Whitening and brightening composition and cosmetic thereof

Abstract

The invention discloses a whitening and brightening composition and a cosmetic thereof. The whitening and brightening composition is prepared from ascorbyl tetraisopalmitate, tranexamic acid, Brigtenyl, LightSKN CN, a resveratrol fermentation product, fermented lotus essence and super vitamin A, brigtenyl is a mixture composed of a first solvent, glycerin and diglucosyl gallic acid; lightSKN CN is a mixture composed of a second solvent, 1, 3-propylene glycol, xanthophyll, lecithin, sodium ascorbate and vitamin E; the resveratrol fermentation product is a mixture composed of a third solvent, a pichia pastoris fermentation lysate filtrate and resveratrol; the fermented lotus seed essence is a mixture composed of a fourth solvent, butanediol and a lotus seed extract; the super vitamin A is a mixture of isosorbide dimethyl ether and hydroxyl pinacolone retinoate. The whitening and brightening composition not only can inhibit melanin generation, reduce melanin transfer and accelerate melanin metabolism, but also can remove excessive free radicals in skin, so that the effects of long-acting skin whitening and skin brightening are achieved.

Description

[0001] A whitening and brightening composition and its cosmetic Technical Field This invention belongs to the field of cosmetic technology, and in particular relates to a whitening and brightening composition and its cosmetics. Background Technology

[0002] With social progress and improved living standards, personal image and skin health are receiving increasing attention. Skin whitening, as an important component of beauty and skincare, has always been one of the core demands of the cosmetics market.

[0003] Currently, whitening products on the market face several issues. For example, some whitening products contain controversial ingredients, such as rhododendron alcohol, which may cause adverse reactions such as white patches on the skin. Furthermore, some products have been reported to have excessive mercury levels or contain banned whitening ingredients, raising consumer concerns about the safety of whitening products. Meanwhile, other whitening ingredients, such as arbutin, while having whitening effects, may cause skin irritation or even discoloration of normal skin if the concentration is too high. Therefore, modern consumers no longer simply pursue whiter skin; they pay more attention to health, skin condition, and overall beauty. They expect products to achieve continuous whitening while also providing multiple benefits such as skin nourishment and brightening, and they demand gentle, low-irritant ingredients.

[0004] CN117084959A discloses a composition with whitening effects, comprising ascorbic acid peptides, dimethylmethoxybenzodihydropyranol, fibronectin, *Ligustrum lucidum* extract, and ethylhexyl methoxycinnamate. These substances primarily achieve their whitening effect by inhibiting tyrosinase activity and reducing melanin synthesis. While the whitening ingredients target a wide range of sites, their whitening pathways are relatively limited, posing a challenge to the sustained effectiveness of the product's whitening effect.

[0005] Therefore, there is an urgent need for a whitening and brightening composition and its cosmetic to address the shortcomings of existing technologies. Summary of the Invention

[0006] In view of the above problems, the purpose of this invention is to provide a whitening and brightening composition and the cosmetic thereof, which can achieve long-lasting whitening and brightening effects on the skin.

[0007] To achieve the above objectives, the first aspect of the present invention provides a whitening and brightening composition comprising ascorbate tetraisopalmitate, tranexamic acid, Brightenyl, LightSKN CN, resveratrol ferment, fermented lotus extract, and super vitamin A; Brightenyl is a mixture of a first solvent, glycerol, and disaccharidic gallic acid; LightSKN CN is a mixture of a second solvent, 1,3-propanediol, lutein, lecithin, sodium ascorbate, and vitamin E. The resveratrol ferment is a mixture of a third solvent, Pichia pastoris fermentation lysate filtrate, and resveratrol. Fermented lotus extract is a mixture of a fourth solvent, butylene glycol, and lotus seed extract. Super Vitamin A is a mixture of isosorbide dimethyl ether and hydroxypinazone retinate.

[0008] Compared with existing technologies, the six ingredients in the whitening and brightening composition of this invention—ascorbic acid tetraisopalmitate, tranexamic acid, Brightenyl, LightSKN CN, resveratrol ferment, and super vitamin A—exhibit a strong synergistic effect in inhibiting melanin production and reducing skin pigmentation. Simultaneously, Brightenyl and LightSKN CN work together to slow down the transfer of melanin from the basal layer to the stratum corneum, further reducing the risk of age spots. Furthermore, fermented lotus extract, tranexamic acid, Brightenyl, and super vitamin A work together to promote skin cell differentiation and renewal, accelerating melanin metabolism and elimination, which helps to fade spots and brighten skin tone. In addition, ascorbic acid tetraisopalmitate, Brightenyl, and resveratrol ferment have a synergistic effect to exert a powerful antioxidant effect, clearing excess free radicals in the skin and maintaining a healthy skin condition, which further enhances the whitening and brightening effect. In summary, the whitening and brightening composition of the present invention selectively uses seven substances as raw materials: ascorbate tetraisopalmitate, tranexamic acid, Brightenyl, LightSKN CN, resveratrol ferment, fermented lotus extract, and super vitamin A. Through multiple mechanisms of action, it can not only effectively inhibit melanin production and reduce melanin transfer, but also accelerate melanin metabolism and remove excess free radicals in the skin, thereby achieving long-lasting whitening and brightening effects on the skin.

[0009] Further, by weight, the whitening and brightening composition of the present invention comprises 0.1 to 3 parts of ascorbic acid tetraisopalmitate, 0.3 to 4 parts of tranexamic acid, 0.1 to 2 parts of Brightenyl, 0.05 to 2 parts of LightSKN CN, 0.1 to 3 parts of resveratrol ferment, 0.1 to 1.5 parts of fermented lotus extract, and 0.1 to 3 parts of super vitamin A.

[0010] Furthermore, the Brightenyl of the present invention is a mixture of a first solvent, glycerol, and disaccharidic gallic acid in a mass ratio of 25~50:50~74:1~5.

[0011] Furthermore, the LightSKN CN of the present invention is a mixture of a second solvent, 1,3-propanediol, lutein, lecithin, sodium ascorbate and vitamin E in a mass ratio of 65~87:10~30:2.5~3.5:1~3:0.1~0.3:0.01~0.03.

