CN108721348A - A kind of asiaticoside liposome and preparation method thereof - Google Patents
A kind of asiaticoside liposome and preparation method thereof Download PDFInfo
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Abstract
A kind of asiaticoside liposome of present invention proposition and preparation method thereof, belongs to drug and medicine manufacture technology field.Asiaticoside fat limbs include lecithin, cholesterol, asiaticoside and ultra-pure water, and the mass ratio of lecithin and cholesterol is 4-8 ﹕ 1；The mass ratio of lecithin and asiaticoside is 20-40：1；The volume ratio of organic phase and water phase is 5-7 ﹕ 1.Method：Lecithin, cholesterol are weighed by a certain percentage, and lecithin, cholesterol are dissolved in chloroform；The aqueous solution of asiaticoside is added, ice-water bath ultrasound forms uniform emulsion；By emulsion rotary evaporation to gel state is formed, appropriate ultra-pure water solution is added；Continuing revolving makes colloid fall off in 1 hour, and ice-water bath ultrasound is up to liposome beneficial effects of the present invention：The present invention have good percutaneous abilities and slow release effect, can be permanently effective act on lesion, realize better therapeutic effect.
Description
Technical field
The invention belongs to drug and medicine manufacture technology field, more particularly to a kind of asiaticoside liposome and its preparation
Method.
Background technology
Asiaticoside (centella total glucosides, CTG) is the extract of samphire centella,
Active ingredient is triterpene type saponin(e and its derivative species, wherein with the content highest of asiaticosid, madecassoside, activity is most
By force.Modern pharmacological studies have shown that：CTG can not only promote cell growth, accelerating wound healing to repair skin injury, also have
It is anti-oxidant, the effects that antiulcer, anti-inflammatory.Clinically it is usually used in operation wound, burn, the treatment of the diseases such as hyperplastic scar.But
Due to being mostly polarity macromolecular in CTG, it is not easy to reach diseased region through skin epidermis, simple rush, which is oozed, to be fully achieved
Treat the purpose of disease.
By drug encapsulation in liposome, good transdermal enhancing effect can be not only played, also drug can be made as few as possible
Into blood circulation, skin focus is concentrated on, forms drug depot, slow releasing pharmaceutical is Utopian dermal topical application carrier.
Compared with common external preparation, liposome can increase the therapeutic index of drug, reduce administration number of times and dosage, improve patient's
Compliance.It is examined it is therefore desirable to optimize the preparation process of CTG liposomes, and to its physicochemical property and transdermal test in vitro characteristic
It examines.
Invention content
For the formulation optimization problem of asiaticoside liposome, the present invention passes through on the basis of early stage work study
Optimize the preparation process of asiaticoside liposome using single factor test combination Box-Behnken effect surface methods.
A kind of asiaticoside liposome, including lecithin, cholesterol, asiaticoside and ultra-pure water, and lecithin with
The mass ratio of cholesterol is 4-8 ﹕ 1；The mass ratio of lecithin and asiaticoside is 20-40：1；The volume of organic phase and water phase
Than for 5-7 ﹕ 1.
Further, 23.22 ﹕ 1 of mass ratio of 4 ﹕ 1 of mass ratio of lecithin and cholesterol, lecithin and asiaticoside,
7 ﹕ 1 of volume ratio of organic phase and water phase.
A kind of preparation method of asiaticoside liposome, includes the following steps：
S1, lecithin, cholesterol are weighed by a certain percentage, lecithin, cholesterol are dissolved in chloroform；
S2, the aqueous solution for adding asiaticoside, ice-water bath ultrasound, form uniform emulsion；
S3, by emulsion rotary evaporation to gel state is formed, appropriate ultra-pure water solution is added；
S4, continue revolving and so that colloid is fallen off in 1 hour, ice-water bath ultrasound is up to liposome.
Further, it is described by emulsion rotary evaporation to gel state is formed, appropriate ultra-pure water solution, hydration temperature is added
It is 50 DEG C.
