Whitening and brightening composition and application thereof

By developing a whitening and brightening composition containing mulberry root extract, cherry rice extract and cardamom seed extract, the problems of poor whitening effect and poor safety of existing products have been solved, and efficient and safe whitening has been achieved Effects and increases the skin's transparency and brightness.

CN119385903APending Publication Date: 2025-02-07FANKE (GUANGDONG) BIOTECHNOLOGY CO LTD
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Patent Information

Application Number
CN202411363926.7
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2024-09-28
Publication Date
2025-02-07

AI Technical Summary

Technical Problem

The existing whitening and brightening products have problems such as poor whitening effect, poor safety and stability, and the whitening mechanism is single, which cannot effectively solve the pigmentation problems caused by free radicals and inflammatory factors.

Method used

Develop a whitening and brightening composition, including mulberry root extract, cherry rice extract, cardamom seed extract and other components, and by inhibiting tyrosinase activity, blocking melanin synthesis pathway, activating melanin brake signals, etc. mechanism to achieve safe and efficient whitening effects.

Benefits of technology

The composition can efficiently whiten and brighten, eliminate free radicals at the source, inhibit inflammatory factors, avoid activation of melanin synthesis and color deposition after inflammation, increase skin transparency and brightness, and also have good stability and safety.

✦ Generated by Eureka AI based on patent content.

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Abstract

The invention relates to the technical field of cosmetics, in particular to a whitening and brightening composition and application thereof. The whitening and brightening composition is prepared from the following components in parts by weight: mulberry root extract, butanediol, aminopropanol ascorbic acid phosphate, nostoc sphaeroids kutz extract, epigallocatechin gallyl glucoside, citrus peel extract, alpinia katsumadai seed extract, olive leaf extract and water. The composition disclosed by the invention is mild, safe and non-irritant to a human body, and through the synergistic effect of various active ingredients, free radicals are eliminated from the source, inflammatory factors are inhibited, and activation of melanin synthesis and chromaticity after inflammation are avoided. Besides, for the melanin with the activated synthesis path, the activity of tyrosinase is inhibited by inhibiting the generation of alpha-MSH, the brake signal of the melanin is activated, and the generation of the melanin is inhibited.
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Description

Technical Field

[0001] The present invention relates to the technical field of cosmetics, and more particularly to a whitening and brightening composition and application thereof. Background Art

[0002] At present, the whitening and brightening products on the market have various problems such as poor whitening and brightening effects, poor safety and stability. Traditional whitening and brightening ingredients are either not stable enough, such as VC, which is easy to change color and lose activity, and arbutin, which is easy to decompose and produce hydroquinone, which is harmful to the human body; or they are slow to take effect and have little effect, such as niacinamide and tranexamic acid; or they are too irritating, such as 4-butylresorcinol.

[0003] In general, the whitening products on the market generally have the following problems:

[0004] (1) The whitening mechanism is single and only controls the activation, generation, and transport pathways of melanin. There is no corresponding solution to pigmentation problems caused by free radicals, inflammatory factors, etc.

[0005] (2) Too much pursuit of quick results, products are too irritating, some products fail to achieve whitening effects, and also bring new problems to consumers' skin.

[0006] (3) The whitening agents used have poor stability and are prone to discoloration and inactivation, resulting in only a few active ingredients being absorbed by the skin and taking effect. Summary of the invention

[0007] Based on the above background, the purpose of the present invention is to develop a safe, stable and effective whitening and brightening product.

[0008] To achieve the above object, the present invention is implemented through the following technical solutions:

[0009] A whitening and brightening composition comprises the following components in parts by weight: 0.1-10 parts of mulberry root extract, 0.1-3 parts of kudzu vine extract, 0.05-0.1 parts of cardamom seed extract, and the balance of water.

[0010] Optionally, the following components are included in parts by weight: 0.5-1 part of mulberry root extract, 0.5-2 parts of kudzu vine extract, 0.05-0.1 part of cardamom seed extract, and the balance water.

[0011] Optionally, other active ingredients are also included.

[0012] Optionally, the other active ingredients include at least one of moisturizing ingredients, antioxidant ingredients, and whitening ingredients.

[0013] Optionally, the moisturizing ingredient is butylene glycol.

[0014] Optionally, the antioxidant component includes at least one of aminopropanol ascorbyl phosphate, epigallocatechin galloside, and olive leaf extract.

