CN109431829B - Hydroxyasiaticoside liposome and preparation method and application thereof - Google Patents

Hydroxyasiaticoside liposome and preparation method and application thereof Download PDF

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CN109431829B
CN109431829B CN201811540375.1A CN201811540375A CN109431829B CN 109431829 B CN109431829 B CN 109431829B CN 201811540375 A CN201811540375 A CN 201811540375A CN 109431829 B CN109431829 B CN 109431829B
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madecassoside
liposome
collagen
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skin
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CN109431829A (en
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胡克
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Guangzhou Chenxi Chemical Co ltd
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/02Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/14Liposomes; Vesicles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34Alcohols
    • A61K8/345Alcohols containing more than one hydroxy group
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/40Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
    • A61K8/42Amides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/55Phosphorus compounds
    • A61K8/553Phospholipids, e.g. lecithin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/63Steroids; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/64Proteins; Peptides; Derivatives or degradation products thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/64Proteins; Peptides; Derivatives or degradation products thereof
    • A61K8/65Collagen; Gelatin; Keratin; Derivatives or degradation products thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/92Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
    • A61K8/922Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of vegetable origin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783Angiosperms [Magnoliophyta]
    • A61K8/9789Magnoliopsida [dicotyledons]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/02Preparations for care of the skin for chemically bleaching or whitening the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/08Anti-ageing preparations

Abstract

The invention relates to a madecassoside liposome and a preparation method and application thereof, wherein the madecassoside liposome comprises, by mass, 0.1-8.0% of madecassoside, 3.0-10.0% of phospholipid, 0.5-5.0% of cholesterol, 0.05-1.0% of ceramide, 0.5-2.0% of plant essential oil, 10.0-25.0% of polyalcohol, 0.5-2.0% of antioxidant, 0.5-5.0% of collagen, 0.1-1.0% of fibroblast growth factor, 0.5-2.0% of honeysuckle extract and the balance of water. The madecassoside liposome prepared by the invention can promote the madecassoside to permeate into the skin and has long-acting effect, and the components can play a synergistic effect, promote the regeneration of fibroblasts, condition the skin, increase the elasticity and moisture of the skin, remove free radicals, supplement collagen, achieve the regeneration of cells, increase the elasticity of the skin and remove striae gravidarum.

Description

Hydroxyasiaticoside liposome and preparation method and application thereof
Technical Field
The invention belongs to the technical field of cosmeceutics, and particularly relates to a madecassoside liposome, and a preparation method and application thereof.
Background
The striae gravidarum is mainly formed by that the striae gravidarum is influenced by hormone in the gestation period, the elastic fibers and the collagen fibers of the skin are damaged or broken to different degrees due to the expansion of the abdomen, the skin becomes thin and thin, and pink or purple wave stripes with different widths and different lengths appear on the skin of the abdominal wall; after delivery, these streaks gradually disappear, leaving white or silvery-white shiny scar lines, i.e. stretch marks.
A common method for eliminating stretch marks includes: the skin changing method comprises the following steps: by using the chemical stripping agent, adverse reactions are easily caused, so that the cuticle is thinned and the skin is sensitive; ② essential oil aromatherapy: the method has long treatment course, high requirement on aromatherapy workers and unobvious effect; ③ laser therapy: the method is not suitable for large-area treatment and is easy to cause skin sensitivity; grinding method: the physical grinding process is painful and can easily cause skin damage.
The prior products for removing pregnancy on the market have single effect and cannot realize multiple synergistic effects, and the application effect is influenced because the products are difficult to reach the dermis of the skin. The madecassoside has the functions of scar repair, antibiosis, anti-inflammation and fibroblast regeneration promotion, but has poor external treatment effect because the madecassoside belongs to polar macromolecules and is difficult to permeate through the skin.
Disclosure of Invention
Aiming at the defects of the prior art, the invention provides the madecassoside liposome and the preparation method and the application thereof, the prepared madecassoside liposome has reasonable components, can effectively promote active ingredients to penetrate through the skin cuticle to enter the deep tissue of the skin, and plays a synergistic role; meanwhile, the liposome has the advantages of large drug-loading rate, good stability and high safety, and the preparation method is simple and easy to control.
In order to achieve the above object, the present invention provides the following technical solutions:
a madecassoside liposome comprises the following components by mass percent: 0.1 to 8.0 percent of madecassoside, 3.0 to 10.0 percent of phospholipid, 0.5 to 5.0 percent of cholesterol, 0.05 to 1.0 percent of ceramide, 0.5 to 2.0 percent of plant essential oil, 10.0 to 25.0 percent of polyalcohol, 0.5 to 2.0 percent of antioxidant, 0.5 to 5.0 percent of collagen, 0.1 to 1.0 percent of fibroblast growth factor and the balance of water; the particle size of the madecassoside liposome is 100-190 nm.
