CN109431829A - A kind of madecassoside liposome and its preparation method and application - Google Patents
A kind of madecassoside liposome and its preparation method and application Download PDFInfo
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Abstract
The present invention relates to a kind of madecassoside liposome and its preparation method and application, the madecassoside liposome is calculated by percentage to the quality by the water of 0.1%~8.0% madecassoside, 3.0%~10.0% phosphatide, 0.5%~5.0% cholesterol, 0.05%~1.0% ceramide, 0.5%~2.0% plants essential oil, 10.0%~25.0% polyalcohol, 0.5%~2.0% antioxidant, 0.5%~5.0% collagen, 0.1%~1.0% fibroblast growth factor, 0.5%~2.0% Honegsukle flower P.E and surplus.Madecassoside liposome prepared by the present invention can promote madecassoside skin permeation and play long-acting, each component can play synergistic effect, promote fibroblast regeneration, conditioning skin, increases elasticity of skin and moisture, removes free radical, replenishing collagen, reach cytothesis, increase elasticity of skin, dispels striae of pregnancy.
Description
Technical field
The invention belongs to medicine adornment technical fields, and in particular to a kind of madecassoside liposome and preparation method thereof and answer
With.
Background technique
The formation of striae of pregnancy is mainly that gestational period load-bearing that twilight is rung, and the bulge of abdomen makes the elastic fibers and collagen of skin
By different degrees of damage or fracture due to external force pulls, thinning of skin attenuates fiber, abdominal skin occur width it is different,
Pink or aubergine wave stripe different in size；After childbirth, these stripeds can fade away, and leaving white or silvery white has
The scar strain line of gloss, i.e. striae of pregnancy.
The method of common elimination striae of pregnancy includes: 1. to change skin method: Chemical peeling agent used, adverse reaction is easily caused,
Cause cuticula thinning, skin occurs sensitive；2. essential oil champignon method: this method course for the treatment of is long, and more demanding to virtue treatment teacher, effect
Fruit is unobvious；3. laser therapy: this method is not suitable for large area treatment, is easy to cause skin sensitive；4. filing: physics mill
It peels and skin painful and be easy to cause skin injury.
The commercially available product action and efficacy for dispelling gestation upper at present is single, is unable to multi-efficiency synergistic effect, and be difficult to
Skin corium up to skin affects using effect.Although madecassoside has scar reparation, antibacterial, anti-inflammatory, promotion at fibre
The effect of cytothesis is tieed up, but is difficult to since it belongs to polarity macromolecular through skin, external curing effect is poor.
Summary of the invention
In view of the deficiencies of the prior art, the present invention provides a kind of madecassoside liposome and preparation method thereof and answer
With prepared madecassoside liposome components are reasonable, can effectively facilitate active constituent enters skin through keratoderma
Skin deep tissues, and play synergistic effect；Meanwhile the liposome has the advantages that drugloading rate is big, stability is good, highly-safe,
And preparation method simplicity is easily-controllable.
In order to achieve the above-mentioned object of the invention, the present invention the following technical schemes are provided:
A kind of madecassoside liposome, component and constituent mass percentage are as follows: 0.1%~8.0% madacasso
Careless glycosides, 3.0%~10.0% phosphatide, 0.5%~5.0% cholesterol, 0.05%~1.0% ceramide, 0.5%~2.0%
Plants essential oil, 10.0%~25.0% polyalcohol, 0.5%~2.0% antioxidant, 0.5%~5.0% collagen, 0.1%
The water of~1.0% fibroblast growth factor and surplus；Madecassoside liposomal particle size is 100~190nm.
Preferential, madecassoside liposome also includes that mass percent is 0.5%~2.0% Honegsukle flower P.E,
For the Honegsukle flower P.E weight in terms of medicinal material, the extracting method of the Honegsukle flower P.E beats powder after drying for honeysuckle, then
It is extracted with 75~80% ethyl alcohol, extracting solution is dry to medicinal extract.Honegsukle flower P.E be honeysuckle chromocor extract, mainly at
It is divided into Flavonoid substances.
