星点设计-响应面法优化积雪草苷阳离子脂质体的处方 点击下载
论文标题: 星点设计-响应面法优化积雪草苷阳离子脂质体的处方
英文标题:
中文摘要: 目的:优化积雪草苷阳离子脂质体的处方,并对其体外释药特性进行考察。方法:采用薄膜分散法制备脂质体;以包封率、载药量为指标,以积雪草苷与磷脂质量比(药脂比,X1)、胆固醇与磷脂质量比(X2)、D-甘露糖质量浓度(X3)为因素,采用星点设计-响应面法优化处方;以十二烷基硫酸钠为介质,采用透析袋法考察加入1%十八胺所制阳离子脂质体的体外释药特性,并与积雪草苷的溶液及普通脂质体进行比较。结果:最优处方为X1 0.07、X2 0.17、X3 0.03 g/ml,所得积雪草苷脂质体的包封率为(75.529±1.071)%、载药量为(2.539±0.029)%(n=3),与预测值的偏差分别为-0.217%与0.205%;脂质体加入1%十八胺后其电位由     -5.6 mV变为20.8 mV,证实形成阳离子脂质体。积雪草苷溶液、普通脂质体、阳离子脂质体的体外累积释药率分别为89.13%(12 h)、87.58%(72 h)、94.46%(72 h),后者释药符合Weibull模型。结论:所得积雪草苷阳离子脂质体包封率较高,可持续72 h释药。
英文摘要: 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.
期刊: 2016年第27卷第16期
作者: 任翔,刘琨,张莉
英文作者: REN Xiang,LIU Kun,ZHANG Li
关键字: 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: Asiaticoside; Cationic liposomes; Formulation optimization; Central composite design-response surface method; Drug release in vitro
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