Preferably, the madecassoside liposome also comprises 0.5-2.0 wt% of honeysuckle extract, the honeysuckle extract is calculated by the medicinal materials, the honeysuckle extract is extracted by drying honeysuckle, pulverizing, extracting with 75-80% ethanol, and drying the extract to obtain an extract. The flos Lonicerae extract is flavone extract of flos Lonicerae, and its main ingredient is flavone.
The honeysuckle activity becomes a flavonoid compound, mainly containing luteolin, glucoside, hyperin and the like, and researches show that the flavonoid compound has good effects of scavenging free radicals, resisting inflammation and the like. However, the research result of the invention shows that the honeysuckle extract prepared by the invention can promote the transdermal penetration of the active ingredient madecassoside in the madecassoside liposome; meanwhile, the honeysuckle extract and the fibroblast growth factor act on synthesis of fibroblasts and collagen cells together, the fibroblast growth factor promotes synthesis of the fibroblasts and the collagen cells, the honeysuckle extract effectively controls proliferation of the fibroblasts and collagen metabolism, and is used for cooperating with repair of striae gravidarum of madecassoside to achieve the effect of repairing without scars, and scars caused by disordered accumulation of collagen due to excessive proliferation of the fibroblasts are avoided.
Preferably, the phospholipid is one or more of soybean lecithin, egg yolk lecithin, hydrogenated lecithin, hydroxylated lecithin, phosphatidylcholine and phosphatidyldiethanolamine.
Preferably, the ceramide is one or a mixture of more of ceramide I, ceramide II and ceramide IIIA.
Preferably, the plant essential oil is a mixture of two or more of carrot seed oil, rose essential oil, olive oil and shea butter. The plant essential oil is a mixture of carrot seed oil, rose essential oil, olive oil and shea butter, and the carrot seed oil can strengthen red blood cells, improve skin color, fade spots and enable skin to be firmer and more elastic; the rose essential oil can promote cell metabolism and cell regeneration function and strengthen the discharge of cytotoxin; the olive oil is rich in monounsaturated fatty acids such as squalene, vitamin E, K, A, D and phenolic antioxidant substances, and can eliminate facial wrinkles and prevent skin aging; the avocado oil is high-antioxidant oil, can better permeate the skin to perform deep skin injury nursing, has a certain antibacterial effect, and has a certain effect of resisting interference of bacteria on cell repair. The mixture of carrot seed oil, rose essential oil, olive oil and shea butter oil is used for improving the repair of the striae gravidarum in multiple effects.
Preferably, the polyhydric alcohol is one or a mixture of more of 1, 3-butanediol, propylene glycol, 1, 2-pentanediol and 1, 2-hexanediol.
Preferably, the antioxidant is one or more of quercetin, alpha-tocopherol and astaxanthin. Quercetin is a flavonoid substance, has antioxidant and antiinflammatory effects, and can enhance the effect of madecassoside together with flos Lonicerae extract.
Preferably, the collagen is a mixture of two or more of deep sea cod skin collagen, coconut collagen and silk collagen. Based on the pathological and physiological characteristics of stretch marks, the prevention and reduction of stretch marks requires the use of targeting dermal fibroblasts, which can play a role in activating cell proliferation and stimulating metabolism, in particular increasing the content of elastic fibers and collagen in the skin. The collagen has the specific skin repairing and regenerating effects, and can stimulate the generation of new collagen, support skin cells, and play the roles of moisturizing and inhibiting wrinkles. The collagen is supplemented by using a mixture of deep sea cod skin collagen, coconut collagen and silk collagen. After the deep sea cod skin collagen, the coconut collagen and the silk collagen are prepared into the nano liposome, the skin can effectively permeate through the epidermis, and necessary collagen is provided for repairing striae gravidarum.
The invention provides a preparation method of madecassoside liposome in the technical scheme, which comprises the following steps:
(1) preparing an oil phase, namely melting phospholipid, cholesterol and ceramide at the water bath temperature of 65-80 ℃, adding an antioxidant, and uniformly mixing for later use;
(2) preparing an aqueous phase: adding madecassoside, polyalcohol and collagen into purified water according to the formula amount, stirring and heating to 65-80 ℃ to dissolve the madecassoside, the collagen and the polyalcohol for later use;
(3) preparing colostrum: dropwise adding the oil phase prepared in the step (1) into the water phase prepared in the step (2), continuously stirring, and performing high-speed shearing emulsification at 10000 rpm for 2 min to obtain primary emulsion;
(4) preparing liposome: preserving the temperature of the primary emulsion prepared in the step (3) at 70 ℃, treating the primary emulsion by high-pressure homogenizing equipment, wherein the pressure is 500-1500 bar, the cycle time is 2-8 times, and cooling to 50 ℃;
(5) adding plant essential oil, fibroblast growth factor and flos Lonicerae extract into (4), stirring at 800 bar, homogenizing under high pressure for 1 time, and cooling to obtain madecassoside liposome.
