A transdermal composition with whitening and freckle-removing effects and a preparation method thereof

Abstract

The application provides a transdermal composition with whitening and freckle-removing effects and a preparation method thereof, and belongs to the technical field of cosmetics.The transdermal composition comprises whitening and freckle-removing active ingredients; the whitening and freckle-removing active ingredients comprise niacinamide, arbutin, glycerol, water, and further comprise plant extracts and fermented extracts.The plant extracts comprise extracts of Silybum marianum, Sarcandra glabra and Radix Paeoniae Rubra.The fermented extracts are obtained by fermentation of soybean seed coat extract, Cystoseira biseriata extract and Rhodobryum roseum extract by a composite fermentation agent.The composite fermentation agent comprises Bacillus alvei, Lactobacillus murinus and Streptomyces olivaceus.The transdermal composition prepared by the application not only has good whitening and freckle-removing effects and transdermal properties, but also can maintain its appearance state when the external temperature changes.

Description

Technical Field

[0001] This invention belongs to the field of cosmetic technology, specifically relating to a transdermal composition with whitening and freckle-removing effects and its preparation method. Background Technology

[0002] Skin whitening and blemish-reducing compositions typically refer to formulations consisting of one or more ingredients with whitening and skin-pigmentation-reducing functions. These compositions aim to reduce age spots, freckles, and other pigmentation on the skin through various mechanisms, achieving a skin-whitening effect. These ingredients can be naturally derived extracts, chemically synthesized active substances, or a combination of both.

[0003] Currently, commonly used skin-whitening and spot-removing ingredients include arbutin, niacinamide, resveratrol, and green tea extract. Among them, arbutin can inhibit the activity of tyrosinase and reduce melanin production; niacinamide can reduce the transfer of melanin to the stratum corneum, thereby helping to alleviate the problems of pigmentation and uneven skin tone; resveratrol has antioxidant effects, which helps protect the skin from damage and indirectly supports the whitening effect; green tea extract contains antioxidants such as catechins, which can reduce UV damage and prevent excessive melanin accumulation.

[0004] Although the above ingredients can have a whitening and spot-removing effect, the actual whitening and spot-removing effect is quite limited in actual use. The specific drawbacks are as follows:

[0005] (1) Niacinamide and arbutin have relatively large molecular weights, which may prevent them from penetrating deep into the skin and have slow transdermal absorption, resulting in their inability to achieve their whitening and spot-removing effects in actual use.

[0006] (2) Niacinamide and arbutin are prone to deterioration when the temperature changes, which affects the appearance and stability of cosmetics.

[0007] (3) Niacinamide or arbutin alone have limited whitening and spot-removing effects, and the cosmetic ingredients are poorly designed. Summary of the Invention

[0008] The purpose of this invention is to provide a transdermal composition with whitening and freckle-removing effects and its preparation method, so as to solve the problems of poor transdermal effect, unreasonable component design and susceptibility to external environmental influences of the above-mentioned whitening and freckle-removing compositions.

[0009] To achieve the above objectives, the present invention provides the following technical solution:

[0010] The first aspect of the present invention provides a transdermal composition with whitening and freckle-removing effects. The raw materials of the transdermal composition include whitening and freckle-removing functional ingredients, which include nicotinamide, arbutin, glycerin and water in a mass ratio of (0.2-0.4):(0.5-0.8):(0.1-0.3):(3-5).

[0011] Preferably, the whitening and spot-removing ingredients include niacinamide, arbutin, glycerin and water in a mass ratio of (0.3-0.4):(0.6-0.8):(0.2-0.3):(4-5).

[0012] Preferably, the whitening and spot-removing ingredients include niacinamide, arbutin, glycerin and water in a mass ratio of 0.3:0.7:0.2:4.5.

[0013] Preferably, the raw materials of the transdermal composition also include emollients, emulsifiers, fillers, thickeners, transdermal absorption enhancers, and water; the whitening and spot-removing active ingredients also contain plant extracts and fermented extracts;

[0014] The transdermal composition comprises the following ingredients by weight percentage:

[0015] The product contains 10-15% whitening and spot-removing active ingredients, 5-40% emulsifier, 0.5-30% emulsifier, 0.1-20% filler, 0.1-10% thickener, 1-3% transdermal absorption enhancer, and the balance being water.

[0016] The whitening and spot-removing ingredients, in a mass ratio of (0.2-0.4):(0.5-0.8):(0.1-0.3):(5-10):(3-5):1, include niacinamide, arbutin, glycerin, water, plant extracts, and fermented extracts;

[0017] The plant extracts, in a mass ratio of (1.5–3.5):(0.5–1):1, include milk thistle extract, coralberry extract, and red peony root extract;

[0018] The fermented extract was obtained by fermenting soybean seed coat extract, seaweed extract and red bean extract mixed in a mass ratio of (0.8-1):(3-4):1 with a compound fermentation agent.

