Skin-whitening flexible liposome as well as preparation method and application thereof
By combining liposomes with licorice charone, photolicorice and Magnolia bark extracts with flexible agents and phospholipids to form liposomes, the whitening active composition is solved, and the existing whitening ingredients are poor water solubility and poor stability in cosmetics are achieved, achieving higher whitening effects and better skin safety.
Patent Information
- Application Number
- CN202510150867.3
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2025-02-11
- Publication Date
- 2025-05-13
AI Technical Summary
Existing whitening ingredients such as hydroquinol, high concentrations of vitamin C or fruit acid can cause skin irritation, redness, dryness and sensitivity in cosmetics, while their water solubility and poor stability, resulting in inactivation and instability when used in cosmetics.
Using the technique of whitening flexible liposomes, liposomes are formed by forming liposomes with flexible agents and phospholipids, using the technique of whitening flexible liposomes, enhancing its stability and improving permeability.
The transdermal amount and permeability of the whitening active ingredients are significantly improved, the skin irritation is reduced, the stability and sustained release of the composition are enhanced, and the better whitening effect is achieved, while reducing toxicity and environmental pollution.
Smart Images

Figure CN119970578A_ABST
Abstract
Description
Technical Field
[0001] The invention relates to the technical field of cosmetics, and in particular to a whitening flexible liposome and a preparation method and application thereof. Background Art
[0002] With the continuous development of skin care products, people are paying more and more attention to active ingredients, especially active ingredients with whitening effects. More and more people are beginning to focus on how to reduce skin irritation, whiten gently, and use effective active ingredients for a long time. However, some whitening ingredients used on the market, such as hydroquinone, high-concentration vitamin C or fruit acid, although they have significant whitening effects, may irritate the skin, causing redness, dryness and even sensitivity. Finding whitening ingredients that are both effective and gentle is a big challenge. Plant extracts with whitening effects from natural sources have become our main focus, and in the dissolving whitening active ingredient room, the synthetic surfactants used have certain toxicity problems to human skin, which can easily increase skin irritation and further cause skin problems. At the same time, they also have certain pollution to the environment. Summary of the invention
[0003] The purpose of the present invention is to overcome the shortcomings of the prior art and provide a whitening flexible liposome and its preparation method and application. The whitening flexible liposome of the present invention overcomes the problems of poor water solubility, poor stability and easy inactivation of the whitening active composition in cosmetics, and has a good sustained release effect, and in particular, increases the selection of natural softeners to make it better integrated with the skin barrier, thereby significantly increasing the transdermal amount and permeation amount of the whitening active ingredient.
[0004] To achieve the above object, the technical solution adopted by the present invention is:
[0005] In a first aspect, the present invention provides a whitening flexible liposome, comprising an internal whitening active composition and an outer liposome: the internal whitening active composition comprises licorice chalcone, glabridin, and Magnolia officinalis bark extract; the outer liposome comprises a softening agent and phospholipids.
[0006] Licorice chalcone (Glycyrrhizin or Glycyrrhizic Acid) is a kind of extract from the root of Glycyrrhiza inflata. It has multiple biological activities, including anti-inflammatory, antioxidant and skin protection properties. Licorice chalcone can inhibit the activity of tyrosinase, thereby reducing the production of melanin. Its anti-inflammatory properties can help alleviate skin inflammation caused by ultraviolet radiation or other stimuli, indirectly prevent pigmentation, and help brighten the skin. As a powerful antioxidant, licorice chalcone can help scavenge free radicals, protect the skin from oxidative damage, maintain the health and brightness of the skin, and it may also help improve uneven skin color and enhance overall skin brightness by promoting the normal growth and metabolism of skin cells. However, licorice chalcone has poor water solubility, which limits its application in certain drug delivery systems and also affects its absorption and bioavailability in the body.
[0007] Glabridin is a natural compound extracted from specific plants, mainly from the root of the leguminous plant Glycyrrhiza glabra, and is considered to be a highly biologically active ingredient. Glabridin has powerful antioxidant, anti-inflammatory and skin whitening effects. However, glabridin also has poor water solubility and poor stability in the formula. It is easily affected by factors such as temperature, light, and pH value, which can reduce its activity or cause color changes.