Application of madecassoside liposome in cosmeceutical and skin care product for preventing and treating striae gravidarum is provided. The madecassoside liposome can be used directly, or added into various skin care products with effects such as cream, lotion, essence, gel, etc.
The invention has the beneficial effects that:
1. active ingredients with different effects such as madecassoside and the like are conveyed to the deep layer of the skin by adopting a novel conveying system of liposome, the average particle size is 100-190 nm, the particle size can ensure that the active ingredients can penetrate through the horny layer and can also ensure that the active ingredients are retained in the skin, the accumulated permeation amount and the retention amount of the madecassoside are improved, the active ingredients are continuously released, the effective concentration is maintained for a long time, and the skin care effect is better exerted.
2. The madecassoside liposome prepared by the invention has the advantages that the functions of all active ingredients are complemented and the synergistic effect is exerted, and the madecassoside has the functions of promoting the regeneration of fibroblasts, inhibiting inflammatory reaction, accelerating wound healing and the like; the plant essential oil has the effects of conditioning skin, increasing skin elasticity and keeping skin moisture; the antioxidant has effects of scavenging free radicals and delaying aging; the collagen has the functions of supplementing the collagen content of the skin, increasing the skin elasticity and the like.
3. The honeysuckle extract can promote the transdermal penetration of an active ingredient of madecassoside liposome, and simultaneously acts on the synthesis of fibroblasts and collagen cells together with fibroblast growth factors, so that the proliferation of the fibroblasts and the collagen metabolism are effectively controlled, the repair of striae gravidarum of the madecassoside is cooperated, the effect of repairing without scars is achieved, and the excessive proliferation of the fibroblasts is avoided.
4. The mixture of the carrot seed oil, the rose essential oil, the olive oil and the shea butter oil has multiple effects of improving the repair of striae gravidarum, promoting cell metabolism and cell regeneration, and enabling the skin to be firmer and more elastic; can improve skin color and lighten speckles; can eliminate facial wrinkles and prevent skin aging; can resist bacteria, enhance skin penetration, reduce interference, and care deep skin.
Drawings
FIG. 1 is the cumulative permeation of in vitro transdermal experiments for examples 4, 6-8 and comparative example 1.
FIG. 2 is a graph showing the 12h retention of the in vitro transdermal experiments of examples 4, 6 to 8 and comparative example 1.
Detailed Description
The madecassoside liposome provided by the invention comprises the following components in percentage by mass: 0.1 to 8.0 percent of madecassoside, 3.0 to 10.0 percent of phospholipid, 0.5 to 5.0 percent of cholesterol, 0.05 to 1.0 percent of ceramide, 0.5 to 2.0 percent of plant essential oil, 10.0 to 25.0 percent of polyalcohol, 0.5 to 2.0 percent of antioxidant, 0.5 to 5.0 percent of collagen, 0.1 to 1.0 percent of fibroblast growth factor, 0.5 to 2.0 percent of honeysuckle extract and the balance of water.
The invention provides a preparation method of the madecassoside liposome, which comprises the following steps:
(1) preparing an oil phase, namely melting phospholipid, cholesterol and ceramide at the water bath temperature of 65-80 ℃, adding an antioxidant, and uniformly mixing for later use;
(2) preparing an aqueous phase: adding madecassoside, polyalcohol and collagen into purified water according to the formula amount, stirring and heating to 65-80 ℃ to dissolve the madecassoside, the collagen and the polyalcohol for later use;
(3) preparing colostrum: dropwise adding the oil phase prepared in the step (1) into the water phase prepared in the step (2), continuously stirring, and performing high-speed shearing emulsification at 10000 rpm for 2 min to obtain primary emulsion;
(4) preparing liposome: preserving the temperature of the primary emulsion prepared in the step (3) at 70 ℃, treating the primary emulsion by high-pressure homogenizing equipment, wherein the pressure is 500-1500 bar, the cycle time is 2-8 times, and cooling to 50 ℃;
(5) adding plant essential oil, fibroblast growth factor and flos Lonicerae extract into (4), stirring at 800 bar, homogenizing under high pressure for 1 time, and cooling to obtain madecassoside liposome.
In the invention, the preparation process of the oil phase and the water phase dissolution is not limited in sequence.
The present invention is further described by way of examples to provide the skilled person with a better understanding of the present invention, and the preferred embodiments of the present invention are to be considered as illustrative only and not limiting the present invention in any way.