[0019] The compound fermentation agent includes Bacillus vesicularis, Lactobacillus murineis and Streptomyces oliveri in a mass ratio of (6-10):(2.5-4):1.

[0020] To address the issue of poor practical efficacy in existing whitening and freckle-removing compositions, this invention redesigns the composition of commonly used ingredients such as niacinamide and arbutin. By utilizing the synergistic effects of multiple substances, the whitening and freckle-removing effects of the composition are improved. The whitening and freckle-removing active ingredients in this invention include four substances: niacinamide, arbutin, plant extracts, and fermentation extracts. These four substances work synergistically with the skin to enhance the whitening and freckle-removing effect. The reasons are as follows: Niacinamide can inhibit melanin formation and reduce pigmentation. Niacinamide also has anti-inflammatory properties, which can help reduce pigmentation caused by skin inflammation. Arbutin inhibits melanin synthesis by inhibiting the activity of tyrosinase. The plant extracts, including milk thistle, coralberry, and red peony root, contain various antioxidants, such as polyphenols, which can scavenge free radicals, reduce oxidative stress damage to the skin, and regulate skin cell metabolism, promoting healthy cell renewal. The fermentation extracts, including soybean seed coat, seaweed, and red bean, not only provide strong antioxidant protection but also promote skin moisturizing, repair, and whitening effects through multiple mechanisms. When the four substances in this invention are used simultaneously in the specified proportions, niacinamide and arbutin can work together to inhibit melanin production, the antioxidant properties of the plant extracts can protect the skin from damage and reduce inflammation, while the fermented extracts provide additional nutritional support and promote skin health. This multifaceted protective and repair mechanism makes the composition outstanding in whitening and spot removal, and the interaction of the four substances can further enhance the whitening effect.

[0021] This invention utilizes various plant extracts, including milk thistle extract, coralberry extract, red peony root extract, soybean seed coat extract, seaweed extract, and red bean extract. While these extracts enhance the whitening and spot-removing effects, further research revealed that the appearance of the prepared composition easily changes when the external temperature environment changes, affecting subsequent use. The reason for this is likely that the plant extracts contain multiple substances with varying physicochemical properties. Some components may be more sensitive to temperature changes, exhibiting precipitation and discoloration over time and temperature fluctuations, and potentially disrupting the emulsion system. To address this issue, this invention employs a compound microbial fermentation process on the soybean seed coat extract, seaweed extract, and red bean extract. This not only maintains the whitening and spot-removing effects but also improves their appearance stability. The reason for this is that during fermentation, microorganisms can transform complex organic molecules into simpler, smaller molecules. These transformed components are often more stable and less susceptible to temperature changes. Furthermore, fermentation reduces the content of certain unstable components, improving the overall stability of the extract. Surfactants that may be produced during microbial fermentation also help improve the stability of the emulsion system, reducing damage caused by temperature changes. Fermentation products may also possess emulsifying properties, which help maintain the homogeneity of the emulsion system and prevent oil-water separation. This invention, through a mixed fermentation process using compound fermentation agents, enables the emulsion system to remain stable under temperature variations.

[0022] Preferably, the emollient is one or more of the following: caprylic / capric triglyceride, squalane, avocado oil, shea butter, jojoba oil, glycerin, butylene glycol, hexane glycol, pentane glycol, polydimethylsiloxane, polydimethylsiloxane alcohol, PEG-11 methyl ether polydimethylsiloxane, phytosterol, phytosterol / octyldodecyl lauroyl glutamate, hydrogenated polyisobutylene, rapeseed oil, polydecene, soybean oil, olive oil, isododecane, isohexadecane, stearyl alcohol, and behenyl alcohol.

[0023] Preferably, the emulsifier is one or more of the following: olive oil PEG-7 esters, PEG-8 caprylic / capric glycerides, sorbitan olive oil esters, polysorbate-20, lauryl ether-23, PEG-40 stearate, stearyl ether-21, a mixture of palmitol and PEG-75 stearate and glyceryl stearate and stearyl ether-20, polysorbate-80, soybean lecithin PC60, a mixture of glyceryl stearate and PEG-75 stearate, poloxamer 407, PEG-30 dihydroxystearate, and cetearyl ether-25.