The present invention advantageous effects be：Madecassoside, centella in the asiaticoside liposome of the present invention
It is respectively that 52.10%, 45.97%, CTG liposomes, 2 kinds of ingredient percutaneous rates are smaller than raw material that the external 12h of glycosides, which adds up release rate,
Drug solns, liposome group show apparent slow release；The skin hold-up of 2 kinds of active ingredients of liposome group is above aqueous solution
Control group prompts drug to focus primarily upon skin focus, and slow releasing function is generated in the form of reservoir.
Description of the drawings
In order to keep the purpose of the present invention, technical solution and advantageous effect clearer, the present invention provides following attached drawing and carries out
Explanation：
Fig. 1 is A and B (1), A and the reciprocation of C (2), B and C (3) to Y1The contour map (a) and three-dimensional of influence
Effect surface figure (b)；
Fig. 2 is A and B (1), A and the reciprocation of C (2), B and C (3) on the Y2 contour maps (a) influenced and three-dimensional
Effect surface figure (b)；
Fig. 3 is the electron microscope (a), particle diameter distribution (b) and Zeta potential (c) of CTG liposomes；
The curve of Fig. 4 madecassosides (a), asiaticosid (b) Cumulative release amount Q and time t；
Fig. 5 is the curve that madecassoside, asiaticosid accumulate transdermal amount Qn and time t；
Fig. 6 is madecassoside, asiaticosid skin hold-up Qs and time t block diagram；
Wherein：A indicates the mass ratio of lecithin-cholesterol；B indicates the mass ratio of lecithin-CTG；C indicates organic phase-
The volume ratio of water phase；Y1The encapsulation rate of asiaticosid；Y2The encapsulation rate of madecassoside.
Specific implementation mode
In order to make those skilled in the art be better understood when the purpose of the present invention, technical solution and advantageous effect, below
It is completely described with attached drawing is illustrated in conjunction with specific embodiments.
Embodiment 1
1, the measurement of CTG liposome encapsulations
CTG liposomes are taken, methanol demulsification is added, 0.22 μm of membrane filtration takes total drug that subsequent filtrate measures liposome to contain
Measure WAlways.Liposome and free drug are detached using ultra-filtration centrifuge tube, separately take CTG liposomes in ultra-filtration centrifuge tube, 4000r/
Min centrifugations 20min takes outer tube solution, measures the content W trips of free drug.Encapsulation rate is calculated as follows：
YEncapsulation rate=(1-WTrip/WAlways) × 100%
2, the screening of CTG method for preparing lipidosome
1) film dispersion method weighs lecithin 200mg, cholesterol 50mg, chloroform dissolving, and rotary evaporation is to forming uniform fat
Matter film.Continue to vacuumize 20min and eliminates organic solvent.The aqueous solution oscillation hydration 1h that CTG is added makes film separation.Ice-water bath
Ultrasound extremely forms liposome turbid liquor.Centella, glycosides madecassoside encapsulation rate be respectively 65.50%, 56.79%.
2) alcohol injection weighs lecithin 200mg, cholesterol 50mg, and absolute ethyl alcohol dissolving slowly at the uniform velocity instills CTG
Aqueous solution, 300r/min constant temperature stir 1h, revolving remove ethyl alcohol, ice-water bath it is ultrasonic CTG liposomes.Asiaticosid, hydroxyl product
The encapsulation rate of Asiaticoside is respectively 61.77%, 52.51%.
3) reverse phase evaporation weighs lecithin 200mg, cholesterol 50mg, is dissolved in chloroform, and the aqueous solution of CTG, ice water is added
Bath ultrasound, forms uniform emulsion.Appropriate aqueous solution is added to gel state is formed in rotary evaporation, and continuing revolving 1h keeps colloid de-
It falls.Ice-water bath ultrasound is up to liposome.Asiaticosid, madecassoside encapsulation rate be respectively 74.11%, 60.05%.
Above 3 kinds of methods have larger water capacity with liposome prepared by reverse phase evaporation, are suitable for water soluble drug
Encapsulating, the encapsulation rate highest of CTG liposomes.Therefore select reverse phase evaporation for the preparation of CTG liposomes.
