New use of ginsenoside liposome shell material, liposome and application and cosmetic
By using ginsenoside liposome shells to load cosmetic active ingredients, the problems of unsatisfactory effects and skin barrier obstruction in existing hair loss treatments are solved. This achieves targeted follicle penetration of active substances and improves safety, thus directly combating hair loss.
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Patents(China)
- Current Assignee / Owner
- INCIPIRIT TECH (GUANGZHOU) CO LTD
- Filing Date
- 2025-11-18
- Publication Date
- 2026-04-28
AI Technical Summary
Existing hair loss treatments are not very effective and have strong adverse reactions. The skin's stratum corneum barrier hinders the effective penetration of active ingredients and makes it difficult to target hair follicles. Traditional liposomes using cholesterol pose safety risks.
Using ginsenosides as the shell material for liposomes, cosmetic active ingredients are loaded onto them. By replacing cholesterol with ginsenosides, ginsenoside liposomes are prepared to promote transdermal absorption of active ingredients and target hair follicles, thereby directly combating hair loss by combining the active substances of ginsenosides.
It improves the permeability and safety of active ingredients in cosmetics, enhances the penetration ability of hair follicles, and ginsenosides themselves have the effects of inhibiting 5α-reductase activity, promoting the proliferation of hair papilla cells, and anti-inflammatory and soothing effects, thus improving hair loss problems.
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Figure CN121154434B_ABST
Abstract
Description
Technical Field
[0001] This invention relates to the field of new materials for daily chemical products, and in particular to a new use of ginsenoside liposome shell material, liposomes and their applications in cosmetics. Background Technology
[0002] Hair loss affects approximately 2% of the world's population. Its causes include the cyclical activity of hair follicles and the depletion of hair follicle stem cells. Factors such as hormone levels, genetic predisposition, oxidative stress, loss of extracellular matrix proteins in hair follicle cells, medications, and inflammation can all influence the hair loss process to varying degrees, leading to a shortened anagen phase, a prolonged telogen phase, and even damage and atrophy of hair follicles.
[0003] There are two pathways for the transdermal absorption of active ingredients: the transepidermal route and the appendage route. The transepidermal route involves the active ingredient penetrating the stratum corneum to enter the active epidermis and then diffusing into the dermis. The appendage route refers to the absorption of the active ingredient through hair follicles, sebaceous glands, and sweat glands. Transdermal absorption is an important pathway for treating hair loss; however, the stratum corneum barrier hinders the effective penetration of active ingredients and is the main barrier to local delivery of active ingredients. Therefore, developing a delivery system that can promote the penetration of active ingredients through the stratum corneum, effectively target hair follicles, and enhance follicle penetration is urgently needed.
[0004] Liposomes can facilitate the penetration of active ingredients into the skin through hydration, penetration mechanisms, fusion mechanisms, and the pilosebaceous gland pathway. Liposomes can encapsulate lipid-soluble active ingredients within the lipid bilayer and water-soluble active ingredients within liposome vesicles, forming monolayers or multilayers of liposomes. This enhances the stability of the active ingredients while promoting their transdermal absorption and reaching the target site in the pilosebaceous follicle.
[0005] Liposome membranes are mainly composed of phospholipids and cholesterol, which are the main components of biological membranes and have advantages such as biodegradability, biocompatibility, and high safety. Excessive cholesterol intake increases the risk of diseases such as hyperlipidemia and tumors; moreover, cholesterol is easily oxidized to produce cholesterol oxidation products, which have certain cytotoxicity and potential carcinogenicity, affecting the stability and safety of formulations.
[0006] Ginsenosides have a molecular structure similar to cholesterol and can replace cholesterol in interacting with phospholipids, stabilizing the lipid bilayer structure. When they act as carriers, they can create transient gaps when in contact with the cell membrane, promoting the penetration of active substances, and the integrity of the cell membrane can be restored in a short time.
[0007] Currently, the main medications for treating hair loss are minoxidil and finasteride. However, the efficacy of these drugs in their marketed formulations is not ideal, and they have significant adverse reactions. Ginsenosides, derived from natural herbs, are mild and non-irritating, and can treat hair loss through multiple mechanisms and pathways. Firstly, they directly combat the main culprit of hair loss (by inhibiting 5α-reductase activity, reducing the production of dihydrotestosterone (the main cause of hair loss); as an androgen receptor inhibitor, they competitively inhibit the binding of dihydrotestosterone to androgen receptors, negatively regulating downstream hair loss pathways). Secondly, they nourish and revitalize hair follicles (promoting the production of vascular endothelial growth factor, dilating blood vessels; increasing alkaline phosphatase activity, promoting the proliferation of dermal papilla cells). Thirdly, they improve the scalp microenvironment, preventing hair loss from its root cause (promoting collagen production, anti-inflammatory and soothing effects, relieving emotional stress).
[0008] Therefore, it is proposed to prepare ginsenoside liposomes by using ginsenosides as carriers to encapsulate active ingredients, promoting transdermal absorption of active substances, targeting and enhancing the penetration of active substances into hair follicles, and enabling ginsenosides to synergistically enhance the effects of other active substances, thus exerting both the intrinsic activity of ginsenosides and the formulation function. Ginsenoside liposomes have good targeted penetration ability into hair follicles and show promising application prospects in improving hair follicle-related problems such as hair loss, acne, and folliculitis.
[0009] Chinese patent application 202110633703.8 discloses the use of a ginsenoside composition in the preparation of a drug for preventing and treating hair loss by acting on hair follicle tissue. The ginsenoside composition comprises ginsenoside Rg1, ginsenoside Re, and ginsenoside CK, wherein ginsenoside Rg1 and ginsenoside Re are the main active ingredients, and ginsenoside CK is an auxiliary ingredient. Furthermore, the application also provides the use of the above-mentioned ginsenoside composition in the preparation of a drug that enhances the activity of hair follicle tissue. The drug is directly applied or sprayed onto the scalp to induce resting hair follicles to enter a regeneration cycle, thereby promoting hair growth.
[0010] However, a closer look at the instructions reveals that the method involves spraying ginsenosides directly onto the scalp surface, rather than using them as a carrier loaded with active ingredients.
[0011] Chinese patent application 201911068741.2 discloses a ginsenoside liposome and its preparation method, which is composed of ginsenosides, phospholipids and cholesterol, wherein the mass ratio of ginsenosides to phospholipids is 1:2 to 1:10 and the mass ratio of phospholipids to cholesterol is 2:1 to 8:1.
[0012] The scheme also discloses a method for preparing ginsenoside liposomes as described above. Phospholipids and cholesterol are selected as carriers to simulate cell membrane structural components. Ginsenoside liposomes are prepared by organic solvent injection. The liposomes have uniform particle size distribution and high encapsulation rate, which can enhance cell uptake function and improve the transdermal absorption capacity of ginsenosides. Moreover, the process is simple to operate, which is conducive to the application and development of ginsenoside liposomes in topical skin preparations or cosmetics.