[0024] Preferably, the filler is one or more of the following: titanium dioxide, mica, boron nitride, polymethylsilsesquioxane, diatomaceous earth, kaolin, cellulose acetate, aluminum octyl succinate starch, talc, barium sulfate, and volcanic ash.

[0025] Preferably, the thickener is one or more of the following: hydroxyethyl cellulose, xanthan gum, carbomer, polymer EMT-10, polyacrylate crosspolymer-6, sodium acrylate / sodium acryloyl dimethyl taurate copolymer, acryloyl dimethyl taurate amine / VP copolymer, acrylate / C10-30 alkyl acrylate crosspolymer, polyvinyl alcohol, gum arabic, and hydroxypropyl starch phosphate.

[0026] Preferably, the transdermal absorption enhancer comprises peppermint oil, lauryl acetonide, and N-acetylproline pentanol ester in a mass ratio of (2-4):(8-10):1.

[0027] To enhance the whitening and spot-removing effects of whitening and spot-removing compositions, it is essential to focus not only on the composition's ingredient design to maximize efficacy but also on skin absorbability, ensuring that the added whitening and spot-removing ingredients penetrate deep into the skin for excellent transdermal absorption. This invention specifically limits the types and proportions of transdermal absorption enhancers, thereby improving the product's transdermal properties. The reasons are as follows: Peppermint oil, lauryl azone, and N-acetylproline pentanol ester can synergistically improve the transdermal absorption of whitening and spot-removing ingredients. The cooling sensation of peppermint oil temporarily increases skin temperature and promotes local blood circulation, facilitating the faster penetration of ingredients such as niacinamide and arbutin into the deeper layers of the skin through the stratum corneum. Lauryl azone effectively promotes the transdermal absorption of active ingredients in plant extracts and fermented extracts because it increases their lipophilicity, making them easier to cross the skin barrier. N-acetylproline pentanol ester increases skin hydration, loosening the stratum corneum and facilitating better penetration of water-soluble ingredients such as niacinamide and arbutin into the skin. When these three transdermal absorption enhancers are mixed in a certain proportion, they can complement each other to form an effective enhancement system.

[0028] Preferably, the preparation method of the fermentation extract is as follows:

[0029] S11: Mix soybean seed coat extract, seaweed extract and sea buckthorn extract in a certain proportion to obtain a mixture;

[0030] S12: Add compound fermentation agent to the mixture, the inoculum amount of compound fermentation agent is 6-8 wt%, then add water, the mass of the added water is 15-20 times that of the mixture, continuously introduce oxygen, ferment at 28-32℃ for 5-7 days to obtain fermentation liquid;

[0031] S13: Filter the fermentation broth to obtain filtrate, sterilize the filtrate at 100-110℃ for 30-60 min, then centrifuge the filtrate, collect the supernatant, freeze-dry it to obtain the fermentation extract.

[0032] A second aspect of the present invention provides a method for preparing a transdermal composition with whitening and freckle-removing effects, comprising the following steps:

[0033] S1: Wet and disperse the thickener in water to obtain a mixture;

[0034] S2: Add emollient and filler to the mixture in step S1, heat to 60-80℃, and homogenize at 2500-3500r / min for 3-5min to ensure complete dispersion;

[0035] S3: Add emulsifier to step S2, homogenize at 2500-3500 r / min for 3-5 min to ensure complete emulsification, and add whitening and spot-removing ingredients and transdermal absorption promoter while stirring and cooling to obtain transdermal composition.

[0036] Compared with the prior art, the advantages and beneficial effects of the present invention are as follows:

[0037] 1. This invention contains a variety of ingredients with whitening and spot-removing effects, including niacinamide, arbutin, plant extracts, and fermented extracts. Through scientific formulation, a multi-effect synergistic effect is achieved. This synergistic effect can not only improve the whitening and spot-removing effect, but also enhance the skin's self-repair ability and overall health.

[0038] 2. This invention utilizes fermentation technology to process plant extracts, which improves the stability of the active ingredients and reduces changes in the composition's appearance caused by external factors such as temperature. Furthermore, the small molecules produced during fermentation are more easily absorbed by the skin and are also more stable.

[0039] 3. In this invention, peppermint oil, lauryl azone, and N-acetylproline pentanol ester are used as transdermal absorption enhancers. These ingredients can effectively promote the transdermal absorption of whitening and spot-removing ingredients, thereby improving their bioavailability and enabling the active ingredients to reach the deep layers of the skin more quickly and deeply to exert their effects.