[0008] Magnolia officinalis is a traditional Chinese medicine. Magnolia officinalis bark extract contains a variety of active ingredients, such as magnolol and honokiol, which have antioxidant, anti-inflammatory and skin conditioning properties. Magnolia officinalis bark extract has strong antioxidant properties, can effectively remove free radicals in the body, protect the skin from oxidative damage, and help maintain the skin's whiteness and luster. Its anti-inflammatory properties can help reduce skin inflammation and reduce pigmentation caused by inflammation, which indirectly assists in the whitening effect. However, as a natural product extract, its bioavailability is often low, which affects its efficacy.
[0009] The present invention combines licochalcone, glabridin and magnolia officinalis bark extract to achieve a synergistic effect of whitening.
[0010] However, since the stability of the above-mentioned whitening components is poor, in order to enhance the stability of the composition composed of these whitening components, the present invention uses a liposome composed of a flexible agent and phospholipids to encapsulate the above-mentioned composition to enhance its stability. The present invention disrupts the phospholipid bilayer structure of the liposome by adding a flexible agent (i.e., a flexible surfactant), increases the fluidity and flexibility of the phospholipids, and enables the prepared liposome to pass through the stratum corneum through mechanisms such as extrusion deformation after external use, reach the dermis and even enter the blood circulation, and has stronger permeability and whitening effect.
[0011] As a preferred embodiment of the first aspect, in the internal whitening active composition, the mass percentage of licorice chalcone is 0.1-2%, the mass percentage of glabridin is 0.1-2%, and the mass percentage of Magnolia officinalis bark extract is 0.1-2%.
[0012] Illustratively, the mass percentage of licorice chalcone may be any value of 0.1%, 0.3%, 0.5%, 0.7%, 0.9%, 1.0%, 1.2%, 1.4%, 1.6%, 1.8%, 2.0%, or a range thereof.
[0013] The mass percentage of glabridin may be any value of 0.1%, 0.3%, 0.5%, 0.7%, 0.9%, 1.0%, 1.2%, 1.4%, 1.6%, 1.8%, 2.0% or a range thereof.
[0014] The mass percentage of the Magnolia officinalis bark extract may be any value of 0.1%, 0.3%, 0.5%, 0.7%, 0.9%, 1.0%, 1.2%, 1.4%, 1.6%, 1.8%, 2.0% or a range thereof.
[0015] Preferably, the internal whitening active composition comprises the following components in percentage by mass: 1% of licorice chalcone, 1% of glabridin, and 1% of Magnolia officinalis bark extract.
[0016] The present invention has found that when the mass percentage of licorice chalcone, glabridin and Magnolia officinalis bark extract is limited to 0.1-2%, the whitening penetration effect of the whitening flexible liposome of the present invention is better, especially when it is 1%, the effect is the best.
[0017] As a preferred implementation of the first aspect, the licorice chalcone is any one of licorice chalcone A, licorice chalcone B, licorice chalcone C, licorice chalcone D or any combination thereof.
[0018] The present invention studies licochalcone A, licochalcone B, licochalcone C and licochalcone D respectively, and finds that the four licochalcones can achieve the effect of the present invention.
[0019] Preferably, the licorice chalcone is licorice chalcone A.
[0020] The present invention has found that when the licorice chalcone is licorice chalcone A, the whitening and penetration effect of the whitening flexible liposome of the present invention is the best.
[0021] As a preferred embodiment of the first aspect, the Magnolia officinalis bark extract includes honokiol and magnolol.
[0022] The present invention studies honokiol and magnolol respectively, and finds that both honokiol and magnolol can achieve the effect of the present invention.
[0023] Preferably, the Magnolia officinalis bark extract is honokiol.
[0024] The present invention has found that when the Magnolia officinalis bark extract is honokiol, the whitening and penetration effect of the whitening flexible liposome of the present invention is the best.
[0025] As a preferred embodiment of the first aspect, the mass ratio of the phospholipid to the softener is: phospholipid: softener = (1-3): (5-12).
[0026] Exemplarily, the mass ratio of the phospholipid to the softener may be any value or range thereof among 1:5, 1:8, 1:10, 1:12, 3:5, 3:6, 3:8, 3:10, 3:12.
