Skin moisturizer with whitening, freckle removing and dull yellow improving functions and preparation method of skin moisturizer

Abstract

The invention belongs to the technical field of biology, and particularly relates to skin moisturizer with whitening, freckle removing and dull yellow improving functions and a preparation method of the skin moisturizer. The composition is prepared from the following substances in parts by mass: 0.5 to 1 part of pomelo seed extract, 1 to 2 parts of liquorice root extract, 0.5 to 1.5 parts of radix angelicae dahuricae extract, 0.5 to 1 part of rhizoma polygoni cuspidati extract, 0.5 to 1 part of mandelic acid, 1 to 2 parts of ascorbyl palmitate and 0.5 to 1 part of magnesium palmitoyl glutamate. The composition disclosed by the invention inhibits the generation of stains and promotes the degradation of melanin through multiple channels, so that the comprehensive whitening and freckle-removing effects from the source to the tail end are realized. Compared with a single-component whitening product, the composition provided by the invention has the advantages that through the synergistic effect of multiple channels, the problem of color spots of the skin can be effectively improved, and the skin is recovered to be white and bright.

Description

Technical Field

[0001] This invention belongs to the field of biotechnology, specifically relating to a skin care lotion with whitening, spot-removing, and dullness-improving effects, and its preparation method. Background Technology

[0002] Pigmentation is a common problem in the field of cosmetic dermatology, seriously affecting the overall appearance of the skin. The causes of pigmentation are varied, including ultraviolet radiation, genetic factors, endocrine disorders, medication side effects, chronic diseases, and unhealthy lifestyle habits. Among these, ultraviolet radiation is one of the main causes of pigmentation, as it stimulates melanocytes to produce excessive melanin, leading to melasma, freckles, age spots, and other pigmentation issues. Furthermore, with age, the skin's metabolic capacity gradually declines, slowing down melanin metabolism, which also makes the skin more prone to forming and worsening pigmentation.

[0003] The formation of age spots is mainly related to the production, transport, and metabolism of melanin. Melanin is a biological pigment synthesized by melanocytes, and its synthesis process is regulated by multiple factors. Ultraviolet radiation is one of the important factors inducing age spots, as it activates the activity of tyrosinase in melanocytes, promoting melanin synthesis. In addition, endocrine disorders can also lead to increased melanocyte activity, thus causing age spots such as melasma. Melanin synthesized by melanocytes is transferred to keratinocytes via melanosomes and gradually excreted from the body through keratinocyte metabolism. If the rate of melanin metabolism slows down, or if the activity of melanocytes increases abnormally, melanin will accumulate excessively in the skin, forming age spots.

[0004] Traditional skin-lightening products often rely on single whitening ingredients, such as vitamin C, kojic acid, and arbutin. While these ingredients can inhibit melanin production to some extent, their effects are limited, and they suffer from poor stability and are prone to oxidation. Some chemical skin-lightening ingredients, although possessing a strong ability to inhibit melanin production, are highly irritating to the skin and may cause adverse reactions such as allergies, redness, swelling, and itching. Long-term use may also damage the skin barrier function, making the skin more sensitive and fragile. Summary of the Invention

[0005] The purpose of this invention is to provide a skin care lotion with whitening, spot-removing, and dullness-improving effects, and its preparation method. This invention provides a composition with whitening, spot-removing, and dullness-improving functions. By weight, the composition comprises the following substances: 0.5-1 parts grapefruit seed extract, 1-2 parts licorice extract, 0.5-1.5 parts angelica dahurica extract, 0.5-1 parts polygonum cuspidatum extract, 0.5-1 parts mandelic acid, 1-2 parts ascorbyl palmitate, and 0.5-1 parts magnesium palmitoyl glutamate.

[0006] The present invention also provides a skin care liquid with whitening, spot removal and dullness improvement functions, the skin care liquid comprising the composition described in the above technical solution.

[0007] Preferably, the skin care liquid comprises the following components: 5%wt~10%wt of liposomes, 0.1%wt~0.3%wt of sodium hyaluronate, 0.05%wt~0.2%wt of tocopherol, 0.2%wt~0.5%wt of thickener, 2%wt~4%wt of emulsifier, 0.1%wt~0.3%wt of defoamer, 0.3%wt~0.8%wt of preservative, and the balance being water; by weight, the liposomes comprise: 10~30 parts of the composition of claim 1, 50~100 parts of egg yolk lecithin, and 10~20 parts of cholesterol.