[0040] 4. The components used in the composition of the present invention are all substances that exist in nature or are obtained through biological fermentation. Compared with chemically synthesized components, these natural components are generally considered to be safer, milder, less irritating to the skin, and suitable for long-term use. Detailed Implementation

[0041] The technical solutions in the embodiments of the present invention will be clearly and completely described below. Obviously, the described embodiments are only some embodiments of the present invention, and not all embodiments. Based on the embodiments of the present invention, all other embodiments obtained by those skilled in the art without creative effort are within the scope of protection of the present invention.

[0042] Example 1

[0043] This embodiment provides a transdermal composition with whitening and freckle-removing effects, the components of which are shown in Table 1.

[0044] Table 1 Composition of the composition

[0045]

[0046]

[0047] The transdermal absorption enhancer, in a mass ratio of 3:9:1, includes peppermint oil, lauryl acetonide, and N-acetylproline pentanol ester.

[0048] The whitening and spot-removing ingredients, in a mass ratio of 0.3:0.7:0.2:7:4:1, include niacinamide, arbutin, glycerin, water, plant extracts, and fermented extracts.

[0049] The plant extracts, in a mass ratio of 2:0.8:1, include milk thistle extract, coralberry extract, and red peony root extract;

[0050] Milk thistle extract was purchased from Hunan Langlin Bioresources Co., Ltd.

[0051] The herb extract was purchased from Lanzhou Waterles Biotechnology Co., Ltd.

[0052] The extract of Paeonia lactiflora was purchased from Xi'an Yuno Biotechnology Co., Ltd.

[0053] The preparation method of the fermentation extract is as follows:

[0054] S11: Mix soybean seed coat extract, seaweed extract and sea buckthorn extract in a certain proportion to obtain a mixture; the mass ratio of soybean seed coat extract, seaweed extract and sea buckthorn extract is 0.9:3.5:1;

[0055] Soybean seed coat extract was purchased from Shaanxi Guanchen Biotechnology Co., Ltd.

[0056] The extract of large-leaf seaweed was purchased from Ningxia Xiangcao Biotechnology Co., Ltd.

[0057] Sea red bean extract was purchased from Lanzhou Waterles Biotechnology Co., Ltd.

[0058] S12: Add compound fermentation agent to the mixture, the inoculum amount of compound fermentation agent is 7wt%, then add water, the mass of the added water is 18 times that of the mixture, continuously introduce oxygen, ferment at 30℃ for 6 days to obtain fermentation liquid;

[0059] The compound fermentation agent includes Bacillus vesiclei, Lactobacillus murineis, and Streptomyces oliveri in a mass ratio of 8:3:1.

[0060] Bacillus vesicles were purchased from Shanghai Chen Microbial Technology Co., Ltd., model number GDMCC 800145;

[0061] Lactobacillus murineis was purchased from Shanghai Chen Microbial Technology Co., Ltd., model number CICC 23144;

[0062] Streptomyces oliveri was purchased from Shanghai Chen Microbial Technology Co., Ltd., model number CICC 11001;

[0063] S13: Filter the fermentation broth to obtain filtrate, sterilize the filtrate at 105℃ for 40 min, then centrifuge the filtrate, collect the supernatant, freeze-dry it to obtain the fermentation extract.

[0064] A method for preparing a transdermal composition with whitening and freckle-removing effects includes the following steps:

[0065] S1: Wet and disperse the thickener in water to obtain a mixture;

[0066] S2: Add emollient and filler to the mixture in step S1, heat to 65°C, and homogenize at 3000r / min for 3min to ensure complete dispersion;

[0067] S3: Add emulsifier to step S2, homogenize at 3000r / min for 5min to ensure complete emulsification, and add whitening and spot-removing ingredients and transdermal absorption promoter while stirring and cooling to obtain transdermal composition.

[0068] Example 2

[0069] The difference between this embodiment and Embodiment 1 is the composition and dosage of the whitening and spot-removing active ingredients. In this embodiment, the whitening and spot-removing active ingredients comprise 12% by mass.

[0070] In this embodiment, the whitening and spot-removing ingredients, in a mass ratio of 0.2:0.6:0.3:8:4:1, include niacinamide, arbutin, glycerin, water, plant extracts, and fermented extracts.

[0071] The plant extracts, in a mass ratio of 2.2:0.6:1, include milk thistle extract, coralberry extract, and red peony root extract;

[0072] The preparation method of the fermentation extract is as follows:

[0073] S11: Mix soybean seed coat extract, seaweed extract and sea buckthorn extract in a certain proportion to obtain a mixture; the mass ratio of soybean seed coat extract, seaweed extract and sea buckthorn extract is 0.8:3.8:1;

[0074] S12: Add compound fermentation agent to the mixture, the inoculum amount of compound fermentation agent is 8%, then add water, the amount of water added is 20 times that of the mixture, continuously introduce oxygen, ferment at 28℃ for 7 days to obtain fermentation liquid;

[0075] The compound fermentation agent includes Bacillus vesiclei, Lactobacillus murineis, and Streptomyces oliveri in a mass ratio of 8.5:3:1.