[0012] Furthermore, the resveratrol ferment of the present invention is a mixture of a third solvent, Pichia pastoris fermentation lysate filtrate, and resveratrol in a mass ratio of 57~79.5:20~40:0.5~3.

[0013] Furthermore, the fermented lotus extract of the present invention is a mixture of a fourth solvent, butylene glycol, and lotus seed extract in a mass ratio of 58~79.9:20~40:0.1~2.

[0014] Furthermore, the super vitamin A of the present invention is a mixture of isosorbide dimethyl ether and hydroxypinazone retinate in a mass ratio of 80~95:5~20.

[0015] Accordingly, a second aspect of the present invention also provides a cosmetic, including a commonly used base for cosmetic topical formulations, and further including the aforementioned whitening and brightening composition.

[0016] Furthermore, the dosage form of the cosmetic of the present invention includes at least one of ointment, lotion, serum and cream.

[0017] Further, by weight, the commonly used matrix of the present invention includes 0.1 to 1 part thickener, 3 to 15 parts moisturizer, 1 to 4 parts emulsifier, 0.5 to 5 parts oil, 0.03 to 0.25 parts antioxidant, 0.5 to 5 parts soothing component, 0.5 to 1.8 parts antibacterial agent, 60 to 85 parts fifth solvent, and 1 to 15 parts whitening and brightening composition. Detailed Implementation

[0018] The claims of the present invention will be further described in detail below with reference to specific embodiments, but this does not constitute any limitation on the present invention. Any limited modifications made by any person within the scope of protection of the claims of the present invention are still within the scope of protection of the claims of the present invention.

[0019] This invention provides a whitening and brightening composition comprising ascorbate tetraisopalmitate, tranexamic acid, Brightenyl, LightSKN CN, resveratrol ferment, fermented lotus extract, and super vitamin A. Further, by weight parts, it comprises 0.1-3 parts ascorbate tetraisopalmitate, 0.3-4 parts tranexamic acid, 0.1-2 parts Brightenyl, 0.05-2 parts LightSKN CN, 0.1-3 parts resveratrol ferment, 0.1-1.5 parts fermented lotus extract, and 0.1-3 parts super vitamin A.

[0020] The content of ascorbate tetraisopalmitate can be, but is not limited to, 0.1 parts, 0.5 parts, 1 part, 1.3 parts, 1.8 parts, 2.1 parts, 2.5 parts, and 3.0 parts. Ascorbate tetraisopalmitate (VCIP) is a fat-soluble derivative of vitamin C, and its mildness is much higher than that of vitamin C, making it especially suitable for sensitive skin. In addition, it can promote collagen regeneration, reduce inflammation, treat acne, reduce melanin synthesis, and has antioxidant effects.

[0021] The content of tranexamic acid can be, but is not limited to, 0.3 parts, 0.6 parts, 1 part, 1.3 parts, 1.8 parts, 2.1 parts, 2.5 parts, 3.0 parts, 3.5 parts, and 4.0 parts. Tranexamic acid can prevent the interaction between melanocytes and keratinocytes, inhibiting melanin synthesis; it can also activate autophagy, activate MAPK / ERK, promote the degradation of MITF, downregulate the expression of melanin-related proteins, and inhibit melanin production; and inhibit UVB-induced pigmentation, removing age spots, melasma, etc. In addition, tranexamic acid is non-irritating, non-toxic, and has no side effects on the eyes and skin. It is biodegradable and is a mild, safe, and highly effective whitening ingredient.

[0022] The content of Brightenyl can be, but is not limited to, 0.1 parts, 0.3 parts, 0.5 parts, 0.8 parts, 1.0 parts, 1.2 parts, 1.5 parts, 1.8 parts, and 2.0 parts. Although VCIP is more stable than pure vitamin C, it retains the core antioxidant properties of vitamin C, and therefore still has a certain degree of oxidative sensitivity, thus affecting its whitening and brightening effect. Based on this, the active ingredient in Brightenyl is disaccharidated gallic acid, which has antioxidant and free radical scavenging effects. Therefore, Brightenyl can delay the oxidation of VCIP, thereby improving the whitening and brightening effect. In addition, disaccharidated gallic acid can also inhibit tyrosinase activity and MITF activity, thereby reducing melanin production; it can also bind to galactose receptors, thereby inhibiting melanin transfer and melanin accumulation; it also has a photoprotective effect to prevent DNA damage, reducing exogenous damage, which also helps maintain the healthy state of the skin; in addition, it can also inhibit Nf-kB and PGE2 inflammatory factors, thereby reducing pigmentation and brightening and evening out skin tone. In addition, Brightenyl is also very gentle on the skin.

[0023] The content of LightSKN CN can be, but is not limited to, 0.05 parts, 0.1 parts, 0.2 parts, 0.3 parts, 0.5 parts, 0.8 parts, 1.0 parts, 1.2 parts, 1.5 parts, 1.8 parts, and 2.0 parts. LightSKN CN possesses an intelligent melanin regulation mechanism. It does not alter the activity of tyrosinase in melanocytes, but only reduces inflammation and melanocyte proliferation under conditions conducive to melanin production. Therefore, it can be used to balance skin tone and eliminate blemishes. Under conditions of melanin production, LightSKN selectively reduces melanin production by regulating nitric oxide synthesis, and it also reduces melanin transfer by decreasing the activity of p70S6 kinase. Furthermore, LightSKN CN has low skin irritation.

[0024] The content of resveratrol fermentation product can be, but is not limited to, 0.1 parts, 0.2 parts, 0.3 parts, 0.5 parts, 0.8 parts, 1.0 parts, 1.2 parts, 1.5 parts, 1.8 parts, 2.0 parts, 2.5 parts, 2.8 parts, and 3.0 parts. Resveratrol is a natural antioxidant found in plants. It can effectively scavenge or inhibit the generation of free radicals, inhibit lipid peroxidation, and regulate the activity of antioxidant-related enzymes. Therefore, the combination of Brightenyl and resveratrol fermentation product can effectively delay the oxidation of VCIP, thereby effectively improving the whitening and brightening effect. In addition, resveratrol fermentation product can inhibit cell proliferation and has a significant inhibitory effect on the activity of intracellular tyrosinase, thereby achieving the effect of whitening and removing blemishes. Furthermore, resveratrol fermentation product is obtained through a fermentation process. The metabolites produced during fermentation can help neutralize or reduce components that may cause skin irritation. Therefore, compared with unfermented resveratrol, resveratrol fermentation product is gentler.