[0013] Further examination of the instructions for this scheme reveals that the ginsenoside liposomes prepared by this scheme encapsulate ginsenosides inside the liposomes to improve the transdermal permeability of ginsenosides, rather than using ginsenosides as a shell material. Furthermore, this scheme has not been applied to products that act on hair follicles.
[0014] The following literature provides information on the use of ginsenosides as liposome shell materials:
[0015] Publication number CN120114392A discloses a ginsenoside liposome, its preparation method, and its application. As seen through its embodiments, the preparation method involves using ginsenoside liposomes as a shell material. It further discloses its cosmetic applications and specifies that the ginsenoside is protopanaxadiol and / or protopanatriol. Preferably, the protopanaxadiol is 20-(S)-protopanaxadiol, and the protopanatriol is preferably 20-(S)-protopanatriol.
[0016] This approach primarily focuses on the use of ginsenosides as a liposome shell material to improve their permeability. It does not investigate other applications of ginsenosides as a liposome shell material.
[0017] The applicant has discovered some new phenomena in its ongoing research on liposomes of ginsenosides, and hereby files this case. Summary of the Invention
[0018] The purpose of this invention is to provide a new use for ginsenoside liposome shell material. After loading cosmetic active ingredients, the ginsenoside liposome shell material can act on hair follicles, improve the permeability of cosmetic active ingredients, and enhance the anti-hair loss effect.
[0019] In addition, this invention also discloses a liposome, its application, and cosmetics.
[0020] To achieve the above objectives, this application discloses:
[0021] The use of ginsenoside liposome shell material to load cosmetic active ingredients; the ginsenoside liposome shell material contains ginsenosides;
[0022] The ginsenosides are one or more combinations of protopanaxadiol-type ginsenosides and protopanatriol-type ginsenosides;
[0023] The protopanaxadiol type saponin is at least one of Rg3, Rh2, Rg5, Rb1, Rh3, Rk1, and Rk2;
[0024] The protopanaxadiol saponins are at least one of Rk3, Rh4, Rh1, Rg2, and Rg1.
[0025] In the above-mentioned uses, the ginsenosides are any combination of the following:
[0026] Combination 1: Ginsenoside Rg1 12-28wt%; Ginsenoside Re 10-16wt%; Ginsenoside Rb1 12-28wt%; Ginsenoside Rb2 13-22wt%; Ginsenoside Rc 13-22wt%;
[0027] Combination 2: Ginsenoside Rg1 30-50 wt%; Ginsenoside Re 48-72 wt%;
[0028] Combination 3: Ginsenoside Rb1 28-50wt%; Ginsenoside Rb2 25-40wt%; Ginsenoside Rc 33-45wt%;
[0029] Combination 4: 20(S)-ginsenoside Rg2 8-16wt%; 20(R)-ginsenoside Rg2 7-15wt%; 20(S)-ginsenoside Rh1 17-25wt%; 20(R)-ginsenoside Rh1 16-23wt%; ginsenoside Rk3 5-12wt%; ginsenoside Rh4 16-26wt%;
[0030] More preferably, combination 4: 20(S)-ginsenoside Rg2 9-16wt%; 20(R)-ginsenoside Rg2 10-15wt%; 20(S)-ginsenoside Rh1 19-25wt%; 20(R)-ginsenoside Rh1 18-23wt%; ginsenoside Rk3 8-12wt%; ginsenoside Rh4 19-26wt%;
[0031] Combination 5: Ginsenoside Rk3 25-35wt%; Ginsenoside Rh4 65-75wt%;
[0032] Combination 6: 20(S)-ginsenoside Rg3 15-25wt%; 20(R)-ginsenoside Rg3 35-45wt%; ginsenoside Rg5 9-15wt%; 20(S)-ginsenoside Rh2 4-6wt%; 20(R)-ginsenoside Rh2 10-17wt%; ginsenoside Rk1 5-7wt%;
[0033] More preferably, combination 6: 20(S)-ginsenoside Rg3 18-24 wt%; 20(R)-ginsenoside Rg3 35-45 wt%; ginsenoside Rg5 11-15 wt%; 20(S)-ginsenoside Rh2 4-6 wt%; 20(R)-ginsenoside Rh2 13-17 wt%; ginsenoside Rk1 5-7 wt%;
[0034] Combination 7: 20(S)-Ginsenoside Rh2 20-30wt%; 20(R)-Ginsenoside Rh2 30-50wt%; Ginsenoside Rh3 10-20wt%; Ginsenoside Rk1 5-15wt%; Ginsenoside Rk2 2-8wt%;
[0035] The sum of the weight percentages of each ginsenoside in any of the above combinations is 100%.
[0036] In the above-mentioned applications, the shell material is made of phospholipids and ginsenosides; the mass ratio of phospholipids to ginsenosides is 1-10:1-5;
[0037] The phospholipids are one or more combinations of natural phospholipids (soybean lecithin, egg yolk lecithin, and cephalin) and / or synthetic phospholipids (hydrogenated lecithin, dipalmitoylphosphatidylcholine, dipalmitoylphosphatidylethanolamine, distearate phosphatidylcholine, myristoylphosphatidylcholine, and sphingomyelin).
[0038] In the above-mentioned uses, the cosmetic active ingredients are: type XVII collagen, type III collagen, type I collagen, soluble collagen, fibronectin, mussel protein, hydrolyzed yeast protein, hydrolyzed rice protein, hydrolyzed soybean protein, hydrolyzed silk, Artemia extract, plankton extract, adenosine, amino acids, tripeptide-1 copper, tetrahydromethylpyrimidine carboxylic acid, palmitoyl tetrapeptide-7, biotin, tripeptide-1, myristoyl pentapeptide-17, myristoyl hexapeptide-16, acetyl tetrapeptide-3, octapeptide-2, pentapeptide-20, astaxanthin, niacinamide, salicylic acid, menthol, panthenol, caffeine, ceramide, Platycladus orientalis leaf extract, ginger root extract, Polygonum multiflorum root extract, Angelica sinensis root extract, Sophora flavescens root extract, Scutellaria baicalensis root extract, Salvia miltiorrhiza root extract, Forsythia suspensa fruit extract, pea extract, and Ganoderma lucidum extract. Poria cocos extract, Commiphora stricta leaf extract, Eriobotrya japonica leaf extract, Glycyrrhiza glabra root extract, Centella asiatica extract, Tea extract, Matricaria champaca flower extract, Osmanthus fragrans flower extract, Rosemary leaf extract, Ylang-ylang flower extract, Ylang-ylang flower oil, Dipotassium glycyrrhizate, Diaminopyrimidine oxide, Minoxidil, Finasteride, Dexamethasone, Hydrocortisone, Salicylic acid, Azelaic acid, Mandelic acid, Glycolic acid, Gluconolactone, Citric acid, Tranexamic acid, Ascorbic acid, Tetrahydromethylpyrimidinecarboxylic acid, Tripeptide-1 Copper, hydrolyzed sodium hyaluronate, ceramide, arbutin, squalane, allantoin, nicotinamide, zinc PCA, zinc oxide, colloidal sulfur, glycine, arginine, dipotassium glycyrrhizate, papain, rosemary, guaiac wood extract, Yunnan Paris extract, purslane extract, witch hazel extract, thyme extract, centella asiatica extract, white willow bark extract, matrine, sophora flavescens root extract, salvia miltiorrhiza root extract, cinnamon bark extract, meadowsweet flower extract, eucalyptus leaf extract, menthol, peppermint leaf oil, adenosine, bisabolol, oligopeptide-1, dipotassium glycyrrhizate, quaternary ammonium salt-73, and selenium disulfide.