[0076] S13: Filter the fermentation broth to obtain filtrate, sterilize the filtrate at 105℃ for 30 min, then centrifuge the filtrate, collect the supernatant, freeze-dry it to obtain the fermentation extract.

[0077] Comparative Example 1

[0078] The difference between this comparative example and Example 1 is that the mass ratio of the plant extracts is different, and the proportion of *Sarcandra glabra* extract added is increased.

[0079] In this comparative example, the mass ratio of milk thistle extract, coralberry extract, and red peony root extract was 2:2:1.

[0080] Comparative Example 2

[0081] The difference between this comparative example and Example 1 is that the mass ratios of soybean seed coat extract, seaweed extract, and red bean extract in the fermented extract are different, and the proportion of soybean seed coat extract added is increased.

[0082] In this comparative example, the mass ratio of soybean seed coat extract, seaweed extract, and sea buckthorn extract was 2:3.5:1.

[0083] Comparative Example 3

[0084] The difference between this comparative example and Example 1 is that the mass ratio of the compound fermentation agent used in the preparation of the fermentation extract is different, and the proportion of Lactobacillus murineis added is increased.

[0085] In this comparative example, the mass ratio of Bacillus vesicularis, Lactobacillus murineis, and Streptomyces oliveri was 8:6:1.

[0086] Comparative Example 4

[0087] The difference between this comparative example and Example 1 is that the type of compound fermentation agent is different. In this comparative example, Bacillus aureus is replaced with Bacillus licheniformis, which was purchased from Shanghai Chen Microbial Technology Co., Ltd., model GDMCC1.182.

[0088] Comparative Example 5

[0089] The difference between this comparative example and Example 1 is that the type of compound fermentation agent is different. In this comparative example, Lactobacillus murineis is replaced with Lactobacillus plantarum, which was purchased from Shanghai Chen Microbial Technology Co., Ltd., model CICC 23135.

[0090] Comparative Example 6

[0091] The difference between this comparative example and Example 1 is that the type of compound fermentation agent is different. In this comparative example, Streptomyces oliveii is replaced with Streptomyces grayi, which was purchased from Shanghai Chen Microbial Technology Co., Ltd., model CICC 11002.

[0092] Comparative Example 7

[0093] The difference between this comparative example and Example 1 is that the mass ratio of the whitening and spot-removing active ingredients is different, and the proportion of arbutin added is increased.

[0094] The whitening and freckle-removing ingredients in this comparative sample are in a mass ratio of 0.3:1.5:0.2:7:4:1 and include niacinamide, arbutin, glycerin, water, plant extracts, and fermented extracts.

[0095] Comparative Example 8

[0096] The difference between this comparative example and Example 1 is that the ingredients for whitening and spot-removing effects are different; no fermentation extract was added in this comparative example.

[0097] The whitening and spot-removing ingredients in this comparative sample, in a mass ratio of 0.3:0.7:0.2:7:4, include niacinamide, arbutin, glycerin, water, and plant extracts.

[0098] Comparative Example 9

[0099] The difference between this comparative example and Example 1 is that the ingredients for whitening and spot-removing effects are different; no plant extracts were added in this comparative example.

[0100] The whitening and freckle-removing ingredients in this comparative sample, in a mass ratio of 0.3:0.7:0.2:7:1, include niacinamide, arbutin, glycerin, water, and fermentation extract.

[0101] Comparative Example 10

[0102] The difference between this comparative example and Example 1 is that the ingredients for the whitening and spot-removing effects are different. This comparative example does not add fermented extracts, but directly adds unfermented soybean seed coat extract, seaweed extract and red bean extract to the whitening and spot-removing effects ingredients.

[0103] The whitening and freckle-removing ingredients in this comparative example, in a mass ratio of 0.3:0.7:0.2:7:4:1, include niacinamide, arbutin, glycerin, water, plant extracts, and plant raw materials; the plant raw materials are soybean seed coat extract, seaweed extract, and red bean extract, in a mass ratio of 0.9:3.5:1.

[0104] Comparative Example 11

[0105] The difference between this comparative example and Example 1 is that the mass ratio of the transdermal absorption enhancer is different.

[0106] In this comparative example, the transdermal absorption enhancers included peppermint oil, lauryl azone, and N-acetylproline pentanol ester in a mass ratio of 8:9:1.

