星点设计-效应面法优化穿心莲总内酯固体脂质纳米粒处方

Formula optimization of total lactones in Andrographis-loaded solid lipid nanoparticles by central composite design-response surface methodology

目的优选穿心莲总内酯固体脂质纳米粒(TLA-SLN)的处方。方法以穿心莲中4种内酯类成分包封率的满意度函数作为评价指标,采用冷却高压均质法制备穿心莲总内酯固体脂质纳米粒,考察药脂比、磷脂脂质比、Tween-80在水中质量分数对评价指标的影响,并运用星点设计-效应面法对结果进行多元线性和二项式拟合,优选最佳的工艺条件。结果从相关系数及各指标二项式拟合方程均优于多元线性回归方程,冷却压均质工艺能有效制备固体脂质纳米粒,优化的最佳处方为药脂比为10%、磷脂脂质比1.25、Tween-80在水中的质量分数为4%,实测值与理论预测值偏差小于7%。结论星点设计-效应面法能有效优选穿心莲总内酯固体脂质纳米粒处方。

AIM To optimize the formula of total lactones in Andrographis-loaded solid lipid nanoparticles （TLA-SLN）. METHODS TLA-SLN was prepared by cold-high pressure homogenization technique. With the desirability functions of the entrapment efficiency of four lactones as the evaluation index, the influences of the ratios of drug to lipide, lecithin to lipide and concentration of Tween-80 in water on it were investigated. Central composite design-response surface methodology was applied to the optimal conditions for TLA-SLN preparation, and the data were analyzed using multi-linear equation and second-order polynomial equation. RESULTS The correlation coefficients of second-order polynomial equation was prior to multi-linear equation. The TLA-SLN formulation was optimized as ratio of drug to lipide of 7% , lecithin to lipide of 1.25, and Tween-80 concentration of 4%. The deviations of desirability function values between the observed and the predicted were less than 7%. CONCLUSION Central composite design-response surface methodology is successfully used to optimize the formulation of TLA-SLN.