[0025] The content of fermented lotus extract can be, but is not limited to, 0.1 parts, 0.2 parts, 0.3 parts, 0.5 parts, 0.8 parts, 1.0 parts, 1.2 parts, and 1.5 parts. Specifically, fermented lotus extract can be obtained through fermentation with Lactobacillus plantarum. This ingredient is gentle and suitable for various skin types. Fermented lotus extract can improve skin texture, repair pigmentation, accelerate skin metabolism, and promote the excretion of melanin.

[0026] The content of super vitamin A can be, but is not limited to, 0.1 parts, 0.2 parts, 0.3 parts, 0.5 parts, 0.8 parts, 1.0 parts, 1.2 parts, 1.5 parts, 1.8 parts, 2.0 parts, 2.5 parts, 2.8 parts, and 3.0 parts. Super vitamin A is a derivative of vitamin A that combines the advantages of retinol and retinoic acid derivatives, but significantly reduces irritation. Super vitamin A can promote cell differentiation and renewal, evening out skin tone; it can also inhibit tyrosinase activity, effectively fading pigmentation such as age spots. Moreover, compared to traditional vitamin A derivatives, it is gentler to use and suitable for a wider range of skin types.

[0027] In summary, the addition of Brightenyl effectively prevents photodamage and protects the skin from environmental aggressors. Simultaneously, the synergistic effect of VCIP, tranexamic acid, Brightenyl, LightSKN CN, resveratrol ferment, and super vitamin A effectively reduces melanin production, thereby lowering the likelihood of pigmentation. Furthermore, the dual action of Brightenyl and LightSKN CN not only targets melanin production but also reduces melanin transfer, further minimizing the risk of age spots. The synergistic effect of fermented lotus extract, tranexamic acid, Brightenyl, and super vitamin A promotes skin cell differentiation and renewal, accelerating melanin metabolism and elimination. This process helps fade existing spots and brightens the complexion, restoring a natural radiance. More importantly, the combination of VCIP, Brightenyl, and resveratrol ferment provides powerful antioxidant effects, eliminating excess free radicals and maintaining healthy skin. Therefore, this invention selects the above seven substances as raw materials. Through the above four mechanisms of action, it can not only effectively inhibit melanin production and reduce melanin transfer, but also accelerate melanin metabolism and remove excess free radicals in the skin, thereby achieving long-lasting whitening and brightening effects on the skin.

[0028] Specifically, the Brightenyl of the present invention is a mixture of a first solvent, glycerol, and disaccharidated gallic acid in a mass ratio of 25-50:50-74:1-5. More specifically, the mass ratio of the first solvent, glycerol, and disaccharidated gallic acid may be, but is not limited to, 30:60:1, 25:52:3, 45:67:4, or 50:55:2. Preferably, the first solvent is water.

[0029] Specifically, in the LightSKN CN of the present invention, the mass ratio of the second solvent, 1,3-propanediol, lutein, lecithin, sodium ascorbate, and vitamin E is 65~87:10~30:2.5~3.5:1~3:0.1~0.3:0.01~0.03. More specifically, the mass ratio of these six substances can be, but is not limited to, 65:20:3:2:0.1:0.01 or 75:25:2.7:2.2:0.2:0.02. Preferably, the second solvent is water.

[0030] Specifically, the resveratrol fermentation product of the present invention is a mixture of a third solvent, Pichia pastoris fermentation lysate filtrate, and resveratrol in a mass ratio of 57-79.5:20-40:0.5-3. More specifically, the mass ratio of the third solvent, Pichia pastoris fermentation lysate filtrate, and resveratrol can be, but is not limited to, 58:30:0.5, 72:34:1, or 62:22:1.7. Preferably, the third solvent is water.

[0031] Specifically, the fermented lotus extract of the present invention is a mixture of a fourth solvent, butylene glycol, and lotus seed extract in a mass ratio of 58-79.9:20-40:0.1-2. More specifically, the mass ratio of the fourth solvent, butylene glycol, and lotus seed extract may be, but is not limited to, 60:25:1, 65:21:0.8, or 76:33:1.4. Preferably, the fourth solvent is water.

[0032] Specifically, the super vitamin A of the present invention is a mixture of isosorbide dimethyl ether and hydroxypinazone retinate in a mass ratio of 80-95:5-20. More specifically, the mass ratio of isosorbide dimethyl ether and hydroxypinazone retinate may be, but is not limited to, 80:20, 85:15, 90:10, or 95:5.

[0033] Accordingly, the present invention also provides the application of the above-mentioned whitening and brightening composition in cosmetics. By mixing the whitening and brightening composition with a commonly used base of cosmetic topical formulations, corresponding ointment, lotion, serum and cream type cosmetics can be formed.

[0034] Specifically, by weight, the commonly used matrix includes 0.1 to 1 part thickener, 3 to 15 parts moisturizer, 1 to 4 parts emulsifier, 0.5 to 5 parts oil, 0.03 to 0.25 parts antioxidant, 0.5 to 5 parts soothing component, 0.5 to 1.8 parts antibacterial agent, and 60 to 85 parts fifth solvent, while the whitening and brightening composition is 1 to 15 parts. More specifically, the content of thickener may be, but is not limited to, 0.1 parts, 0.3 parts, 0.5 parts, 0.8 parts, or 1.0 parts; the content of humectant may be, but is not limited to, 3 parts, 4.5 parts, 6.5 parts, 9.8 parts, 12.0 parts, or 15.0 parts; the content of oil may be, but is not limited to, 0.5 parts, 1.5 parts, 2.5 parts, 3.2 parts, 3.8 parts, or 5.0 parts; and the content of antioxidant may be, but is not limited to, 0.05 parts, 0.10 parts, 0.15 parts, 0.2 parts, 0.22 parts, or 0. 25 parts; the content of the soothing component may be, but is not limited to, 0.5 parts, 1.5 parts, 2.5 parts, 3.2 parts, 3.8 parts, or 5.0 parts; the content of the antibacterial agent may be, but is not limited to, 0.5 parts, 0.8 parts, 1.0 parts, 1.2 parts, 1.5 parts, or 1.8 parts; the content of the fifth solvent may be, but is not limited to, 60 parts, 65 parts, 70 parts, 75 parts, 80 parts, or 85 parts; the content of the whitening and brightening composition may be, but is not limited to, 1 part, 5 parts, 7 parts, 9 parts, 10 parts, 12 parts, 14 parts, or 15 parts. Specifically, the fifth solvent is water.