[0107] Performance testing

[0108] (1) Security Testing

[0109] Test samples: transdermal compositions prepared in the examples and comparative examples;

[0110] Testing method: Safety will be tested by a third-party testing agency. Select an area not exceeding 50mm². 2 A suitable patch applicator with a depth of approximately 1 mm was used. Approximately 0.02 g of the test substance was added to the applicator using a closed patch test method. The applicator was applied to the flexor side of the subject's forearm. After 24 hours, the test substance was removed. Skin reactions were observed 48 hours after removal, and the results were recorded according to the skin reaction grading standards in the "Cosmetic Safety Technical Regulations 2015". The test results are shown in Table 2.

[0111] The skin reaction grading criteria are as follows:

[0112] Grade 0: Negative reaction;

[0113] Grade 1: Suspicious reaction; only slight erythema;

[0114] Grade 2: Weak positive reaction (erythema reaction); erythema, infiltration, edema, and papules may be present;

[0115] Grade 3: Strong positive reaction (herpes reaction); erythema, infiltration, edema, papules, vesicles; the reaction may extend beyond the tested area;

[0116] Grade 4: Extremely strong reaction (confluent herpes simplex reaction); obvious erythema, severe infiltration, edema, confluent herpes simplex, reaction extending beyond the test area.

[0117] Table 2 Security Test Results

[0118]

[0119]

[0120] As can be seen from Table 2, the compositions prepared in the examples and comparative examples are relatively safe and can be used for subsequent experiments.

[0121] (2) Stability test

[0122] Test samples: transdermal compositions prepared in the examples and comparative examples;

[0123] Test method: The transdermal compositions prepared in the examples and comparative examples were placed under conditions of 45°C in the dark, 25°C in the dark, -15°C in the dark, cyclic at 45°C and -15°C, and 25°C under light, respectively, and their appearance was observed after three months. The 45°C and -15°C cycle specifically refers to placing the transdermal composition under 45°C in the dark for 3 days, and then under -15°C in the dark for 3 days, and then repeating this cycle.

[0124] After conducting the above experiments, the appearance test results were represented by grades 1, 2, 3, and 4. Grade 1 indicates no obvious change in appearance, grade 2 indicates the precipitation of trace amounts of substance, grade 3 indicates the precipitation of a small amount of substance, and grade 4 indicates the precipitation of a large amount of substance. The test results are shown in Table 3.

[0125] Table 3 Stability Test Results

[0126]

[0127]

[0128] As can be seen from Table 3, the transdermal compositions prepared in Examples 1-2 did not show significant changes in appearance after three months under high and low temperatures or light exposure, while the appearance of Comparative Examples 1-11 all showed varying degrees of deterioration and precipitation, indicating that the compositions prepared in this invention have good stability.

[0129] (3) Spot removal effect test

[0130] Test samples: transdermal compositions prepared in the examples and comparative examples;

[0131] Volunteer selection: 260 test subjects with an average age of 25-35 years; healthy skin without damage, and with a lot of spots on their faces; 20 subjects for each example and comparative example, and the average test results were taken.

[0132] Test method: Apply the sample twice daily, morning and evening, for 12 weeks. Volunteers applied 0.5g of the transdermal composition to their entire face. The melanin index of a fixed spot before and after using the transdermal composition was measured using a Mexameter melanin analyzer. The test results are shown in Table 4.

[0133] Melanin reduction rate = (Melanin index before using the transdermal composition - Melanin index after using the transdermal composition) / Melanin index before using the transdermal composition × 100%.

[0134] Table 4 Results of the Spot Removal Effect Test

[0135]

[0136]

[0137] (4) Whitening effect test

[0138] Test samples: transdermal compositions prepared in the examples and comparative examples;

[0139] Subject selection: 260 test subjects with an average age of 25-35 years; with healthy and undamaged skin; 20 subjects for each example and comparative example, and the average test results were taken.

[0140] Test method: Apply the sample to the face twice daily, morning and evening. Apply 0.5g of the test sample to one side of the face randomly, while the other side serves as a control group without the test sample. Skin samples were tested before sample use (D0) and 56 days after sample use (D56).

[0141] The testing items are:

[0142] 1) The Mexameter@MX18 skin melanin analyzer is used to detect skin melanin;

[0143] 2) The Colorimeter@CL200 skin color meter is used to detect skin glossiness.

[0144] The test results are shown in Table 5. In the control group, melanin production increased and skin luster decreased.

[0145] Melanin reduction rate = (Melanin index before using the transdermal composition - Melanin index after using the transdermal composition) / Melanin index before using the transdermal composition × 100%.