3, CTG liposomes single factor exploration
1) mass ratio of lecithin-cholesterol
The mass ratio of fixed lecithin-CTG is 20 ﹕ 1, and the volume ratio of organic-aqueous is 5 ﹕ 1, and aqueous vehicles are super for 2ml
Pure water, the mass ratio for choosing lecithin-cholesterol are respectively that 2 ﹕ 1,3 ﹕ 1,4 ﹕ 1,5 ﹕ 1,6 ﹕ 1 prepare liposome, are shown in Table 1, as a result
Show：With the increase of lecithin, the encapsulation rate of two kinds of ingredients is in the trend of first increases and then decreases；When lecithin-cholesterol
Quality it is smaller when (2:1,3:1), in hydration stage, colloid falls off difficulty, and standing overnight liposome solutions, to generate flocculation heavy
Shallow lake phenomenon prompts the mass ratio of lecithin-cholesterol to have preferable stability in 4-8 ﹕ 1.
Influence of the mass ratio of 1 lecithin of table-cholesterol to CTG encapsulation rates
2) mass ratio of lecithin-CTG
The mass ratio of fixed lecithin-cholesterol is 4 ﹕ 1, and the ratio of organic-aqueous is 5：1, aqueous vehicles are that 2ml is ultrapure
Water, the mass ratio for choosing lecithin-CTG are respectively that 1 ﹕ 1,5 ﹕ 1,10 ﹕ 1,20 ﹕ 1,40 ﹕ 1 prepare liposome, are shown in Table 2, as a result table
It is bright：The mass ratio of lecithin-CTG is the notable factor for influencing liposome encapsulation, and excessive or too small encapsulation rate is relatively low, wherein
When the mass ratio of lecithin-CTG is 20 ﹕ 1, liposome encapsulation is high.
Influence of the mass ratio of 2 lecithin-CTG of table to CTG encapsulation rates
3) volume ratio of organic-aqueous
The mass ratio of fixed lecithin-cholesterol is 4 ﹕ 1, and the mass ratio of lecithin-CTG is 20：1, aqueous vehicles 2ml
Ultra-pure water, the ratio for choosing organic-aqueous is 4 ﹕ 1,5 ﹕ 1,6 ﹕ 1,7 ﹕ 1,8 ﹕ 1 prepare liposome, is shown in Table 3, the results showed that：When having
For the volume ratio of machine phase-water phase in 5-7 ﹕ 1, the emulsion of formation is more uniform, no lamination, and encapsulation rate is high.
Influence of the volume ratio of 3 organic-aqueous of table to CTG encapsulation rates
Embodiment 2
1, the experimental data of CTG liposomes formulation optimization
To advanced optimize CTG liposome prescriptions, on the basis of single factor exploration, the matter of lecithin-cholesterol is chosen
Amount than (A), 3 notable variables of volume ratio (C) of the mass ratio (B) of lecithin-CTG, organic-aqueous, with asiaticosid,
Encapsulation rate Y1, Y2 of madecassoside are response, are optimized, are passed through using Box-Behnken effect surface methods
Dseign-Expert softwares carry out response surface analysis to experimental result, test arrangement and the results are shown in Table 4, and variance analysis is shown in Table 5.
