【摘要】 目的筛选出表阿霉素脂质体的最佳处方。方法采用三因素三水平的Box-Behnken设计,利用响应曲面法对影响表阿霉素脂质体包封率和载药量的主要因素(脂质体膜材料中胆固醇与氢化磷脂的摩尔比,脂质体溶液中的磷脂浓度,表阿霉素与氢化磷脂的质量比)进行研究,以脂质体的包封率和载药量为响应函数,建立相应的数学模型,优化处方。结果最优处方是脂质体膜材料中胆固醇与氢化磷脂的摩尔比为0.8,脂质体溶液中的磷脂浓度为10mmol/L,表阿霉素与氢化磷脂的质量比为0.18。结论Box-Behnken实验设计法用于表阿霉素脂质体处方的优化筛选是可行的,数学模型的预测值与实验观察值相符。更多还原

【Abstract】 Purpose To optimize the formulation parameters of an epirubicin liposome preparation for maximum encapsulation efficiency and drug loading amount.Methods A three-factor,three-level Box-Behnken experimental design was employed,with the molar rate of Chol:HSPC(X1),the phospholipid concentration of liposomes(X2),the quality rate of epirubicin:HSPC(X3) as the independent variables.The response variable was encapsulation efficiency and drug loading amount.Results The optimization formulation was as follows:X1,X2 and X3 levels of 0.8,10mmol/L and 0.18,respectively.Conclusions The observed responses are in close agreement with the predicted values of the mathematic models,and the Box-Behnken design is suitable for optimizing the formulation of epirubicin liposome.更多还原