[0035] Specifically, by mass, the thickener includes 0.1 to 0.6 parts of acrylate / C10-30 alkanol acrylate crosspolymer and 0.1 to 1 part of polymeric emulsifying thickener NS.

[0036] Specifically, by weight, the moisturizer includes 1 to 8 parts butylene glycol, 0.5 to 5 parts betaine, 0.01 to 0.1 parts sodium hyaluronate, and 0.1 to 3 parts oat β-glucan.

[0037] Specifically, by weight, the emulsifier includes 0.2 to 1 part polysorbate-80, 0.2 to 0.8 parts A165 (a mixture of glyceryl stearate and PEG-100 stearate) and 1 to 3 parts Emulium Mellifera.

[0038] Specifically, by mass, the oil comprises 0.5 to 5 parts isononyl isononanoate and 0.1 to 1 part tocopheryl acetate.

[0039] Specifically, by mass, the antioxidant includes 0.05 to 0.25 parts of butylated hydroxytoluene and 0.001 to 0.03 parts of sodium metabisulfite.

[0040] Specifically, the soothing component includes Soothing Cream, and also includes at least one of the following: Kava Pepper Extract, Bisabolol, Dipotassium Glycyrrhizate, Witch Hazel Extract, and a plant-based soothing agent. Preferably, the soothing component is a mixture of 0.5-3 parts by weight of Soothing Cream and 0.3-2 parts by weight of Kava Pepper Extract. More specifically, Soothing Cream is a mixture of butylene glycol, water, Astragalus membranaceus root extract, Saposhnikovia divaricata root extract, Calendula officinalis flower extract, Albizia julibrissin flower extract, and Gastrodia elata root extract in a mass ratio of 70-85:5-10:3-5:1-3:1-2:0.5-1:0.5-1. Soothing Cream can effectively inhibit histamine-induced itching, effectively inhibit the release of inflammatory factors / mediators (IL-1α, IL-6, TNF-α, PGE2), effectively reduce capillary permeability in sensitive states, and relieve redness and swelling symptoms during allergies, improving skin sensitivity from five dimensions: relieving itching, reducing redness, reducing swelling, relieving tightness, and relieving stinging sensation. Kava pepper extract specifically comprises extracts of kava pepper leaves, roots, and stems. Its main active ingredients are kava lactone and kava pyranone, which have good soothing and calming effects, helping to reduce skin inflammation and redness. It provides excellent care for sensitive skin or skin irritated by external factors. Therefore, this invention selectively chooses Soothing Cream and kava pepper extract as soothing components. Through synergistic effects, the product's gentleness is increased, and the occurrence of sensitive reactions is reduced.

[0041] Specifically, the antibacterial agent is a mixture of 0.2 to 0.8 parts by weight of 1,2-hexanediol and 0.3 to 1 part by weight of HL-01.

[0042] Specifically, the preparation method of the above-mentioned cosmetics includes the following steps: (1) Add the fifth solvent, part of the thickener and part of the humectant to the aqueous phase pot, stir and heat to 75~80℃, and keep warm for 5~10min after fully dissolving; (2) Add the emulsifier, oil, and some antioxidants to the oil phase pot, stir and heat to 70~78℃, and dissolve completely; (3) Add the mixture obtained in step (2) to the mixture obtained in step (1) and stir until homogenized and fully emulsified; (4) When the temperature drops to 60~65℃, add another part of the thickener and stir well; (5) When the temperature drops to 45~50℃, add the antibacterial agent and another part of the antioxidant and stir evenly; (6) Continue cooling to below 40°C, then add another portion of moisturizer, whitening and brightening composition and soothing component in sequence, and stir well; (7) Cool to room temperature, discharge and let stand, take samples and test them to ensure they pass the test before filling.

[0043] To better illustrate the purpose, technical solution, and beneficial effects of this invention, the invention will be further described below in conjunction with specific embodiments.

[0044] Specifically, details of the raw materials used in the examples and comparative examples are as follows:

[0045] Example 1 This embodiment provides a whitening and brightening essence, comprising, by weight, 0.21 parts of acrylate / C10-30 alkyl acrylate crosspolymer, 0.3 parts of high molecular weight emulsifier and thickener NS, 0.5 parts of polysorbate-80, 0.4 parts of A165, 1.5 parts of Emulium Mellifera, 1 part of isononyl isononanoate, 0.3 parts of tocopheryl acetate, 5 parts of butylene glycol, 1 part of betaine, 0.03 parts of sodium hyaluronate, 2 parts of oat β-glucan, 0.1 part of butylated hydroxytoluene, 0.005 parts of sodium metabisulfite, 9.25 parts of whitening and brightening composition, 2 parts of Soothing Cream, 1 part of Kava pepper extract, 0.3 parts of 1,2-hexanediol, 0.7 parts of HL-01, and 74.4 parts of water; wherein the whitening and brightening composition comprises 2 parts of ascorbate tetraisopalmitate, 2 parts of tranexamic acid, 1.2 parts of Brightenyl, and 1 part of LightSKN. CN, 1 part resveratrol ferment, 0.3 parts fermented lotus extract, 1.75 parts super vitamin A.