Table 4：Response surface analysis scheme and experimental result
Table 5：Variance analysis
| Soruces of variation | Quadratic sum | Degree of freedom | F values | P values | Soruces of variation | Quadratic sum | Degree of freedom | F values | P values |
| Y1Model | 988.37 | 9 | 19.28 | 0.0004 | Y2Model | 1143.31 | 9 | 17.44 | 0.0005 |
| A | 294.76 | 1 | 51.74 | 0.0002 | A | 160.38 | 1 | 22.02 | 0.0022 |
| B | 132.11 | 1 | 23.19 | 0.0019 | B | 217.67 | 1 | 29.88 | 0.0009 |
| C | 52.99 | 1 | 9.3 | 0.0186 | C | 100.32 | 1 | 13.77 | 0.0075 |
| AB | 1.51 | 1 | 0.27 | 0.6222 | AB | 1.04 | 1 | 0.14 | 0.7167 |
| AC | 59.44 | 1 | 10.43 | 0.0144 | AC | 235.93 | 1 | 32.39 | 0.0007 |
| BC | 138.89 | 1 | 24.38 | 0.0017 | BC | 155.88 | 1 | 21.4 | 0.0024 |
| A2 | 3.83 | 1 | 0.67 | 0.4395 | A2 | 5.27 | 1 | 0.72 | 0.4231 |
| B2 | 285.24 | 1 | 50.07 | 0.0002 | B2 | 241.04 | 1 | 33.09 | 0.0007 |
| C2 | 8.14 | 1 | 1.43 | 0.2708 | C2 | 13.06 | 1 | 1.79 | 0.2224 |
| Residual error | 39.88 | 7 | Residual error | 50.99 | 7 | ||||
| Lose analog values | 24.88 | 3 | 2.21 | 0.2292 | Lose analog values | 22.53 | 3 | 1.06 | 0.4604 |
| Pure error | 15 | 4 | Pure error | 28.46 | 4 | 7.12 |
2, models fitting
Analyzing processing is carried out to data using Design-Expert softwares, with evaluation index Y1、Y2Mould is carried out to independent variable
Type process of fitting treatment, with related coefficient (R2) and confidence level (P) be model of fit evaluation.Obtain secondary multinomial regression equation:Y1=-
27.54 +11.77A-0.74B+23.46C-0.03AB-1.92AC+0.49BC-0.24A2-0.06B2-1.39C2, Y2
=-127.24+23.84A-1.24B-39.91C+0.02AB-3.84AC+0.52BC-0.27A2-0.05B2-1.76
C2, the size of every absolute coefficient directly reflects influence degree of each factor to analog value in fit equation, and coefficient is just
The negative direction for reflecting its influence.The influence sequence of preparation process known to equation is the volume ratio > lecithins of organic-aqueous
The mass ratio of the mass ratio > lecithin-CTG of fat-cholesterol.
The model dependency coefficients R known to fitting result2(R1 2=0.9612, R2 2=0.9573) it is all higher than 0.95, explanation
There is high correlation between measured value and predicted value, can accurately predict actual conditions；Correct coefficient of determination R2 Adj(R1 2 Adj=
0.911 3, R2 2 Adj=0.9073), illustrate that the experimental error is smaller, operation is credible；Model P values are respectively less than 0.01, and the model is quasi-
It is right higher, great statistical significance.It loses and intends item P values more than 0.05, model, which loses, to be intended not significantly, which can preferably intend
True effect surface is closed, can be used to reflect the mass ratio of lecithin-cholesterol, the mass ratio of lecithin-CTG, organic-aqueous
Influence of the volume ratio to liposome encapsulation, model can be used for optimizing the preparation process of CTG liposomes.
3, parameter prediction and process optimization
Make contour and three-dismensional effect surface chart by multiple regression equation, the best prescription of prediction CTG liposomes matches,
Results model Y1See Fig. 1, model Y2See Fig. 2.
It was found from regression coefficient significance test result：In model Y1In：A (P=0.0002), B (P=0.0019), C2
(P=0.0002), BC (P=0.0017) item is extremely notable, and significantly, other do not show by C (P=0.0184), AC (P=0.0144)
It writes；Model Y2In：A (P=0.0022), B (P=0.0009), C2 (P=0.0002), BC (P=0.0024), C (P=
0.0075), AC (P=0.0007) item is extremely notable, other are not notable；It follows that influence of each factor to response is simultaneously
Non- simple linear relationship, there are reciprocations between selected factor.
The contour map and three-dismensional effect surface chart of effect surface can it is intuitively interactive strong and weak between reaction factor and
The value of each factor under optimal conditions.Contour is oval and more intensive, then shows influence of the influence factor to response
Greatly, reciprocation is strong；Response surface 3D figures are more bent, are precipitous, show that reciprocation is more apparent.Model Y1In, AC, BC effect surface etc.
