Preparation of cationic liposome and application of cationic liposome in cosmetics

Abstract

The invention belongs to the field of pharmaceutical preparations and cosmetics, and particularly relates to a cationic liposome containing plant extracts as well as a preparation method and application of the cationic liposome. The preparation method comprises the following steps: co-melting or dissolving a cacumen biotae extract, a ginger root extract, a ginseng root extract and a lipid component in a proper organic solvent system, concentrating, adding into a hydration medium, and homogenizing to prepare the cationic liposome containing the plant extract component. According to the invention, the lipid component is taken as a carrier, so that the transdermal performance and bioavailability of the three plant extracts and the active components contained in the three plant extracts can be improved, and the three plant extracts and the active components can penetrate through the cuticle of the skin to the greatest extent, so that the efficacy is effectively exerted.

Description

Technical Field

[0001] This invention belongs to the field of cosmetics, specifically relating to a cationic liposome containing arborvitae leaf extract, ginger root extract, and ginseng root extract, as well as its preparation method and application. Background Technology

[0002] Thuja orientalis leaf extract is extracted from the branches and leaves of the cypress family plant. Traditional Chinese medicine records that it has the effects of cooling the blood and stopping bleeding, promoting hair growth and darkening hair. It contains volatile oils, flavonoids and various trace elements, which have a good care effect on the scalp, can promote hair growth and improve hair loss. Studies have shown that the main active ingredients in thuja orientalis leaf extract, such as kaempferol and quercetin, can reduce the concentration of dihydrotestosterone (DHT) by inhibiting 5α-reductase activity, thus alleviating androgenetic alopecia (Zhang Y. (2018). Study on the Active Fraction and Component CE of Thuja orientalis for Hair Growth and Their Preparations [Shenyang Pharmaceutical University]).

[0003] Ginger (ZINGIBER OFFICINALE) root extract is a substance extracted from fresh ginger, a plant used both as medicine and food with a wide range of applications. Studies have shown that ginger root extract mainly contains bioactive substances such as gingerol, gingerol, gingerene, shogaol, myrrhene, α-curcumene, linalool, eucalyptol, and α-borneol; among them, gingerol and shogaol can act on pathways such as PI3K / Akt and VEGF, activate the proliferation of hair follicle stem cells and improve scalp blood supply, thus playing a role in preventing hair loss and promoting hair growth (Dhariwala MY, Ravikumar P. (2019). An Overview of Herbal Alternatives in Androgenetic Alopecia. Journal of Cosmetic Dermatology, 18(4):966-975.).

[0004] Ginseng extract (PANAX GINSENG) is extracted from the roots, stems, and leaves of the ginseng plant (Panax ginseng), a member of the Araliaceae family. It contains various active substances such as ginsenosides and is widely used in health products and pharmaceuticals. According to a literature review, ginsenoside Re in ginseng extract can activate the Shh signaling pathway in hair follicle stem cells, inducing hair follicles to enter the growth phase and thus promoting hair growth (Choi BY. (2018). Hair-Growth Potential of Ginseng and Its Major Metabolites: A Review on Its Molecular Mechanisms. International Journal of Molecular Sciences, 19(9):2703.).

[0005] The above studies indicate that extracts of Platycladus orientalis leaves, ginger root, and ginseng root all contain active substances that can effectively improve hair loss and promote hair regeneration. However, since anti-hair loss and hair growth cosmetics are mainly used by applying them topically and rinsing them off, the bioactive substances contained in these extracts need to cross the skin's stratum corneum barrier and epidermal barrier to enter the dermis and exert their effects. Therefore, how to achieve efficient transdermal absorption of active substances has become a significant challenge in the research and development of anti-hair loss and hair growth cosmetics.

[0006] Through long-term research, the inventors discovered that encapsulating the above three plant extracts with lipids to form cationic liposomes and then applying them can significantly improve the skin penetration of the bioactive substances, thereby promoting the skin's absorption of the active substances and enhancing their function in preventing hair loss and promoting hair growth. Summary of the Invention

[0007] The primary technical problem to be solved by this invention is to provide a cationic liposome containing arborvitae leaf extract, ginger root extract, and ginseng root extract with good transdermal absorption properties.

[0008] The liposomes of this invention contain, by weight percentage, the following components: 0.05%-5% Platycladus orientalis leaf extract, 0.05%-5% ginger root extract, 0.05%-5% ginseng root extract, 5%-15% phospholipids, 0.05%-5% cationic lipids, 0.1%-40% softening agent, 5%-15% stabilizer, and the remainder being antioxidants and preservatives.

[0009] Preferably, it contains: 0.5%-3% of Platycladus orientalis leaf extract, 0.5%-3% of ginger root extract, 0.5%-3% of ginseng root extract, 10%-15% of phospholipids, 1%-5% of cationic lipids, 10%-30% of a softening agent, 10%-15% of a stabilizer, and the remainder being antioxidants and preservatives.