[0146] Skin gloss improvement rate = (Skin gloss after using the transdermal composition - Skin gloss before using the transdermal composition) / Skin gloss before using the transdermal composition × 100%.

[0147] Table 5. Whitening Effect Test Results

[0148] Example 1 28.1 25.5 Example 2 25.5 23.6 Comparative Example 1 17.6 14.2 Comparative Example 2 16.8 13.6 Comparative Example 3 14.2 12.5 Comparative Example 4 12.5 10.8 Comparative Example 5 13.4 11.5 Comparative Example 6 12.0 12.7 Comparative Example 7 10.8 9.2 Comparative Example 8 8.7 7.5 Comparative Example 9 7.9 6.9 Comparative Example 10 11.6 10.1 Comparative Example 11 15.4 12.5 control group -8.5 -6.6

[0149] As can be seen from the above performance test results, the transdermal compositions of Examples 1-2 have good whitening and spot-removing effects and good appearance stability. In particular, the comprehensive performance of Example 1 is the most outstanding. This is mainly because the whitening and spot-removing ingredients in this invention are designed and a specific proportion of plant extracts and fermentation extracts are added.

[0150] The comparative examples, lacking the necessary technical solutions, showed significantly inferior performance compared to the examples in relevant performance tests. Comparative Example 1, by altering the mass ratio of plant extracts, showed a decrease in the stability and whitening / spot-removing effects of the composition, demonstrating that the mass ratio of plant extracts has a certain impact on the overall performance of the composition. Comparative Example 2, by altering the proportion of plant materials in the fermented extract, also affected the stability and whitening / spot-removing effects of the composition, indicating that the proportion of raw materials in the fermented extract has a certain impact on the overall performance of the composition. Comparative Example 3, by altering the mass ratio of the compound fermentation agent in the fermented extract, further affected the stability and whitening / spot-removing effects of the composition, indicating that the proportion of the compound fermentation agent has a significant impact on the overall performance of the transdermal composition in this invention. Comparative Examples 4-6, by altering the type of one agent in the compound fermentation agent, showed a significant impact on the stability and whitening / spot-removing effects of the transdermal composition, both of which decreased significantly. Comparative Example 7 altered the proportions of the four substances in the whitening and spot-removing active ingredients. Comparative Examples 8 and 9 did not add fermented extracts and plant extracts, respectively. The results show that the stability and whitening / spot-removing effect of the prepared transdermal compositions decreased, indicating that the four whitening / spot-removing active ingredients in this invention have a synergistic effect. Only when the four substances are combined in a specific proportion can a synergistic effect be produced, maximizing the overall effect of the transdermal composition. Comparative Example 10 did not ferment the soybean seed coat extract, seaweed extract, and red bean extract. The results show that the stability of the prepared transdermal composition decreased significantly, and the whitening / spot-removing effect also decreased significantly. This indicates that the special fermentation of these four raw materials in this invention can improve the stability of the transdermal composition and further enhance the whitening / spot-removing effect. Comparative Example 11 varied the mass ratio of the transdermal absorption enhancer. The results showed that the whitening and spot-removing effect of the prepared transdermal composition significantly decreased. This indicates that the four whitening and spot-removing active ingredients in this invention can only achieve maximum skin absorption when the transdermal absorption enhancer is used in a specific ratio. The whitening and spot-removing active ingredients and the transdermal absorption enhancer in this invention can synergistically improve the transdermal properties and whitening and spot-removing effect of the transdermal composition. These experimental results further demonstrate the importance of the technical solution defined in this invention for its technical effect.

[0151] The above description represents the preferred embodiments of the present invention. It should be noted that those skilled in the art can make various improvements and modifications without departing from the principles of the present invention, and these improvements and modifications should also be considered within the scope of protection of the present invention.

Claims

1. A transdermal composition with whitening and freckle-removing effects, characterized in that, The transdermal composition comprises the following ingredients by weight percentage: The product contains 10-15% whitening and spot-removing ingredients, 5-40% emulsifier, 0.5-30% emulsifier, 0.1-20% filler, 0.1-10% thickener, 1-3% transdermal absorption enhancer, and the balance being water. The whitening and spot-removing ingredients are composed of niacinamide, arbutin, glycerin, water, plant extracts and fermentation extracts in a mass ratio of (0.2-0.4):(0.5-0.8):(0.1-0.3):(5-10):(3-5):

1. The plant extract is composed of milk thistle extract, coral grass extract and red peony root extract in a mass ratio of (1.5-3.5):(0.5-1):

