沉淀法制备甲基莲心碱聚乳酸-羟基乙酸共聚物纳米粒

Preparation of neferine-loaded PLGA nanoparticles using precipitation method

目的:制备甲基莲心碱聚乳酸-羟基乙酸共聚物纳米粒(Nef-PLGA-NPs)。方法:以聚乳酸-羟基乙酸共聚物(PLGA)为载体,丙酮为有机溶剂,通过正交试验设计优化沉淀法制备甲基莲心碱PLGA纳米粒的工艺。结果:最佳工艺条件为:PLGA的质量浓度为10 mg.mL-1,Nef的质量浓度为1.0 mg.mL-1,水相与有机相的体积比为20∶1。纳米粒平均包封率为(85.3±0.8)%,平均载药量为(7.75±0.07)%,平均粒径为(82.9±1.2)nm。结论:优化条件下采用沉淀法制备的甲基莲心碱PLGA纳米粒包封率高、载药量大,平均粒径小。

OBJECTIVE To prepare neferine-loaded PLGA nanoparticles （Nef-PLGA NPs）. METHODS Nanoparticales were prepared by a precipitation method with poly （lactic-co glycolic） acid （PLGA） as carrier material and acetone as organic solvent, then optimize the formulations by design of orthogonality. RESULTS The best preparation condition： the concentra tion of PLGA was 10 mg·mL^-1 , the concentration of Nef was 1.0mg·mL^-1 , the ratio of water phase and organic phase was 20： 1. The average encapsulation efficiency of resultant nanopartieles was（85.3 ±0. 8） %, the average drug loading was（7. 75 ±0. 07）%, the mean particle size was（82. 9 ±1.2）nm. CONCLUSION Under the optimum conditions, Nef-loaded PI.GA nano-particles prepared by a precipitation method are found to be a high encapsulation efficiency and drug loading, a smaller particle size.