[0010] The phospholipids used in the liposomes of the present invention can be selected from one or more of the following: soybean lecithin, egg yolk lecithin, distearyl phosphatidylcholine, dipalmitoyl phosphatidylcholine and dimyristoyl phosphatidylcholine, preferably one or more of soybean lecithin and egg yolk lecithin.

[0011] The cationic lipids used in the liposomes of the present invention may be selected from one or more of the following: DC-cholesterol, lauroyl lysine amide, 1,2-dioleyl-3-dimethylamino-propane, stearamine, 1,3-dioleoxy-2-(6-carboxys-speramido)propane, trimethyl-2,3-dioleoyloxypropylammonium bromide and methyl 4-(N,N-dimethylamino)butyrate (dilinoleyl) ester, preferably DC-cholesterol;

[0012] The flexible agent used in the liposomes of the present invention may be selected from one or more of the following: polysorbate 80, cholic acid, sodium cholate, sodium deoxycholate, fatty acid sorbitan 80, polyoxyethylene (2) cetyl ether, propylene glycol and anhydrous ethanol, preferably one or more of polysorbate 80 and propylene glycol.

[0013] The stabilizer used in the liposomes of the present invention may be selected from one or more of the following: cholesterol, stigmasterol, sitosterol, ceramide, oleic acid, sodium oleate, poloxamer, monooleate, caprylic acid, caprylic acid, and caprylic / capric acid, preferably one or more of the following: cholesterol, ceramide, oleic acid, and poloxamer.

[0014] The antioxidants used in the liposomes of the present invention may be selected from one or more of the following: vitamin E, butylated hydroxyanisole, butylated hydroxytoluene, propyl gallate, ascorbic acid, sodium metabisulfite and ethylenediaminetetraacetic acid, preferably one or more of vitamin E and ascorbic acid;

[0015] The preservatives used in the liposomes of the present invention may be selected from one or more of p-hydroxyacetophenone, ethyl p-hydroxybenzoate and phenoxyethanol, preferably one or more of p-hydroxyacetophenone and phenoxyethanol.

[0016] The present invention also provides a method for preparing the above-mentioned liposomes, which comprises the following steps in sequence:

[0017] (1) Preparation of lipid solution: Take the formula amount of arborvitae leaf extract, ginger root extract and ginseng root extract, mix with the formula amount of phospholipid, cationic lipid, softener and stabilizer, melt and mix at 60-95℃;

[0018] (2) Preparation of lipid hydration suspension: The lipid solution prepared in (1) is added to deionized water at 60-85℃, and antioxidants and preservatives are added in the same amount as formulated. The mixture is stirred and dispersed to form lipid hydration suspension.

[0019] (3) Preparation of liposomes: The liposomes can be obtained by treating the lipid hydrated suspension with one or more of the following techniques: homogenization, sonication and shearing.

[0020] Another method for preparing the above-mentioned liposomes provided by the present invention comprises the following steps:

[0021] (1) Preparation of lipid solution: Take the formula amount of arborvitae leaf extract, ginger root extract and ginseng root extract, mix with the formula amount of phospholipid, cationic lipid, softener and stabilizer, add an appropriate amount of ethanol to dissolve, and evaporate the ethanol at 50-85℃ using rotary evaporation process until a lipid film layer is formed at the bottom of the solution.

[0022] (2) Preparation of lipid hydration suspension: Add deionized water at 60-85℃ to the lipid solution prepared in (1), and add antioxidants and preservatives in the prescribed amount at the same time. Stir and disperse to form lipid hydration suspension.

[0023] (3) Preparation of liposomes: The liposomes can be obtained by treating the lipid hydrated suspension with one or more of the following techniques: homogenization, sonication and shearing.

[0024] In any of the aforementioned methods for preparing the liposomes, the processing method in step (3) is high-pressure homogenization or shear homogenization.

[0025] The liposomes of the present invention can be used as part of a cosmetic formulation to prepare any suitable form of cosmetic, such as shampoo, shower gel, facial cleanser, skin serum, scalp serum, skin cream, skin lotion, face mask, eye mask, face cream, eye cream, etc., and applied to the skin surface by conventional methods.

[0026] In addition to the advantages of general liposomes, the cationic liposomes of the present invention also have the properties of anti-aggregation, strong skin affinity and strong flexibility, thereby improving the transdermal absorption efficiency of active ingredients.

[0027] Studies have shown that the liposomes of this invention possess strong anti-aggregation capabilities in aqueous systems. Ordinary liposomes are typically uncharged and are prone to aggregation in aqueous systems due to van der Waals forces, affecting their dispersibility and even stability, thus deteriorating transdermal absorption efficiency. The anti-aggregation property of the cationic liposomes of this invention stems from the addition of cationic lipids. These cationic lipids impart the same charge to the liposomes, causing them to repel each other and thus preventing aggregation, thereby improving their dispersibility and transdermal absorption efficiency.