[0008] Preferably, the thickener is carbomer, xanthan gum, trehalose, or hydroxyethyl cellulose.

[0009] Preferably, the emulsifier is soybean lecithin or glyceryl stearate.

[0010] Preferably, the defoamer is lanolin.

[0011] Preferably, the preservative is methylparaben, phenoxyethanol, or sodium benzoate.

[0012] This invention also provides a method for preparing the skin care liquid described in the above technical solution, the method comprising the following steps: Egg yolk lecithin and cholesterol were mixed and dissolved in anhydrous ethanol. The mixture was then rotary evaporated at 50-65°C for 15-30 minutes to form a film, which was then vacuum dried for 8 hours to obtain a dried film. The composition was dissolved in anhydrous ethanol to obtain a composition solution. The dried film was mixed with the composition solution, PBS buffer was added and stirred until homogeneous, and then sonicated at 200-300W for 25 minutes. The mixture was then filtered to obtain liposomes. Water was heated to 70-80°C, and then thickener, sodium hyaluronate and tocopherol were added and stirred until homogeneous. The mixture was then cooled to 40-45°C to obtain an aqueous phase. An emulsifier was heated to 40-50°C, and then liposomes and an antifoaming agent were added and mixed until homogeneous to obtain an oil phase. The aqueous phase was added to the oil phase and emulsified. The mixture was then cooled to 25-30°C, and a preservative was added and stirred until homogeneous to obtain a skin care solution.

[0013] Preferably, the mass-to-volume ratio of the PBS buffer to the composition is 1g:5~10mL.

[0014] Preferably, the stirring conditions are 300~800 rpm; the emulsification conditions are: stirring at 1000~2000 rpm for 5~10 min.

[0015] The beneficial effects of this invention are: In the composition of this invention, licorice extract is rich in licorice flavonoids, which can effectively inhibit the activity of tyrosinase, thereby reducing melanin production. The active ingredients in angelica dahurica extract and polygonum cuspidatum extract (such as angelicin and resveratrol) can regulate intracellular signaling pathways, inhibiting melanocyte proliferation and melanin synthesis. These components reduce melanocyte activity by affecting intracellular signal transduction, thereby reducing melanin production. Grapefruit seed extract and ascorbyl palmitate have strong antioxidant capabilities, neutralizing free radicals and reducing oxidative stress on melanocytes. Free radicals are one of the important factors leading to increased melanin production; through their antioxidant effects, they can effectively reduce melanin production and prevent the formation of age spots. Mandelic acid is a natural α-hydroxy acid (AHA) that can promote the metabolism of the stratum corneum and accelerate the renewal of epidermal cells. By promoting the shedding of the stratum corneum, melanin-containing keratinocytes can be quickly expelled from the body, thereby reducing the accumulation of age spots. Ascorbate palmitate is a vitamin C derivative with reducing properties. It can reduce dopaquinone in melanin granules to dopa, thereby breaking down the melanin granules. This reducing action can effectively degrade existing melanin, gradually fading age spots.

[0016] This invention adds the composition to the emulsion in the form of liposomes, which is more conducive to promoting the efficient delivery of active ingredients to the deep layers of the skin and improving the utilization rate of the ingredients. At the same time, liposomes themselves also have a certain moisturizing effect, which helps to repair the skin barrier, enhance the skin's water retention capacity, and further improve skin texture.

[0017] The skin care liquid of the present invention has good stability, and the components work synergistically with each other, making it difficult for chemical reactions or separation to occur.

[0018] The emulsifier, thickener, defoamer, and preservative in the skin care liquid of this invention are all common and safe skin care ingredients, and their dosage is strictly controlled within a reasonable range, which complies with relevant regulations. They are safe and non-irritating to human skin and are suitable for long-term use.

[0019] The skin care liquid of this invention has excellent whitening, spot-removing, and dullness-improving effects. It can comprehensively improve a variety of skin problems, such as roughness, dullness, and pigmentation, making the skin healthier, smoother, and more delicate after use. It improves the overall texture and appearance of the skin, reduces the damage of the external environment to the skin, and delays the skin aging process. Detailed Implementation

[0020] To further illustrate the present invention, the solutions provided by the present invention will be described in detail below with reference to the embodiments, but they should not be construed as limiting the scope of protection of the present invention.