[0039] Meanwhile, the present invention also discloses a liposome, comprising a ginsenoside liposome shell material as described above and an inclusion, wherein the inclusion comprises a cosmetic active ingredient.
[0040] In the liposomes described above, the contents account for 0.0001% to 90% of the total weight of the liposomes.
[0041] In the aforementioned liposomes, the cosmetic active ingredients are: type XVII collagen, type III collagen, type I collagen, soluble collagen, fibronectin, mussel protein, hydrolyzed yeast protein, hydrolyzed rice protein, hydrolyzed soybean protein, hydrolyzed silk, Artemia extract, plankton extract, adenosine, amino acids, tripeptide-1 copper, tetrahydromethylpyrimidine carboxylic acid, palmitoyl tetrapeptide-7, biotin, tripeptide-1, myristoyl pentapeptide-17, myristoyl hexapeptide-16, acetyl tetrapeptide-3, octapeptide-2, pentapeptide-20, astaxanthin, niacinamide, salicylic acid, menthol, panthenol, caffeine, ceramide, Platycladus orientalis leaf extract, ginger root extract, Polygonum multiflorum root extract, Angelica sinensis root extract, Sophora flavescens root extract, Scutellaria baicalensis root extract, Salvia miltiorrhiza root extract, Forsythia suspensa fruit extract, pea extract, and Ganoderma lucidum extract. Poria cocos extract, Commiphora stricta leaf extract, Eriobotrya japonica leaf extract, Glycyrrhiza glabra root extract, Centella asiatica extract, Tea extract, Matricaria champaca flower extract, Osmanthus fragrans flower extract, Rosemary leaf extract, Ylang-ylang flower extract, Ylang-ylang flower oil, Dipotassium glycyrrhizate, Diaminopyrimidine oxide, Minoxidil, Finasteride, Dexamethasone, Hydrocortisone, Salicylic acid, Azelaic acid, Mandelic acid, Glycolic acid, Gluconolactone, Citric acid, Tranexamic acid, Ascorbic acid, Tetrahydromethylpyrimidinecarboxylic acid, Tripeptide-1 Copper, hydrolyzed sodium hyaluronate, ceramide, arbutin, squalane, allantoin, nicotinamide, zinc PCA, zinc oxide, colloidal sulfur, glycine, arginine, dipotassium glycyrrhizate, papain, rosemary, guaiac wood extract, Yunnan Paris extract, purslane extract, witch hazel extract, thyme extract, centella asiatica extract, white willow bark extract, matrine, sophora flavescens root extract, salvia miltiorrhiza root extract, cinnamon bark extract, meadowsweet flower extract, eucalyptus leaf extract, menthol, peppermint leaf oil, adenosine, bisabolol, oligopeptide-1, dipotassium glycyrrhizate, quaternary ammonium salt-73, and selenium disulfide.
[0042] Furthermore, the present invention also discloses the use of liposomes as described above in the preparation of cosmetics.
[0043] In the above-mentioned uses, the cosmetic is a cosmetic that acts on hair follicles and is used to promote the penetration of cosmetic active ingredients into hair follicles.
[0044] Finally, the present invention also discloses a cosmetic containing 0.0001 to 100 wt% of any of the liposomes described above.
[0045] Among the aforementioned cosmetics, the cosmetics are serums, freeze-dried powders, facial cleansers, lotions, face creams, face masks, shampoos, conditioners, hair creams, or shampoo powders.
[0046] This application has at least the following beneficial effects:
[0047] This invention utilizes ginsenosides to replace the traditional cholesterol liposome structure, which can: 1) increase the stability and safety of liposomes; 2) enhance the absorption of active ingredients through hair follicles and target and improve the penetration ability of active ingredients into hair follicles; and 3) ginsenosides themselves have active ingredient efficacy, which can improve hair follicle problems by inhibiting 5α-reductase activity, reducing the production of dihydrotestosterone (a major cause of hair loss); promoting the production of vascular endothelial growth factor and dilating blood vessels; increasing alkaline phosphatase activity and promoting the proliferation of dermal papilla cells; and promoting collagen production, anti-inflammatory and soothing effects, and relieving emotional stress. Attached Figure Description
[0048] Figure 1 Transdermal absorption fluorescence image of ginsenoside liposomes loaded with Nile Red (a lipid-soluble active ingredient);
[0049] Figure 2 Transdermal absorption fluorescence image of ginsenoside liposomes loaded with FITC-COL17 (water-soluble active ingredient). Detailed Implementation
[0050] The present invention will now be clearly and completely described in conjunction with embodiments thereof. It should be noted that, unless otherwise specified in the embodiments, conditions are performed under conventional conditions or conditions recommended by the manufacturer. Reagents or instruments whose manufacturers are not specified are all commercially available products. Unless otherwise specified, all parts used in the embodiments of the present invention are parts by weight.
[0051] The ginsenosides used in this embodiment were produced by Hezhimei (Guangzhou) Biotechnology Co., Ltd.
[0052] Example 1
[0053] Soybean lecithin, ginsenosides and Nile Red (NR) were dissolved in ethanol to obtain an oil phase. The oil phase was poured into a round-bottom flask, placed on a rotary evaporator, and the solvent was evaporated under vacuum. The evaporation continued until a uniform lipid film was formed inside the round-bottom flask.
[0054] Water (aqueous phase) was poured into a round-bottom flask to hydrate the lipid film and obtain a lipid dispersion aqueous solution with a final Nile Red concentration of 2.5 μg / mL.
[0055] The obtained lipid dispersion aqueous solution was homogenized under high pressure at 20,000 PSI for 5 cycles to obtain ginsenoside liposomes loaded with Nile Red (it should be noted that the role of Nile Red (lipid-soluble substance) in this application is only to fluorescently label the shell material of ginsenoside liposomes, and has no other substantial functional role).
[0056] The mass ratio of soybean lecithin to ginsenosides is 6:1.
[0057] The range of ginsenoside components in this embodiment is as follows:
[0058] Ginsenoside Rg1 26wt%
[0059] Ginsenoside Re 15wt%
[0060] Ginsenoside Rb1 20wt%
[0061] Ginsenoside Rb2 17wt%
[0062] Ginsenoside Rc 22wt%.
[0063] Example 2
[0064] Basically the same as Example 1, except for the ginsenoside components:
[0065] Ginsenoside Rg1 40wt%
[0066] Ginsenoside Re 60 wt%.