[0028] Studies have also shown that the liposomes of the present invention have strong skin affinity. This is because the stratum corneum of human skin carries a negative charge, and the positively charged cationic liposomes are easily attracted by the structure of the stratum corneum and infiltrate the surface of the stratum corneum, thereby increasing the chance of the liposomes and the active substances contained therein coming into contact with the skin and improving the transdermal absorption efficiency.

[0029] Furthermore, the deformability of the liposomes of the present invention is significantly stronger than that of ordinary liposomes. For example, cationic liposomes with an average particle size of 200 nm can pass through pores with a pore size half their own size. This ability stems from the inhomogeneity of their lipid membrane, as the lipid membrane contains surfactants that tend to aggregate in highly tortuous regions. Therefore, the surface energy that the liposomes need to overcome during deformation is greatly reduced, thus endowing the liposomes with high deformability. This deformability makes it easier for liposome particles to pass through the stratum corneum barrier and the epidermal barrier, which is beneficial to improving the transdermal absorption efficiency and actual efficacy of the liposomes and the active ingredients they carry. Attached Figure Description

[0030] Figure 1 The images show a comparison of the morphology of cationic liposomes and ordinary liposomes after 72 hours of static treatment; the left image shows the morphology of the cationic liposomes described in Example 9 after treatment, and the right image shows the morphology of the ordinary liposomes described in Comparative Example 1 after treatment. Detailed Implementation

[0031] Example 1

[0032] Take 0.5g of Platycladus orientalis leaf extract, 0.5g of ginger root extract, 0.5g of ginseng root extract, 5g of soybean lecithin, 1.5g of DC-cholesterol, 10g of polysorbate 80, and 10g of cholesterol in a 100ml beaker and stir and mix them in a 95℃ water bath. After complete melting and mixing, transfer the lipid solution in the beaker to about 60ml of 85℃ deionized water, and add 0.05g of ascorbic acid and 0.05g of p-hydroxyacetophenone. After stirring evenly, add deionized water to 100g. Pass the resulting lipid hydration suspension through a high-pressure homogenizer to obtain cationic liposomes containing plant extracts.

[0033] Example 2

[0034] Take 0.5g of Platycladus orientalis leaf extract, 0.5g of ginger root extract, 0.5g of ginseng root extract, 5g of soybean lecithin, 1.5g of DC-cholesterol, 10g of polysorbate 80, 10g of cholesterol, and 25g of anhydrous ethanol into a 250ml round-bottom flask and stir to mix. After the materials are fully dissolved in anhydrous ethanol, rotary evaporate the anhydrous ethanol at 80℃ until a thin lipid layer appears at the bottom of the solution. Stop rotary evaporation, add about 60ml of 60℃ deionized water to the round-bottom flask, and add 0.05g of ascorbic acid and 0.05g of p-hydroxyacetophenone. Stir well and then add deionized water to bring the total volume to 100g. Pass the resulting lipid hydration suspension through a high-pressure homogenizer to obtain cationic liposomes containing plant extracts.

[0035] Example 3

[0036] Take 0.5g of Platycladus orientalis leaf extract, 0.5g of ginger root extract, 0.5g of ginseng root extract, 5g of soybean lecithin, 1.5g of DC-cholesterol, 10g of polysorbate 80, and 10g of cholesterol in a 100ml beaker and stir and mix them in a 95℃ water bath. After complete melting and mixing, transfer the lipid solution in the beaker to about 60ml of 85℃ deionized water, and add 0.05g of ascorbic acid and 0.05g of p-hydroxyacetophenone. After stirring evenly, add deionized water to 100g. Homogenize the resulting lipid hydration suspension by high-speed shearing to obtain cationic liposomes containing plant extracts.

[0037] Example 4

[0038] Take 1g of Platycladus orientalis leaf extract, 1g of ginger root extract, 1g of ginseng root extract, 5g of soybean lecithin, 5g of egg yolk lecithin, 3g of DC-cholesterol, 15g of polysorbate 80, and 5g of cholesterol in a 100ml beaker and stir them together in a 90℃ water bath. After they are completely melted and mixed, transfer the lipid solution in the beaker to about 60ml of 85℃ deionized water, and add 0.05g of ascorbic acid and 0.05g of p-hydroxyacetophenone. Stir well and then add deionized water to make up to 100g. Pass the resulting lipid hydration suspension through a high-pressure homogenizer to obtain cationic liposomes containing plant extracts.