[0021] The present invention does not impose any special limitation on the source of each substance in the composition; any conventional commercially available product is acceptable. In this embodiment of the invention, grapefruit seed extract was purchased from Xi'an Jingmei Biotechnology Co., Ltd., CAS number 90045-43-5, with a purity of 99%; licorice extract was purchased from Hubei Baidu Chemical Co., Ltd., CAS number 97676-23-8, catalog number BD6837, with a purity of 99%; angelica dahurica extract was purchased from Shaanxi Sinote Biotechnology Co., Ltd., with a purity of 99%; polygonum cuspidatum extract was purchased from Xi'an Jingmei Biotechnology Co., Ltd., CAS number 501-36-0, with a purity of 99%; mandelic acid was purchased from Hubei Jiangmin Taihua Chemical Co., Ltd., (DL-mandelic acid) CAS number 611-72-3, with a purity of 99%; ascorbyl palmitate was purchased from Anhui Runtian Biotechnology Co., Ltd., CAS number 137-66-6, with a purity of 99%; and magnesium palmitoyl glutamate was purchased from TargetMol, catalog number T33868, CAS number 38079-66-2, with a purity of 100%.

[0022] Example 1 Take 0.8 parts of grapefruit seed extract, 1.5 parts of licorice extract, 1 part of angelica dahurica extract, 0.8 parts of polygonum cuspidatum extract, 0.8 parts of mandelic acid, 1.5 parts of ascorbyl palmitate and 0.5 parts of magnesium palmitoyl glutamate, mix them evenly, and dissolve them in anhydrous ethanol. The amount of anhydrous ethanol should be enough to completely dissolve the composition to obtain a composition solution.

[0023] Example 2 Take 0.5 parts of grapefruit seed extract, 1 part of licorice extract, 1.5 parts of angelica extract, 1 part of polygonum cuspidatum extract, 0.5 parts of mandelic acid, 1 part of ascorbyl palmitate and 0.5 parts of magnesium palmitoyl glutamate, mix them evenly, and dissolve them in anhydrous ethanol. The amount of anhydrous ethanol should be enough to completely dissolve the composition to obtain a composition solution.

[0024] Example 3 Take 1 part grapefruit seed extract, 2 parts licorice extract, 1.5 parts angelica extract, 0.5 parts knotweed extract, 0.5 parts mandelic acid, 2 parts ascorbyl palmitate and 0.5 parts palmitoyl glutamate magnesium, mix them evenly, and dissolve them in anhydrous ethanol. The amount of anhydrous ethanol should be enough to completely dissolve the composition to obtain a composition solution.

[0025] Comparative Example 1 The difference from Example 1 is that Polygonum cuspidatum extract is not used.

[0026] Take 1.6 parts of grapefruit seed extract, 1.5 parts of licorice extract, 1 part of angelica extract, 0.8 parts of mandelic acid, 1.5 parts of ascorbyl palmitate and 0.5 parts of magnesium palmitoyl glutamate, mix them evenly, and dissolve them in anhydrous ethanol. The amount of anhydrous ethanol should be enough to completely dissolve the composition to obtain a composition solution.

[0027] Comparative Example 2 The difference from Example 1 is that Angelica dahurica extract is not used.

[0028] Take 1.8 parts of grapefruit seed extract, 1.5 parts of licorice extract, 0.8 parts of Polygonum cuspidatum extract, 0.8 parts of mandelic acid, 1.5 parts of ascorbyl palmitate and 0.5 parts of magnesium palmitoyl glutamate, mix them evenly, and dissolve them in anhydrous ethanol. The amount of anhydrous ethanol should be enough to completely dissolve the composition to obtain a composition solution.

[0029] Comparative Example 3 The difference from Example 1 is that ascorbic acid is used instead of ascorbyl palmitate.

[0030] Take 0.8 parts of grapefruit seed extract, 1.5 parts of licorice extract, 1 part of angelica dahurica extract, 0.8 parts of polygonum cuspidatum extract, 0.8 parts of mandelic acid, 1.5 parts of ascorbic acid and 0.5 parts of palmitoyl glutamate magnesium, mix them evenly, and dissolve them in anhydrous ethanol. The amount of anhydrous ethanol should be enough to completely dissolve the composition to obtain a composition solution.