[0027] Preferably, the mass ratio of the phospholipid to the softener is 3:10.
[0028] The present invention has found that when the mass ratio of phospholipid to softener is limited to the range of (1-3): (5-12), the whitening penetration effect of the flexible liposome of the whitening composition of the present invention is better, especially when it is 3:10, the effect is the best.
[0029] As a preferred embodiment of the first aspect, the softening agent is any one of sophorolipids, ginsenosides, and sapindus saponins, or any combination thereof.
[0030] The present invention studies sophorolipids, ginsenosides and sapindus saponins respectively, and finds that sophorolipids, ginsenosides and sapindus saponins can all achieve the effects of the present invention.
[0031] Preferably, the softening agent is ginsenoside.
[0032] The present invention has found that when ginsenoside is used as a natural softener, the solubility of the active whitening composition components in the whitening flexible liposome can be improved, and the addition amount of other synthetic substances can be reduced, thereby reducing the toxicity caused by other excipients. Therefore, the whitening flexible liposome prepared by the present invention has lower toxicity and better biocompatibility than conventional liposomes. At the same time, the present invention uses a natural softener to reduce the problems of environmental pollution and toxicity to the human body caused by chemical synthetic surfactants, which is safer, greener and more environmentally friendly, and has stronger permeability and whitening effect.
[0033] As a preferred embodiment of the first aspect, the whitening flexible liposomes further include cyclodextrin and polyols.
[0034] The present invention uses a cyclodextrin-polyol low eutectic solvent to improve the solubility of licorice chalcone, glabridin and magnolol in a whitening active composition in an aqueous solution.
[0035] As a preferred embodiment of the first aspect, the cyclodextrin is hydroxypropyl β-cyclodextrin or methyl β-cyclodextrin; or / and the polyol is any one of glycerol, diglycerol, 1,2-butanediol, 1,3-propylene glycol, sorbitol or any combination thereof.
[0036] Cyclodextrin (CD) is a type of cyclic oligosaccharide obtained by hydrolyzing starch with cyclodextrin glucose transferase. It is usually composed of 6 to 12 pyranose glucose units connected by α-(1,4) glycosidic bonds, including α-CD, β-CD, γ-CD, and cyclodextrin derivatives (cyclodextrin and its derivatives, CDs) with different functional groups such as methyl, hydroxypropyl, carboxymethyl, sulfobutyl introduced into them.
[0037] Preferably, the polyol is 1,2-butanediol.
[0038] As a preferred embodiment of the first aspect, the whitening flexible liposomes include the following components in mass percentage: 0.1-2% of licorice chalcone, 0.1-2% of glabridin, 0.1-2% of magnolia officinalis bark extract, 1-3% of phospholipids, 5-10% of softening agent, 5-30% of cyclodextrin, 12-40% of polyol, and the balance is water.
[0039] Preferably, the polyol is any one of glycerol, diglycerol, 1,2-butanediol, 1,3-propylene glycol, sorbitol or any combination thereof, wherein the mass percentages of diglycerol, 1,2-butanediol, 1,3-propylene glycol and sorbitol are each independently 2-20%; the mass percentage of glycerol is 10-20%.
[0040] In a second aspect, the present invention provides a method for preparing the whitening flexible liposome, which comprises the following steps:
[0041] (1) Add cyclodextrin, polyol, licorice chalcone, glabridin, Magnolia officinalis bark extract, and a softener into a container, and heat and stir until completely dissolved to form phase A;
[0042] (2) Add phospholipids, glycerol and water to another container, heat and stir to dissolve, and this is phase B;
[0043] (3) During the shearing process, phase A is added to phase B for shearing to obtain colostrum, which is then homogenized.
[0044] As a preferred implementation of the second aspect, in the step (3), the shearing time is 5 min, the shearing speed is 1000 r / min, and the shearing temperature is 45°C; or / and, the homogenization temperature is 45°C±5°C, the number of homogenization times is 6 times, and the homogenization pressure is 600 bar.
[0045] Compared with the prior art, the present invention has the following beneficial effects:
[0046] The present invention uses flexible liposomes to encapsulate the whitening composition, with an encapsulation rate of more than 90%. It has good stability and can greatly overcome the characteristics of the whitening composition being difficult to dissolve in water, having poor stability and being easy to inactivate, so that it can be better applied in cosmetics.