[0039] Example 5

[0040] Take 1g of Platycladus orientalis leaf extract, 1g of ginger root extract, 1g of ginseng root extract, 5g of soybean lecithin, 5g of egg yolk lecithin, 4.5g of DC-cholesterol, 10g of polysorbate 80, 5g of propylene glycol, 5g of cholesterol, and 5g of poloxamer 407 and mix them in a 100ml beaker. Heat in a 90℃ water bath and stir until completely melted and mixed. Transfer the lipid solution in the beaker to about 50ml of 85℃ deionized water, add 0.05g of vitamin E and 0.05g of phenoxyethanol, stir well, and then add deionized water to 100g. Pass the resulting lipid hydration suspension through a high-pressure homogenizer to obtain cationic liposomes containing plant extracts.

[0041] Example 6

[0042] Take 1g of Platycladus orientalis leaf extract, 1g of ginger root extract, 1g of ginseng root extract, 5g of soybean lecithin, 5g of egg yolk lecithin, 4.5g of DC-cholesterol, 15g of polysorbate 80, 5g of cholesterol, and 5g of poloxamer 407 and place them in a 100ml beaker. Stir and mix them in a 90℃ water bath. After they are completely melted and mixed, transfer the lipid solution in the beaker to about 50ml of 85℃ deionized water. At the same time, add 0.05g of vitamin E and 0.05g of phenoxyethanol, stir well, and then add deionized water to 100g. Pass the resulting lipid hydration suspension through a high-pressure homogenizer to obtain cationic liposomes containing plant extracts.

[0043] Example 7

[0044] Take 2g of Platycladus orientalis leaf extract, 2g of ginger root extract, 2g of ginseng root extract, 5g of soybean lecithin, 10g of egg yolk lecithin, 5g of DC-cholesterol, 10g of propylene glycol, 5g of cholesterol, 3g of ceramide, and 2g of oleic acid and place them in a 100ml beaker. Stir and mix them in a 90℃ water bath. After they are completely melted and mixed, transfer the lipid solution in the beaker to about 50ml of 85℃ deionized water. At the same time, add 0.05g of vitamin E and 0.05g of phenoxyethanol, stir well, and then add deionized water to 100g. Homogenize the resulting lipid hydration suspension by high-speed shearing to obtain cationic liposomes containing plant extracts.

[0045] Example 8

[0046] 3g of Platycladus orientalis leaf extract, 3g of ginger root extract, 3g of ginseng root extract, 10g of soybean lecithin, 5g of egg yolk lecithin, 5g of DC-cholesterol, 15g of polysorbate 80, 8g of cholesterol, 2g of oleic acid, and 40g of anhydrous ethanol were mixed in a 250ml round-bottom flask. After the materials were fully dissolved in the anhydrous ethanol, the anhydrous ethanol was rotary evaporated at 80℃ until a thin lipid layer appeared at the bottom of the solution. The rotary evaporation was then stopped, and about 40ml of 60℃ deionized water was added to the round-bottom flask. At the same time, 0.05g of ascorbic acid and 0.05g of p-hydroxyacetophenone were added. After stirring evenly, deionized water was added to bring the total volume to 100g. The resulting lipid hydration suspension was passed through a high-pressure homogenizer to obtain cationic liposomes containing plant extracts.

[0047] Example 9

[0048] Take 3g of Platycladus orientalis leaf extract, 3g of ginger root extract, 3g of ginseng root extract, 15g of soybean lecithin, 5g of DC-cholesterol, 15g of polysorbate 80, 8g of cholesterol, and 2g of oleic acid in a 100ml beaker and stir and mix them in a 90℃ water bath. After complete melting and mixing, transfer the lipid solution in the beaker to about 45ml of 85℃ deionized water, and add 0.05g of ascorbic acid and 0.05g of phenoxyethanol. Stir well and then add deionized water to 100g. Homogenize the resulting lipid hydration suspension by high-speed shearing to obtain cationic liposomes containing plant extracts.

[0049] Comparative Example 1

[0050] Take 3g of Platycladus orientalis leaf extract, 3g of ginger root extract, 3g of ginseng root extract, 15g of soybean lecithin, 5g of DC-cholesterol, 8g of cholesterol, and 2g of oleic acid in a 100ml beaker and stir and mix them in a 90℃ water bath. After complete melting and mixing, transfer the lipid solution in the beaker to about 45ml of 85℃ deionized water, and add 0.05g of ascorbic acid and 0.05g of phenoxyethanol. Stir well and then add deionized water to 100g. Homogenize the resulting lipid hydration suspension by high-speed shearing to obtain cationic liposomes containing plant extracts but without a softening agent.

[0051] Comparative Example 2

[0052] Take 3g of Platycladus orientalis leaf extract, 3g of ginger root extract, 3g of ginseng root extract, 15g of soybean lecithin, 15g of polysorbate 80, 8g of cholesterol, and 2g of oleic acid in a 100ml beaker and stir and mix them in a 90℃ water bath. After complete melting and mixing, transfer the lipid solution in the beaker to about 45ml of 85℃ deionized water, add 0.05g of ascorbic acid and 0.05g of phenoxyethanol, stir evenly, and then add deionized water to 100g. Homogenize the resulting lipid hydration suspension by high-speed shearing to obtain ordinary liposomes containing plant extracts.