[0067] Example 3
[0068] Basically the same as Example 1, except for the ginsenoside components:
[0069] Ginsenoside Rb1 28wt%
[0070] Ginsenoside Rb2 32wt%
[0071] Ginsenoside Rc 40wt%.
[0072] Example 4
[0073] Basically the same as Example 1, except for the ginsenoside components:
[0074] 20(S)-Ginsenoside Rg2 8-16wt%;
[0075] 20(R)-Ginsenoside Rg2 7-15wt%;
[0076] 20(S)-Ginsenoside Rh1 17-25wt%;
[0077] 20(R)-Ginsenoside Rh1 16-23wt%;
[0078] Ginsenoside Rk3 5-12wt%;
[0079] Ginsenoside Rh4 16-26wt%.
[0080] This embodiment specifically verifies the following combinations, as shown in Table 1;
[0081] Table 1. Ginsenoside Formula Table (Unit: wt%)
[0082] N1 N1-2 N1-3 N1-4 N1-5 20(S)-Ginsenoside Rg2 14 15 8 16 16 20(R)-Ginsenoside Rg2 11 15 15 7 15 20(S)-Ginsenoside Rh1 22 23 19 25 17 20(R)-Ginsenoside Rh1 21 22 23 16 23 Ginsenoside Rk3 10 9 9 12 5 Ginsenoside Rh4 22 16 26 24 24 total 100 100 100 100 100
[0083] In subsequent verification of the present invention, it was found that the performance of groups N1-2 to N1-5 was similar to that of group N1.
[0084] Example 5
[0085] Basically the same as Example 1, except for the ginsenoside components:
[0086] Ginsenoside Rk3 25wt%;
[0087] Ginsenoside Rh4 75wt%.
[0088] Example 6
[0089] Basically the same as Example 1, except for the ginsenoside components:
[0090] 20(S)-Ginsenoside Rg3 15-25wt%;
[0091] 20(R)-Ginsenoside Rg3 35-45wt%;
[0092] Ginsenoside Rg5 9-15wt%;
[0093] 20(S)-Ginsenoside Rh2 4-6wt%;
[0094] 20(R)-Ginsenoside Rh2 10-17wt%;
[0095] Ginsenoside Rk1 5-7wt%.
[0096] This embodiment specifically verified the following combination, as shown in Table 2;
[0097] Table 2. Ginsenoside Formula Table (Unit: wt%)
[0098] N2 N2-2 N2-3 N2-4 N2-5 20(S)-Ginsenoside Rg2 24 25 23 24 15 20(R)-Ginsenoside Rg2 42 35 38 45 45 20(S)-Ginsenoside Rh1 11 10 15 9 12 20(R)-Ginsenoside Rh1 4 6 6 5 5 Ginsenoside Rk3 13 17 13 10 16 Ginsenoside Rh4 6 7 5 7 7 total 100 100 100 100 100
[0099] In subsequent verification of this invention, it was found that the performance of groups N2-2 to N2-5 was similar to that of group N2.
[0100] Example 7
[0101] Basically the same as Example 1, except for the ginsenoside components:
[0102] 20(S)-Ginsenoside Rh2 30wt%;
[0103] 20(R)-Ginsenoside Rh2 37wt%;
[0104] Ginsenoside Rh3 18wt%;
[0105] Ginsenoside Rk1 7wt%;
[0106] Ginsenoside Rk2 8wt%.
[0107] Example 8
[0108] 1. Preparation of ginsenoside liposome shell material:
[0109] Soybean lecithin and ginsenosides were dissolved in ethanol at a mass ratio of 6:1 to obtain an oil phase. The oil phase was poured into a round-bottom flask, placed on a rotary evaporator, and the solvent was evaporated under vacuum. The evaporation continued until a uniform lipid film was formed inside the round-bottom flask.
[0110] Pour water (aqueous phase) into a round-bottom flask to hydrate the lipid film and obtain a lipid dispersion aqueous solution;
[0111] The obtained lipid dispersion aqueous solution was homogenized under high pressure at 20,000 PSI for 5 cycles to obtain blank liposomes (ginsenoside liposome shell material).
[0112] Among them, ginsenoside components:
[0113] Ginsenoside Rg1 26wt%
[0114] Ginsenoside Re 15 wt%
[0115] Ginsenoside Rb1 20wt%
[0116] Ginsenoside Rb2 17wt%
[0117] Ginsenoside Rc 22wt%.
[0118] 2. Preparation of the composition:
[0119] COL17 (type XVII collagen, a water-soluble substance) and blank liposomes were mixed at a mass ratio of 0.01:99.99 in the dark and at 37°C for 4 h to obtain the composition, with a final concentration of COL17 of 100 μg / mL.
[0120] To facilitate subsequent observation of the penetration effect of the active substance, the aforementioned "COL17" is actually "FITC-COL17" that has undergone fluorescent labeling treatment. The specific preparation process of the fluorescently labeled "FITC-COL17" is as follows:
[0121] COL17 (type XVII collagen) was dissolved in sodium bicarbonate buffer solution (pH=9) to obtain the first solution, and FITC was dissolved in dimethyl sulfoxide to obtain the second solution. The first and second solutions were shaken at 4°C in the dark for 12 h at a ratio of COL17:FITC = 50:1 (m / m). Then, the solutions were separated by dextran gel (G25) column chromatography to obtain FITC-COL17.
[0122] Example 9
[0123] This is basically the same as Example 8, except that the ginsenoside components are:
[0124] Ginsenoside Rg1 40wt%
[0125] Ginsenoside Re 60wt%.
[0126] Example 10
[0127] This is basically the same as Example 8, except that the ginsenoside components are:
[0128] Ginsenoside Rb1 28wt%
[0129] Ginsenoside Rb2 32wt%
[0130] Ginsenoside Rc 40wt%.
[0131] Example 11
[0132] This is basically the same as Example 8, except that the ginsenoside components are:
[0133] 20(S)-Ginsenoside Rg2 14wt%;
[0134] 20(R)-Ginsenoside Rg2 11wt%;
[0135] 20(S)-Ginsenoside Rh1 22wt%;
[0136] 20(R)-Ginsenoside Rh1 21wt%;
[0137] Ginsenoside Rk3 10wt%;
[0138] Ginsenoside Rh4 22wt%.
[0139] Example 12
[0140] This is basically the same as Example 8, except that the ginsenoside components are:
[0141] Ginsenoside Rk3 25wt%;
[0142] Ginsenoside Rh4 75wt%.
[0143] Example 13
[0144] This is basically the same as Example 8, except that the ginsenoside components are:
[0145] 20(S)-Ginsenoside Rg3 24wt%;
[0146] 20(R)-Ginsenoside Rg3 42wt%;
[0147] Ginsenoside Rg5 11wt%;
[0148] 20(S)-Ginsenoside Rh2 4wt%;
[0149] 20(R)-Ginsenoside Rh2 13wt%;
[0150] Ginsenoside Rk1 6wt%.