The activity of honeysuckle becomes flavone compound, mainly there is Luteolin, glucoside, Hyperoside etc., studies
Show that flavone compound has the effects that good removing free radical, anti-inflammatory.But result of study of the present invention shows the present invention
The Honegsukle flower P.E of preparation can promote active constituent madecassoside in madecassoside liposome transdermal；Gold simultaneously
Honeysuckle flower extract is synthesized with fibroblast growth factor collective effect in fibroblast and collagenocyte, and fibroblast is raw
The long factor promotes fibroblast and collagenocyte synthesis, and Honegsukle flower P.E is to fibroblast proliferation and collagenic supersession
Effectively control, the reparation of the striae of pregnancy for the madecassoside that cooperates achieve the effect that repair and preventing from scar, avoid into fiber finer
Born of the same parents' hyper-proliferative causes the unordered accumulation of collagen to cause scar.
Preferential, the phosphatide is soybean lecithin, egg yolk lecithin, hydrolecithin, hydroxylated lecithin, phosphatidyl
The mixture of one or more of choline, phosphatidyl diethanol amine.
Preferably, the ceramide is one or more of ceramide I, ceramide II, Cera
Mixture.
It is preferential, the plants essential oil be carrot seed oil, Rosa Damascana, olive oil, two kinds in Butyrospermum parkii oil or
A variety of mixtures.Plants essential oil of the present invention uses the mixture of carrot seed oil, Rosa Damascana, olive oil, Butyrospermum parkii oil,
Carrot seed oil can strengthen red blood cell, can improve the colour of skin, desalinate spot, keep skin more consolidation flexible；Rosa Damascana can promote
Into cell metabolism and cytothesis function, strengthen cytotoxic discharge；Olive oil squalene rich in etc. is single not
Saturated fatty acid and vitamin E, K, A, D etc. and phenols antioxidant, can eliminate facial wrinkles, prevent skin aging；Butter
Fruit tree oil is a kind of oil of high anti-oxidation, the nursing of deep skin damage can be preferably carried out through skin, while having certain
Antibacterial action, there is certain interference effect for resisting bacterium to cell repair when.Use carrot seed oil, Rosa Damascana, olive
Olive oil, Butyrospermum parkii oil mixture to the reparation of striae of pregnancy play multi-efficiency improvement.
It is preferential, the polyalcohol be one of 1,3-BDO, propylene glycol, 1,2- pentanediol, 1,2- hexylene glycol or
Several mixtures.
Preferential, the antioxidant is the mixture of one or more of Quercetin, alpha-tocopherol, astaxanthin.Mongolian oak
Pi Su be a kind of Flavonoid substances, existing anti-oxidant, anti-inflammatory effect, but can enhance jointly with Honegsukle flower P.E madacasso grass
The effect of glycosides.
Preferably, the collagen is deep-sea cod collagen, in coconut collagen, silk collagen
Two or more mixtures.Pathology, physiologic character based on striae of pregnancy, prevention reduce striae of pregnancy and use are needed to target skin
Skin fibroblast can be proliferated and be stimulated elastomer and glue in metabolism, especially increase skin by active cell
Former protein content plays a role.The distinctive skin repairing of collagen and regeneration effect, can stimulate new collagen raw
At, and then Skin Cell is propped up, moisturizing is played and inhibits wrinkle.The present invention uses deep-sea cod collagen, coconut palm
Sub- collagen, silk collagen mixture carry out collagen supplement.Deep-sea cod collagen, coconut collagen
Albumen, silk collagen can effectively penetrate epidermis, provide necessary glue for striae of pregnancy reparation after being prepared into nano liposomes
Former albumen.
The present invention provides a kind of preparation method of madecassoside liposome described in above-mentioned technical proposal, including it is as follows
Step:
(1) it prepares oily phase: phosphatide, cholesterol, ceramide being melted in 65~80 DEG C of bath temperature conditions, added anti-
Oxidant is uniformly mixed, spare；
(2) it prepares water phase: madecassoside, polyalcohol, collagen is added in formula ratio purified water, stirring is simultaneously
65~80 DEG C of heating makes madecassoside, collagen, polyalcohol dissolution, spare；
(3) it prepares colostrum: oil prepared by step (1) is mutually added dropwise in the water phase of step (2) preparation and is stirred continuously,
10000rpm high speed shearing emulsification 2min again, obtains colostrum；
(4) it prepares liposome: colostrum prepared by step (3) is kept the temperature under the conditions of 70 DEG C, then set by high-pressure homogeneous
Standby equipment is handled, and pressure is 500bar~1500bar, and cycle-index is 2~8 times, is cooled to 50 DEG C；
(5) plants essential oil, fibroblast growth factor, Honegsukle flower P.E are added in (4), are stirred evenly,
800bar, it is high-pressure homogeneous 1 time, cooling to get madecassoside liposome.