[0053] Comparative Example 3

[0054] Take 15g of soybean lecithin, 5g of DC-cholesterol, 15g of polysorbate 80, 8g of cholesterol, and 2g of oleic acid in a 100ml beaker and stir them together in a 90℃ water bath. After they are completely melted and mixed, transfer the lipid solution in the beaker to about 45ml of 85℃ deionized water, and add 0.05g of ascorbic acid and 0.05g of phenoxyethanol. Stir well and then add deionized water to 100g. Homogenize the resulting lipid hydration suspension by high-speed shearing to obtain blank cationic liposomes without plant extracts.

[0055] Example 10

[0056] Take an appropriate amount of the liposomes described in Example 9 and prepare a scalp serum according to the following formulation and process:

[0057] According to the raw material content in the table below, take the formula amount of sodium alginate, glycerol, and the cationic liposomes described in Example 9, dissolve them in an appropriate amount of deionized water; slowly add triethanolamine to adjust the pH of the solution to 7.4±0.1, and add deionized water to 100g.

[0058] Ingredient name Ingredient content (w / w) Deionized water Up to 100% Sodium alginate 0.65％ Triethanolamine Appropriate amount Glycerol 3％ Cationic liposomes containing plant extracts 20％

[0059] Comparative Example 4

[0060] Take an appropriate amount of the ordinary liposomes containing plant extracts described in Comparative Example 2, and prepare a scalp serum according to the following formula and process: According to the raw material content in the table below, take the formula amount of sodium alginate, glycerol, and the ordinary liposomes described in Comparative Example 2, and dissolve them in an appropriate amount of deionized water; slowly add triethanolamine, adjust the pH of the solution to 7.4±0.1, and add deionized water to 100g.

[0061] Ingredient name Ingredient content (w / w) Deionized water Up to 100% Sodium alginate 0.65％ Triethanolamine Appropriate amount Glycerol 3％ Common liposomes containing plant extracts 20％

[0062] Comparative Example 5

[0063] Take an appropriate amount of the blank liposomes without plant extracts described in Comparative Example 3, and prepare a non-liposome-included control for scalp serum according to the following formulation and process:

[0064] According to the raw material content in the table below, take the formula amount of sodium alginate, glycerol, and blank liposomes described in Comparative Example 3, dissolve them in an appropriate amount of deionized water; slowly add triethanolamine to adjust the pH of the solution to 7.4±0.1, and add deionized water to 100g.

[0065]

[0066]

[0067] Comparative Example 6

[0068] Take an appropriate amount of the blank liposomes without plant extracts described in Comparative Example 3, and prepare a blank control of scalp serum according to the following formulation and process:

[0069] According to the raw material content in the table below, take the formula amount of sodium alginate, glycerol, and blank liposomes described in Comparative Example 3, dissolve them in an appropriate amount of deionized water; slowly add triethanolamine to adjust the pH of the solution to 7.4±0.1, and add deionized water to 100g.

[0070] Ingredient name Ingredient content (w / w) Deionized water Up to 100% Sodium alginate 0.65％ Triethanolamine Appropriate amount Glycerol 3％ Blank cationic liposomes 20％

[0071] Example 11

[0072] Take an appropriate amount of the cationic liposomes containing plant extracts described in Example 9, and prepare an anti-hair loss and hair growth shampoo according to the following formulation and process:

[0073] Based on the raw material content in the table below, take the appropriate amount of each ingredient and dissolve it completely in deionized water.

[0074] Ingredient name Ingredient content (w / w) Deionized water Up to 100% Sodium lauryl ether sulfate 13.5％ Cocamidopropyl Betaine 9.5％ Decyl glucoside 5.5％ Sodium lauroyl sarcosinate 30 2％ Polyethylene glycol 6000 distearate 0.75％ EDTA-2Na 0.05％ Cationic liposomes containing plant extracts 15％

[0075] Comparative Example 7

[0076] Take appropriate amounts of the blank liposomes without plant extracts described in Comparative Example 3, and the Platycladus orientalis leaf extract, ginger root extract, and ginseng root extract used in Example 9, and prepare a non-liposome-included control standard for anti-hair loss and hair growth shampoo according to the following formulation and process:

[0077] Based on the raw material content in the table below, take the appropriate amount of each ingredient and dissolve it completely in deionized water.

[0078]

[0079]

[0080] Comparative Example 8

[0081] Take the blank liposomes without plant extracts described in Comparative Example 3 and prepare a blank control product for anti-hair loss and hair growth shampoo according to the following formulation and process:

[0082] Based on the raw material content in the table below, take the appropriate amount of each ingredient and dissolve it completely in deionized water.