[0047] The preparation method of the present invention is simple, and the reagents used are few and the dosage is also small. By better controlling a small amount of reagents, the reagents interact with each other to achieve an outstanding wrapping effect on the whitening composition. The good sustained-release effect can better exert the advantages of the whitening composition, while solving the pain points of its application in cosmetics, and can significantly increase the cumulative skin penetration of active ingredients. BRIEF DESCRIPTION OF THE DRAWINGS
[0048] Figure 1 This is an electron microscopic image of the whitening flexible liposome of the present invention;
[0049] Figure 2 This is a diagram showing the results of an in vitro transdermal penetration experiment of the whitening flexible liposomes of the present invention. DETAILED DESCRIPTION
[0050] In order to better illustrate the purpose, technical solutions and advantages of the present invention, the present invention will be further described below in conjunction with specific embodiments.
[0051] Licorice chalcone A was purchased from Chenfeng Natural Herbal Medicine (Beijing) Technology Co., Ltd., item number SHCI130124006, product name Licorice chalcone A;
[0052] Licorice chalcone B was purchased from Chenfeng Natural Herbal Medicine (Beijing) Technology Co., Ltd., item number SHCI130124005, product name Licorice chalcone B;
[0053] Licorice chalcone C was purchased from Chenfeng Natural Herbal Medicine (Beijing) Technology Co., Ltd., item number SHCI130124004, product name Licorice chalcone C;
[0054] Licorice chalcone D was purchased from Chenfeng Natural Herbal Medicine (Beijing) Technology Co., Ltd., item number SHCI130124003, product name Licorice chalcone D;
[0055] Glabridin was purchased from Guangzhou Qingnang Biotechnology Co., Ltd., product number QN24041601, product name Glabridin;
[0056] Honokiol was purchased from Hunan Heguang Biotechnology Co., Ltd., product number 24013101, product name honokiol;
[0057] Magnolol was purchased from Hunan Heguang Biotechnology Co., Ltd., product number 24013102, product name Magnolol;
[0058] Ginsenoside was purchased from Guangzhou Qingnang Biotechnology Co., Ltd., product number QN24032601, product name ginsenoside;
[0059] Sophorolipids were purchased from Guangzhou Zhaoheng Trading Development Co., Ltd., item number SL50FF06-202404-02, product name SOFOBOTON TM SL50 FF06;
[0060] Sapindus mukorossi saponins were purchased from Guangdong Santi New Materials Technology Co., Ltd., item number 2021092501, product name Sapindus mukorossi extract S1;
[0061] Diglycerin was purchased from Guangzhou Zhaoheng Trading Development Co., Ltd., item number 23092601, product name Diglycerin S;
[0062] Phospholipids were purchased from Guangzhou Qingnang Biotechnology Co., Ltd., product number QN24031601, product name phospholipids;
[0063] Glycyrrhizic acid was purchased from Guangzhou Baihaobo Co., Ltd., product name: Glycyrrhizic acid;
[0064] Arbutin was purchased from Guangzhou Baihaobo Co., Ltd., product name: Arbutin;
[0065] Tocopherol was purchased from Guangzhou Meifu Trading Co., Ltd., the product name is Tocopherol 99%.
[0066] Examples 1 to 13 and Comparative Examples 1 to 11
[0067] The components and mass percentages of the whitening flexible liposomes of Examples 1 to 13 and Comparative Examples 1 to 11 are shown in Table 1.
[0068] Table 1:
[0069]
[0070]
[0071] Note: The "remainder" of water means that the amount of water added is the sum of the mass percentages of each component added to the whitening flexible liposome is 100%.
[0072] This embodiment also provides a method for preparing whitening flexible liposomes, comprising the following steps:
[0073] (1) Add cyclodextrin, polyol, licorice chalcone, glabridin, Magnolia officinalis bark extract, and a softener into a container according to the ratios of the above Examples 1-13 or Comparative Examples 1-11, and heat and stir until completely dissolved to obtain Phase A;
[0074] (2) Add phospholipids, glycerol and water to another container, heat and stir to dissolve, and this is phase B;
[0075] (3) During the shearing process, phase A is added to phase B for shearing, the shearing time is 5 min, the shearing speed is 1000 r / min, the shearing temperature is 45°C, and colostrum is obtained; then, the phase is homogenized, the homogenization temperature is 45°C±5°C, the homogenization times are 6 times, and the homogenization pressure is 600 bar, to obtain the flexible liposomes of the whitening composition of the present invention.