[0031] Comparative Example 4 The difference from Example 1 is that palmitoyl glutamate magnesium is not used.

[0032] Take 0.8 parts of grapefruit seed extract, 1.5 parts of licorice extract, 1 part of angelica extract, 0.8 parts of polygonum cuspidatum extract, 0.8 parts of mandelic acid and 2 parts of ascorbyl palmitate, mix them evenly, and dissolve them in anhydrous ethanol. The amount of anhydrous ethanol should be enough to completely dissolve the composition to obtain a composition solution.

[0033] Test Example 1 The composition solutions of Examples 1 to 3 and Comparative Examples 1 to 4 were diluted with PBS buffer to a total composition concentration of 1 mg / mL.

[0034] B16 cells were planted at a density of 1 × 10⁶ cells per well. 4 Cells were seeded at a density of 1000 cells per well in 96-well plates and cultured at 37°C with 5% CO2 for 24 hours to allow the cells to adhere. The cells were then divided into groups 1-7, a blank control group, and a positive control group, with 3 replicates in each group.

[0035] Blank control group: Add 100 μL of culture medium without the composition to each well.

[0036] Positive control group: 100 μL of kojic acid was added to each well.

[0037] Group 1: Add 100 μL of the whitening composition solution prepared in Example 1 to each well.

[0038] Group 2: Add 100 μL of the whitening composition solution prepared in Example 2 to each well.

[0039] Group 3: Add 100 μL of the whitening composition solution prepared in Example 3 to each well.

[0040] Group 4: Add 100 μL of the whitening composition solution prepared in Comparative Example 1 to each well.

[0041] Group 5: Add 100 μL of the whitening composition solution prepared in Comparative Example 2 to each well.

[0042] Group 6: Add 100 μL of the whitening composition solution prepared in Comparative Example 3 to each well.

[0043] Group 7: Add 100 μL of the whitening composition solution prepared in Comparative Example 4 to each well.

[0044] After culturing for another 48 hours, the reaction substrate was added according to the instructions of the tyrosinase activity assay kit. After incubation at 37°C for a certain period of time, the stop solution was added, and the absorbance was measured at 490 nm using an ELISA reader to calculate the tyrosinase activity inhibition rate.

[0045]

[0046] B16 cells were spaced at 2 × 10⁶ cells per well. 4 Cells were seeded at a density of 1000 cells per well in 6-well plates and cultured at 37°C with 5% CO2 for 24 hours to allow the cells to adhere. The cells were then divided into experimental group, blank control group, and positive control group.

[0047] Blank control group: Add 2 mL of culture medium without the composition.

[0048] Positive control group: Add 2 mL of α-arbutin.

[0049] Group 1: Add 2 mL of the whitening composition solution prepared in Example 1 to each well.

[0050] Group 2: Add 2 mL of the whitening composition solution prepared in Example 2 to each well.

[0051] Group 3: Add 2 mL of the whitening composition solution prepared in Example 3 to each well.

[0052] Group 4: Add 2 mL of the whitening composition solution prepared in Comparative Example 1 to each well.

[0053] Group 5: Add 2 mL of the whitening composition solution prepared in Comparative Example 2 to each well.

[0054] Group 6: Add 2 mL of the whitening composition solution prepared in Comparative Example 3 to each well.

[0055] Group 7: Add 2 mL of the whitening composition solution prepared in Comparative Example 4 to each well.

[0056] After culturing for 72 hours, cells were collected, lysed with lysis buffer, and melanin was extracted. Melanin was dissolved in lysis buffer, and absorbance was measured at 405 nm using an ELISA reader to calculate the melanin content reduction rate.

[0057] The results are shown in Table 1.

[0058] Table 1. Inhibition rate of tyrosinase activity and reduction rate of melanin content of whitening compositions

[0059] As shown in Table 1, the whitening composition provided by the present invention can effectively inhibit the activity of tyrosinase and effectively reduce melanin production.

