摘要:
目的:优化改良自乳化溶剂扩散法制备冬凌草甲素聚乳酸纳米粒的制备工艺。方法:采用星点设计-效应面法,以冬凌草甲素在有机相中的浓度、载体在有机相中的浓度和水相与有机相的比例为考察因素,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模型,经效应面法预测最佳工艺条件。结果:优化的最佳因素范围为药物浓度X1:0.5～0.8 mg/mL;载体浓度X2:1.6～2.6 mg/mL;水油比X3:1～1.5。以优化条件制备的样品平均粒径为98.5 nm,包封率为（28.86±0.93）%,载药量为（8.23±0.35）%。结论:星点设计-效应面法适用于冬凌草甲素聚乳酸纳米粒的工艺优化,所建立的数学模型预测性良好。
Abstract:
Objective : To optimize the formulation of oridonin-loaded PLA nanoparticles with modified spontaneous emulsification solvent diffusion method. Methods :Applying central composite design and response surface method,choose the concentration of drug in organic phase,the concentration of PLA in organic phase and the ratio of water phase to organic phase as the influence factors.The evaluation parameters included entrapment efficiency,drug loading rate and particle size.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 : TThe range of the optimal conditions were the concentration of drug in organic phase 0.5～0.8 mg/mL,the concentration of PLA in organic phase 1.6～2.6 mg/mL,the ratio of water phase to organic phase 1～1.5 According to the optimal conditions,the mean particle size,entrapment efficiency and drug loading rate were 98.5 nm,（28.86 ±0.93） % and（8.23 ±0.35） %,respectively. Conclusion :The central composite design and response surface method are useful for the optimization of preparing oridonin-loaded PLA nanoparticles.The established model could predict the parameter of the formulations exactly and properly.
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