A kind of application of madecassoside liposome in the medicine adornment, effect skin care item of prevention and treatment striae of pregnancy.Madacasso
Careless glycosides liposome can be used directly, can also be made an addition in all kinds of effect skin care item, such as creme, lotion, Essence, gel.
The beneficial effects of the present invention are:
1, the active constituent of the different efficacies such as madecassoside is transported to using this novel delivery system of liposome
Deep skin, average grain diameter are 100~190nm, the partial size not only can guarantee active constituent through cuticula, but also can guarantee activity at
Divide and be detained in skin, improves madecassoside Percutaneous permeability and hold-up, sustained release activity ingredient, long period dimension
It holds in effective concentration, preferably performance skin-care effect.
2, each active component function complementation plays synergistic effect, hydroxyl in madecassoside liposome prepared by the present invention
Asiaticosid has the function of to promote fibroblast regeneration, inhibit inflammatory reaction, accelerating wound healing etc.；Plants essential oil, which has, to be adjusted
Skin is managed, increases elasticity of skin, keep skin moisture；Antioxidant has effects that remove free radical, delay senescence；Collagen egg
It is white to have the function of to supplement skin collagen content, increase elasticity of skin etc..
3, Honegsukle flower P.E can promote active constituent madecassoside in madecassoside liposome transdermal, simultaneously
It is synthesized with fibroblast growth factor collective effect in fibroblast and collagenocyte, makes fibroblast proliferation and collagen
Effective control of metabolism, the reparation of the striae of pregnancy for the madecassoside that cooperates achieve the effect that repair and preventing from scar, avoid into
Fibrocyte hyper-proliferative.
4, carrot seed oil, Rosa Damascana, olive oil, Butyrospermum parkii oil mixture the reparation of striae of pregnancy is played it is multiple
Effect improves, and can promote cell metabolism and cytothesis function, keep skin more consolidation flexible；The colour of skin can be improved, desalinated
Spot；Facial wrinkles can be eliminated, skin aging is prevented；Can antibacterial and enhance it is transdermal, reduce interfere simultaneously carrying out deep lifting.
Detailed description of the invention
Fig. 1 is that embodiment 4,6~8 and 1 percutaneous penetration of comparative example add up transit dose.
Fig. 2 is 1 percutaneous penetration 12h hold-up of embodiment 4,6~8 and comparative example.
Specific embodiment
Madecassoside liposome provided by the invention, including form by mass percentage as follows: 0.1%~8.0%
Madecassoside, 3.0%~10.0% phosphatide, 0.5%~5.0% cholesterol, 0.05%~1.0% ceramide, 0.5%
~2.0% plants essential oil, 10.0%~25.0% polyalcohol, 0.5%~2.0% antioxidant, 0.5%~5.0% collagen egg
The water of white, 0.1%~1.0% fibroblast growth factor, 0.5%~2.0% Honegsukle flower P.E and surplus.
The present invention provides the preparation methods of above-mentioned madecassoside liposome, include the following steps:
(1) it prepares oily phase: phosphatide, cholesterol, ceramide being melted in 65~80 DEG C of bath temperature conditions, added anti-
Oxidant is uniformly mixed, spare；
(2) it prepares water phase: madecassoside, polyalcohol, collagen is added in formula ratio purified water, stirring is simultaneously
65~80 DEG C of heating makes madecassoside, collagen, polyalcohol dissolution, spare；
(3) it prepares colostrum: oil prepared by step (1) is mutually added dropwise in the water phase of step (2) preparation and is stirred continuously,
10000rpm high speed shearing emulsification 2min again, obtains colostrum；
(4) it prepares liposome: colostrum prepared by step (3) is kept the temperature under the conditions of 70 DEG C, then set by high-pressure homogeneous
Standby equipment is handled, and pressure is 500bar~1500bar, and cycle-index is 2~8 times, is cooled to 50 DEG C；
(5) plants essential oil, fibroblast growth factor, Honegsukle flower P.E are added in (4), are stirred evenly,
800bar, it is high-pressure homogeneous 1 time, cooling to get madecassoside liposome.
In the present invention, the oily phase, the preparation process of aqueous phase dissolved do not have the limitation of sequencing.