[0060] Example 4 Take 50 parts of egg yolk lecithin and 10 parts of cholesterol, mix them evenly, dissolve them in anhydrous ethanol, and rotary evaporate at 55°C for 20 minutes to form a film. Then vacuum dry for about 5 hours. When the film surface has no obvious ethanol odor and the texture is relatively brittle, the drying can be stopped to obtain the dried film. Mix the dried film with the composition solution prepared in Example 1, add PBS buffer, stir evenly at 800 rpm, and then sonicate at 250W for 25 minutes. Filter through a 0.45 μm filter membrane to obtain liposomes.

[0061] Take 86g of water and heat it to 70℃. Then add 0.2g of carbomer, 0.2g of sodium hyaluronate and 0.1g of tocopherol, stir until evenly dispersed, and cool to 40℃~45℃ to obtain the aqueous phase. Take 3g of soybean lecithin and heat it to 45℃. Add 10g of liposomes and 0.2g of lanolin, stir at 600rpm for 2~3min, and mix evenly to obtain the oil phase. Slowly add the aqueous phase to the oil phase, stir at 1200rpm for 8min to emulsify, cool to 30℃, add 0.3g of methylparaben, stir evenly, and obtain the skin care liquid.

[0062] Example 5 Take 50 parts of egg yolk lecithin and 10 parts of cholesterol, mix them evenly, dissolve them in anhydrous ethanol, and rotary evaporate at 55°C for 20 minutes to form a film. Then vacuum dry for about 5 hours. When the film surface has no obvious ethanol odor and the texture is relatively brittle, the drying can be stopped to obtain the dried film. Mix the dried film with the composition solution prepared in Example 2, add PBS buffer, stir evenly at 800 rpm, and then sonicate at 250W for 25 minutes. Filter through a 0.45 μm filter membrane to obtain liposomes.

[0063] Heat 86g of water to 75℃, then add 0.2g of carbomer, 0.2g of sodium hyaluronate and 0.1g of tocopherol, stir until evenly dispersed, and cool to 40℃~45℃ to obtain the aqueous phase; heat 3g of soybean lecithin to 45℃, add 10g of liposomes and 0.2g of lanolin, stir at 600rpm for 2~3min, and mix evenly to obtain the oil phase; slowly add the aqueous phase to the oil phase, stir at 1200rpm for 8min to emulsify, cool to 30℃, add 0.3g of methylparaben, stir evenly to obtain the skin care liquid.

[0064] Example 6 Take 50 parts of egg yolk lecithin and 10 parts of cholesterol, mix them evenly, dissolve them in anhydrous ethanol, and rotary evaporate at 55°C for 20 minutes to form a film. Then vacuum dry for about 5 hours. When the film surface has no obvious ethanol odor and the texture is relatively brittle, the drying can be stopped to obtain the dried film. Mix the dried film with the composition solution prepared in Example 3, add PBS buffer, stir evenly at 800 rpm, and then sonicate at 250W for 25 minutes. Filter through a 0.45 μm filter membrane to obtain liposomes.

[0065] Heat 86.2g of water to 80℃, then add 0.2g of carbomer, 0.2g of sodium hyaluronate and 0.1g of tocopherol, stir until evenly dispersed, and cool to 40℃~45℃ to obtain the aqueous phase; heat 3g of soybean lecithin to 45℃, add 10g of liposomes and 0.3g of lanolin, stir at 600rpm for 2~3min, and mix evenly to obtain the oil phase; slowly add the aqueous phase to the oil phase, stir at 1200rpm for 8min to emulsify, cool to 30℃, add 0.3g of methylparaben, stir evenly to obtain the skin care solution.

[0066] Comparative Example 5 The difference from Example 4 is that the composition is not prepared into liposomes.

[0067] Take 86g of water and heat it to 70℃. Then add 0.2g of carbomer, 0.2g of sodium hyaluronate and 0.1g of tocopherol, and stir until uniformly dispersed. Cool down to 40℃~45℃ to obtain the aqueous phase. Take 3g of soybean lecithin and heat it to 45℃. Add 0.2g of lanolin and stir until uniform. Then add the composition solution prepared in Example 1 directly to the above mixture and stir at 600rpm for 2~3min. After mixing evenly, obtain the oil phase. Slowly add the aqueous phase to the oil phase and stir at 1200rpm for 8min to emulsify. After cooling to 30℃, add 0.3g of methylparaben and stir evenly to obtain the skin care liquid.