[0076] Test Example 1 Whitening Efficacy Test:
[0077] Melanocytes B16-F10 were seeded in 6-well plates (1×10 5 / well), and on the second day, different test substances (whitening flexible liposomes of Examples 1-13 and Comparative Examples 1-11) were added to the cells in advance for 1 hour, and then 1 μmol / L of the inducer α-MSH was added, and a control group (containing only α-MSH, i.e., α-MSH model group) was set up. After the two acted together for 48 hours, the cells were collected for subsequent determination, and the final results were calibrated with cell counts. The drug treatment concentrations were 1 μmol / L, respectively, and the composition substances were added in equal molar ratios. The inhibition rate was the ratio of the difference between the results of the control group and the test group to the results of the control group.
[0078] (1) Determination of melanin content: Collect the cell pellet from each well and add 0.4 mL of 1 mol / L NaOH solution (containing 10% DMSO by volume), incubate at 80° C. for 30 min, and measure the absorbance at 490 nm.
[0079] Melanin content inhibition rate % = melanin content per gram of protein in the experimental group / melanin content per gram of protein in the α-MSH model group × 100%.
[0080] (2) Tyrosinase activity assay: Melanocyte B16-F10 precipitate was collected from each well and 0.5 mL of 0.5% sodium deoxycholate solution was added. The cells were lysed on ice for 15 min, then rewarmed at 37°C and 0.25 mL of 0.3% DOPA solution was added. The cells were reacted at 37°C for 30 min and the absorbance was measured at 475 nm.
[0081] Tyrosinase activity inhibition rate (%) = tyrosinase activity per gram of protein in the experimental group / tyrosinase activity per gram of protein in the α-MSH model group × 100%.
[0082] Test Example 2 In vitro percutaneous penetration test:
[0083] The Bama Xiang pig skin was fixed between the receiving pool and the supply pool, and the test sample was added to the receiving pool. Phosphate buffer solution (PBS, pH 7.4) was used as the receiving solution, and the mixture was stirred at a speed of 300r / min and a temperature of 37°C. 0.5mL of the receiving solution was taken into an EP tube at 4 and 8h, respectively, and analyzed by HPLC to calculate the cumulative skin permeation of glabridin per unit area after 4 and 8h. After 4 and 8h, the pig skin was washed, cut into pieces and ground, and an appropriate amount of methanol was added for centrifugation. The supernatant was analyzed by HPLC to calculate the skin retention of glabridin per unit area.
[0084] The calculation method of the cumulative transdermal amount of glabridin per unit area is as follows:
[0085]
[0086] Wherein, Q: cumulative transdermal amount; A: effective diffusion area; V0 and Vi: volume of saline in the receiving pool; Ci: drug concentration in the receiving solution from the first sampling to the last sampling; Cn: drug concentration in the receiving solution at the time of this sampling.
[0087] The calculation method for the cumulative retention of methanol per unit area is as follows:
[0088] Cumulative retention per unit area (μg / cm 2 )=(V×C) / A
[0089] Wherein, V: volume of methanol used to soak pigskin; C: concentration of methanol solution after soaking and ultrasonication of pigskin; A: effective diffusion area.
[0090] The results of test case 1 and test case 2 are shown in Table 2:
[0091] Table 2:
[0092]
[0093]
[0094] It can be seen from Table 2 that the melanin content inhibition rate and tyrosinase activity inhibition rate of the whitening composition flexible liposomes prepared in Examples 1-13 are higher than those in Comparative Examples 1-11.
[0095] It can be seen from Examples 1-3 and Comparative Examples 1-2 that the content of each component in the whitening flexible liposome has an effect on the efficacy of the whitening flexible liposome. When the content of each component is limited within the scope of the present invention, the whitening effect of the whitening flexible liposome is better. At the same time, it can be seen from Examples 1-3 that when the addition amount of the component is the ratio of Example 2, the whitening effect of the whitening flexible liposome is the best.
