, preventing the production of melanin and the entry of melanin granules into the dermis. The specific test method is as follows:

[0060] 1. Materials and Reagents

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

[0062] Reagents: Human matrix metalloproteinase 1 (MMP-1) ELISA kit (Shanghai Enzyme-Linked Biotechnology, catalog number: ml038199), Human tumor necrosis factor α (TNF-α) ELISA kit (Shanghai Enzyme-Linked Biotechnology, catalog number: ml077385), Phosphate buffer (PBS, pH 7.4).

[0063] Instruments: UVA irradiation lamp (irradiation dose 20 mJ / cm²), 96-well cell culture plate, Incubator (37±1℃, 90±5% humidity, 5v / v%) ).

[0064] 2. Experimental Grouping

[0065] Control group: Culture medium without test samples.

[0066] Sample groups: culture media containing 0.1 wt% of the whitening compositions of Examples 1-7 and Comparative Examples 1-4, respectively.

[0067] 3. Testing Procedures

[0068] (1) Cell Culture: Human fibroblasts (HSF) were resuscitated, centrifuged, and resuspended in DMEM medium containing 10% fetal bovine serum. The cell suspension was seeded into 96-well plates at a density of 2000 cells / well, with 100 μL of culture medium added to each well. Incubate in an incubator for 24 hours to ensure cell adhesion and growth.

[0069] (2) UVA radiation modeling: Discard the original culture medium and add 100 μL of PBS solution to each well. Irradiate the cells with a UVA lamp at a dose of 20 mJ / cm² to simulate ultraviolet damage. Discard the PBS immediately after irradiation to avoid residue affecting subsequent experiments.

[0070] (3) Sample treatment: The samples were divided into a control group and a sample group. Control group: 100 μL of fresh culture medium was added to each well. Sample group: 100 μL of culture medium containing 0.1 wt% whitening composition was added to each well. The control group and the sample group were cultured for 48 h to allow the cells to fully respond to the effects of the sample.

[0071] (4) Indicator detection:

[0072] ①MMP-1 content determination: Cells were lysed according to the kit instructions, and the supernatant was collected. The absorbance at 450 nm was measured by ELISA, and the MMP-1 concentration (pg / mL) was calculated.

[0073] ② TNF-α content determination: The concentration of TNF-α (pg / mL) was detected by the same method as above.

[0074] The MMP-1 inhibition rate and TNF-α inhibition rate were calculated according to the following method. The higher the inhibition rate, the better the composition is in repairing the basement membrane and preventing basement membrane damage.

[0075] ;

[0076] Specific data are shown in Table 1. Result interpretation: A higher inhibition rate indicates a more significant protective and repairing effect of the composition on basement membrane damage.

[0077] Test Example 2: Experiment on Inhibiting Zebrafish Melanin Production

[0078] The pigmentation-related genes in zebrafish are highly similar to those in humans in terms of sequence and regulatory mechanisms. Furthermore, zebrafish are transparent and easily observed under a microscope, making them a common substitute for human melanin inhibition experiments. This test directly verifies the inhibitory effect of the composition on melanin production in vivo by detecting its inhibition rate on melanin in zebrafish. Both dermal and epidermal pigmentation are caused by melanin accumulation. Therefore, the higher the inhibition rate of the composition on melanin, the better the improvement in pigmentation. The specific test method is as follows:

[0079] 1. Materials and Reagents

[0080] Biological material: zebrafish embryos 6-8 hours after fertilization (selection criteria: normal morphology, developed to the blastocyst stage);

[0081] Reagents: Zebrafish embryo culture medium (containing methylene blue for antifungal purposes), phenylthionamide solution (PTU, concentration 1.5 mg / mL, used to inhibit melanocyte migration), and whitening composition test samples of Examples 1-7 and Comparative Examples 1-4 (mass concentration 10 wt%, dissolved in fish embryo culture medium).

[0082] Zebrafish embryo culture medium: Prepared by dissolving 2940mg anhydrous calcium chloride, 1233mg magnesium sulfate heptahydrate, 630mg sodium bicarbonate, 55mg potassium chloride, and 1g methylene blue in 10L of water. The pH value is 6.5-8.5. All chemicals are of analytical grade.