1. The fermentation extract is a mixture of soybean seed coat extract, seaweed extract and sea buckthorn extract in a mass ratio of (0.8-1):(3-4):

1. The fermentation broth is obtained by fermentation with a compound fermentation agent. The fermentation broth is filtered to obtain filtrate. The filtrate is sterilized at 100-110℃ for 30-60 min. Then the filtrate is centrifuged, the supernatant is collected, and the fermentation extract is obtained by freeze drying. The compound fermentation agent includes Bacillus vesiclei, Lactobacillus murineis, and Streptomyces oliveri in a mass ratio of (6-10):(2.5-4):

1. Milk thistle extract was purchased from Hunan Langlin Biological Resources Co., Ltd.; coral grass extract was purchased from Lanzhou Waterles Biotechnology Co., Ltd.; red peony root extract was purchased from Xi'an Yuno Bioengineering Co., Ltd.; soybean seed coat extract was purchased from Shaanxi Guanchen Biotechnology Co., Ltd.; large-leaved seaweed extract was purchased from Ningxia Xiangcao Biotechnology Co., Ltd.; sea buckthorn extract was purchased from Lanzhou Waterles Biotechnology Co., Ltd.; Bacillus vesicularis was purchased from Shanghai Chen Microbial Technology Co., Ltd., model number GDMCC 800145; Lactobacillus murineis was purchased from Shanghai Chen Microbial Technology Co., Ltd., model number CICC23144; Streptomyces oliveri was purchased from Shanghai Chen Microbial Technology Co., Ltd., model number CICC 11001. The transdermal absorption enhancer, in a mass ratio of (2-4):(8-10):1, includes peppermint oil, lauryl acetonide, and N-acetylproline pentanol ester.

2. The transdermal composition with whitening and freckle-removing effects according to claim 1, characterized in that: The emollient is one or more of the following: caprylic / capric triglyceride, squalane, avocado oil, shea butter, jojoba oil, dimethicone, dimethicone alcohol, PEG-11 methyl ether dimethicone, phytosterol, hydrogenated polyisobutylene, rapeseed oil, polydecene, soybean oil, olive oil, isododecane, isohexadecane, stearyl alcohol, and behenyl alcohol; The emulsifier is one or more of the following: olive oil PEG-7 ester, PEG-8 caprylic / capric glyceride, sorbitan olive oil ester, polysorbate-20, lauryl alcohol polyether-23, PEG-40 stearate, stearyl alcohol polyether-21, polysorbate-80, soybean lecithin PC60, poloxamer 407, PEG-30 dihydroxystearate, and cetearyl alcohol polyether-25; The filler is one or more of the following: titanium dioxide, mica, boron nitride, polymethylsilsesquioxane, diatomaceous earth, kaolin, cellulose acetate, aluminum octyl succinate starch, talc, barium sulfate, and volcanic ash. The thickener is one or more of the following: hydroxyethyl cellulose, xanthan gum, carbomer, polymer EMT-10, polyacrylate crosspolymer-6, sodium acrylate / sodium acryloyl dimethyl taurate copolymer, acryloyl dimethyl taurate amine / VP copolymer, acrylate / C10-30 alkyl acrylate crosspolymer, polyvinyl alcohol, gum arabic, and hydroxypropyl starch phosphate.

3. The transdermal composition with whitening and freckle-removing effects according to claim 1, characterized in that: The preparation method of the fermentation extract is as follows: S11: Mix soybean seed coat extract, seaweed extract and sea buckthorn extract in a certain proportion to obtain a mixture; S12: Add compound fermentation agent to the mixture, the inoculum amount of compound fermentation agent is 6-8wt%, then add water, the mass of the added water is 15-20 times that of the mixture, continuously introduce oxygen, ferment at 28-32℃ for 5-7 days to obtain fermentation liquid; S13: Filter the fermentation broth to obtain filtrate, sterilize the filtrate at 100-110℃ for 30-60 min, then centrifuge the filtrate, collect the supernatant, freeze-dry it to obtain the fermentation extract.

4. A method for preparing a transdermal composition with whitening and freckle-removing effects according to any one of claims 1-3, characterized in that: Includes the following steps: S1: Wet and disperse the thickener in water to obtain a mixture; S2: Add emollient and filler to the mixture in step S1, heat to 60-80℃, and homogenize at 2500-3500r / min for 3-5min to ensure complete dispersion; S3: Add emulsifier to step S2, homogenize at 2500-3500r / min for 3-5min to ensure complete emulsification, and add whitening and spot-removing ingredients and transdermal absorption promoter while stirring and cooling to obtain transdermal composition.

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