[0046] This embodiment provides a method for preparing a whitening and brightening essence, the steps of which include: (1) Add water, acrylic (ester) / C10-30 alkyl acrylate crosspolymer, butanediol, betaine, and sodium hyaluronate to an aqueous phase pot, stir and heat to 80°C, and keep warm for 10 min after fully dissolving; (2) Add polysorbate-80, A165, emulium Mellifera, isononyl isononanoate, tocopheryl acetate, and butylated hydroxytoluene to an oil phase pot and stir and heat to 75°C to dissolve completely; (3) Add the mixture obtained in step (2) to the mixture obtained in step (1) and stir until homogenized and fully emulsified; (4) When the temperature drops to 62°C, add the high molecular weight emulsifying thickener NS and stir until homogeneous; (5) When the temperature drops to 50°C, add 1,2-hexanediol, HL-01, and sodium metabisulfite and stir until homogeneous; (6) Continue cooling to 37°C, then add oat β-glucan, ascorbic acid tetraisopalmitate, tranexamic acid, Brightenyl, LightSKN CN, resveratrol ferment, fermented lotus extract, and super vitamin A in sequence. Add Soothing Cream and Kava Pepper Extract, and stir well; (7) Cool to room temperature, discharge and let stand for 24 hours, take samples and test them to ensure they pass the test before filling.

[0047] Example 2 This embodiment provides a whitening and brightening essence, comprising, by weight, 0.15 parts of acrylate / C10-30 alkyl acrylate crosspolymer, 0.6 parts of high molecular weight emulsifier and thickener NS, 0.2 parts of polysorbate-80, 0.8 parts of A165, and 2 parts of emulium. Mellifera, 2 parts isononyl isononanoate, 1 part tocopheryl acetate, 2 parts butylene glycol, 3 parts betaine, 0.01 parts sodium hyaluronate, 0.4 parts oat beta-glucan, 0.15 parts butylated hydroxytoluene, 0.01 parts sodium metabisulfite, 1.1 parts whitening and brightening composition, 0.5 parts soothing agent, 2 parts kava pepper extract, 0.2 parts 1,2-hexanediol, 1 part HL-01, 82.88 parts water; wherein the whitening and brightening composition includes 0.1 parts ascorbic acid tetraisopalmitate, 0.3 parts tranexamic acid, 0.1 parts Brightenyl, 0.2 parts LightSKN CN, 0.1 parts resveratrol ferment, 0.1 parts fermented lotus extract, and 0.2 parts super vitamin A.

[0048] This embodiment provides a method for preparing a whitening and brightening essence, the steps of which include: (1) Add water, acrylic (ester) / C10-30 alkanol acrylate crosspolymer, butanediol, betaine, and sodium hyaluronate to an aqueous phase pot, stir and heat to 78°C, and keep warm for 10 min after fully dissolving; (2) Add polysorbate-80, A165, emulium Mellifera, isononyl isononanoate, tocopheryl acetate, and butylated hydroxytoluene to an oil phase pot and stir and heat to 72°C to dissolve completely; (3) Add the mixture obtained in step (2) to the mixture obtained in step (1) and stir until homogenized and fully emulsified; (4) When the temperature drops to 65°C, add the high molecular weight emulsifying thickener NS and stir until homogeneous; (5) When the temperature drops to 48°C, add 1,2-hexanediol, HL-01, and sodium metabisulfite and stir until homogeneous; (6) Continue cooling to 35℃, then add oat β-glucan, ascorbic acid tetraisopalmitate, tranexamic acid, Brightenyl, LightSKN CN, resveratrol ferment, fermented lotus extract, and super vitamin A in sequence. Add Soothing Cream and Kava Pepper Extract, and stir well; (7) Cool to room temperature, discharge and let stand for 20 hours, and fill after sampling and testing.

[0049] Example 3 This embodiment provides a whitening and brightening essence, comprising, by weight, 0.35 parts of acrylate / C10-30 alkyl acrylate crosspolymer, 0.5 parts of high molecular weight emulsifier and thickener NS, 0.7 parts of polysorbate-80, 0.3 parts of A165, 2 parts of Emulium Mellifera, 4 parts of isononyl isononanoate, 0.1 parts of tocopheryl acetate, 6 parts of butylene glycol, 0.5 parts of betaine, 0.1 parts of sodium hyaluronate, 3 parts of oat β-glucan, 0.2 parts of butylated hydroxytoluene, 0.005 parts of sodium metabisulfite, 15 parts of whitening and brightening composition, 3 parts of soothing cream, 0.5 parts of kava pepper extract, 0.8 parts of 1,2-hexanediol, 0.5 parts of HL-01, and 62.45 parts of water; wherein the whitening and brightening composition includes 3 parts of ascorbate tetraisopalmitate, 3 parts of tranexamic acid, 2 parts of Brightenyl, and 2 parts of LightSKN. CN, 2 parts resveratrol ferment, 1 part fermented lotus extract, 2 parts super vitamin A.

[0050] This embodiment provides a method for preparing a whitening and brightening essence, the steps of which include: (1) Add water, acrylic (ester) / C10-30 alkanol acrylate crosspolymer, butanediol, betaine, and sodium hyaluronate to an aqueous phase pot, stir and heat to 75°C, and keep warm for 10 minutes after fully dissolving; (2) Add polysorbate-80, A165, emulium Mellifera, isononyl isononanoate, tocopheryl acetate, and butylated hydroxytoluene to an oil phase pot and stir and heat to 70°C to dissolve completely; (3) Add the mixture obtained in step (2) to the mixture obtained in step (1) and stir until homogenized and fully emulsified; (4) When the temperature drops to 61°C, add the high molecular weight emulsifying thickener NS and stir until homogeneous; (5) When the temperature drops to 45°C, add 1,2-hexanediol, HL-01, and sodium metabisulfite and stir until homogeneous; (6) Continue cooling to 33℃, then add oat β-glucan, ascorbic acid tetraisopalmitate, tranexamic acid, Brightenyl, LightSKN CN, resveratrol ferment, fermented lotus extract, and super vitamin A in sequence. Add Soothing Cream and Kava Pepper Extract, and stir well; (7) Cool to room temperature, discharge and let stand for 30 hours, take samples and test them to ensure they pass the test before filling.