[0083] 2. Experimental Grouping

[0084] Control group: 200 μL embryo culture medium;

[0085] Control group: 200 μL of embryo culture medium containing 1.5 mg / mL PTU;

[0086] Sample group: 200 μL of embryo culture medium containing (1.5 mg / mL PTU + 10 wt% whitening composition);

[0087] 3. Operating Procedures

[0088] (1) Embryo culture: Healthy zebrafish embryos were collected 6-8 h 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 plates were placed in a constant temperature incubator at 28℃ with a light cycle of 14 h light / 10 h dark, and cultured until 48 hpf (hourly embryonic age).

[0089] (2) Sample preparation and photography:

[0090] Embryo fixation: Gently peel off the chorionic membrane of the embryo with tweezers to avoid damaging the fish.

[0091] Positioning adjustment: Place the embryo on a glass slide with its back facing up, and cover it with 3% methylcellulose to fix it in place.

[0092] Microscopic imaging: Images were taken using a stereomicroscope with uniform parameters.

[0093] (3) Quantitative analysis of melanin

[0094] Image import: Open the captured image using ImageJ and convert it to 8-bit grayscale format.

[0095] Region marking: Manually delineate the head and back of the yolk sac (avoiding the extension of the yolk sac).

[0096] Intensity measurement: Calculate the average gray value of pixels within the selected area as the melanin content index (MCI).

[0097] The zebrafish melanin inhibition rate was calculated using the following method. A higher inhibition rate indicates that the composition has a better effect on inhibiting melanin production and improving pigmentation.

[0098] The calculation method is as follows:

[0099] Results: A higher inhibition rate indicates a stronger ability of the composition to inhibit melanin production. Specific data are shown in Table 1, and the zebrafish melanin inhibition comparison chart is shown below. Figure 1 .

[0100] Table 1. Test results of whitening compositions in each group

[0101] Group MMP-1 inhibition rate (%) TNF-α inhibition rate (%) Melanin inhibition rate (%) Example 1 71.52 53.65 42.32 Example 2 69.28 49.62 38.82 Example 3 69.53 49.07 38.81 Example 4 66.15 46.90 35.15 Example 5 66.45 46.25 35.56 Example 6 62.19 42.78 31.75 Example 7 62.24 42.21 32.90 Comparative Example 1 23.20 12.31 11.35 Comparative Example 2 21.07 14.40 12.01 Comparative Example 3 22.41 14.97 11.96 Comparative Example 4 21.79 12.81 11.55

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

[0103] As shown in Table 1, and combining the data from Example 1 and Comparative Examples 1-4, the combination of the four components—oxygenated resveratrol, VC ethyl ether, mullein extract, and spearmint extract—significantly improved the MMP inhibition rate, TNF-α inhibition rate, and melanin inhibition rate compared to the combinations of the four components in Comparative Examples 1-4, which used only three of the four components. This indicates that the four components—oxygenated resveratrol, VC ethyl ether, mullein extract, and spearmint extract—can synergistically inhibit collagen degradation and the production of inflammatory factors, prevent damage to the skin's basement membrane, repair the basement membrane, and prevent the production of melanin and the entry of melanin granules into the dermis. This is likely because oxidized resveratrol has three main effects: first, it inhibits human tyrosinase activity, directly blocking melanin production, and simultaneously downregulates premelanosome protein (PMEL) expression, reducing melanosome structure formation; second, it increases the thickness of the basement membrane by inhibiting the cross-linking of advanced glycation end products (AGEs) and type IV collagen, repairing the dermal barrier structure and blocking melanin penetration into the dermis; and finally, it has a photoprotective effect, preventing melanocytes from producing melanosomes when stimulated by ultraviolet radiation. VC ethyl ether can scavenge free radicals to reduce oxidative stress damage to the basement membrane structure and promote the regeneration of type I and type IV collagen in the basement membrane, increasing collagen fiber density. Its amphiphilic properties also promote the penetration of other ingredients, allowing them to deeply repair the basement membrane. Mullein extract has the effect of preventing UV damage and blocking light signal transmission, and can also achieve an immediate brightening effect by absorbing ultraviolet radiation. On the one hand, the extract of basil can synergistically inhibit melanin formation with resveratrol, and on the other hand, it can synergistically scavenge free radicals and resist glycation with VC ethyl ether. It also has anti-inflammatory and soothing effects, which can repair barrier damage and strengthen the basement membrane.