[0096] Since the contents of the components in Comparative Example 1-2 are not within the scope of the present invention, the whitening effect is inferior to that of Example 1-3.
[0097] It can be seen from Examples 1 and 4-6 that when Licorice Chalcone A (Example 1) is selected, the whitening effect of the whitening flexible liposome is better.
[0098] It can be seen from Examples 1 and 7 that when honokiol (Example 1) is selected, the whitening effect of the whitening flexible liposome is better.
[0099] It can be seen from Examples 1 and 8-9 that when ginsenoside (Example 1) is selected, the whitening effect of the whitening flexible liposome is better.
[0100] It can be seen from Examples 1 and 10 that when hydroxypropyl β-cyclodextrin (Example 1) is selected, the whitening effect of the whitening flexible liposome is better.
[0101] It can be seen from Examples 1 and 11-13 that when 1,2-butanediol (Example 1) is selected, the whitening effect of the whitening flexible liposome is better.
[0102] It can be seen from Comparative Examples 3-6 that the whitening effect of Comparative Examples 3-6 is poor. This is because any one of licochalcone, glabridin, Magnolia officinalis bark extract, and softening agent is missing in Comparative Examples 3-6, and the synergistic effect between licochalcone, glabridin, Magnolia officinalis bark extract, and softening agent cannot be achieved, thereby reducing the whitening effect of the whitening flexible liposome.
[0103] It can be seen from Comparative Examples 7-11 that the whitening effects of Comparative Examples 7-11 are poor. This is because Comparative Example 7 replaced licorice chalcone with glycyrrhizic acid, Comparative Example 8 replaced glabridin with arbutin, Comparative Example 9 replaced Magnolia officinalis bark extract with totophenol, Comparative Example 10 replaced ginsenosides with hydrogenated castor oil-40, and Comparative Example 11 replaced ginsenosides with Tween-80, which failed to achieve the synergistic effect between licorice chalcone, glabridin, Magnolia officinalis bark extract, and ginsenoside, thereby reducing the whitening effect of the whitening flexible liposomes.
[0104] Test Example 3 Stability Test:
[0105] Sample: whitening liposomes 1-3 prepared in 3 parallel runs in Example 1;
[0106] Reference substance: common solubilizing whitening composition; the common solubilizing whitening composition comprises: 0.1% by mass of glabridin, 0.1% by mass of honokiol, and 0.1% by mass of licorice chalcone A. The preparation method is: accurately weigh 0.1% glabridin, 0.1% by mass of honokiol, and 0.1% by mass of licorice chalcone A respectively into a suitable container, add 2% CO40 and 3% butanediol for solubilization, and then add the remaining water according to the percentage.
[0107] Stability test method: Place the sample and reference substance at 50℃, -20℃, and 25℃ for 3 months for stability test, and measure the glabridin content after 3 months. The operation is as follows:
[0108] Accurately measure 0.5 g of sample and reference substance respectively, add methanol to dissolve and dilute to the scale and shake well, ultrasonicate for 5 minutes to completely destroy the liposomes of whitening flexible liposomes, filter with a 0.45 μm microporous filter membrane, inject into liquid chromatograph, and calculate the drug content (i.e., glabridin content) by the main peak area using the external standard method.
[0109] Encapsulation efficiency test method: Use ultrafiltration centrifugation to separate the whitening flexible liposomes and the unencapsulated free whitening active composition, and the operation is as follows:
[0110] Accurately measure 0.5 g of the sample and place it in an ultrafiltration centrifuge tube (with a molecular weight cutoff of 10 kD). Centrifuge at 10,000 r / min for 30 min. Take the filtrate after centrifugation and transfer it to a 5 mL volumetric flask. Add methanol to dissolve and dilute to the scale and shake well. After filtering with a 0.45 μm microporous filter membrane, inject it into a liquid chromatograph and calculate the free drug content (i.e., glabridin content) in the supernatant by the external standard method based on the main peak area.
[0111] Encapsulation rate % = (weight of drug added - weight of free drug in supernatant) / weight of drug added × 100%
[0112] Feed drug quality: The glabridin content is measured after the liposomes of the whitening flexible liposomes are completely destroyed by using methanol ultrasound for 5 minutes.