[0083] Ingredient name Ingredient content (w / w) Deionized water Up to 100% Sodium lauryl ether sulfate 13.5％ Cocamidopropyl Betaine 9.5％ Decyl glucoside 5.5％ Sodium lauroyl sarcosinate 30 2％ Polyethylene glycol 6000 distearate 0.75％ EDTA-2Na 0.05％ Blank cationic liposomes 15％

[0084] Experimental Example 1

[0085] Take appropriate amounts of the newly prepared cationic liposomes described in Example 9, the newly prepared cationic liposomes without softening agent described in Comparative Example 1, and deionized water; under the pumping of a 0.2 MPa constant pressure peristaltic pump (Jiaming Fluid, purchased from Nanjing Runze Fluid Control Equipment Co., Ltd.), the rate V of deionized water passing through a 0.1 μm polyvinylidene fluoride (PVDF) microporous membrane filter (Millipore, purchased from Shanghai Aiyan Biotechnology Co., Ltd.) was measured. WATER The rate V of cationic liposomes passing through a PVDF filter Lipo_Flex And the rate V of cationic liposomes without softening agents passing through a PVDF filter. Lipo_Norm And according to the public statement P=V Lipo / V WATER The relative permeability of the two liposomes was calculated by multiplying by 100%. Each experiment was repeated three times in parallel. The experimental results are shown in the table below.

[0086]

[0087] As shown in the table above, the relative permeability of the cationic liposomes described in Example 9 through a 0.1 μm PVDF filter under an external pressure of 0.2 MPa is significantly higher than that of the cationic liposomes without a flexible agent described in Comparative Example 1, indicating that the softness and deformability of the liposomes described in this invention are significantly better than those of ordinary liposomes without a flexible agent.

[0088] Experiment Example 2

[0089] Take appropriate amounts of the newly prepared cationic liposomes described in Example 9 and the newly prepared ordinary liposomes described in Comparative Example 2, dilute them at a ratio of 1:20, and then apply 50 μl of each to a glass slide. Incubate at room temperature (25°C) in a humidified chamber for 72 hours. Remove the slides and allow the diluted solution to air dry naturally. Then, use a scanning electron microscope (LEO1530VP, Germany LEO Ltd) to measure the liposome particle size and describe the liposome morphology and aggregation state. The resulting scanning electron microscope images (sample × 5000) are shown below. Figure 1 As shown in the figure, the cationic liposomes containing plant extracts of the present invention are spherical in appearance, with a particle size concentrated in the range of 150-300 nm and an average particle size of about 200 nm; and compared with the ordinary liposomes described in Comparative Example 1, the cationic liposomes described in Example 9 have significantly better anti-aggregation properties.

[0090] Experimental Example 3

[0091] Appropriate amounts of the newly prepared cationic liposomes described in Example 9 and the newly prepared ordinary liposomes described in Comparative Example 2 were diluted separately and their zeta potentials were measured using a nanoparticle size and zeta potential analyzer (Malvern zeta-size Nano ZS, Malvern Instrument Ltd, UK). Each experiment was repeated three times in parallel, and the experimental results are shown in the table below:

[0092]

[0093] As shown in the table above, the ζ-potential of the cationic liposome particles described in Example 9 is >20mV, and the absolute value of the ζ-potential is significantly higher than that of the ordinary liposomes described in Comparative Example 2, indicating that the liposome particles carry a positive charge, which is beneficial to their affinity and penetration into the stratum corneum of the skin.

[0094] Experiment Example 4

[0095] Twelve 8-10 week old female nude mice (purchased from the Comparative Medicine Center of Yangzhou University) were sacrificed. Skin from the same area on their backs was harvested, subcutaneous tissue was carefully removed, and the skin was temporarily stored at 4°C. A modified Franz diffusion chamber was used to fix the skin from the mouse backs into the diffusion chamber, with the keratin layer facing the supply chamber and the dermis layer facing the receiving chamber, ensuring close contact between the dermis and the receiving solution (0.9% physiological saline). The contact area between the skin tissue and the receiving solution was 1.0 cm². 2 The volume of the liquid to be received is 4.5 ml, and the temperature of the constant temperature water bath is 32℃.

[0096] Take 1 ml each of the scalp serum described in Example 10, the scalp serum described in Comparative Example 4, the non-liposome inclusion standard of the scalp serum described in Comparative Example 5, and the blank standard of the scalp serum described in Comparative Example 6, and place them in the supply chamber, then evenly coat them onto the surface of the skin sample. Under continuous stirring, take 1 ml of the receiving solution at 3h, 6h, 9h, 12h, 18h, and 24h after coating the liposomes, filter it through a 0.45μm PVDF microporous membrane, and determine the concentrations of representative bioactive substances kaempferol, gingerol, and ginsenoside Re in the sample by high performance liquid chromatography (HPLC). Each experiment was repeated in triplicate. The HPLC conditions were as follows: Agilent 1100 HPLC system equipped with a 4.6×250mm C18 silica gel column and a G1314A VWD variable wavelength scanning UV detector; the mobile phase was acetonitrile-0.2% glacial acetic acid (35:65); the mobile phase flow rate was 1 ml / min; and the column temperature was room temperature.

