星点设计-效应面法优化丹参酮ⅡA纳米粒的制备工艺

 目的研究星点设计-效应面法优化沉淀法制备丹参酮ⅡA-PLGA纳米粒制备工艺的可行性。方法以PVA浓度、药物在有机相中的浓度、PLGA与药物的用量比以及水相与有机相的体积比为考察因素,以包封率、载药量及药物利用率为考察指标,根据星点设计原理进行实验安排,并用多元线性回归及二项式拟合建立指标与因素之间的数学关系,经效应面法预测最佳工艺条件。结果各指标的二项式拟合方程均优于多元线性回归方程,以优化条件制备的样品平均粒径为225nm,包封率为(95.49±0.68)%、载药量为(2.03±0.03)%、药物利用率为(38.42±0.65)%。结论星点设计-效应面法适用于丹参酮ⅡA-PLGA纳米粒的工艺优化,所建立的数学模型预测性良好。

Optimized Preparation of Tanshinones Ⅱ A-Loaded Nanoparticles by Central Composite Design and Response Surface Method

OBJECTIVE To study the feasibility of optimizing the formulation of tanshinones ⅡA-loaded PLGA nanoparticles with nanoprecipitation method by central composite design and response surface method.METHODS The influence factors included the concentration of PVA,the concentration of drug in organic phase,the ratio of PLGA to drug and the ratio of water phase to organic phase.The evaluation parameters included entrapment efficiency,drug loading and recovery of drug.Experiments were done on the theory of central composite design.The data were simulated using multi-linear equation and second-order polynomial equation.The possibly optimal formulation was predicted by response surface method.RESULTS The results showed that the latter was prior to the former.According to the optimal conditions,the mean diameter,entrapment efficiency,drug loading and recovery of drug were 225 nm,(95.49±0.68)%,(2.03±0.03)% and(38.42±0.65)%,respectively.CONCLUSION The central composite design and response surface method are useful for the optimization of preparing tanshinones ⅡA-loaded PLGA nanoparticles.The estimation of the established model is good.