The high oval reciprocation of line chart is strong, but BC effect surface 3D figure curved surface bending degree is slightly larger, and BC is to influence asiaticosid encapsulating
The dominating interaction factor of rate.Model Y2In, AC effect surface contour maps are oval, and the 3D figure curved surface gradients are precipitous, show AC
It is most strong to madecassoside encapsulation rate value reciprocation.Design-Expert softwares preferably go out best liposome preparation prescription：
23.22 ﹕ 1 of mass ratio of mass ratio 4 ﹕ 1, lecithin-CTG of lecithin-cholesterol, 7 ﹕ 1 of volume ratio of organic-aqueous.
Embodiment 3
1, the preparation of confirmatory experiment
3 batches of CTG liposomes are prepared by optimal preparation process, measure the encapsulation rate of two kinds of ingredients, asiaticosid actual measurement is average
Encapsulation rate is 84.94%, RSD 1.51%, which is 87.30%；The average encapsulation rate of madecassoside actual measurement
For 75.85%, RSD 2.26%, predicted value 78.67%.The measured value of each index is close with predicted value, and relative deviation is low
In 3%, show that the model has good predictability, and process stabilizing is feasible.
2, CTG liposomes, grain size and Zeta potential measure
Using the form of scanning electron microscopic observation CTG liposomes, take liposome appropriate, be diluted to debita spissitudo, drop on a small quantity in
On glass slide, natural air drying, then after vacuum metallizing, observes its form at room temperature.It is flat that liposome is surveyed using laser particle analyzer
Equal particle diameter distribution and Zeta potential.As shown in Figure 3, the results showed that liposome is adhered in class ball-type, surface rounding, nothing, grain size
For 201.7nm, Zeta potential is -15.7mv.
3, the outer drug release determination of CTG Via Liposomes
Using《Chinese Pharmacopoeia》Four dissolution rates of version in 2015 are surveyed with third method (small-radius curve track) in drug release determination method
It is fixed, relevant parameter：37.5 DEG C of temperature, rotating speed 120r/min, dissolution medium are the physiological saline 100ml of degassing.Precision pipettes
CTG liposome turbid liquors and each 6ml of raw material medicine solution are respectively placed in the bag filter handled well, are tightened and are tied to digestion instrument stirring
On paddle, micropore is crossed respectively at 1,2,3,4,5,6,7,8,10,12h positioning draw solution 2ml (while supplementing 2 ml of equality of temperature medium)
After filter membrane, HPLC method sample detections calculate the Cumulative release amount Q at sample each time point, and map to time t, see Fig. 4.As a result
Show：It is respectively 52.10%, 45.97% that the external 12h of madecassoside, asiaticosid, which adds up release rate, in liposome；Have
Apparent slow release effect, in contrast, almost release is complete in free drug 7h.
Embodiment 4
1, the preparation of isolated skin
Use 8%Na2S solution sloughs the hair of mouse web portion, for 24 hours afterwards puts to death mouse, removes skin of abdomen, uses physiology salt
Water is cleaned, and is set in physiological saline, in 4 DEG C of preservations.
2, in vitro transdermal test
Using Franz diffusion cell methods, in vitro transdermal test is carried out.By skin be fixed on diffusion cell supply chamber and receiving chamber it
Between, precision pipettes CTG liposome turbid liquors, raw material medicine solution 2mL in skin surface respectively, and 20% ethyl alcohol-life is added in acceptance pool
Brine is managed, emptying bubble makes corium side be completely attached to receiving liquid.Bath temperature is 32 DEG C, magnetic stirring speed 200r/
min.Respectively at 4,8,12,16,20, for 24 hours, take out and receive medium 2mL, while the fresh reception for adding into acceptance pool equivalent is situated between
Matter.The reception medium of taking-up measures content after 0.22 μm of filtering with microporous membrane.With Qn=(VAlwaysCn+ΣCn-1VIt takes(Qn is)/A
Accumulate transdermal amount, VAlwaysFor acceptance pool volume, Cn is the sub-sampling measured concentration, and n indicates sampling number；V is each sample volume,
A is infiltrating area) unit of account area accumulation infiltration capacity.It is mapped with Qn-t, sees Fig. 5, and carry out to percutaneous absorption rate curve
Models fitting, as a result asiaticosid, madecassoside meet zero-order release model in aqueous solution.Percutaneous rate fit equation
Respectively Qn=28.50t-58.87, R2=0.995；Qn=16.46t-37.01, R2=0.983.Asiaticosid, madacasso
Careless glycosides liposome meets higuchi drug release models, and percutaneous rate fit equation is respectively Qn=139.74 t1/2- 241.2, R2=
0.987；Qn=67.93t1/2- 50.34, R2=0.988.The result shows that 2 kinds of ingredient percutaneous rates of CTG liposomes are smaller than original
Expect that drug solns, liposome group show apparent slow release.