[0104] Based on the data from Examples 1-7, it can be seen that when the weight ratio of oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract is (1-5):(1-3):(1-2):(0.1-0.3), the composition has a better effect on skin repair and whitening.

[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 face creams at a concentration of 3 wt% to obtain face creams of Application Examples 1-7 and Comparative Application Examples 1-4. The formulations are shown in Table 2.

[0107] The preparation methods of the face creams in Application Examples 1-7 and Comparative Application Examples 1-4 include the following steps:

[0108] The preparation method of face cream includes the following steps:

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

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

[0111] Table 2. Cream formulations for Application Examples 1-7 and Comparative Application Examples 1-4

[0112]

[0113] Comparative Application Example 5

[0114] The face cream in Comparative Application Example 5 does not contain the whitening composition, but uses an equal amount of deionized water instead of the composition, and the preparation method is the same as in Application Example 1.

[0115] Test Example 3: Efficacy Test of Face Cream

[0116] This test case verifies the anti-aging and barrier-repairing effects of the face creams used in Examples 1-7 and the comparison examples 1-5. The experimental data are shown in Table 3.

[0117] Diagnostic criteria: Meets the clinical diagnostic criteria of the "Clinical Diagnostic and Efficacy Criteria for Melasma (2003 Revised Edition)" formulated by the Pigmentary Diseases Group of the Dermatology and Venereology Committee of the Chinese Association of Integrative Medicine: ① Light brown to dark brown patches on the face, with clear borders, symmetrical distribution, no inflammatory reaction, and no scaling; ② No obvious subjective symptoms; ③ Seasonal disease, worse in summer and milder in winter; ④ Exclusion of pigmentation caused by diseases such as Riehl's melanosis and actinic tinea flatis.

[0118] Inclusion criteria: Sixty women aged 50-65 years diagnosed with symmetrical melasma on the face by a dermatologist were selected according to the *Cosmetic Safety Technical Specifications* (2015) and randomly divided into 12 groups of 5 participants each. Under normal circumstances, volunteers applied the product to their entire face, taking 1g of cream twice a day and massaging it in until absorbed. The improvement of facial indicators was quantified using instruments in an air-conditioned room with a temperature of 21±1℃ and humidity of 50±10%, and high-resolution facial images were captured using VISIA-CR. The test results were collected before use, 28 days after use, and 56 days after use.

[0119] Melasma Severity Index (MASI): Quantitative assessment is performed based on the area (A), depth of color (D), and evenness of color (H) of melasma. The four regions are: forehead (F) 30%, right cheek (MR) 30%, left cheek (ML) 30%, and jawline (C) 10%. The severity and area of ​​melasma are assessed by scoring according to the proportion of pigmentation in each of these four areas.

[0120] Color depth rating: 0 None, 1 Slight, 2 Mild, 3 Moderate, 4 Severe;

[0121] The uniformity score was: 0 None, 1 Slight, 2 Mild, 3 Significant, 4 Maximum;

[0122] Melasma area score: 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.

[0123] Prefrontal cortex score = 0.3 × (D + H) × A;

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

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

[0126] Mandibular score = 0.1 × (D + H) × A;

[0127] MASI Total Score = Sum of the scores above.

[0128] Melasma color: Using a Mexameter MX 18 probe, three points were randomly measured at the center and edge of the melanin spot, and melanin data were recorded;

[0129] Skin barrier: The transcutaneous water loss (TEWL) value at the cheekbone location was measured using the Tewameter™ Hex transcutaneous water loss meter.