The invention will be further described by way of example below, and those skilled in the art is allow to better understand this
Invention, specific embodiment preferred for this invention should be understood to be merely illustrative of, rather than limit this hair in any way
It is bright.
Embodiment 1
(1) oily phase is prepared: by 3.0% soybean lecithin, 0.5% cholesterol, 0.05% ceramide I in 65~80 DEG C of water-baths
The melting of temperature condition adds 2.0% alpha-tocopherol and is uniformly mixed, spare；
(2) prepare water phase: by 0.1% madecassoside, 10.0% propylene glycol, 0.2% deep-sea cod collagen,
0.3% coconut collagen is added in 82.25% purified water, and stirring and heating 65~80 DEG C makes to dissolve, spare；
(3) it prepares colostrum: oil prepared by step (1) is mutually added dropwise in the water phase of step (2) preparation and is stirred continuously,
10000rpm high speed shearing emulsification 2min again, obtains colostrum；
(4) it prepares liposome: colostrum prepared by step (3) is kept the temperature under the conditions of 70 DEG C, then set by high-pressure homogeneous
Standby processing, pressure 500bar, cycle-index are 3 times, are cooled to 50 DEG C；
(5) by 0.4% Rosa Damascana, 0.1% Butyrospermum parkii oil, 0.1% fibroblast growth factor, 1.0% gold and silver
Flower extract is added in (4), is stirred evenly, 800bar, high-pressure homogeneous 1 time, cooling to get madecassoside liposome.
The madecassoside liposomal particle size is 115.6nm, encapsulation rate 95.7%.
Embodiment 2
(1) oily phase is prepared: by 1.0% phosphatidyl choline, 2.0% egg yolk lecithin, 5% cholesterol, 0.1% ceramide
II melts in 65~80 DEG C of bath temperature conditions, adds 1.5% alpha-tocopherol and is uniformly mixed, spare；
(2) water phase is prepared: by 5% madecassoside, 10.0% propylene glycol, 5.0%1,3- butanediol, 0.5% deep-sea
Cod collagen, 0.5% coconut collagen are added in 68.3% purified water, stir and heat 65~80 DEG C make it is molten
Solution, it is spare；
(3) it prepares colostrum: oil prepared by step (1) is mutually added dropwise in the water phase of step (2) preparation and is stirred continuously,
10000rpm high speed shearing emulsification 2min again, obtains colostrum；
(4) it prepares liposome: colostrum prepared by step (3) is kept the temperature under the conditions of 70 DEG C, then set by high-pressure homogeneous
Standby processing, pressure 1000bar, cycle-index are 2 times, are cooled to 50 DEG C；
(5) 0.1% carrot seed oil, 0.5% olive oil, 0.1% fibroblast growth factor are added in (4),
It stirs evenly, 800bar, high-pressure homogeneous 1 time, it is cooling to get madecassoside liposome.The madecassoside liposome
Partial size is 135.3nm, encapsulation rate 88.4%.
Embodiment 3
(1) prepare oily phase: by 2.0% hydrolecithin, 1.0% hydroxylated lecithin, 1.0% phosphatidyl diethanol amine,
3.0% cholesterol, 0.5% Cera are melted in 65~80 DEG C of bath temperature conditions, add 0.5% alpha-tocopherol,
0.1% astaxanthin is uniformly mixed, spare；
(2) water phase is prepared: by 1.0% madecassoside, 10.0% propylene glycol, 15.0%1,2- pentanediol, 1.0% coconut palm
Sub- collagen, 1.0% fibroin are added in 60.4% purified water, and stirring and heating 65~80 DEG C makes to dissolve, spare；
(3) it prepares colostrum: oil prepared by step (1) is mutually added dropwise in the water phase of step (2) preparation and is stirred continuously,
10000rpm high speed shearing emulsification 2min again, obtains colostrum；
(4) it prepares liposome: colostrum prepared by step (3) is kept the temperature under the conditions of 70 DEG C, then set by high-pressure homogeneous
Standby processing, pressure 1500bar, cycle-index are 2 times, are cooled to 50 DEG C；
(5) by 0.5% carrot seed oil, 0.5% Butyrospermum parkii oil, 1.0% fibroblast growth factor, 1.5% gold medal
Honeysuckle flower extract is added in (4), is stirred evenly, 800bar, high-pressure homogeneous 1 time, cooling to get madecassoside lipid
Body.The madecassoside liposomal particle size is 100.5nm, encapsulation rate 89.7%.