[0015] Optionally, the whitening ingredient is citrus peel extract.

[0016] In the present invention, tyrosinase is a key enzyme in the synthesis of melanin. Mulberry (MORUS ALBA) root extract contains a variety of active ingredients, such as flavonoids, polysaccharides, etc. Such substances can inhibit the activity of tyrosinase and reduce the production of melanin. Thereby preventing the production of melanin from the source and reducing the pigmentation of the skin. The extract of Nostoc sphaeroides (NOSTOC sphaeroides) is rich in a variety of nutrients, such as polysaccharides, vitamins, etc., which can inhibit the production of α-MSH (α-melanocyte stimulating hormone), thereby inhibiting the synthesis of MITF (melanocyte inducing transcription factor), reducing the content of tyrosinase, and inhibiting the production of melanin by blocking the synthesis pathway. The seed extract of ALPINIA KATSUMADAI is a melanin brake, which reduces the synthesis of melanin by activating the brake signal PLD-mTOR-S6K1 of melanin, and whitens and lightens spots safely and efficiently.

[0017] Butanediol is firstly a non-toxic, non-irritating, refreshing moisturizer; secondly, it is an excellent active ingredient dispersant that can disperse active ingredients including vitamin C, with better performance than other polyols. At the same time, a high content of butanediol has a certain antibacterial effect, avoiding the addition of additional preservatives, and the raw material is milder and more applicable.

[0018] Aminopropanol ascorbyl phosphate is a new generation of VC derivatives. It has excellent whitening effects by inhibiting abnormal pigmentation on the skin and reducing the production of melanin. It can resist ultraviolet radiation and comprehensively protect the skin. It can also effectively promote the production of collagen, making the skin fuller and more lustrous.

[0019] Epigallocatechin gallate glucoside (EGCG) is a key active ingredient in green tea, with powerful antioxidant activity, 25 times more potent than vitamin C. It can scavenge free radicals, reduce damage to cell oxidation, protect the skin from UV radiation and environmental pollution, and inhibit inflammatory responses, reducing redness and sensitivity.

[0020] Hydroxytyrosol contained in olive (OLEA EUROPAEA) leaf extract is considered to be the most powerful antioxidant and can effectively scavenge active free radicals.

[0021] Desmoplakin is a protein that connects the inner and outer cells and plays an important role in the formation of keratin filaments in the epidermis. Desmoplakin connects keratin and cell desmosomes, giving cells strength and tension. Citrus (CITRUS RET I CULATA) peel extract increases the content of desmoplakin between cells, thereby making cells tighter and making the skin smoother, while increasing the skin's transparency and brightness.

[0022] Another object of the present invention is to provide a use of the above-mentioned whitening and brightening composition in the preparation of cosmetics.

[0023] Optionally, the cosmetic is any one of an aqueous solution, cream, lotion, spray, facial mask, essence, facial cleanser, facial cleanser, or other common dosage forms of cosmetics.

[0024] The above embodiments provided by the present invention have the following beneficial effects:

[0025] (1) Multiple active ingredients interact with each other to effectively whiten and brighten the skin, eliminate free radicals at the source, inhibit inflammatory factors, and avoid the activation of melanin synthesis and pigmentation after inflammation. In addition, for melanin whose synthesis pathway has been activated, it inhibits the activity of tyrosinase by inhibiting the production of α-MSH (α-melanocyte stimulating hormone) and other pathways, activating the brake signal of melanin and inhibiting the production of melanin.

[0026] (2) Desmoplakin is a protein that connects the inner and outer cells. It connects keratin and cell desmosomes, giving cells strength and tension. By increasing the content of desmoplakin between cells, cells become tighter and skin becomes smoother and brighter. At the same time, by effectively promoting the production of collagen, the skin becomes fuller and more lustrous, thereby increasing the skin's transparency and photosensitivity.

[0027] (3) Polyols are carefully selected as suitable solvents. The formula does not contain any additional preservatives and is gentle and non-irritating to use. DETAILED DESCRIPTION

[0028] The technical scheme of the present invention is further described below in conjunction with the embodiments. Obviously, the described embodiments are only part of the embodiments of the present invention, rather than all of the embodiments. Based on the embodiments in the present invention, all other embodiments obtained by ordinary technicians in the field without creative work are within the scope of protection of the present invention. The methods or operations used in the embodiments, unless otherwise specified, are conventional methods or conventional operations in the art.