[0130] The calculation formula is as follows:

[0131] Melasma improvement rate = (MASI) 使用前 -MASI 使用后 ) / MASI 使用前 ×100%;

[0132] Melasma color improvement rate = (Melasma color area) 使用前 -Area of ​​melasma color 使用后 ) / Area of ​​melasma color 使用前 ×100%;

[0133] 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 subject comparison chart is shown in […]. Figure 2 .

[0134] Table 2. Human trial results for each group of face creams

[0135]

[0136] The whitening effect of the application examples is represented by the improvement rate of the severity of melasma (MASI) and the improvement rate of melasma color, while the repair effect on barrier damage is represented by the improvement rate of TEWL value.

[0137] Depend on Figure 2 It can be seen that after 28 days of use, the face cream in Application Example 1 showed a significant improvement in the fading of melasma on the forehead and under the eyes of the subjects compared with the control application example 5, indicating that the face cream with added whitening composition has good whitening, spot removal and repair effects.

[0138] As shown in Table 2, the data from Application Example 1 and Comparative Application Examples 1-5 indicate that the combination of four ingredients—oxidized resveratrol, VC ethyl ether, mullein extract, and spearmint extract—in Example 1 significantly improved the skin whitening, spot removal, and barrier repair effects compared to the combinations in Comparative Examples 1-5. This demonstrates that these four ingredients can synergistically repair the basement membrane, enhance the skin's resistance to external stimuli such as ultraviolet radiation, avoid the risk of skin damage from inflammation and oxidative stress, and also affect melanin synthesis and metabolism, reducing the formation of stubborn pigmentation and fading existing stubborn pigmentation.

[0139] Based on the data from Application Examples 1-7, it can be seen that when the weight ratio of oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract is (1-1.2):(1-2):(0.5-0.8):(0.1-0.8), the composition has better barrier repair and anti-aging effects.

[0140] In summary, the whitening composition of the present invention, through the synergistic effect of four components—oxidized resveratrol, VC ethyl ether, mullein extract, and spearmint extract—can prevent damage to the skin's basement membrane and repair the basement membrane by inhibiting collagen degradation and the production of inflammatory factors, thereby preventing the production of melanin and the entry of melanin granules into the dermis, thus achieving a synergistic repair and whitening effect.

[0141] 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 composition containing oxidized resveratrol for deep fading of pigmentation, characterized in that, It is composed of the following components: oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract, wherein the weight ratio of oxidized resveratrol, VC ethyl ether, mullein extract and spearmint extract is (1-1.2):(1-2):(0.5-0.8):(0.1-0.8).

2. The application of the whitening composition containing oxidized resveratrol for deep fading of pigmentation as described in claim 1 in the preparation of cosmetics, characterized in that, The cosmetic is a face cream, and the amount of the composition added is 3% of the total weight of the cosmetic.

3. A face cream, characterized in that, The raw materials include the following weight percentages: The whitening composition of claim 1 comprises 3% of the following: 0.05%-0.3% thickener, 0.5%-1% moisturizer, 1-10% emulsifier, 0.5%-3% preservative, 0.01%-0.3% pH adjuster, and 0.01%-1% fragrance, with the balance being deionized water; wherein the thickener is ammonium acryloyl dimethyl taurate / VP copolymer and xanthan gum, the moisturizer is glycerin, butylene glycol, and trehalose, the emulsifier is polydimethylsiloxane alcohol, propyl heptyl octanoate, PEG / PPG-14 / 7 dimethyl ether, and polymethylsilsesquioxane, the preservative is 1,3-propanediol, p-hydroxyacetophenone, and 1,2-hexanediol, and the pH adjuster is arginine.

4. The method for preparing the face cream according to claim 3, characterized in that, Includes the following steps: S1. Mix the humectant, thickener and part of the deionized water, homogenize at 75-85℃ to obtain the aqueous phase, then add the emulsifier and stir evenly to obtain the emulsion. S2. When the temperature of the emulsion in S1 drops to 55-65℃, add the preservative. When the system temperature drops to 35-45℃, add the components of the whitening composition, fragrance and remaining deionized water, stir evenly, and finally add pH adjuster to adjust the pH to obtain the face cream.

Citation Information

Patent Citations

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