Embodiment 4
(1) oily phase is prepared: by 5.0% hydrolecithin, 2.0% cholesterol, 0.5% ceramide in 65~80 DEG C of water-baths
The melting of temperature condition adds 0.5% alpha-tocopherol, 0.1% astaxanthin, 0.5% Quercetin and is uniformly mixed, spare；
(2) prepare water phase: by 2.0% madecassoside, 10.0%1,3- butanediol, 5.0%1,2- pentanediol,
1.0% deep-sea cod collagen is added in 67.4% purified water, and stirring and heating 65~80 DEG C makes to dissolve, spare；
(3) it prepares colostrum: oil prepared by step (1) is mutually added dropwise in the water phase of step (2) preparation and is stirred continuously,
10000rpm high speed shearing emulsification 2min again, obtains colostrum；
(4) it prepares liposome: colostrum prepared by step (3) is kept the temperature under the conditions of 70 DEG C, then set by high-pressure homogeneous
Standby processing, pressure 800bar, cycle-index are 3 times, are cooled to 50 DEG C；
(5) by 1.0% carrot seed oil, 0.5% Rosa Damascana, 0.5% fibroblast growth factor, 2.0% gold and silver
Flower extract is added in (4), is stirred evenly, 800bar, high-pressure homogeneous 1 time, cooling to get madecassoside liposome.
The madecassoside liposomal particle size is 146.2nm, encapsulation rate 93.5%.
Embodiment 5
(1) oily phase is prepared: by 5.0% hydroxylated lecithin, 5.0% phosphatidyl choline, 2.0% cholesterol, 1.0% nerve
Amide is melted in 65~80 DEG C of bath temperature conditions, add 0.5% astaxanthin, 0.5% Quercetin be uniformly mixed, it is spare；
(2) water phase is prepared: by 8.0% madecassoside, 8.0% propylene glycol, 8.0%1,3- butanediol, 5.0%1,2-
Hexylene glycol, 2.0% deep-sea cod collagen, 3.0% fibroin are added in 49.3% purified water, are stirred and are heated
65~80 DEG C make to dissolve, spare；
(3) it prepares colostrum: oil prepared by step (1) is mutually added dropwise in the water phase of step (2) preparation and is stirred continuously,
10000rpm high speed shearing emulsification 2min again, obtains colostrum；
(4) it prepares liposome: colostrum prepared by step (3) is kept the temperature under the conditions of 70 DEG C, then set by high-pressure homogeneous
Standby processing, pressure 1000bar, cycle-index are 4 times, are cooled to 50 DEG C；
(5) by 0.5% Rosa Damascana, 1.5% Butyrospermum parkii oil, 0.2% fibroblast growth factor, 0.5% gold and silver
Flower extract is added in (4), is stirred evenly, 800bar, high-pressure homogeneous 1 time, cooling to get madecassoside liposome.
The madecassoside liposomal particle size is 188.7nm, encapsulation rate 91.8%.
Embodiment 6
(1) oily phase is prepared: by 3.0% hydrolecithin, 2.0% egg yolk lecithin, 2.0% cholesterol, 0.5% neural acyl
Amine is melted in 65~80 DEG C of bath temperature conditions, add 0.5% alpha-tocopherol, 0.5% astaxanthin be uniformly mixed, it is spare；
(2) water phase is prepared: deeply by 2.0% madecassoside, 10.0% propylene glycol, 8.0%1,3- butanediol, 1.0%
Extra large cod collagen, 2.0% silk collagen are added in 65.3% purified water, and stirring and heating 65~80 DEG C makes
Dissolution, it is spare；
(3) it prepares colostrum: oil prepared by step (1) is mutually added dropwise in the water phase of step (2) preparation and is stirred continuously,
10000rpm high speed shearing emulsification 2min again, obtains colostrum；
(4) it prepares liposome: colostrum prepared by step (3) is kept the temperature under the conditions of 70 DEG C, then set by high-pressure homogeneous
Standby processing, pressure 800bar, cycle-index are 3 times, are cooled to 50 DEG C；
(5) by 1.0% carrot seed oil, 0.5% olive oil, 0.5% Butyrospermum parkii oil, 0.2% fibroblastic growth
The factor, 1.0% Honegsukle flower P.E are added in (4), are stirred evenly, 800bar, high-pressure homogeneous 1 time, cooling to get hydroxyl product
Asiaticoside liposome.The madecassoside liposomal particle size is 177.3nm, encapsulation rate 95.2%.
