星点设计效应面法优化盐酸米托蒽醌脂质体制备工艺

Optimization of Preparation of Mitoxantrone Hydrochloride Loaded Liposomes by Using Central Composite Design Response Surface Methodology

目的 借助星点设计效应面法确定盐酸米托蒽醌脂质体最优制备工艺。方法 采用冷冻干燥-pH梯度法制备盐酸米托蒽醌脂质体,以包封率(Y)为评价指标,考察盐酸米托蒽醌脂质体制备过程中载药温度(X 1)、载药时间(X 2)及药脂比(X 3)对制剂的影响,并以效应面法预测最优的制备工艺。结果 优化制备工艺中载药温度59℃,载药时间14min,药脂比1∶ 6.7(w/w),采用以上工艺制备三批脂质体平均包封率为99.1±0.4%。结论 星点设计效应面法所建立的数学模型可以较好的用于盐酸米托蒽醌脂质体制备工艺的优化。

OBJECTIVE To optimize the preparation process of mitoxantrone h ydrochloride loaded liposomes by using central composite design response surface methodology (RSM-CCD). METHODS Liposomes were prepared by fre eze drying-pH gradient method.Encapsulation efficiency (Y) was taken as a resp onse variable,and incubation temperature (X 1),incubation time (X 2),drug t o lipid ratio (X3) were selected as independent variables.The optimal prepara tion process was predicted by response surface methodomogy. RESULTS The optimal levels of X 1,X 2,X 3 were 59℃,14min and 1∶ 6.7(w/w)res pectively.T he mean encapsulation efficiency was 99.1± 0.4%. CONCLUSION T he model established by the RSM-CCD method could be used for optimization of th e preparation of mitoxantrone hydrochloride loaded liposomes.