[0151] Example 14
[0152] This is basically the same as Example 8, except that the ginsenoside components are:
[0153] 20(S)-Ginsenoside Rh2 30wt%;
[0154] 20(R)-Ginsenoside Rh2 37wt%;
[0155] Ginsenoside Rh3 18wt%;
[0156] Ginsenoside Rk1 7wt%;
[0157] Ginsenoside Rk2 8wt%.
[0158] Example 15
[0159] This is essentially the same as Example 4, except that a mixture of soy lecithin and hydrogenated soy lecithin is used instead of soy lecithin, and the mass ratio of soy lecithin to hydrogenated soy lecithin is 1:1.
[0160] Example 16
[0161] It is basically the same as Example 4, except that hydrogenated soybean lecithin is used instead of soybean lecithin.
[0162] Example 17
[0163] Soybean lecithin and ginsenosides were dissolved in ethanol to obtain an oil phase. The oil phase was poured into a round-bottom flask, placed on a rotary evaporator, and the solvent was evaporated under vacuum. The evaporation continued until a uniform lipid film was formed inside the round-bottom flask.
[0164] An aqueous solution (aqueous phase) containing copper tripeptide-1 was poured into a round-bottom flask to hydrate the lipid film and obtain a lipid dispersion aqueous solution containing 0.01-0.5 wt% copper tripeptide-1.
[0165] The obtained lipid dispersion aqueous solution was homogenized under high pressure at 20,000 PSI for 5 cycles to obtain ginsenoside liposomes loaded with tripeptide-1 copper.
[0166] The mass ratio of soybean lecithin to ginsenosides is 6:1.
[0167] Among them, ginsenoside components:
[0168] 20(S)-Ginsenoside Rg2 14wt%;
[0169] 20(R)-Ginsenoside Rg2 11wt%;
[0170] 20(S)-Ginsenoside Rh1 22wt%;
[0171] 20(R)-Ginsenoside Rh1 21wt%;
[0172] Ginsenoside Rk3 10wt%;
[0173] Ginsenoside Rh4 22wt%.
[0174] Example 18
[0175] Soybean lecithin and ginsenosides were dissolved in ethanol to obtain an oil phase. The oil phase was poured into a round-bottom flask, placed on a rotary evaporator, and the solvent was evaporated under vacuum. The evaporation continued until a uniform lipid film was formed inside the round-bottom flask.
[0176] An aqueous solution (aqueous phase) containing tetrahydromethylpyrimidine carboxylic acid was poured into a round-bottom flask to hydrate the lipid film and obtain a lipid dispersion aqueous solution containing 0.1-2.0 wt% tetrahydromethylpyrimidine carboxylic acid.
[0177] The obtained lipid dispersion aqueous solution was homogenized under high pressure at 20,000 PSI for 5 cycles to obtain ginsenoside liposomes loaded with tetrahydromethylpyrimidine carboxylic acid.
[0178] The mass ratio of soybean lecithin to ginsenosides is 6:1.
[0179] Among them, ginsenoside components:
[0180] 20(S)-Ginsenoside Rg2 14wt%;
[0181] 20(R)-Ginsenoside Rg2 11wt%;
[0182] 20(S)-Ginsenoside Rh1 22wt%;
[0183] 20(R)-Ginsenoside Rh1 21wt%;
[0184] Ginsenoside Rk3 10wt%;
[0185] Ginsenoside Rh4 22wt%.
[0186] Example 19
[0187] Soybean lecithin, ginsenosides and palmitoyl tetrapeptide-7 (containing 0.02-0.5 wt%) were dissolved in ethanol to obtain an oil phase. The oil phase was poured into a round-bottom flask, placed on a rotary evaporator, and the solvent was evaporated under vacuum. The evaporation continued until a uniform lipid film was formed inside the round-bottom flask.
[0188] Pour water (aqueous phase) into a round-bottom flask to hydrate the lipid film and obtain a lipid dispersion aqueous solution.
[0189] The obtained lipid dispersion aqueous solution was homogenized under high pressure at 20,000 PSI for 5 cycles to obtain ginsenoside liposomes loaded with palmitoyl tetrapeptide-7.
[0190] The mass ratio of soybean lecithin to ginsenosides is 6:1.
[0191] Among them, ginsenoside components:
[0192] 20(S)-Ginsenoside Rg2 14wt%;
[0193] 20(R)-Ginsenoside Rg2 11wt%;
[0194] 20(S)-Ginsenoside Rh1 22wt%;
[0195] 20(R)-Ginsenoside Rh1 21wt%;
[0196] Ginsenoside Rk3 10wt%;
[0197] Ginsenoside Rh4 22wt%.
[0198] Example 20
[0199] Soybean lecithin and ginsenosides were dissolved in ethanol to obtain an oil phase. The oil phase was poured into a round-bottom flask, placed on a rotary evaporator, and the solvent was evaporated under vacuum. The evaporation continued until a uniform lipid film was formed inside the round-bottom flask.
[0200] An aqueous solution (aqueous phase) containing oligopeptide-1 was poured into a round-bottom flask to hydrate the lipid film and obtain a lipid dispersion aqueous solution containing 0.01-0.5 wt% oligopeptide-1.
[0201] The obtained lipid dispersion aqueous solution was homogenized under high pressure at 20,000 PSI for 5 cycles to obtain ginsenoside liposomes loaded with oligopeptide-1.
[0202] The mass ratio of soybean lecithin to ginsenosides is 6:1.
[0203] Among them, ginsenoside components:
[0204] 20(S)-Ginsenoside Rg2 14wt%;
[0205] 20(R)-Ginsenoside Rg2 11wt%;
[0206] 20(S)-Ginsenoside Rh1 22wt%;
[0207] 20(R)-Ginsenoside Rh1 21wt%;
[0208] Ginsenoside Rk3 10wt%;
[0209] Ginsenoside Rh4 22wt%.
[0210] Example 21
[0211] The results are basically the same as those in Examples 8, 17, 18 and 19, except that the ginsenoside liposomes encapsulate type XVII collagen, tripeptide-1 copper, tetrahydromethylpyrimidine carboxylic acid and palmitoyl tetrapeptide-7 in a mass ratio of 1:5:10:2.
[0212] Ginsenoside components:
[0213] Ginsenoside Rg1 26wt%
[0214] Ginsenoside Re 15wt%
[0215] Ginsenoside Rb1 20wt%
[0216] Ginsenoside Rb2 17wt%
[0217] Ginsenoside Rc 22wt%.
[0218] Example 22
[0219] It is basically the same as Example 21, except that,
[0220] Ginsenoside components:
[0221] Ginsenoside Rg1 40wt%
[0222] Ginsenoside Re 60wt%.
[0223] Example 23
[0224] This is essentially the same as Example 21, except for the ginsenoside components:
[0225] Ginsenoside Rb1 28wt%
[0226] Ginsenoside Rb2 32wt%
[0227] Ginsenoside Rc 40wt%.