Embodiment 7
(1) oily phase is prepared: by 3.0% hydrolecithin, 2.0% egg yolk lecithin, 2.0% cholesterol, 0.5% neural acyl
Amine is melted in 65~80 DEG C of bath temperature conditions, is added 1.0% alpha-tocopherol and is uniformly mixed, spare；
(2) water phase is prepared: by 2.0% madecassoside, 5.0% propylene glycol, 8.0%1,3- butanediol, 1.0% deep-sea
Cod collagen, 2.0% silk collagen are added in 71.3% purified water, stir and heat 65~80 DEG C make it is molten
Solution, it is spare；
(3) it prepares colostrum: oil prepared by step (1) is mutually added dropwise in the water phase of step (2) preparation and is stirred continuously,
10000rpm high speed shearing emulsification 2min again, obtains colostrum；
(4) it prepares liposome: colostrum prepared by step (3) is kept the temperature under the conditions of 70 DEG C, then set by high-pressure homogeneous
Standby processing, pressure 800bar, cycle-index are 3 times, are cooled to 50 DEG C；
(5) by 1.0% carrot seed oil, 0.5% olive oil, 0.5% Butyrospermum parkii oil, 0.2% fibroblastic growth
The factor is added in (4), is stirred evenly, 800bar, high-pressure homogeneous 1 time, cooling to get madecassoside liposome.The hydroxyl
Base asiaticosid liposomal particle size is 168.5nm, encapsulation rate 88.5%.
Embodiment 8
(1) prepare oily phase: by 2.0% hydrolecithin, 2.0% phosphatidyl choline, 1.0% phosphatidyl diethanol amine,
2.0% cholesterol, 0.5% ceramide are melted in 65~80 DEG C of bath temperature conditions, and it is equal to add the mixing of 1.0% alpha-tocopherol
It is even, it is spare；
(2) prepare water phase: by 2.0% madecassoside, 10.0%1,3- butanediol, 8.0%1,2- pentanediol,
3.0%1,2- hexylene glycols, 1.0% deep-sea cod collagen, 1.0% fibroin are added in 63.6% purified water,
Stirring and heating 65~80 DEG C makes to dissolve, spare；
(3) it prepares colostrum: oil prepared by step (1) is mutually added dropwise in the water phase of step (2) preparation and is stirred continuously,
10000rpm high speed shearing emulsification 2min again, obtains colostrum；
(4) it prepares liposome: colostrum prepared by step (3) is kept the temperature under the conditions of 70 DEG C, then set by high-pressure homogeneous
Standby processing, pressure 800bar, cycle-index are 3 times, are cooled to 50 DEG C；
(5) by 1.0% carrot seed oil, 0.5% Butyrospermum parkii oil, 0.2% fibroblast growth factor, 1.2% gold medal
Honeysuckle flower extract is added in (4), is stirred evenly, 800bar, high-pressure homogeneous 1 time, cooling to get madecassoside lipid
Body.The madecassoside liposomal particle size is 156.1nm, encapsulation rate 92.8%.
The preparation of 1 madecassoside creme of comparative example
According to conventional creme preparation method, with 3.0% stearic acid, 4.5% glycerin monostearate, 5.0% 16
Alcohol, 6.0% dimethyl silicone polymer are oily phase, are melted in 75 DEG C of water-baths；With 2.0% madecassoside, 10.0% glycerol,
5.0% propylene glycol, 0.3% triethanolamine and 64.2% purified water dissolve in 75 DEG C of water-baths as water phase；It is stirred two-phase
And emulsify, the creme to get content for 2.0% madecassoside is cooled down, as embodiment 4, embodiment 6, embodiment 7 and reality
Apply the control formulation of example 8.
Embodiment 9
After Examples 1 to 8 madecassoside liposome is placed 30 days in room temperature closed container, the character of sample is checked
And partial size.
1 Examples 1 to 8 madecassoside liposome stability result of table
Test result shows: Examples 1 to 8 sample soilless sticking phenomenon prepared by the present invention, prepared sample are placed
After 30 days, significant changes do not occur for character and partial size, still meet practical application request, show according to component used in the present invention
Madecassoside liposome character is prepared with content to stablize, especially madecassoside is still stable in high concentration,
Do not occur partial crystallization and leakage phenomenon.