[0051] Comparative Example 1 Comparative Example 1 provides a whitening and brightening essence and its preparation method. Comparative Example 1 is basically the same as Example 1. The only difference between Comparative Example 1 and Example 1 is that ascorbic acid tetraisopalmitate was removed and the water content was adjusted from 74.4 parts to 76.4 parts.

[0052] Comparative Example 2 Comparative Example 2 provides a whitening and brightening essence and its preparation method. Comparative Example 2 is basically the same as Example 1. The only difference between Comparative Example 2 and Example 1 is that tranexamic acid was removed and the water content was adjusted from 74.4 parts to 76.4 parts.

[0053] Comparative Example 3 Comparative Example 3 provides a whitening and brightening essence and its preparation method. Comparative Example 3 is basically the same as Example 1. The only difference between Comparative Example 3 and Example 1 is that Brightenyl was removed and the water content was adjusted from 74.4 parts to 75.6 parts.

[0054] Comparative Example 4 Comparative Example 4 provides a whitening and brightening essence and its preparation method. Comparative Example 4 is basically the same as Example 1. The only difference between Comparative Example 4 and Example 1 is that LightSKN CN was removed and the water content was adjusted from 74.4 parts to 75.4 parts.

[0055] Comparative Example 5 Comparative Example 5 provides a whitening and brightening essence and its preparation method. Comparative Example 5 is basically the same as Example 1. The only difference between Comparative Example 5 and Example 1 is that the resveratrol fermentation product was removed and the water content was adjusted from 74.4 parts to 75.4 parts.

[0056] Comparative Example 6 Comparative Example 6 provides a whitening and brightening essence and its preparation method. Comparative Example 6 is basically the same as Example 1. The only difference between Comparative Example 6 and Example 1 is that the fermented lotus essence was removed and the water content was adjusted from 74.4 parts to 74.7 parts.

[0057] Comparative Example 7 Comparative Example 7 provides a whitening and brightening essence and its preparation method. Comparative Example 7 is basically the same as Example 1. The only difference between Comparative Example 7 and Example 1 is that: super vitamin A was removed and the water content was adjusted from 74.4 parts to 76.15 parts.

[0058] The stability and gentleness of the whitening and brightening essences in Examples 1-3 were tested according to the following test methods, and the results are shown in Table 1.

[0059] Stability test: Test sample: Whitening and brightening essence provided in Examples 1-3.

[0060] Test method: 30 g of each test sample was placed in sample bottles A1-A3, and all sample bottles were simultaneously placed in the same biochemical incubator for one month at a temperature of 45℃. Similarly, 30 g of each test sample was placed in sample bottles B1-B3, and all sample bottles were simultaneously placed in the same biochemical incubator for one month at a temperature of -16℃. Each test sample showed slight discoloration at 45℃, but no discoloration or precipitation was observed at -16℃, indicating that the product provided by this invention has good heat and cold resistance stability.

[0061] Mildness test: Test sample: Whitening and brightening essence provided in Examples 1-3.

[0062] Test Method: The chorioallantoic membrane (CAM) is a respiratory membrane surrounding the chicken embryo. Because the surface of the chicken embryo's CAM is richly vascularized, it can be considered a complete organism. This experiment utilizes the intact, clear, and transparent vascular system of the mid-stage hatched chicken embryo's CAM. A certain amount of the test substance is directly contacted with the chicken embryo's CAM. After a specified exposure time, changes in chorioallantoic membrane toxicity indicators (such as hemorrhage, coagulation, and vascularization) are observed, scored, and the mathematical average is calculated to assess the irritant properties of the test substance.

[0063] (1)Chicken embryo preparation: Fertilized chicken embryos of breeds such as White Leghorn chicken, with the weight of the chicken embryos being 50 g - 60 g, and preferably SPF chicken embryos, are placed in an incubator for incubation. The temperature is controlled at 37.5°C ± 0.5°C, the relative humidity is 55% - 70%, and the frequency of egg turning is 3 times / h - 6 times / h. On the 8th day of incubation, the eggs are examined with an egg candler, and unfertilized and inactive chicken embryos are discarded. Chicken embryos with well-developed blood vessels are selected, and the position of the air chamber is marked on the eggshell surface.

[0064] (2)Testing process: Each group has at least 6 chicken embryos, and negative and positive controls need to be set for each experiment. The experiment starts on the 9th day. Carefully peel off the part of the eggshell in the air chamber with a dental curved forceps, drip a few drops of normal saline on the eggshell membrane surface to make it fully wet, pour out the saline after wetting, and then carefully remove the eggshell membrane with forceps, ensuring that the exposed chorioallantoic membrane is intact without any damage. Take 0.3 ml / 0.3 g of the test substance and directly apply it to the CAM. Spread it as much as possible to ensure that the coverage area reaches at least 50%. After acting for 3 minutes, gently rinse the surface of the CAM with double-distilled water, complete the rinsing within 30 seconds, pour out the liquid, and immediately observe the degree of change in each toxic effect under a stereomicroscope. Score according to capillary bleeding, coagulation, and vascular lysis conditions (ES).

[0065] (3)Result observation: Bleeding: Blood flows out from the blood vessels or capillaries of the CAM. According to no bleeding, mild bleeding, moderate bleeding, and severe bleeding, scores of 0, 1, 2, and 3 are given respectively.

[0066] Coagulation: Refers to the protein denaturation inside and outside the blood vessels, manifested as thrombosis, wall swelling, appearance of coagulation points inside and outside the blood vessels, and milky turbidity outside the blood vessels. According to no coagulation, mild coagulation, moderate coagulation, and severe coagulation, scores of 0, 1, 2, and 3 are given respectively.

[0067] Vascular lysis: Refers to the ablation of blood vessels on the CAM membrane. According to no vascular lysis, mild vascular lysis, moderate vascular lysis, and severe vascular lysis, scores of 0, 1, 2, and 3 are given respectively.

[0068] (4)Result calculation and evaluation Calculate the average score of ES according to the following formula. If ES ≤ 12, it indicates no / mild irritation; if 12 < ES < 16, it indicates moderate irritation; if ES ≥ 16, it indicates severe irritation.