Example 1
(1) Preparing an oil phase, namely melting 3.0% of soybean phospholipid, 0.5% of cholesterol and 0.05% of ceramide I at the water bath temperature of 65-80 ℃, adding 2.0% of alpha-tocopherol, and uniformly mixing for later use;
(2) preparing an aqueous phase: adding 0.1% of madecassoside, 10.0% of propylene glycol, 0.2% of deep sea cod skin collagen and 0.3% of coconut collagen into 82.25% of purified water, stirring and heating to 65-80 ℃ for dissolving for later use;
(3) preparing colostrum: dropwise adding the oil phase prepared in the step (1) into the water phase prepared in the step (2), continuously stirring, and performing high-speed shearing emulsification at 10000 rpm for 2 min to obtain primary emulsion;
(4) preparing liposome: preserving the temperature of the primary emulsion prepared in the step (3) at 70 ℃, treating the primary emulsion by high-pressure homogenizing equipment, wherein the pressure is 500 bar, the cycle time is 3 times, and cooling to 50 ℃;
(5) adding 0.4% of rose essential oil, 0.1% of butyrospermum parkii oil, 0.1% of fibroblast growth factor and 1.0% of honeysuckle extract into the mixture in the step (4), stirring uniformly at 800 bar, homogenizing for 1 time under high pressure, and cooling to obtain the madecassoside liposome. The madecassoside liposome has a particle size of 115.6 nm and an entrapment rate of 95.7%.
Example 2
(1) Preparing an oil phase, namely melting 1.0% of phosphatidylcholine, 2.0% of egg yolk lecithin, 5% of cholesterol and 0.1% of ceramide II at the water bath temperature of 65-80 ℃, and then adding 1.5% of alpha-tocopherol to mix uniformly for later use;
(2) preparing an aqueous phase: adding 5% of madecassoside, 10.0% of propylene glycol, 5.0% of 1, 3-butanediol, 0.5% of deep sea cod skin collagen and 0.5% of coconut collagen into 68.3% of purified water, stirring and heating to 65-80 ℃ for dissolving for later use;
(3) preparing colostrum: dropwise adding the oil phase prepared in the step (1) into the water phase prepared in the step (2), continuously stirring, and performing high-speed shearing emulsification at 10000 rpm for 2 min to obtain primary emulsion;
(4) preparing liposome: preserving the temperature of the primary emulsion prepared in the step (3) at 70 ℃, treating the primary emulsion by high-pressure homogenizing equipment, wherein the pressure is 1000 bar, the cycle time is 2 times, and cooling to 50 ℃;
(5) adding 0.1% of carrot seed oil, 0.5% of olive oil and 0.1% of fibroblast growth factor into the mixture obtained in the step (4), stirring uniformly at 800 bar, homogenizing for 1 time under high pressure, and cooling to obtain the madecassoside liposome. The madecassoside liposome has a particle size of 135.3 nm and an entrapment rate of 88.4%.
Example 3
(1) Preparing an oil phase, namely melting 2.0% of hydrogenated lecithin, 1.0% of hydroxylated lecithin, 1.0% of phosphatidyl diethanolamine, 3.0% of cholesterol and 0.5% of ceramide IIIA at the water bath temperature of 65-80 ℃, adding 0.5% of alpha-tocopherol and 0.1% of astaxanthin, and uniformly mixing for later use;
(2) preparing an aqueous phase: adding 1.0% of madecassoside, 10.0% of propylene glycol, 15.0% of 1, 2-pentanediol, 1.0% of coconut collagen and 1.0% of fibroin into 60.4% of purified water, stirring and heating to 65-80 ℃ for dissolving for later use;
(3) preparing colostrum: dropwise adding the oil phase prepared in the step (1) into the water phase prepared in the step (2), continuously stirring, and performing high-speed shearing emulsification at 10000 rpm for 2 min to obtain primary emulsion;
(4) preparing liposome: preserving the temperature of the primary emulsion prepared in the step (3) at 70 ℃, treating the primary emulsion by high-pressure homogenizing equipment, wherein the pressure is 1500 bar, the cycle time is 2 times, and cooling to 50 ℃;
(5) adding 0.5% of carrot seed oil, 0.5% of avocado oil, 1.0% of fibroblast growth factor and 1.5% of honeysuckle extract into the mixture in the step (4), stirring uniformly at 800 bar, homogenizing under high pressure for 1 time, and cooling to obtain the madecassoside liposome. The madecassoside liposome has a particle size of 100.5 nm and an entrapment rate of 89.7%.
Example 4
(1) Preparing an oil phase, namely melting 5.0% of hydrogenated lecithin, 2.0% of cholesterol and 0.5% of ceramide at the water bath temperature of 65-80 ℃, adding 0.5% of alpha-tocopherol, 0.1% of astaxanthin and 0.5% of quercetin, and uniformly mixing for later use;
(2) preparing an aqueous phase: adding 2.0% of madecassoside, 10.0% of 1, 3-butanediol, 5.0% of 1, 2-pentanediol and 1.0% of deep sea cod skin collagen into 67.4% of purified water, stirring and heating to 65-80 ℃ for dissolving for later use;
(3) preparing colostrum: dropwise adding the oil phase prepared in the step (1) into the water phase prepared in the step (2), continuously stirring, and performing high-speed shearing emulsification at 10000 rpm for 2 min to obtain primary emulsion;
(4) preparing liposome: preserving the temperature of the primary emulsion prepared in the step (3) at 70 ℃, treating the primary emulsion by high-pressure homogenizing equipment, wherein the pressure is 800 bar, the cycle time is 3 times, and cooling to 50 ℃;
(5) adding 1.0% of carrot seed oil, 0.5% of rose essential oil, 0.5% of fibroblast growth factor and 2.0% of honeysuckle extract into the mixture obtained in the step (4), stirring uniformly at 800 bar, homogenizing under high pressure for 1 time, and cooling to obtain the madecassoside liposome. The madecassoside liposome has a particle size of 146.2 nm and an entrapment rate of 93.5%.
