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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 echinacoside (ECH) poly (lactic-co-glycolic acid) (PLGA) nanoparticles. Methods: PLGA as the drug carrier, the use of complex emulsion solvent evaporation prepared echinacoside nanoparticles. The mass concentration of PLGA, poloxamer 188 (F68) concentration and the volume ratio of oil phase in inner water phase were taken as the targets respectively. The encapsulation efficiency and particle size were used as evaluation indexes. The Box-Behnken effect surface method Filter the best prescription. Results: The optimal formulation was 5.00% of PLGA (w / v), 2.57% of F68 (w / v) and 1: 1.63 (0.86) of the inner aqueous phase. The particle size of the obtained nanoparticles was (149.42 ± 1.56) nm , The entrapment efficiency was (88.39 ± 2.18)%, close to the model predictive value. In vitro release test results show that it has a sustained release effect. Conclusion: Box-Behnken effect surface optimization of echinacosin PLGA nanoparticles prescription is effective and feasible.