[0029] The present invention divides the components used into phase A and phase B, as shown in the following Table 1:

[0030] Table 1 Component classification table

[0031]

[0032]

[0033] The components and their weight fractions of the compositions of Examples 1-3 and Comparative Examples 1-7 are shown in Tables 2 and 3 below:

[0034] Table 2 Example composition formula

[0035] Components Example 1 Example 2 Example 3 Mulberry Root Extract 1 0.7 0.5 Butanediol 60 70 75 Aminopropanol ascorbyl phosphate 0.2 0.5 1 Pueraria Extract 2 1 0.5 Epigallocatechin Galloside 0.02 0.04 0.05 Citrus peel extract 1 1.5 2 Alpinia cymbopogon Seed Extract 0.05 0.08 0.1 Olive Leaf Extract 0.2 0.3 0.5 water 35.53 25.88 20.35

[0036] Table 3 Comparative Example Composition Formula

[0037]

[0038]

[0039] Weigh the components according to the proportions shown in Table 2 and Table 3, heat phase A to 60-65°C to dissolve and become transparent; then cool to room temperature, add phase B raw materials, and dissolve evenly under 38-40KHz ultrasonic stirring; after standing for 24 hours, filter through resin to obtain the corresponding whitening and brightening composition.

[0040] The efficacy of the compositions prepared in Examples 1-3 and Comparative Examples 1-7 was evaluated.

[0041] 1. DPPH free radical scavenging rate determination experiment

[0042] Take 2 mL of each of the whitening and brightening compositions prepared in Examples 1-3 and Comparative Examples 1-7, and mix with 8 mL of 1×10 -4 mol / L DPPH-ethanol solution was mixed, shaken evenly, and placed in a dark place at 25°C to avoid light for reaction for 30 minutes, then the mixed solution was placed in a centrifuge and centrifuged at 7000rpm for 5 minutes, and the supernatant after centrifugation was taken to measure the absorbance A1 at a wavelength of 517nm; 2mL of anhydrous ethanol was taken for the same operation, and the absorbance A2 was measured; 2mL of deionized water was taken for the same operation, and the absorbance A3 was measured; 2mL of 1mg / mL vitamin C solution was taken as a positive control, and 3 parallel experiments were set up for each group to calculate the average value. According to the DPPH scavenging rate formula DPPH scavenging rate = [1-(A1-A2) / A3] × 100%, the free radical scavenging ability of the antioxidant and anti-glycation compositions of different groups was calculated, and the test results are shown in Table 4.

[0043] Table 4 Antioxidant data of Examples and Comparative Examples

[0044]

[0045] It can be seen from Table 4 that, compared with Comparative Examples 1-7, the DPPH radical scavenging rates of the whitening and brightening compositions prepared in Examples 1-3 are all above 70%, while in Comparative Examples 1-7, due to the lack of one of the raw material components, the DPPH radical scavenging rates of the whitening and freckle-removing compositions prepared are all relatively low, which indicates that the whitening and brightening compositions prepared by using mulberry root extract, butylene glycol, aminopropanol ascorbyl phosphate, kudzu vine extract, epigallocatechin galloside, citrus peel extract, cardamom seed extract, olive leaf extract, and water in the present invention have a higher DPPH radical scavenging rate and good antioxidant effect; compared with Examples 1-3, the DPPH scavenging rates have increased and decreased, and the DPPH scavenging rate of Example 3 is the best, which indicates that Example 3 is the best combination.

[0046] 2. Stability test experiment

[0047] (1) First, the products obtained in Examples 1-3 and Comparative Examples 8-10 were mixed and diluted with water at a volume ratio of 1:10, and then their pH values ​​were measured at room temperature.

[0048] (2) The products obtained in Examples 1-3 and Comparative Examples 8-10 were subjected to heat resistance, cold resistance and hot and cold cycle tests, and the test conditions were as follows: (a) after being kept at 48±2°C for 3 months, physical and chemical tests and appearance judgment were performed after the products were restored to room temperature; (b) after being kept at -18±2°C for 3 months, physical and chemical tests and appearance judgment were performed after the products were restored to room temperature; (c) after being kept at 48°C, room temperature and -18°C for 24 hours, the products were cycled three times in this order, and physical and chemical tests and appearance judgment were performed after the products were restored to room temperature. The test method was QB / T 2660. After the test, the results are shown in Table 5 below.