Example 5
(1) Preparing an oil phase, namely melting 5.0% of hydroxylated lecithin, 5.0% of phosphatidylcholine, 2.0% of cholesterol and 1.0% of ceramide at the water bath temperature of 65-80 ℃, and then adding 0.5% of astaxanthin and 0.5% of quercetin to mix uniformly for later use;
(2) preparing an aqueous phase: adding 8.0% of madecassoside, 8.0% of propylene glycol, 8.0% of 1, 3-butanediol, 5.0% of 1, 2-hexanediol, 2.0% of deep sea cod skin collagen and 3.0% of fibroin into 49.3% of purified water, stirring and heating to 65-80 ℃ for dissolving for later use;
(3) preparing colostrum: dropwise adding the oil phase prepared in the step (1) into the water phase prepared in the step (2), continuously stirring, and performing high-speed shearing emulsification at 10000 rpm for 2 min to obtain primary emulsion;
(4) preparing liposome: preserving the temperature of the primary emulsion prepared in the step (3) at 70 ℃, treating the primary emulsion by high-pressure homogenizing equipment, wherein the pressure is 1000 bar, the cycle time is 4 times, and cooling to 50 ℃;
(5) adding 0.5% rose essential oil, 1.5% shea butter, 0.2% fibroblast growth factor, and 0.5% flos Lonicerae extract into (4), stirring, homogenizing at 800 bar under high pressure for 1 time, and cooling to obtain madecassoside liposome. The madecassoside liposome has a particle size of 188.7 nm and an entrapment rate of 91.8%.
Example 6
(1) Preparing an oil phase, namely melting 3.0% of hydrogenated lecithin, 2.0% of egg yolk lecithin, 2.0% of cholesterol and 0.5% of ceramide at the water bath temperature of 65-80 ℃, adding 0.5% of alpha-tocopherol and 0.5% of astaxanthin, and uniformly mixing for later use;
(2) preparing an aqueous phase: adding 2.0% of madecassoside, 10.0% of propylene glycol, 8.0% of 1, 3-butanediol, 1.0% of deep sea cod skin collagen and 2.0% of silk collagen into 65.3% of purified water, stirring and heating to 65-80 ℃ for dissolving for later use;
(3) preparing colostrum: dropwise adding the oil phase prepared in the step (1) into the water phase prepared in the step (2), continuously stirring, and performing high-speed shearing emulsification at 10000 rpm for 2 min to obtain primary emulsion;
(4) preparing liposome: preserving the temperature of the primary emulsion prepared in the step (3) at 70 ℃, treating the primary emulsion by high-pressure homogenizing equipment, wherein the pressure is 800 bar, the cycle time is 3 times, and cooling to 50 ℃;
(5) adding 1.0% of carrot seed oil, 0.5% of olive oil, 0.5% of shea butter and 0.2% of fibroblast growth factor into the mixture (4), stirring uniformly at 800 bar, homogenizing under high pressure for 1 time, and cooling to obtain the madecassoside liposome. The madecassoside liposome has particle diameter of 177.3nm and entrapment rate of 95.2%.
Example 7
(1) Preparing an oil phase, namely melting 3.0% of hydrogenated lecithin, 2.0% of egg yolk lecithin, 2.0% of cholesterol and 0.5% of ceramide at the water bath temperature of 65-80 ℃, adding 1.0% of alpha-tocopherol, and uniformly mixing for later use;
(2) preparing an aqueous phase: adding 2.0% of madecassoside, 5.0% of propylene glycol, 8.0% of 1, 3-butanediol, 1.0% of deep sea cod skin collagen and 2.0% of silk collagen into 71.3% of purified water, stirring and heating to 65-80 ℃ for dissolving for later use;
(3) preparing colostrum: dropwise adding the oil phase prepared in the step (1) into the water phase prepared in the step (2), continuously stirring, and performing high-speed shearing emulsification at 10000 rpm for 2 min to obtain primary emulsion;
(4) preparing liposome: preserving the temperature of the primary emulsion prepared in the step (3) at 70 ℃, treating the primary emulsion by high-pressure homogenizing equipment, wherein the pressure is 800 bar, the cycle time is 3 times, and cooling to 50 ℃;
(5) adding 1.0% of carrot seed oil, 0.5% of olive oil, 0.5% of shea butter, 0.2% of fibroblast growth factor and 1.0% of honeysuckle extract into the mixture in the step (4), stirring uniformly at 800 bar, homogenizing for 1 time under high pressure, and cooling to obtain the madecassoside liposome. The madecassoside liposome has a particle size of 168.5nm and an entrapment rate of 88.5%.