[0113] Free drug mass in supernatant: the glabridin content in the supernatant measured by the above-mentioned ultrafiltration centrifugation method.
[0114] Table 3:
[0115]
[0116] From the results in Table 3, it is known that compared with the common solubilized whitening composition, the whitening composition flexible liposomes 1-3 prepared by the present invention are placed at 50°C, -20°C, and 25°C for three months without abnormality, indicating that the whitening flexible liposomes of the present invention have good stability. According to the content detection data, the glabridin content is above 90% after being placed at 50°C for 3 months, while the glabridin content in the common solubilized whitening composition is degraded to 54%, indicating that the whitening flexible liposomes of the present invention can greatly alleviate the degradation of its active ingredients and avoid their inactivation, and the encapsulation rate of the whitening composition flexible liposomes prepared by the present invention reaches more than 90%. The above data results show that the flexible liposomes encapsulate the whitening composition, and the encapsulation rate reaches more than 90%, which has good stability and can greatly overcome the characteristics of the whitening composition being difficult to dissolve in water, poor stability, and easy inactivation.
[0117] from Figure 1 The electron microscopy results showed that the prepared liposomes had uniform appearance and the active ingredients were completely encapsulated in the liposomes, indicating that the liposomes were successfully prepared.
[0118] from Figure 2 The results showed that the cumulative intradermal retention per unit area of the whitening flexible liposomes for 4 and 8 hours was 2.6 times and 2.5 times that of the solubilized whitening composition, respectively, indicating that the whitening flexible liposomes of the present invention have stronger skin permeability and better transdermal effect.
[0119] Finally, it should be noted that the above embodiments are only used to illustrate the technical solution of the present invention rather than to limit the scope of protection of the present invention. Although the present invention has been described in detail with reference to the preferred embodiments, those skilled in the art should understand that the technical solution of the present invention can be modified or replaced by equivalents without departing from the essence and scope of the technical solution of the present invention.
Claims
1. A whitening flexible liposome, characterized in that: The whitening flexible liposome comprises an internal whitening active composition and an outer liposome: The internal whitening active composition includes licorice chalcone, glabridin, and magnolia officinalis bark extract; The outer layer liposome includes a flexible agent and a phospholipid.
2. The whitening flexible liposome according to claim 1, characterized in that: In the internal whitening active composition, the mass percentage of licorice chalcone is 0.1-2%, the mass percentage of glabridin is 0.1-2%, and the mass percentage of Magnolia officinalis bark extract is 0.1-2%.
3. The whitening flexible liposome according to claim 1, characterized in that: The licorice chalcone is any one of licorice chalcone A, licorice chalcone B, licorice chalcone C, licorice chalcone D or any combination thereof.
4. The whitening flexible liposome according to claim 1, characterized in that: The Magnolia officinalis bark extract includes honokiol and magnolol.
5. The whitening flexible liposome according to claim 1, characterized in that: In the outer layer liposome, the mass ratio of the phospholipid to the flexible agent is: phospholipid: flexible agent = (1-3): (5-12).
6. The whitening flexible liposome according to claim 1, characterized in that: The softening agent is any one of sophorolipids, ginsenosides, and sapindus saponins, or any combination thereof.
7. The whitening flexible liposome according to claim 1, characterized in that: The whitening flexible liposome further comprises cyclodextrin, polyol and water.
8. The whitening flexible liposome according to claim 7, characterized in that: The cyclodextrin is hydroxypropyl β-cyclodextrin or methyl β-cyclodextrin; or / and, The polyol is any one of glycerol, diglycerol, 1,2-butylene glycol, 1,3-propylene glycol, sorbitol or any combination thereof.
9. A method for preparing the whitening flexible liposome according to any one of claims 1 to 8, characterized in that: The steps include: (1) Add cyclodextrin, polyol, licorice chalcone, glabridin, Magnolia officinalis bark extract, and a softener into a container, and heat and stir until completely dissolved to form phase A; (2) Add phospholipids, glycerol and water to another container, heat and stir to dissolve, and this is phase B; (3) During the shearing process, phase A is added to phase B for shearing to obtain colostrum, which is then homogenized.
10. Use of the whitening flexible liposome according to any one of claims 1 to 8 in the preparation of cosmetics.