3, skin hold-up is tested
Take CTG liposome turbid liquors, raw material medicine solution, carry out transdermal experiment as stated above, respectively 4,8,12,16,
20, the skin after taking penetrating absorption to be administered for 24 hours, gently tries net remained on surface, the circle pieces of skin of radius 8mm is laid with card punch,
It shreds, physiological saline 0.5mL homogenate is added, 1.0mL water-saturated n-butanols, vortex 5min, 13000r/min centrifugation is added
30min detaches organic layer, nitrogen drying.Residue 0.1mL methanol dissolves, vortex 5min mixings, 10000r/min centrifugations
15min takes supernatant HPLC methods to detect, and calculates different time unit area skin hold-up Qs (Qs=Cs × 0.1/A；Cs
Drug quality concentration in the skin samples liquid measured for n-th of time point, A are infiltrating area), see Fig. 6.The result shows that：Through for 24 hours
After transdermal, liposome group madecassoside, asiaticosid skin hold-up be respectively 76.0 μ g/cm2、48.7μg/cm2；
Aqueous solution group is 34.7 μ g/cm2、29.3μg/cm2.After transdermal for 24 hours, the skin hold-up of 2 kinds of active ingredients of liposome group
It is above aqueous solution control group, drug is prompted to focus primarily upon skin focus, slow releasing function is generated in the form of reservoir.
Prepare that there are many Effect of liposome factor, previous experiments have investigated the mass ratio of lecithin-CTG, lecithin-cholesterol
Mass ratio, the type and dosage of organic phase, the factors such as aqueous vehicles type and dosage, hydration temperature encapsulation rate is influenced, hair
Existing fat material solute effect in chloroform is best, and can shape without ultrasound after foaming phenomena, with water phase mixing during formation gel
At uniform emulsion, therefore select chloroform for organic phase；Preliminary experiment prepares liposome with PBS buffer solution (phosphate buffered saline solution),
In hydration stage, gel falls off not exclusively, and residual quantity is big, and occurs lamination after standing overnight, therefore selects ultra-pure water for water
Change medium；Hydration temperature has investigated 40 DEG C, 50 DEG C, 60 DEG C, wherein 50 DEG C of whens it is required hydration time it is short, gel is easy to fall off and fat
Liposome stability is preferable, thus select 50 DEG C for hydration temperature.Lecithin-on the basis of single factor test screens to being affected
The mass ratio of CTG, the mass ratio of cholesterol-lecithin, organic-aqueous volume ratio using Box-Behnken effect surfaces method into
Row Optimum Experiment obtains optimal processing parameter, and is verified to optimal prescription, and relative deviation is smaller, shows the regression model
It can preferably predict the encapsulation rate of CTG liposomes, prediction of result is accurate, true and reliable.It is orthogonal and equal with what is generally used at present
Even design optimization technique is compared, and Box-Behnken effect surfaces method can be analyzed continuously testing each level, is reflecting each factor
While influence in various degree on preparation process, the reciprocation between factor is also intuitively embodied, there is experimental precision height, prediction
The good advantage of property.
Pilot production dialysis during detaching free drug with liposome is longer the time required to finding；Gel column color
Spectrometry, poor reproducibility the phenomenon that drug leakage can occur in elution process because of the dilution of eluant, eluent；Ultrafiltration centrifugal process effect
Preferably, and separation is rapid, therefore uses the encapsulation rate of ultrafiltration centrifugal determination CTG liposomes.