[0228] Example 24
[0229] This is essentially the same as Example 21, except for the ginsenoside components:
[0230] 20(S)-Ginsenoside Rg2 14wt%;
[0231] 20(R)-Ginsenoside Rg2 11wt%;
[0232] 20(S)-Ginsenoside Rh1 22wt%;
[0233] 20(R)-Ginsenoside Rh1 21wt%;
[0234] Ginsenoside Rk3 10wt%;
[0235] Ginsenoside Rh4 22wt%.
[0236] Example 25
[0237] This is essentially the same as Example 21, except for the ginsenoside components:
[0238] Ginsenoside Rk3 25wt%;
[0239] Ginsenoside Rh4 75wt%.
[0240] Example 26
[0241] This is essentially the same as Example 21, except for the ginsenoside components:
[0242] 20(S)-Ginsenoside Rg3 25wt%;
[0243] 20(R)-Ginsenoside Rg3 42wt%;
[0244] Ginsenoside Rg5 9wt%;
[0245] 20(S)-Ginsenoside Rh2 4wt%;
[0246] 20(R)-Ginsenoside Rh2 13wt%;
[0247] Ginsenoside Rk1 7wt%.
[0248] Example 27
[0249] This is essentially the same as Example 21, except for the ginsenoside components:
[0250] 20(S)-Ginsenoside Rh2 30wt%;
[0251] 20(R)-Ginsenoside Rh2 37wt%;
[0252] Ginsenoside Rh3 18wt%;
[0253] Ginsenoside Rk1 7wt%;
[0254] Ginsenoside Rk2 8wt%.
[0255] Example 28
[0256] Soybean lecithin and ginsenosides were dissolved in ethanol to obtain an oil phase. The oil phase was poured into a round-bottom flask, placed on a rotary evaporator, and the solvent was evaporated under vacuum. The evaporation continued until a uniform lipid film was formed inside the round-bottom flask.
[0257] Water (aqueous phase) is poured into a round-bottom flask to hydrate the lipid film and obtain a lipid dispersion aqueous solution.
[0258] The obtained lipid dispersion aqueous solution was homogenized under high pressure at 20,000 PSI for 5 cycles to obtain ginsenoside liposomes.
[0259] The mass ratio of soybean lecithin to ginsenosides is 6:1.
[0260] Among them, ginsenoside components:
[0261] 20(S)-Ginsenoside Rg2 14wt%;
[0262] 20(R)-Ginsenoside Rg2 11wt%;
[0263] 20(S)-Ginsenoside Rh1 22wt%;
[0264] 20(R)-Ginsenoside Rh1 21wt%;
[0265] Ginsenoside Rk3 10wt%;
[0266] Ginsenoside Rh4 22wt%.
[0267] Example 29
[0268] This is essentially the same as Example 28, except for the ginsenoside components:
[0269] 20(S)-Ginsenoside Rg3 24wt%;
[0270] 20(R)-Ginsenoside Rg3 42wt%;
[0271] Ginsenoside Rg5 11wt%;
[0272] 20(S)-Ginsenoside Rh2 4wt%;
[0273] 20(R)-Ginsenoside Rh2 13wt%;
[0274] Ginsenoside Rk1 6wt%.
[0275] Comparative Example 1
[0276] Dissolve Nile Red in water to a final concentration of 2.5 μg / mL.
[0277] Comparative Example 2
[0278] COL17 collagen was dissolved in sodium bicarbonate buffer (pH=9), and FITC was dissolved in dimethyl sulfoxide. The protein was labeled with a COL17:FITC ratio of 50:1 (m / m). The mixture was shaken at 4°C in the dark for 12 h, and then separated by dextran gel (G25) column chromatography to obtain FITC-COL17 with a final concentration of 100 μg / mL.
[0279] Comparative Example 3
[0280] Soybean lecithin, ginsenosides, cholesterol, and Nile red were dissolved in ethanol to obtain an oil phase. The oil phase was poured into a round-bottom flask, placed on a rotary evaporator, and the solvent was evaporated under vacuum. The evaporation continued until a uniform lipid film was formed inside the round-bottom flask.
[0281] Water (aqueous phase) was poured into a round-bottom flask to hydrate the lipid film and obtain a lipid dispersion aqueous solution. The final concentration of Nile Red in the liposomes was 2.5 μg / mL.
[0282] The obtained lipid dispersion aqueous solution was homogenized under high pressure at 20,000 PSI for 5 cycles to obtain liposomes.
[0283] The mass ratio of lecithin, ginsenosides, and cholesterol is 12:1:2.
[0284] Among them, ginsenoside components:
[0285] 20(S)-Ginsenoside Rg2 14wt%;
[0286] 20(R)-Ginsenoside Rg2 11wt%;
[0287] 20(S)-Ginsenoside Rh1 22wt%;
[0288] 20(R)-Ginsenoside Rh1 21wt%;
[0289] Ginsenoside Rk3 10wt%;
[0290] Ginsenoside Rh4 22wt%.
[0291] Comparative Example 4
[0292] 1. Shell material preparation:
[0293] Soybean lecithin, ginsenosides and cholesterol were dissolved in ethanol to obtain an oil phase. The oil phase was poured into a round-bottom flask, placed on a rotary evaporator, and the solvent was evaporated under vacuum. The evaporation continued until a uniform lipid film was formed inside the round-bottom flask.
[0294] Pour water (aqueous phase) into a round-bottom flask to hydrate the lipid film and obtain a lipid dispersion aqueous solution;
[0295] The obtained lipid dispersion aqueous solution was homogenized under high pressure at 20,000 PSI for 5 cycles to obtain the shell material (blank liposome).
[0296] The mass ratio of lecithin, ginsenosides, and cholesterol is 12:1:2.
[0297] Among them, ginsenoside components:
[0298] 20(S)-Ginsenoside Rg2 14wt%;
[0299] 20(R)-Ginsenoside Rg2 11wt%;
[0300] 20(S)-Ginsenoside Rh1 22wt%;
[0301] 20(R)-Ginsenoside Rh1 21wt%;
[0302] Ginsenoside Rk3 10wt%;
[0303] Ginsenoside Rh4 22wt%.
[0304] 2. Preparation of the composition:
[0305] COL17 (type XVII collagen, a water-soluble substance) and blank liposomes were mixed at a mass ratio of 0.01:99.99 in the dark and at 37°C for 4 h to obtain the composition, with a final concentration of COL17 of 100 μg / mL.
[0306] To facilitate subsequent observation of the penetration effect of the active substance, the aforementioned "COL17" is actually "FITC-COL17" that has undergone fluorescent labeling treatment. The specific preparation process of the fluorescently labeled "FITC-COL17" is as follows:
[0307] COL17 (type XVII collagen) was dissolved in sodium bicarbonate buffer solution (pH=9) to obtain the first solution, and FITC was dissolved in dimethyl sulfoxide to obtain the second solution. The first and second solutions were shaken at 4°C in the dark for 12 h at a ratio of COL17:FITC = 50:1 (m / m). Then, the solutions were separated by dextran gel (G25) column chromatography to obtain FITC-COL17.
[0308] Comparative Example 5
[0309] This is essentially the same as Example 17, except that cholesterol is used to partially replace ginsenosides, wherein the mass ratio of lecithin: ginsenosides: cholesterol is 12:1:2.