[0097]

[0098] After obtaining data at all time points, according to the formula Calculate the cumulative permeability per unit area of ​​the target material. Where Q...n C represents the cumulative transmittance per unit area at the nth time point. n C represents the concentration of the target substance in the receiving chamber at the nth time point. i V: Concentration of the target substance in the receiving chamber at time point n-1; V: Total volume of the receiving liquid. i S: Sampling volume, S: Diffusion area.

[0099] The cumulative permeation rate of kaempferol through isolated nude mouse skin in the above experimental examples is shown in the table below:

[0100]

[0101] Cumulative permeation of kaempferol through isolated nude mouse skin at different time points in different groups (ng / cm2)

[0102] The cumulative penetration amount of shogaol through isolated nude mouse skin in the above experimental examples is shown in the table below:

[0103]

[0104] Cumulative penetration of shogaol into isolated nude mouse skin at different time points in different groups (ng / cm) 2 )

[0105] The cumulative permeation amount of ginsenoside Re through isolated nude mouse skin in the above experimental examples is shown in the table below:

[0106]

[0107] Cumulative permeation of ginsenoside Re to isolated nude mouse skin at different time points in different groups (ng / cm²) 2 )

[0108] As shown in the table above, compared with Comparative Example 5, the scalp serums prepared from liposomes containing plant extracts as described in Example 10 and Comparative Example 4 can significantly improve the transdermal absorption rate of representative bioactive substances contained in Platycladus orientalis leaf extract, ginger root extract, and ginseng root extract, namely kaempferol, gingerol, and ginsenoside Re.

[0109] In particular, the scalp serum prepared by cationic liposomes in Example 10 has a higher transdermal absorption rate of its representative bioactive components than the scalp serum prepared by ordinary liposomes in Comparative Example 4. The above experimental results demonstrate that liposomes, especially cationic liposome encapsulation preparations, have a transdermal absorption promoting effect on substances with anti-hair loss and hair growth functions in Platycladus orientalis leaf extract, ginger root extract, and ginseng root extract.

[0110] Experimental Example 5

[0111] In accordance with the specific requirements of the "Test Methods for the Efficacy of Cosmetic Anti-Hair Loss" section of the National Medical Products Administration's Supplementary Testing Methods (No. 17 of 2021) document "Technical Specifications for Cosmetic Safety" (2015 Edition), approximately 20-24 subjects were recruited. The eligible subjects were randomly and equally divided into three groups based on their gender, age, and amount of hair loss: Group 1, Group 2, and the control group, with at least 6 subjects in each group. The anti-hair loss and hair growth shampoo described in Example 11, the non-liposome inclusion complex control of the anti-hair loss and hair growth shampoo described in Comparative Example 7, and the blank control of the anti-hair loss and hair growth shampoo described in Comparative Example 8 were distributed to the subjects respectively.

[0112] Subjects were instructed to use the product correctly according to the instructions for 12 weeks, once every two days, with a dosage of approximately 5-10 ml each time. During the trial, subjects were required to keep a usage diary and strictly adhere to the restrictions. Follow-up visits were conducted before product use and at 4, 8, and 12 weeks after use. Hair loss counting and hair density assessment tests were performed at each visit.

[0113]

[0114] After 12 weeks of continuous use, the hair growth shampoo significantly reduced hair loss and significantly increased local hair density in all subjects.

[0115] In particular, the anti-hair loss and hair growth shampoo prepared from cationic liposomes as described in Example 11 has significantly better anti-hair loss and hair growth effects than the anti-hair loss and hair growth shampoo prepared from non-liposome-encapsulated plant extracts as described in Comparative Example 7. The above experimental results demonstrate that liposomes, especially cationic liposome-encapsulated preparations, have a transdermal absorption promoting effect on substances with anti-hair loss and hair growth functions in Platycladus orientalis leaf extract, ginger root extract, and ginseng root extract. In clinical practice, they can significantly improve the transdermal absorption efficiency of the above extracts and promote their efficacy.

Claims

1. A cationic liposome containing plant extract, characterized by, based on the weight of the liposome, It includes the following components: 0.05%-5% of Platycladus orientalis leaf extract, 0.05%-5% of ginger root extract, 0.05%-5% of ginseng root extract, 5%-15% of phospholipids, 0.05%-5% of cationic lipids, 0.1%-40% of softening agents, 5%-15% of stabilizers, and the remainder being antioxidants and preservatives.