Example 8
(1) Preparing an oil phase, namely melting 2.0% of hydrogenated lecithin, 2.0% of phosphatidylcholine, 1.0% of phosphatidyl diethanolamine, 2.0% of cholesterol and 0.5% of ceramide at the water bath temperature of 65-80 ℃, adding 1.0% of alpha-tocopherol, and uniformly mixing for later use;
(2) preparing an aqueous phase: adding 2.0% of madecassoside, 10.0% of 1, 3-butanediol, 8.0% of 1, 2-pentanediol, 3.0% of 1, 2-hexanediol, 1.0% of deep sea cod skin collagen and 1.0% of fibroin into 63.6% of purified water, stirring and heating to 65-80 ℃ for dissolving for later use;
(3) preparing colostrum: dropwise adding the oil phase prepared in the step (1) into the water phase prepared in the step (2), continuously stirring, and performing high-speed shearing emulsification at 10000 rpm for 2 min to obtain primary emulsion;
(4) preparing liposome: preserving the temperature of the primary emulsion prepared in the step (3) at 70 ℃, treating the primary emulsion by high-pressure homogenizing equipment, wherein the pressure is 800 bar, the cycle time is 3 times, and cooling to 50 ℃;
(5) adding 1.0% of carrot seed oil, 0.5% of avocado tree oil, 0.2% of fibroblast growth factor and 1.2% of honeysuckle extract into the mixture in the step (4), stirring uniformly at 800 bar, homogenizing under high pressure for 1 time, and cooling to obtain the madecassoside liposome. The madecassoside liposome has a particle size of 156.1 nm and an entrapment rate of 92.8%.
Comparative example 1 preparation of a madecassoside cream
According to the conventional cream preparation method, 3.0% of stearic acid, 4.5% of glyceryl monostearate, 5.0% of cetostearyl alcohol and 6.0% of polydimethylsiloxane are used as oil phases and melted in a water bath at 75 ℃; dissolving 2.0% of madecassoside, 10.0% of glycerol, 5.0% of propylene glycol, 0.3% of triethanolamine and 64.2% of purified water in a water bath at 75 ℃; the two phases were mixed with stirring and emulsified and cooled to obtain a cream containing 2.0% of madecassoside, as a control formulation for examples 4, 6, 7 and 8.
Example 9
Examples 1-8 Hydroxyasiaticoside liposomes were left in a closed container at room temperature for 30 days, and then the properties and particle size of the samples were examined.
TABLE 1 examples 1-8 Hydroxyasiaticoside liposomes stability results
Figure 56785DEST_PATH_IMAGE001
The test result shows that: the samples prepared in the embodiments 1-8 have no agglomeration phenomenon, and the prepared samples have no obvious change in properties and particle sizes after being placed for 30 days, and still meet the requirements of practical application, which indicates that the madecassoside liposome prepared according to the components and the content used in the invention has stable properties, particularly the madecassoside is still stable under the condition of high concentration, and the phenomena of crystallization and leakage do not occur.
Example 10
The abdominal skin of male SD rats with the body weight of 200-250 g is used as a barrier layer of a transdermal test. The intact skin is held between the receiving reservoir and the supply reservoir (inner skin layer facing the receiving reservoir). Diffusion cell parameters: effective diffusion area 3.14 cm2The receiving tank volume was about 8.0 ml, and the magnetic stirring speed was 600 rpm. Filling the receiving tank with 1% SDS-10% ethanol-physiological saline as release medium, removing bubbles, stirring, and keeping the temperature to 37.0 + -0.5 deg.C. The skin surface was evenly coated with about 1 g of sample (n = 8), 0.5 ml of receiving fluid was aspirated at 1,2, 4, 6, 8, 10, 12h and supplemented with 0.5 ml of release medium. The concentration of madecassoside in the received solution filtered through a 0.22 μm filter was determined by HPLC. And calculating the cumulative permeation amount of the medicaments at different times.
The cumulative transdermal amount of madecassoside per unit area is calculated according to the following formula:
Figure 905965DEST_PATH_IMAGE002
wherein, Q: accumulating transdermal volume; s: an effective diffusion area; v: receiving the volume of the normal saline in the pool; ci: the concentration of the drug in the receiving solution from the 1 st to the last sampling; cn: the concentration of the drug in the receiving fluid during the sub-sampling; m is0: theoretically weighing the sample; m: the sample is actually weighed.