[0069]

[0070] Table 1 Results of stability and mildness tests

[0071] As shown in Table 1, the whitening and brightening essence of the present invention has good stability and gentleness.

[0072] The whitening and brightening essences of Examples 1-3 and Comparative Examples 1-7 were tested for tyrosinase activity inhibition according to the following test method. The test results are shown in Table 2.

[0073] Tyrosinase activity inhibition test: Test samples: Whitening and brightening essences provided in Examples 1-3 and Comparative Examples 1-7.

[0074] Sample preparation: Prepare samples at a ratio of 0.45 mg sample to 1 mL serum-free culture medium; Cell culture: Mouse B16 melanoma cells were grown to a confluence state, digested with trypsin-EDTA for 5 min, and dispersed by pipetting. The cell suspension was transferred to centrifuge tubes and centrifuged at 1000 rpm for 5 min. The supernatant was discarded, and culture medium was added to prepare a cell suspension. The cell suspension was diluted to a certain concentration with culture medium. Logarithmic growth phase B16 cells were seeded in 96-well plates at a cell density of 7 × 10⁶ cells / well. 4 CFU / mL, 100 μL per well, plated and labeled on the top cover of the cell culture plate. Incubate for 24 h. After 24 h of culture, carefully aspirate the supernatant from the cell culture plate and divide it into blank, positive control, and sample groups. Add the prepared test sample to the sample group, add culture medium containing α-arbutin to the positive control group, and add serum-free culture medium without the drug to the blank group. The addition volume is 100 μL / well, with 4 replicates for each concentration. After addition, incubate for 72 h.

[0075] Intracellular tyrosinase inhibition rate assay: After incubation for 72 h, the supernatant was discarded from cell plates, and 150 μL of 1% Triton X-100 solution was added to each well. The plates were then rapidly frozen at -80°C for 30 min, followed by thawing at room temperature to completely lyse the cells. After pre-warming at 37°C for 5 min, 60 μL of 0.5% L-DOPA solution was added, and the reaction was carried out at 37°C for 2 h. The absorbance (OD) value was measured at 490 nm using a microplate reader. The tyrosinase activity inhibition rate was calculated.

[0076] Tyrosinase activity inhibition rate (%) = (1 - average absorbance value of sample / average absorbance value of blank) × 100%.

[0077] Table 2 Results of Tyrosinase Activity Inhibition Rate

[0078] As shown in Table 2, the six components in the whitening and brightening composition of the present invention—ascorbic acid tetraisopalmitate, tranexamic acid, Brightenyl, LightSKN CN, resveratrol ferment, and super vitamin A—have a good synergistic effect in inhibiting melanin production and reducing skin pigmentation.

[0079] The whitening and brightening essences of Examples 1-3 and Comparative Examples 1-7 were subjected to experiments to inhibit the transfer of existing melanin to epidermal cells according to the following test methods. The test results are shown in Table 3.

[0080] Test samples: Whitening and brightening essences provided in Examples 1-3 and Comparative Examples 1-7.

[0081] Test principle: Melanocytes produce melanin, and melanin granules are transferred to keratinocytes via the dendritic processes of melanocytes. The melanin granules transferred to keratinocytes then ascend with epidermal cells to the stratum corneum, thus forming pigmentation on the skin. Therefore, inhibiting the transfer of melanin granules to epidermal cells solves the problem of melanin transfer.

[0082] Sample preparation: The test sample was added to distilled water to prepare test substances with concentrations of 20 μg / ml and 30 μg / ml.

[0083] Test method: Keratinocytes and melanocytes were co-cultured, and 5 ml of the test substance was added to each culture and incubated at a constant temperature for 6 days. The melanin content was then measured. The blank control group consisted only of co-cultured keratinocytes and melanocytes.

[0084] Table 3 Results of melanin transfer inhibition rate

[0085] As shown in Table 3, the combination of Brightenyl and LightSKN CN in this invention can slow down the transfer of melanin from the basal layer to the stratum corneum, further reducing the risk of pigmentation formation.

[0086] The antioxidant efficacy of the whitening and brightening essences of Examples 1-3 and Comparative Examples 1-7 was tested according to the following test methods, and the test results are shown in Table 4.

[0087] Antioxidant efficacy test: Test samples: Whitening and brightening essences provided in Examples 1-3 and Comparative Examples 1-7.

[0088] Test method: (1) Preparation of DPPH-ethanol solution: Weigh 12 mg of 1,1-diphenyl-2-trinitrophenylpyrrolidone (Macklin, purity greater than 96%) and dissolve it in anhydrous ethanol. Add anhydrous ethanol to make up to 250 mL in a brown volumetric flask. Prepare fresh before use. (2) Sampling test: Take 1 mL of the sample to be tested and 1 mL of DPPH-ethanol solution and add them to a 5 mL brown volumetric flask. Add 3 mL of anhydrous ethanol, shake well, and react in the dark for a period of time. Then, measure the absorbance at a wavelength of 517 nm using a cuvette. (3) Data Analysis: The formula for calculating the free radical scavenging rate (Y) is: Y(%) = [1 - (AB) / (CD)] x 100% Wherein, A is the absorbance value after reacting 1 mL of the test sample with 1 mL of DPPH-ethanol solution in step (2); B is the absorbance value of the ultrapure water solution of the test sample with 1 mL added, that is, replacing 1 mL of ultrapure water with 1 mL of DPPH-ethanol solution in step (2); C is the absorbance value of the test sample without adding 1 mL of DPPH-ethanol solution, that is, replacing 1 mL of the test sample with 1 mL of ultrapure water in step (2); D is the absorbance value of the test sample without adding DPPH-ethanol solution, that is, the absorbance value of the mixture of 2 mL of ultrapure water and 3 mL of anhydrous ethanol. Table 4. Free radical scavenging rate test results

[0089] As shown in Table 4, the ascorbate tetraisopalmitate, Brightenyl, and resveratrol ferment of the present invention have a synergistic effect to exert a powerful antioxidant effect, remove excess free radicals in the skin, and maintain the skin's healthy state, which can further improve the whitening and brightening effect.