2. The liposomes as described in claim 1, characterized in that, The preferred composition is: 0.5%-3% of Platycladus orientalis leaf extract, 0.5%-3% of ginger root extract, 0.5%-3% of ginseng root extract, 10%-15% of phospholipids, 1%-5% of cationic lipids, 5%-15% of softening agent, 5%-10% of stabilizer, and the remainder being antioxidants and preservatives.

3. The liposomes as described in claim 3, characterized in that: The phospholipids are selected from one or more of soybean lecithin, egg yolk lecithin, distearyl phosphatidylcholine, dipalmitoyl phosphatidylcholine, and myristoyl phosphatidylcholine; The cationic lipids are selected from one or more of DC-cholesterol, lauroyl lysine amide, 1,2-dioleyl-3-dimethylamino-propane, stearylamine, 1,3-dioleoxy-2-(6-carboxys-spermine)propane, trimethyl-2,3-dioleoyloxypropylammonium bromide and methyl 4-(N,N-dimethylamino)butyrate (dilinoleyl) ester; The flexing agent is selected from one or more of polysorbate 80, cholic acid, sodium cholate, sodium deoxycholate, fatty acid sorbitan 80, polyoxyethylene (2) cetyl ether, propylene glycol and anhydrous ethanol; The stabilizer is selected from one or more of cholesterol, stigmasterol, sitosterol, ceramide, oleic acid, sodium oleate, poloxamer, monooleate, caprylic acid, caprylic / capric acid, and caprylic / capric acid. The antioxidant is selected from one or more of vitamin E, butylated hydroxyanisole, butylated hydroxytoluene, propyl gallate, ascorbic acid, sodium metabisulfite, and ethylenediaminetetraacetic acid; The preservative is selected from one or more of p-hydroxyacetophenone, ethyl p-hydroxybenzoate, and phenoxyethanol.

4. The liposomes as described in claim 3, characterized in that: Phospholipids are selected from one or more of soybean lecithin and egg yolk lecithin; The cationic lipid is DC-cholesterol; The flexing agent is selected from one or more of polysorbate 80 and propylene glycol; The stabilizer is selected from one or more of cholesterol, ceramide, oleic acid, and poloxamer; Antioxidants are selected from one or more of vitamin E and ascorbic acid; The preservative is selected from one or more of p-hydroxyacetophenone and phenoxyethanol.

5. A method for preparing liposomes containing plant extracts as described in claim 1, characterized in that, Includes the following steps: (5.1) Preparation of lipid solution: Take the formula amount of arborvitae leaf extract, ginger root extract and ginseng root extract, mix with the formula amount of phospholipid, cationic lipid, softener and stabilizer, melt and mix at 60-95℃; (5.2) Preparation of lipid hydration suspension: The lipid solution prepared in (1) is added to deionized water at 60-85℃, and antioxidants and preservatives are added in the same amount as formulated. The mixture is stirred and dispersed to form lipid hydration suspension. (5.3) Preparation of liposomes: The liposomes can be obtained by treating the lipid hydrated suspension with one or more of the following techniques: homogenization, sonication and shearing.

6. A method for preparing cationic liposomes containing plant extracts as described in claim 1, characterized in that, Includes the following steps: (6.1) Preparation of lipid solution: Take the formula amount of arborvitae leaf extract, ginger root extract and ginseng root extract, mix with the formula amount of phospholipid, cationic lipid, softener and stabilizer, add an appropriate amount of ethanol to dissolve, and evaporate the ethanol by rotary evaporation at 50-85℃ until a lipid film layer is formed at the bottom of the solution. (6.2) Preparation of lipid hydration suspension: Add deionized water at 60-85℃ to the lipid solution prepared in (1), and add the prescribed amount of antioxidant and preservative at the same time. Stir and disperse to form lipid hydration suspension. (6.3) Preparation of liposomes: The liposomes can be obtained by treating the lipid hydrated suspension with one or more of the following techniques: homogenization, sonication and shearing.

7. The preparation method according to claim 5 or 6, characterized in that, The processing methods in steps (5.3) and (6.3) are high-pressure homogenization or shear homogenization.

8. The application of liposomes in cosmetics as described in any one of claims 1 to 4, characterized in that: The cosmetic types mentioned include shampoos, shower gels, facial cleansers, skin serums, scalp serums, skin creams, skin lotions, face masks, eye masks, face creams, eye creams, and all other forms of cosmetics.

9. The application of liposomes as described in any one of claims 1 to 4 in cosmetics, characterized in that: The cosmetics mentioned include excipients acceptable in the cosmetics field, including: solvents, solubilizers, preservatives, antioxidants, pH adjusters, penetration enhancers, moisturizers, thickeners, chelating agents, skin protectants, surfactants, emulsifiers, propellants, fragrances, and colorants.

10. The application of liposomes according to any one of claims 9 to 9 in cosmetics, characterized in that: The application of the liposomes in the preparation of cosmetics for preventing hair loss and promoting hair growth.

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