[0310] Comparative Example 6
[0311] This is essentially the same as Example 18, except that cholesterol is used to partially replace ginsenosides, wherein the mass ratio of lecithin: ginsenosides: cholesterol is 12:1:2.
[0312] Comparative Example 7
[0313] This is essentially the same as Example 19, except that cholesterol is used to partially replace ginsenosides, wherein the mass ratio of lecithin: ginsenosides: cholesterol is 12:1:2.
[0314] Comparative Example 8
[0315] This is essentially the same as Example 20, except that cholesterol is used to partially replace ginsenosides, wherein the mass ratio of lecithin: ginsenosides: cholesterol is 12:1:2.
[0316] Test case
[0317] 1. Fluorescent transdermal assay to evaluate the transdermal absorption (hair follicle targeted penetration) of the ginsenoside liposomes of the present invention.
[0318] 1.1 In vitro transdermal diffusion test
[0319] Add receiving fluid (0.9% saline) and a magnetic stir bar to the receiving chamber of the Franz diffusion cell. Cut a piece of pig skin of appropriate size (pig skin is most similar to human skin, including similar stratum corneum, epidermal thickness and hair follicle density, etc.) and fix it between the receiving chamber and the supply chamber of the Franz diffusion cell (stratum corneum facing up, towards the supply chamber). Add receiving fluid until the skin is in close contact with the receiving fluid.
[0320] Place the diffusion cell into the transdermal device, and place 1 mL of test sample (Examples 1-14, Comparative Examples 1-4, and blank (0.9% saline)) in the supply chamber (operate in the dark). Turn on the transdermal device, set the rotation speed to 350 rpm, and maintain the temperature in a constant temperature water bath of (32 ± 1) °C for 24 h of in vitro diffusion.
[0321] 1.2 Frozen sections
[0322] Embedded tissue blocks: Immediately embed the removed skin with OTC embedding agent, place the mold containing the tissue into liquid nitrogen, and remove it when the OCT gel completely turns into a white solid; store it in a -80°C freezer for later use.
[0323] Sectioning: The skin tissue was longitudinally sectioned into 16 μm thick sections using a cryostat.
[0324] Fixation and sectioning: Sections were fixed with acetone, then washed with PBS buffer to remove OCT gel, and stored in a 4°C refrigerator for later use.
[0325] 1.3 Detection and photography
[0326] Mounting and DAPI staining (4',6-diamidinyl-2-phenylindole, a nuclear fluorescent dye used for cell localization, blue fluorescence): Add 1-2 drops of anti-fluorescence quencher (containing DAPI) to the tissue and cover with a coverslip.
[0327] Photography: Observe and photograph the fluorescence image of the longitudinal section of the skin using a fluorescence microscope, take photos, and observe and compare the differences in fluorescence intensity between different groups.
[0328] Experimental results are as follows Figure 1 and Figure 2 .
[0329] like Figure 1As shown, the free Nile Red group (Comparative Example 1) exhibited weak red fluorescence and sparse distribution in deep skin tissue, indicating that Nile Red (a lipid-soluble active ingredient) largely failed to penetrate the stratum corneum barrier. The ginsenoside liposome groups (Examples 1-7) showed stronger red fluorescence than the free Nile Red group (Comparative Example 1), indicating that ginsenoside liposomes can promote skin penetration of lipid-soluble active ingredients. In particular, Ginsenoside liposome Example 4 (composed of ginsenosides Rg2, Rh1, Rh4, and Rk3) and Ginsenoside liposome Example 6 (composed of ginsenosides Rg3, Rg5, Rh2, and Rk1) showed the strongest red fluorescence and deep skin penetration, indicating that the ginsenoside liposomes composed of these two ginsenoside compositions have the strongest skin penetration ability. Compared to liposomes prepared by partially replacing ginsenosides with cholesterol (Comparative Example 3), the ginsenoside liposome group (Example 4) exhibited stronger fluorescence in deep skin tissue and aggregated in hair follicles, indicating that the ginsenoside liposomes' ability to target and penetrate hair follicles was significantly superior to that of ordinary cholesterol liposomes. The ginsenoside liposomes prepared in Examples 15 and 16 showed little difference in appearance and particle size, and their fluorescence penetration intensity was similar. Soybean lecithin and / or hydrogenated soybean lecithin can be used to prepare these liposomes.
[0330] like Figure 2 As shown, a small amount of free macromolecular type XVII collagen (Comparative Example 2, water-soluble active ingredient) enters the skin tissue through skin appendages (hair follicles). The ginsenoside liposome group (Examples 2-14) exhibits stronger green fluorescence than the free protein group (Comparative Example 2), indicating that ginsenoside liposomes can promote the skin penetration of water-soluble active ingredients. In particular, ginsenoside liposomes Example 11 (composed of ginsenosides Rg2, Rh1, Rh4, and Rk3) and Example 13 (composed of ginsenosides Rg3, Rg5, Rh2, and Rk1) show the strongest green fluorescence and a wider fluorescence distribution area in the deep skin tissue, indicating that the ginsenoside liposomes composed of these two ginsenoside compositions have the strongest skin penetration ability. Compared with liposomes prepared by partially replacing ginsenosides with cholesterol (Comparative Example 4), the ginsenoside liposome group (Example 4) showed a wider fluorescence distribution area and stronger fluorescence intensity in the deep skin tissue, and accumulated in the hair follicles. This indicates that ginsenoside liposomes can significantly enhance the transdermal absorption of active ingredients and can target hair follicles for penetration and accumulation. Its penetration ability is significantly better than that of ordinary cholesterol liposomes.
[0331] To further verify whether the ginsenoside combinations shown in Example 4 and Example 6 can exhibit consistent effects within a suitable ratio range, the present invention further adjusted the ginsenoside combinations shown in Examples 4 and 6, referring to the following formulations 1 to 4; the Nile red penetration effect of formulations 1 and 2 is similar to that of Example 4; the Nile red penetration effect of formulations 3 and 4 is similar to that of Example 6; specifically, the formulation information of formulations 1 to 4 is as follows:
[0332] Formula 1: 20(S)-Ginsenoside Rg2 9wt%; 20(R)-Ginsenoside Rg2 15wt%; 20(S)-Ginsenoside Rh1 19wt%; 20(R)-Ginsenoside Rh1 23wt%; Ginsenoside Rk3 8wt%; Ginsenoside Rh4 26wt%;
[0333] Formula 2: 20(S)-Ginsenoside Rg2 16wt%; 20(R)-Ginsenoside Rg2 10wt%; 20(S)-Ginsenoside Rh1 25wt%; 20(R)-Ginsenoside Rh1 18wt%; Ginsenoside Rk3 12wt%; Ginsenoside Rh4 19wt%;
[0334] Formula 3: 20(S)-Ginsenoside Rg3 18wt%; 20(R)-Ginsenoside Rg3 45wt%; Ginsenoside Rg5 11wt%; 20(S)-Ginsenoside Rh2 6wt%; 20(R)-Ginsenoside Rh2 13wt%; Ginsenoside Rk1 7wt%;
[0335] Formula 4: 20(S)-Ginsenoside Rg3 24wt%; 20(R)-Ginsenoside Rg3 35wt%; Ginsenoside Rg5 15wt%; 20(S)-Ginsenoside Rh2 4wt%; 20(R)-Ginsenoside Rh2 17wt%; Ginsenoside Rk 15wt%;
[0336] The above results indicate that ginsenoside liposomes can significantly enhance the transdermal absorption of water-soluble / lipid-soluble active ingredients and can target hair follicles for penetration and accumulation. Their permeability is significantly better than that of free active ingredients and ordinary cholesterol liposomes.
