Box-Behnken效应面法优化松果菊苷PLGA纳米粒处方工艺

Formula optimization of echinacoside-loaded PLGA nanoparticles by Box-Behnken design and response surface method

目的:优化松果菊苷(echinacoside,ECH)聚乳酸羟基乙酸[poly(lactic-co-glycolic acid),PLGA]纳米粒。方法:以PLGA为药物载体,采用复乳溶剂挥发法制备松果菊苷纳米粒。分别以PLGA质量浓度、泊洛沙姆188(poloxamer 188,F68)质量浓度、内水相油相体积比为考察对象,以包封率为和粒径为评价指标,采用Box-Behnken效应面法筛选最优处方。结果:最优处方为PLGA(w/v)5.00%,F68(w/v)2.57%,内水相油相体积比1∶1.163(0.86),所得纳米粒粒径为(149.42±1.56)nm,包封率为(88.39±2.18)%,与模型预测值接近。体外释放试验结果表明其具有缓释效果。结论:采用Box-Behnken效应面法优化松果菊苷PLGA纳米粒的处方是有效、可行的。

Objective： To optimize the formula of echinacoside-loaded PLGA nanoparticles. Methods： The nanoparticles were prepared by the complex emulsion solvent evaporation method using PLGA as drug carriers. The effects of the concentrations of PLGA and poloxamer 188（ F68）,and the internal water-oil phase ratio were investigated. According to the encapsulation efficiency and particle diameter,the formula was optimized by Box-Behnken design and response surface method. Results： The optimal formula was as follows： PLGA（ w / v） concentration was5. 00%,F68（ w / v） concentration was 2. 57%,and internal water-oil phase ratio was 1∶ 1. 163（ 0. 86）,respectively. The particle diameter was（ 149. 42 ± 1. 56） nm and the encapsulation efficiency was（ 88. 39 ± 2. 18） %,which were very close to the predicted values. Moreover,in vitro release tests showed that the prepared nanoparticles had sustained-release effects. Conclusion： It is effective and feasible to apply Box-Behnken design and response surface method for the formula optimization of the echinacoside-loaded PLGA nanoparticles.