Embodiment 10
It is 200~250g male SD rat skin of abdomen as the barrier layer of penetrating absorption using weight.By intact unbroken
Skin is fixed between reception tank and supply pool (skin inner layer is towards reception tank).Diffusion cell parameter: effective diffusion area
3.14cm2, receive pool volume about 8.0ml, magnetic stirring speed 600rpm.Dissolution medium 1%SDS- is full of in reception tank
10% ethyl alcohol-physiological saline excludes bubble, unlatching stirring, and constant temperature to (37.0 ± 0.5) DEG C.Distinguish to skin surface uniform
Coated sample about 1g (n=8) draws receiving liquid 0.5ml, and supplements dissolution medium 0.5ml in 1,2,4,6,8,10,12h.With
HPLC measures the concentration of madecassoside in the receiving liquid through 0.22 μm of membrane filtration.Different time drug accumulation is calculated to penetrate
Amount.
Madecassoside unit area is calculated as follows accumulates transdermal amount:
Wherein, Q: transdermal amount is accumulated；S: effective diffusion area；V: physiological saline volume in reception tank；Ci: the 1 time supreme
Receiving liquid drug concentration when sub-sampling；Cn: receiving liquid drug concentration when the sub-sampling；m0: sample theory sample weighting amount；M: sample
The practical sample weighting amount of product.
The embodiment of the present invention 4,6~8 samples, 1 sample of comparative example are subjected to penetrating absorption.Test result is referring to Fig. 1 and figure
2.From figure 1 it appears that the sample skin cumulative transit dose of embodiment 4,6~8 is above 1 sample of comparative example, the present invention is real
The 12h Percutaneous permeability for applying example 4,6~8 is respectively 2477.5 μ g/cm2、1937.6μg/cm2、2278.3μg/cm2、2074.9μ
g/cm2, comparative example 1 is only 327.1 μ g/cm2；From figure 2 it can be seen that the 12h hold-up of the embodiment of the present invention 4,6~8 is distinguished
For 451.5 μ g/cm2、350.6μg/cm2、415.7μg/cm2、380.6μg/cm2；Comparative example 1 is only 50.8 μ g/cm2.Obviously, originally
The madecassoside of invention transdermal amount with higher and hold-up, thus there is good deep layer repairing effect.
Embodiment 6 contains Honegsukle flower P.E compared to embodiment 7, in the case where containing identical madecassoside, tires out
Product transit dose and 12h hold-up are high, illustrate that Honegsukle flower P.E can promote madecassoside transdermal and be detained.
Embodiment 11
Healthy rabbits 18, weight (2.0 ± 0.2) kg are taken, 6 groups is randomly divided into, every group animal 3, for 24 hours will before experiment
Rabbit skin of back two sides unhairing checks whether skin of unhairing is injured after unhairing for 24 hours, and compromised skin is unfit to do skin irritation examination
It tests.It smears 3 times daily, it is continuous to smear 7 days.Including blank creme group (not giving any drug), comparative example 1, Examples 1 to 4
Skin irritation test is carried out respectively, and test result is shown in Table 2.
2 skin irritation of table observes result
"+" rabbit dermohemia, redness；" ++ " indicates that congested, red and swollen phenomenon still exists, but has increase trend；"-" indicates
Without congested, red and swollen phenomenon.
Test result shows: the embodiment of the present invention 1~4 is applied to a rabbit skin with the sample of blank group, comparative example 1 respectively
Without congested, red and swollen phenomenon, show that Examples 1 to 4 and 1 madecassoside creme of comparative example are nonirritant.
Embodiment 12
Women 120 for having striae of pregnancy between 24~40 years old are chosen, 4 groups is randomly divided into, every group each 30, uses comparison respectively
Example 1 and embodiment 4, embodiment 6, embodiment 7 are applied to abdomen, make skin and slightly massage, 2 times a day.
Curative effect determinate standard, significant: striae of pregnancy is dispelled substantially；Effective: striae of pregnancy has recession；It is invalid: unchanged.
Four groups for the treatment of results are shown in Table 3.
