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% octadecylamine 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% octadecylamine 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 liposomes have high encapsulation efficiency, and can releases for 72 h.
关键词
积雪草苷阳离子脂质体处方优化星点设计-响应面法体外释药
Keywords
AsiaticosideCationic liposomesFormulation optimizationCentral composite design-response surface methodDrug release in vitro