[0068] Test Example 2 Stability test The skin care lotions prepared in Examples 4 to 6 and Comparative Example 5 were used as samples for testing.

[0069] The skin care lotion samples were stored at 45℃±2℃ and 5%±5% relative humidity for accelerated testing. Samples were taken and tested at 1 month, 3 months and 6 months of storage. The results are shown in Table 2.

[0070] Table 2 Accelerated Test Results

[0071] The skincare lotion samples were stored under strong light (4500±500 lx) for light exposure testing. Samples were taken and tested on the 5th and 10th days of storage.

[0072] The skin care liquid samples were stored at high temperature (40℃±2℃) for 10 days, and samples were taken for testing on the 5th and 10th days of storage.

[0073] The results of strong light storage and high temperature storage are shown in Table 3.

[0074] Table 3 Results of high-intensity light storage and high-temperature storage

[0075] As shown in Tables 2 and 3, the present invention prepares the composition into liposomes before preparing the skin care liquid, which can effectively improve the stability of the skin care liquid.

[0076] Although the above embodiments have provided a detailed description of the present invention, they are only some embodiments of the present invention, and not all embodiments. People can obtain other embodiments based on these embodiments without creative effort, and these embodiments all fall within the protection scope of the present invention.

Claims

1. A composition having whitening, freckle-removing, and dullness-improving functions, characterized in that, The composition comprises, by weight, the following substances: Grapefruit seed extract 0.5-1 part, licorice extract 1-2 parts, angelica dahurica extract 0.5-1.5 parts, polygonum cuspidatum extract 0.5-1 part, mandelic acid 0.5-1 part, ascorbyl palmitate 1-2 parts and palmitoyl glutamate magnesium 0.5-1 part.

2. A skin care lotion with whitening, spot-removing, and dullness-improving functions, characterized in that, The skin lotion includes the composition of claim 1.

3. The skin care lotion according to claim 2, characterized in that, The skin care lotion comprises the following ingredients: liposomes 5%wt~10%wt, sodium hyaluronate 0.1%wt~0.3%wt, tocopherol 0.05%wt~0.2%wt, thickener 0.2%wt~0.5%wt, emulsifier 2%wt~4%wt, defoamer 0.1%wt~0.3%wt, preservative 0.3%wt~0.8%wt, and the balance being water; The liposomes, by weight, comprise: 10-30 parts of the composition of claim 1, 50-100 parts of egg yolk lecithin, and 10-20 parts of cholesterol.

4. The skin care lotion according to claim 3, characterized in that, The thickener is carbomer, xanthan gum, trehalose, or hydroxyethyl cellulose.

5. The skin care lotion according to claim 3, characterized in that, The emulsifier is soybean lecithin or glyceryl stearate.

6. The skin care lotion according to claim 3, characterized in that, The defoamer is lanolin.

7. The skin care lotion according to claim 3, characterized in that, The preservative is methylparaben, phenoxyethanol, or sodium benzoate.

8. The method for preparing the skin care lotion according to claim 3, characterized in that, The method includes the following steps: Egg yolk lecithin and cholesterol were mixed and dissolved in anhydrous ethanol. The mixture was then rotary evaporated at 50-65°C for 15-30 minutes to form a film. The film was then vacuum dried for 4-6 hours to obtain a dried film. The composition was dissolved in anhydrous ethanol to obtain a composition solution. The dried film was mixed with the composition solution, PBS buffer was added and stirred until homogeneous. The mixture was then sonicated at 200-300W for 25 minutes and filtered to obtain liposomes. Water is heated to 70℃~80℃, then thickener, sodium hyaluronate and tocopherol are added and stirred until evenly dispersed. The mixture is then cooled to 40℃~45℃ to obtain the aqueous phase. Emulsifier is heated to 40℃~50℃, liposomes and defoamer are added and mixed evenly to obtain the oil phase. The aqueous phase is added to the oil phase and emulsified. The mixture is then cooled to 25℃~30℃, preservative is added, and the mixture is stirred evenly to obtain the skin care lotion.

9. The preparation method according to claim 8, characterized in that, The mass-to-volume ratio of the PBS buffer to the composition is 1g:5~10mL.

10. The preparation method according to claim 8, characterized in that, The stirring conditions are 300~800 rpm; the emulsification conditions are: stirring at 1000~2000 rpm for 5~10 min.

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