The samples of examples 4, 6 to 8 of the present invention and the sample of comparative example 1 were subjected to a skin penetration test. The test results are shown in FIGS. 1 and 2. As can be seen from FIG. 1, the cumulative skin permeation amounts of the samples of examples 4, 6 to 8 are higher than that of the sample of comparative example 1, and the cumulative skin permeation amounts of 12 hours of the samples of examples 4, 6 to 8 of the present invention are 2477.5 μ g/cm2、1937.6 μg/cm2 、2278.3 μg/cm2 、2074.9 μg/cm2Comparative example 1 is only 327.1. mu.g/cm2(ii) a As can be seen from FIG. 2, the 12-hour retention amounts in examples 4 and 6 to 8 of the present invention were 451.5. mu.g/cm, respectively2、350.6 μg/cm2、415.7 μg/cm2 、380.6 μg/cm2(ii) a Comparative example 1 is only 50.8. mu.g/cm2. Obviously, the madecassoside of the invention has higher skin penetration and retention, thus having good deep repair effect.
Example 6 the accumulated permeation amount and the retention amount for 12h were higher in the case of the same madecassoside containing the honeysuckle extract as compared with example 7, which shows that the honeysuckle extract can promote the transdermal penetration and retention of the madecassoside.
Example 11
Taking 18 healthy rabbits (2.0 +/-0.2) kg in weight, randomly dividing the weight into 6 groups, removing hairs from two sides of the back skin of the rabbits 24 hours before an experiment, and checking whether the removed skin is injured 24 hours after the hairs are removed, wherein the injured skin is not suitable for a skin irritation test. The application is carried out 3 times per day for 7 days. The skin irritation test was performed on the blank cream group (without any drug administration), comparative example 1, and examples 1 to 4, respectively, and the test results are shown in table 2.
Table 2 observation of skin irritation
Figure 97912DEST_PATH_IMAGE003
"+" rabbit skin congestion, red swelling; "+ +" indicates that the congestion and red swelling still exist, but there is an increasing trend; "-" indicates no hyperemia or redness and swelling.
The test result shows that: the samples of the blank group and the comparative example 1 are smeared on the skin of the rabbit without congestion and red swelling, which shows that the madecassoside cream of the examples 1 to 4 and the comparative example 1 has no irritation.
Example 12
120 women with striae gravidarum between 24 and 40 years old are selected, randomly divided into 4 groups, 30 women in each group are respectively smeared on the abdomen by using a comparative example 1, an example 4, an example 6 and an example 7, and mild massage is carried out on the skin 2 times a day.
The curative effect judgment standard is remarkable: basically removing striae gravidarum; the method has the following advantages: the striae gravidarum subsides; and (4) invalidation: there was no change.
The results of the four groups are shown in table 3.
TABLE 3 comparison of the effects of treatment of four groups of striae gravidarum
Group of n Is remarkable in that Is effective Invalidation
Example 4 30 9 16 5
Example 6 30 8 17 5
Example 7 30 6 18 6
Comparative example 1 30 1 18 11
The result shows that the madecassoside liposome prepared by the invention has good effect of removing striae gravidarum, and the effect of removing striae gravidarum is better when the madecassoside liposome contains honeysuckle extract, so that the effect of removing striae gravidarum of the madecassoside can be improved. In the comparative example 1, the madecassoside is a non-nano liposome, and the transdermal quantity is small, so that the effect of removing striae gravidarum is poor.

Claims (10)

1. The madecassoside liposome is characterized by comprising the following components in percentage by mass: 0.1 to 8.0 percent of madecassoside, 3.0 to 10.0 percent of phospholipid, 0.5 to 5.0 percent of cholesterol, 0.05 to 1.0 percent of ceramide, 0.5 to 2.0 percent of plant essential oil, 10.0 to 25.0 percent of polyalcohol, 0.5 to 2.0 percent of antioxidant, 0.5 to 5.0 percent of collagen, 0.1 to 1.0 percent of fibroblast growth factor, 0.5 to 2.0 percent of honeysuckle extract and the balance of water;
the particle size of the madecassoside liposome is 100-190 nm;
the extraction method of the honeysuckle extract comprises the steps of drying honeysuckle, pulverizing, extracting with 75-80% ethanol, and drying the extract
Drying to obtain extract.
2. The madecassoside liposome of claim 1, wherein the honeysuckle extract is 2.0% by weight.
3. A liposome of madecassoside according to claim 1 or 2, characterized in that said phospholipids are one or a mixture of several of soya bean lecithin, egg yolk lecithin, hydrogenated lecithin, hydroxylated lecithin, phosphatidylcholine and phosphatidyldiethanolamine.
4. A liposome of madecassoside according to claim 1 or 2, characterized in that the ceramide is one or a mixture of ceramides I, II and IIIA.