[0090] The whitening and brightening essences of Examples 1-3 and Comparative Examples 1-7 were tested for their whitening effects according to the following test methods. The test results are shown in Table 5.

[0091] (1) Recruit 100 volunteers aged 18-60, female or male, with daily skincare habits, and meeting the inclusion and exclusion criteria of the "Cosmetic Safety Technical Specifications". The volunteers were randomly divided into 10 groups and used the products of Examples 1-3 and Comparative Examples 1-7 respectively.

[0092] (2) The whitening effect of skincare products is measured using a skin colorimeter and a skin melanin analyzer. A skin colorimeter is an instrument capable of measuring L*a*b* color space data as defined by the International Commission on Illumination (CIE). The parameters characterizing human skin color are measured using a skin colorimeter or a reflectance spectrophotometer in the L*a*b* color space. The calculation formula is as follows:

[0093] A skin melanin analyzer is an instrument that measures the skin's melanin content (MI) based on the principle of spectral absorption.

[0094] (3) Testing Procedure: The test area is the face. No products (cosmetics or topical medications) should be used on the test area for 2-3 days prior to the test, and the area should not come into contact with water for 1-3 hours before the test. Before the test, the subject needs to cleanse their face and sit quietly for 30 minutes in a laboratory at 21±1℃ and 50±10%RH, without drinking water or beverages. The subject should remain relaxed. After 30 minutes, the laboratory technician will conduct the test and then instruct the subject on how to use the product. The same assessment and testing will be conducted again in weeks 4 and 8. The L*, a*, and b* values ​​of the pigmented area of ​​the test site will be measured using a skin colorimeter. Each test area will be tested three times, and the ITA° value will be recorded and calculated. The higher the ITA° value of the test area, the lighter the skin tone, and vice versa. The MI value of the pigmented area of ​​the test site will be measured using a skin melanin analyzer. Each test area will be tested three times, and the value will be recorded. The lower the MI value of the test area, the lighter the skin tone, and vice versa. If the data is normally distributed, the t-test method is used for statistical analysis; if the data is not normally distributed, the rank-sum test method is used for statistical analysis. All statistical methods use two-tailed tests, with a significance level of α=0.05.

[0095] Table 5. Whitening effect test results

[0096] As shown in Table 5, the whitening and brightening composition of the present invention can achieve long-lasting whitening and brightening effects on the skin. This is because the present invention specifically selects seven substances as raw materials: ascorbate tetraisopalmitate, tranexamic acid, Brightenyl, LightSKN CN, resveratrol ferment, fermented lotus extract, and super vitamin A. Through multiple mechanisms of action, it can not only effectively inhibit melanin production and reduce melanin transfer, but also accelerate melanin metabolism and remove excess free radicals in the skin, thereby achieving long-lasting whitening and brightening effects on the skin.

[0097] 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 and brightening composition, characterized in that, Including ascorbate tetraisopalmitate, tranexamic acid, Brightenyl, LightSKN CN, resveratrol ferment, fermented lotus extract, and super vitamin A; The Brightenyl is a mixture of a first solvent, glycerol, and disaccharidic gallic acid; The LightSKN CN is a mixture of a second solvent, 1,3-propanediol, lutein, lecithin, sodium ascorbate, and vitamin E. The resveratrol ferment is a mixture of a third solvent, Pichia pastoris fermentation lysate filtrate, and resveratrol. The fermented lotus essence is a mixture of a fourth solvent, butylene glycol and lotus seed extract; The super vitamin A is a mixture of isosorbide dimethyl ether and hydroxypinazone retinate.

2. The whitening and brightening composition according to claim 1, characterized in that, By weight, it comprises 0.1 to 3 parts of the ascorbic acid tetraisopalmitate, 0.3 to 4 parts of the tranexamic acid, 0.1 to 2 parts of the Brightenyl, 0.05 to 2 parts of the LightSKN CN, 0.1 to 3 parts of the resveratrol ferment, 0.1 to 1.5 parts of the fermented lotus extract, and 0.1 to 3 parts of the super vitamin A.

3. The whitening and brightening composition according to claim 1, characterized in that, The Brightenyl is a mixture of a first solvent, glycerol, and disaccharidic gallic acid in a mass ratio of 25~50:50~74:1~5.

4. The whitening and brightening composition according to claim 1, characterized in that, The LightSKN CN is a mixture of a second solvent, 1,3-propanediol, lutein, lecithin, sodium ascorbate, and vitamin E in a mass ratio of 65~87:10~30:2.5~3.5:1~3:0.1~0.3:0.01~0.

03.

5. The whitening and brightening composition according to claim 1, characterized in that, The resveratrol ferment is a mixture of a third solvent, Pichia pastoris fermentation lysate filtrate, and resveratrol in a mass ratio of 57~79.5:20~40:0.5~3.

6. The whitening and brightening composition according to claim 1, characterized in that, The fermented lotus extract is a mixture of a fourth solvent, butylene glycol, and lotus seed extract in a mass ratio of 58~79.9:20~40:0.1~2.

7. The whitening and brightening composition according to claim 1, characterized in that, The super vitamin A is a mixture of isosorbide dimethyl ether and hydroxypinazone retinate in a mass ratio of 80~95:5~20.

8. A cosmetic product, characterized in that, It includes common bases for cosmetic topical formulations, and also includes the whitening and brightening composition as described in any one of claims 1 to 7.

9. The cosmetic product as described in claim 8, characterized in that, The dosage form of the cosmetic includes at least one of ointment, lotion, serum and cream.

10. The cosmetic product as described in claim 8, characterized in that, By weight, the commonly used matrix includes 0.1 to 1 part thickener, 3 to 15 parts moisturizer, 1 to 4 parts emulsifier, 0.5 to 5 parts oil, 0.03 to 0.25 parts antioxidant, 0.5 to 5 parts soothing component, 0.5 to 1.8 parts antibacterial agent, and 60 to 85 parts fifth solvent, and the whitening and brightening composition is 1 to 15 parts.

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