[0049] The difference between Comparative Example 8 and Example 1 is that butanediol is replaced by propylene glycol with the same addition content.

[0050] The difference between Comparative Example 9 and Example 2 is that butanediol is replaced by ethanol with the same added content.

[0051] The only difference between Comparative Example 10 and Example 3 is that butanediol is replaced with isosorbide dimethyl ether in an equal amount.

[0052] Table 5 Stability data of Examples 1-3 and Comparative Examples 8-10

[0053]

[0054] It can be seen from Table 5 that, compared with Comparative Examples 8-10, Examples 1-3 did not experience color change, turbidity precipitation, etc. under different temperature environments, and had high stability in a system without adding preservatives; in contrast, the products prepared in Comparative Examples 8-10 showed darkening or precipitation or reduced transparency in different environmental tests, and their stability was insufficient.

[0055] 3. Tyrosinase activity inhibition test

[0056] 0.025 g of the whitening and brightening composition of Examples 1-3 and Comparative Examples 1-7 were respectively placed in test tubes numbered 1-10, 120 μL of phosphate buffer solution and 40 μL of 2.98 mmol / L tyrosine solution (2.98 mmol / L tyrosine solution as a substrate) were added to test tubes 1-10, and an equal amount of the mixed solution in test tubes 1-10 was added to a 96-well plate, and 40 μL of 200 U / mL tyrosinase solution was added to each well after constant temperature in a 37 ° C water bath for 10 min, mixed at room temperature and protected from light, and quickly placed in a multifunctional microplate detector after 15 min of water bath at 37 ° C, and the absorbance at 475 nm was measured, and the tyrosinase inhibition rate was calculated. Repeat the above operation and measure 3 times in parallel. The test results are shown in Table 6:

[0057] Table 6 Tyrosinase activity inhibition data of Examples and Comparative Examples

[0058]

[0059] As can be seen from Table 6, compared with Comparative Examples 1-7, the whitening and brightening composition prepared in Examples 1-3 has a higher inhibition rate on tyrosinase, all greater than 50%, while in Comparative Examples 1-7, due to the lack of one of the raw material components, the whitening and brightening composition prepared has a lower inhibition rate on tyrosinase, which shows that the whitening and brightening composition prepared by the present invention has a good tyrosinase inhibition effect. In particular, when any one of the mulberry root extract, kudzu vine extract, and cardamom seed extract is lacking, the inhibition rate of the whitening and brightening composition on tyrosinase is significantly reduced, which shows that the mulberry root extract, kudzu vine extract, and cardamom seed extract have a synergistic effect in inhibiting tyrosinase activity. Compared with Examples 1-3, the tyrosinase inhibition rate in Example 3 is as high as 58%, indicating that Example 3 is the best combination and has a good whitening and brightening effect.

[0060] 4. Human whitening test

[0061] 200 female volunteers aged 18-60 were recruited and divided into 10 groups. The samples of Examples 1-3 and Comparative Examples 1-7 were used by them respectively. The products were applied to a fixed area of ​​the forehead after cleansing every day. The skin brightness L* value of the forehead area was measured by using the German CK multi-probe skin testing system MPA9 just before using the product and four weeks after using the product to obtain L1 and L2 (L* value represents brightness, the larger the value, the whiter the skin), and then the L* value improvement rate = [(L2-L1) / L1]×100% was obtained, and the average value was finally taken. The measurement results are shown in Table 7:

[0062] Table 7 Human body whitening data

[0063]

[0064] As shown in Table 7, compared with Comparative Examples 1-7, the whitening and brightening compositions prepared in Examples 1-3 have a higher skin L* value improvement rate, all greater than 10%, while in Comparative Examples 1-7, due to the lack of one of the raw material components, the whitening and brightening compositions prepared have a very low skin L* value improvement rate, which shows that the whitening and brightening compositions prepared in the present invention have a good whitening and brightening effect. Compared with Examples 1-3, the skin L* value improvement rate in Example 3 is higher and highest, up to 12.53%, which shows that Example 3 is the best combination and has a good whitening and brightening effect.

