Formulation Optimization of Asiaticoside Cationic Liposomes by Using Central Composite Design-response Surface Method
10.6039/j.issn.1001-0408.2016.16.33
- VernacularTitle:星点设计-响应面法优化积雪草苷阳离子脂质体的处方Δ
- Author:
Xiang REN
;
Kun LIU
;
Li ZHANG
- Publication Type:Journal Article
- Keywords:
Asiaticoside;
Cationic liposomes;
Formulation optimization;
Central composite design-response surface method;
Drug release in vitro
- From:
China Pharmacy
2016;27(16):2272-2275
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE:To optimize the formulation of Asiaticoside cationic liposomes,and to investigate the characteristics of drug release in vitro. METHODS:The thin film dispersion method was used to prepare liposome;using encapsulation efficiency and drug-loading amount as index,the formulation of Asiaticoside liposomes was optimized by central composite design-response surface method with the ratio of drug to lipid(X1),the ratio of cholesterol to lipid(X2)and the concentration of D-mannose(X3) as factors. Using sodium lauryl sulfate as medium,in vitro release characteristics of cationic liposomes prepared with 1%octadecyl-amine was investigated by bag filter method,and compared with those of Asiaticoside solution and common liposome. RESULTS:The optimal formulation was X1 0.07,X2 0.17 and X3 0.03 g/ml. The encapsulation efficiency was (75.529 ± 1.071)%,and drug-loading amount was(2.539±0.029)%(n=3);the deviation from the predicted values were -0.217% and 0.205%;1% oc-tadecylamine was add into formulation to obtain cationic liposomes,and the Zeta potential had changed from -5.6 mV to 20.8 mV. in vitro accumulative release rates of Asiaticoside solution,common liposomes and cationic liposomes were 89.13%(12 h), 87.58%(72 h) and 94.46%(72 h),and the latter was in line with Weibull model. CONCLUSIONS:Asiaticoside cationic lipo-somes have high encapsulation efficiency,and can releases for 72 h.