3 four groups of striae of pregnancy therapeutic effect comparisons of table
| Group | n | Significantly | Effectively | In vain |
| Embodiment 4 | 30 | 9 | 16 | 5 |
| Embodiment 6 | 30 | 8 | 17 | 5 |
| Embodiment 7 | 30 | 6 | 18 | 6 |
| Comparative example 1 | 30 | 1 | 18 | 11 |
The result shows that madecassoside liposome prepared by the present invention have it is good dispel striae of pregnancy effect, work as hydroxyl
Striae of pregnancy better effect is dispelled when containing Honegsukle flower P.E in asiaticosid liposome, dispelling for madecassoside can be improved
Except striae of pregnancy effect.Madecassoside is non-nano liposome in comparative example 1, and transdermal amount is small, causes to dispel striae of pregnancy effect
Difference.
Claims (10)
1. a kind of madecassoside liposome, which is characterized in that the madecassoside liposome presses matter by following component
Measure percentage composition: 0.1%~8.0% madecassoside, 3.0%~10.0% phosphatide, 0.5%~5.0% cholesterol,
0.05%~1.0% ceramide, 0.5%~2.0% plants essential oil, 10.0%~25.0% polyalcohol, 0.5%~2.0%
Antioxidant, 0.5%~5.0% collagen, 0.1%~1.0% fibroblast growth factor and surplus water；
The madecassoside liposomal particle size is 100~190nm.
2. a kind of madecassoside liposome according to claim 1, which is characterized in that the madecassoside rouge
Plastid also include mass percent be 0.5%~2.0% Honegsukle flower P.E, the Honegsukle flower P.E weight in terms of medicinal material,
The extracting method of the Honegsukle flower P.E is powder to be beaten after honeysuckle is dried, then extracted with 75~80% ethyl alcohol, and extracting solution is dry
To medicinal extract.
3. a kind of madecassoside liposome according to claim 1 or 2, which is characterized in that the phosphatide is soybean
One of lecithin, egg yolk lecithin, hydrolecithin, hydroxylated lecithin, phosphatidyl choline, phosphatidyl diethanol amine or
Several mixtures.
4. a kind of madecassoside liposome according to claim 1 or 2, which is characterized in that the ceramide is
The mixture of one or more of ceramide I, ceramide II, Cera.
5. a kind of madecassoside liposome according to claim 1 or 2, which is characterized in that the plants essential oil is
Two or more mixtures during carrot seed oil, Rosa Damascana, olive oil, Butyrospermum parkii are oily.
6. a kind of madecassoside liposome according to claim 1 or 2, which is characterized in that the polyalcohol is 1,
The mixture of one or more of 3- butanediol, propylene glycol, 1,2- pentanediol, 1,2- hexylene glycol.
7. a kind of madecassoside liposome according to claim 1 or 2, which is characterized in that the antioxidant is
The mixture of one or more of Quercetin, alpha-tocopherol, astaxanthin.
8. a kind of madecassoside liposome according to claim 1 or 2, which is characterized in that the collagen is
Deep-sea cod collagen, coconut collagen, two or more mixtures in silk collagen.
9. a kind of madecassoside method for preparing lipidosome, which is characterized in that the preparation method comprises the following steps:
(1) it prepares oily phase: phosphatide, cholesterol, ceramide being melted in 65~80 DEG C of bath temperature conditions, added anti-oxidant
Agent is uniformly mixed, spare；
(2) it prepares water phase: madecassoside, polyalcohol, collagen being added in formula ratio purified water, stirs and heats
65~80 DEG C make madecassoside, collagen, polyalcohol dissolution, spare；
(3) it prepares colostrum: oil prepared by step (1) is mutually added dropwise in the water phase of step (2) preparation and is stirred continuously, then
10000rpm high speed shearing emulsification 2min, obtains colostrum；
(4) it prepares liposome: colostrum prepared by step (3) being kept the temperature under the conditions of 70 DEG C, then is set by high-pressure homogeneous equipment
Standby processing, pressure are 500bar~1500bar, and cycle-index is 2~8 times, are cooled to 50 DEG C；
(5) plants essential oil, fibroblast growth factor, Honegsukle flower P.E are added in (4), are stirred evenly, 800bar,
High-pressure homogeneous 1 time, it is cooling to get.
10. madecassoside liposome described in claim 1~8 any one is protected in the medicine adornment of prevention and treatment striae of pregnancy, effect
Application in skin product.
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