正交实验联用星点设计-效应面法优化紫草素脂质体处方

Optimized formulation of alkanin liposome by a combination of orthogonal design with central composite design/response surface method

目的:用乙醇注入法制备紫草素脂质体,使用正交设计并结合星点设计/效应面法优选最佳处方。方法:以紫草素与脂质比,豆磷脂与胆固醇比,乙醇量与水量比,豆磷脂浓度和甘露醇浓度5个影响因子进行正交实验;进一步采用星点设计优化处方,实验结果进行多元线性和二项式、三项式非线性方程拟合,效应面法确定最佳处方配比。结果:三次多项式是描述各指标与因素之间的最佳模型。优化处方制备脂质体的包封率为85.4%、载药量为5.16%,理论预测值与实测值偏差较小,模型具有良好的预测性。结论:正交设计联用星点设计-效应面优化法筛选脂质体处方是一种简便、可行的实验设计方法。

AIM：To select an optiomal formulation of liposome entrapped alkanin prepared with ethanol injection in the combination of orthogonal design and central composite design/Response surface method.METHODS：Five influencing factors,including ratio of alkanin to liposome and soyabean lecithin to cholesterol,volume ratio of ethanol phase to water phase,soybean concentration and mannitol concentration were chosen as indices by orthogonal design.Then the method utilized the central composite design,which fitted multivariate linear and second/third order nonlinear regression equation,to find out the optimal formulation.RESULTS：Third order regression equation gained made the good prediction about entrapment（85.4%） and alkanin load（5.16%）,and exhibited no significant difference between theoretic value and measured value.CONCLUSION：The combination of orthogonal design with central composite design is a feasible and convenient method to optimize the prescription of alkanin-lipo-some.