Result is investigated from transdermal test in vitro：The Qn-t curves of madecassoside and asiaticosid have similitude,
Reason may be：The chemical constitution, property and molecular weight of the two have similitude.It will be appreciated from fig. 6 that percutaneous dosing early period, CTG fat
Compared with raw material medicine solution no significant difference, increase at any time, liposome transdermal rate gradually drops the percutaneous rate of 2 kinds of ingredients of plastid
It is low；Skin hold-up is experiments have shown that the skin hold-up of liposome group madecassoside, asiaticosid is respectively 76.0 μ g/
cm2、 48.7μg/cm2；Aqueous solution group is 34.7 μ g/cm2、29.3μg/cm2, opposite to improve 1.56 and 1.17 times.The above institute
For embodiment, further detailed description has been carried out to the object, technical solutions and advantages of the present invention, it should be understood that with
Upper illustrated embodiment is only the preferred embodiment of the present invention, is not intended to limit the invention, all spirit in the present invention
With any modification, equivalent substitution, improvement and etc. made for the present invention within principle, should be included in protection scope of the present invention it
It is interior.
Claims (4)
1. a kind of asiaticoside liposome, it is characterised in that：Including lecithin, cholesterol, asiaticoside and ultra-pure water, and
The mass ratio of lecithin and cholesterol is 4-8 ﹕ 1；The mass ratio of lecithin and asiaticoside is 20-40: 1；Organic phase and water
The volume ratio of phase is 5-7: 1.
2. a kind of asiaticoside liposome according to claim 1, it is characterised in that：The quality of lecithin and cholesterol
Than 4 ﹕ 1,23.22 ﹕ 1 of mass ratio of lecithin and asiaticoside, 7 ﹕ 1 of volume ratio of organic phase and water phase.
3. a kind of preparation method of asiaticoside liposome, which is characterized in that include the following steps：
1) lecithin, cholesterol are weighed by a certain percentage, and lecithin, cholesterol are dissolved in chloroform；
2) aqueous solution of asiaticoside is added, ice-water bath ultrasound forms uniform emulsion；
3) by emulsion rotary evaporation to gel state is formed, appropriate ultra-pure water solution is added；
4) continuing revolving makes colloid fall off in 1 hour, and ice-water bath ultrasound is up to liposome.
4. a kind of preparation method of asiaticoside liposome, it is characterised in that：It is described by emulsion rotary evaporation to forming gel
State, is added appropriate ultra-pure water solution, and hydration temperature is 50 DEG C.
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| CN201910181648.6A CN109999070B (en) | 2018-04-27 | 2019-03-11 | Herba centellae total glycoside liposome and preparation process thereof |
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| CN115068352A (en) * | 2022-06-01 | 2022-09-20 | 吉林大学 | Oil-control polypeptide flexible liposome hydrogel and preparation method and application thereof |
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| CN1228042C (en) * | 2003-01-30 | 2005-11-23 | 上海家化联合股份有限公司 | Asiaticoside liposome and its use |
| CN103893122B (en) * | 2014-03-28 | 2017-09-26 | 华南理工大学 | A kind of madecassoside liposome and preparation method and application |
| CN107550849A (en) * | 2017-09-08 | 2018-01-09 | 华南理工大学 | A kind of madecassoside lipidosome gel of local topical and preparation method thereof |
| CN107744502A (en) * | 2017-09-08 | 2018-03-02 | 华南理工大学 | A kind of madecassoside liposome of high encapsulation rate and high stability and preparation method and application |
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| CN115068352A (en) * | 2022-06-01 | 2022-09-20 | 吉林大学 | Oil-control polypeptide flexible liposome hydrogel and preparation method and application thereof |
| CN115068352B (en) * | 2022-06-01 | 2023-10-20 | 吉林大学 | Oil control polypeptide flexible liposome hydrogel and preparation method and application thereof |
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| CN109999070A (en) | 2019-07-12 |
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