5. A liposome of madecassoside according to claim 1 or 2, characterized in that said vegetable essential oil is a mixture of two or more of carrot seed oil, rose essential oil, olive oil, shea butter.
6. A liposome of madecassoside according to claim 1 or 2, characterized in that said polyalcohol is one or a mixture of several of 1, 3-butanediol, propanediol, 1, 2-pentanediol, 1, 2-hexanediol.
7. A liposome of madecassoside according to claim 1 or 2, characterized in that the antioxidant is a mixture of one or more of quercetin, alpha-tocopherol, astaxanthin.
8. A liposome of madecassoside according to claim 1 or 2, characterized in that said collagen is a mixture of two or more of collagen of deep sea cod skin, collagen of coconut, collagen of silk.
9. A method for preparing liposomes of madecassoside according to claim 1, characterized in that it comprises the following steps:
(1) preparing an oil phase, namely melting phospholipid, cholesterol and ceramide at the water bath temperature of 65-80 ℃, adding an antioxidant, and uniformly mixing for later use;
(2) preparing an aqueous phase: adding madecassoside, polyalcohol and collagen into purified water according to the formula amount, stirring and heating to 65-80 ℃ to dissolve the madecassoside, the collagen and the polyalcohol for later use;
(3) preparing colostrum: dropwise adding the oil phase prepared in the step (1) into the water phase prepared in the step (2), continuously stirring, and performing high-speed shearing emulsification at 10000 rpm for 2 min to obtain primary emulsion;
(4) preparing liposome: preserving the temperature of the primary emulsion prepared in the step (3) at 70 ℃, and then treating the primary emulsion by high-pressure homogenizing equipment, wherein the pressure is 500-1500 bar, the cycle time is 2-8 times, and the temperature is reduced to 50 ℃;
(5) adding plant essential oil, fibroblast growth factor and flos Lonicerae extract into (4), stirring at 800 bar, homogenizing under high pressure for 1 time, and cooling.
10. Use of the madecassoside liposome according to any one of claims 1 to 8 for preparing a skin care product with effect of preventing and treating stretch marks.
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CN110251416A (en) * 2019-07-05 2019-09-20 中山中研化妆品有限公司 A kind of Ceramide Complex and preparation method thereof
FR3108037B1 (en) * 2020-03-10 2022-04-01 Farevacare Cosmetic or dermatological composition for maintaining the skin microbiome
CN111973688A (en) * 2020-08-31 2020-11-24 上海珈凯生物科技有限公司 Traditional Chinese medicine composition with effects of relieving scalp inflammation and relieving itching and preparation method thereof
CN112137960B (en) * 2020-09-28 2022-12-20 广州市香雪制药股份有限公司 Essential oil liposome and preparation method and application thereof
CN113083193B (en) * 2021-03-05 2022-07-01 海雅美生物技术(珠海)有限公司 Preparation method of ceramide-loaded centella asiatica extract compound
CN112957284B (en) * 2021-04-08 2023-06-23 广州东智盟化妆品有限公司 Repair essence containing peony seed oil nano-liposomes and preparation method thereof
CN113456594B (en) * 2021-07-06 2022-08-19 浙江宜格企业管理集团有限公司 Method for preparing liposome containing glycyrrhiza inflata extract and madecassoside
CN113576992B (en) * 2021-08-13 2022-12-20 杨卓墩 Skin repair active ingredient for toner
CN114225007B (en) * 2021-11-09 2023-08-25 西安润玉医疗科技有限公司 Whey protein spray for repairing superficial wound surface and preparation method thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101491498A (en) * 2008-01-25 2009-07-29 广州暨南大学医药生物技术研究开发中心 aFGF liposome, preparation method and use thereof
CN103893122A (en) * 2014-03-28 2014-07-02 华南理工大学 Madecassoside lipidosome and preparation method and application thereof
CN107137319A (en) * 2017-05-31 2017-09-08 上海东晟源日化有限公司 A kind of soft quick toxin-expelling and face nourishing frost of nm

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101491498A (en) * 2008-01-25 2009-07-29 广州暨南大学医药生物技术研究开发中心 aFGF liposome, preparation method and use thereof
CN103893122A (en) * 2014-03-28 2014-07-02 华南理工大学 Madecassoside lipidosome and preparation method and application thereof
CN107137319A (en) * 2017-05-31 2017-09-08 上海东晟源日化有限公司 A kind of soft quick toxin-expelling and face nourishing frost of nm

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
无;庆田朋子;《护肤全书 外版书》;江苏凤凰文艺出版社;20180630;第232页 *
无;张景云著;《实用美容药物学》;中国中医药出版社;20060731;第20页 *
胶原蛋白化妆品的保养功用;胡建平著;《鱼胶原蛋白的开发与应用》;四川大学出版社;20140331;第183-184页 *
脂质体的氧化;安红等著;《磷脂化学及应用技术》;中国计量出版社;20060630;第120-121页 *

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