[0337] There are many causes of hair loss, and the effect of using a single active ingredient alone is limited. Ginsenoside liposomes can simultaneously encapsulate both water-soluble and fat-soluble active ingredients. Encapsulation can improve the stability of the active ingredients and enhance their transdermal absorption. Furthermore, ginsenosides themselves have good hair growth induction and anti-inflammatory and soothing abilities. The synergistic effect of multiple active ingredients and ginsenosides, targeting and penetrating hair follicles, shows good application prospects in the treatment of hair loss, acne, folliculitis, and other hair follicle-related diseases.
[0338] 2. Transdermal assay to evaluate the transdermal absorption of the ginsenoside liposomes of the present invention.
[0339] Add receiving fluid (0.9% saline) and a magnetic stir bar to the receiving chamber of the Franz diffusion cell. Cut a piece of detached pigskin of appropriate size and fix it between the receiving chamber and the supply chamber of the Franz diffusion cell (with the stratum corneum facing upwards and towards the supply chamber). Add receiving fluid until the skin is in close contact with the receiving fluid.
[0340] The diffusion cell was placed in the transdermal transdermal analyzer, and 1 mL of test sample (Examples 17-20, Comparative Examples 5-8) was placed in the supply chamber. The transdermal analyzer was turned on, the rotation speed was set to 350 rpm, and the temperature was maintained at (32 ± 1) °C in a constant temperature water bath. After 24 h of in vitro diffusion, the receiving liquid was collected, and the permeability of the active ingredient was determined by high performance liquid chromatography. The transdermal absorption effects of ginsenoside liposomes and cholesterol liposomes were compared. The results are shown in Table 3.
[0341] Table 3 Transmittance Test Results
[0342] Group Transmittance (%) Group Transmittance (%) Example 17 65.59 Comparative Example 5 33.52 Example 18 64.59 Comparative Example 6 45.44 Example 19 41.37 Comparative Example 7 32.21 Example 20 58.11 Comparative Example 8 30.44
[0343] The above results indicate that ginsenoside liposomes have significantly better permeability than ordinary cholesterol liposomes.
[0344] 3. Hair loss counting test
[0345] The ginsenoside liposomes prepared in Examples 21-29 were added to a regular serum (formulas are shown in Table 4) to make a scalp serum. The ginsenoside liposomes prepared in Examples 21-29 were the only active ingredient, while the others were auxiliary raw materials and preservatives without anti-hair loss function.
[0346] Table 4 Formula Table
[0347]
[0348] Process:
[0349] Add water to a pot, slowly sprinkle in carbomer, start stirring, and heat to 85°C;
[0350] Pour the water pot into the main pot, add the premixed mixture of butylene glycol and sodium hyaluronate, maintain 85°C, and stir until well mixed;
[0351] Cool to 60℃, add the aqueous solution of phase B, and stir until homogeneous;
[0352] Cool to 40℃, add the premixed solution of phase C, stir until homogeneous, then add phase D sequentially and stir until homogeneous.
[0353] Material sampling and testing showed a pH of 5.5-6.5, indicating that the material was qualified for discharge.
[0354] Physicochemical properties:
[0355] Appearance: Transparent, serum-like liquid;
[0356] pH: 5.5-6.5.
[0357] Ten subjects were selected, and the number of hair loss cases (using the 60-times combing method) was recorded before use (D0), on day 28 (D28), on day 56 (D56), and on day 84 (D84). The results are shown in Tables 5 and 6.
[0358] Table 5. Statistics on Hair Loss
[0359]
[0360] Table 6. Statistics on Hair Loss Rate
[0361]
[0362] The above tests show that the hair loss count decreased after the subjects used the scalp serum, indicating that ginsenosides themselves have good anti-hair loss effects (as in Examples 28 and 29). Furthermore, with prolonged use, the subjects' hair condition significantly improved, especially in Examples 24 (ginsenoside liposomes composed of ginsenosides Rg2, Rh1, Rh4, and Rk3) and 26 (ginsenoside liposomes composed of ginsenosides Rg3, Rg5, Rh2, and Rk1), where the hair loss count showed the greatest change rate. This indicates that ginsenoside liposomes composed of specific ginsenoside compositions have the strongest skin penetration ability. Ginsenosides can synergistically enhance the effects of various active ingredients, targeting hair follicles for penetration, and have promising application prospects in treating hair loss, acne, folliculitis, and other hair follicle-related diseases.
Claims
1. The use of liposomes in the preparation of cosmetics, wherein the cosmetics act on hair follicles and are used to promote the penetration of active ingredients into the hair follicles; The liposomes include a liposome shell and contents, the contents of which include cosmetic active ingredients; The shell material is made of phospholipids and ginsenosides; the mass ratio of phospholipids to ginsenosides is 1-10:1-5; The ginsenosides mentioned are: Combination 4: 20(S)-ginsenoside Rg2 8-16wt%; 20(R)-ginsenoside Rg2 7-15wt%; 20(S)-ginsenoside Rh1 17-25wt%; 20(R)-ginsenoside Rh1 16-23wt%; ginsenoside Rk3 5-12wt%; ginsenoside Rh4 16-26wt%; The sum of the weight percentages of each ginsenoside in the above combination is 100%.
2. The use according to claim 1, characterized in that, The phospholipids are one or more combinations of soybean lecithin, egg yolk lecithin, cephalin, hydrogenated lecithin, dipalmitoylphosphatidylcholine, dipalmitoylphosphatidylethanolamine, distearate phosphatidylcholine, myristoylphosphatidylcholine, and sphingomyelin.
3. The use according to claim 1, characterized in that, The contents account for 0.0001% to 90% of the total weight of the liposomes.
4. The use according to claim 3, characterized in that, The active ingredients in the cosmetics are oligopeptide-1, tripeptide-1 copper, palmitoyl tetrapeptide-7, type XVII collagen, type III collagen, type I collagen, soluble collagen, fibronectin, arborvitae leaf extract, ginger root extract, Polygonum multiflorum root extract, Angelica sinensis root extract, tetrahydromethylpyrimidine carboxylic acid, ergothioneine, hydroxypropyl tetrahydropyranotriol, adenosine, biotin, caffeine, dipotassium glycyrrhizate, diaminopyrimidine oxide, and zinc PCA.
Citation Information
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