[0065] 5. Safety test experiment

[0066] The whitening and anti-freckle compositions prepared in all the above examples and the control group (deionized water) were subjected to human safety patch tests. The test method was based on the human skin patch test in the "2015 Cosmetic Safety Technical Specifications". The method of the skin occlusion patch test was as follows: 30 people aged 18-60 were selected, and the area of ​​the patch was not more than 50 mm. 2 , a qualified spot test device with a depth of about 1mm, take 0.020mL of the whitening and freckle removal composition prepared in the above examples and comparative examples and put it into the small chamber of the spot tester, the control well is a blank control (no substance is placed), the spot tester with the whitening and brightening composition is applied to the curved side of the forearm of the subject with a low-allergenic tape, and the palm of the hand is gently pressed to make it evenly applied to the skin, and it lasts for 24 hours. Observe the skin reaction according to the standards in Table 8 30 minutes (after the indentation disappears), 24 hours and 48 hours after removing the spot tester containing the whitening and brightening composition, and the results are shown in Table 9:

[0067] Table 8 Skin reaction grading standard for skin occlusive patch test

[0068]

[0069] Table 9 Patch test data

[0070]

[0071]

[0072] As shown in Table 9, the patch test results of the whitening and brightening compositions prepared in Examples 1-3 and the control group (deionized water) were all negative, indicating that the whitening and brightening compositions prepared in the present invention are mild and non-irritating.

[0073] 6. Skin elasticity test

[0074] 100 people aged 18-60 were selected and divided into 10 groups. The skin elasticity value R2 of the test parts before and after use of the samples was tested using a skin elasticity tester (model: MPA580, CK Company, Germany). The change degree of skin elasticity was evaluated based on the difference in skin elasticity before and after use, △R2=R2 (使用后) -R2 (使用前) , the larger the △R2 value, the more the elasticity is enhanced. The test results are recorded as the average value, as shown in Table 10:

[0075] Table 10 Skin elasticity test data

[0076]

[0077] It can be seen from Table 10 that, compared with Comparative Examples 1-7, the whitening and brightening compositions prepared in Examples 1-3 have an increase in skin elasticity greater than 0.35, while in Comparative Examples 1-7, due to the lack of one of the raw material components, the skin elasticity increase of the whitening and brightening compositions prepared is relatively low, which shows that the whitening and brightening composition prepared by using mulberry root extract, butylene glycol, aminopropanol ascorbyl phosphate, kudzu vine extract, epigallocatechin galloside, citrus peel extract, cardamom seed extract, olive leaf extract, and water in the present invention has excellent skin elasticity increase effect; compared with Examples 1-3, the skin elasticity increase of Example 3 is the largest, which shows that Example 3 is the best combination.

[0078] The above is only a preferred embodiment of the present invention, and the protection scope of the present invention is not limited to the above embodiments. All technical solutions under the concept of the present invention belong to the protection scope of the present invention. It should be pointed out that for ordinary technicians in this technical field, some improvements and modifications without departing from the original material of the present invention should also be regarded as the protection scope of the present invention.

Claims

1. A whitening and brightening composition, characterized in that: The invention comprises the following components in parts by weight: 0.1-10 parts of mulberry root extract, 0.1-3 parts of kudzu vine extract, 0.05-0.1 parts of cardamom seed extract and the balance of water.

2. The whitening and brightening composition according to claim 1, characterized in that: The invention comprises the following components in parts by weight: 0.5-1 part of mulberry root extract, 0.5-2 parts of kudzu vine extract, 0.05-0.1 part of cardamom seed extract and the balance of water.

3. The whitening and brightening composition according to claim 1, characterized in that: Other active ingredients are also included.

4. The whitening and brightening composition according to claim 3, characterized in that: The other active ingredients include at least one of moisturizing ingredients, antioxidant ingredients, and whitening ingredients.

5. The whitening and brightening composition according to claim 4, characterized in that: The moisturizing ingredient is butylene glycol.

6. The whitening and brightening composition according to claim 4, characterized in that: The antioxidant component includes at least one of aminopropanol ascorbyl phosphate, epigallocatechin galloside and olive leaf extract.

7. The whitening and brightening composition according to claim 4, characterized in that: The whitening ingredient is citrus peel extract.

8. Use of the whitening and brightening composition according to any one of claims 1 to 7 in the preparation of cosmetics.

9. The use according to claim 8, characterized in that: The cosmetic is any one of an aqueous solution, cream, lotion, spray, facial mask, essence, facial cleanser, and facial cleanser.