改良自乳化-溶剂扩散法制备甲基莲心碱纳米粒的研究

Preparation of neferine nanoparticles by modified self-emulsion solvent diffusion method

目的制备甲基莲心碱纳米粒(NEF-NP),并采用正交试验设计对甲基莲心碱纳米粒制备工艺进行优化。方法以包封率和载药量为评价指标,采用聚乳酸-羟基乙酸共聚物(PLGA)为载体,丙酮-无水乙醇为有机溶剂,通过正交设计优化改良自乳化-溶剂扩散法制备载NEF的PLGA载药纳米粒的处方工艺。结果优化的最佳处方工艺为:PLGA的浓度为20 mg.mL-1,NEF的投药量为3.3 mg,PVA浓度为1.0%,水相与有机相的体积比为8∶1。最佳条件下制得的纳米粒平均包封率达(70.35±1.16)%,载药量(2.33±1.08)%,平均粒径为(213.5±2.7)nm。结论最佳处方工艺制备的NEF-PLGA纳米粒具有较高的包封率、载药量和较小的粒径。

Objective To prepare neferine nanoparticles（NEF-NP）,and optimize the neferine nanoparticle preparation by orthogonal design.Methods According to the entrapment efficiency and drug loading,optimized nanoparticale formulations were prepared by modified self-emulsification-solvent diffusion method with poly（lactic-co-glycolic） acid（PLGA） as the carrier material and acetone-ethanol as the organic solvent by orthogonality design.Results The best preparation condition was： the concentration of PLGA was 20 mg·mL-1,the dosage of NEF was 3.3 mg,the ratio of water phase and organic phase was 8∶1.The average encapsulation efficiency of resultant nanoparticles was（70.35±1.16）%,the drug loading was（2.33±1.08）%,and the mean particle size was（213.5±2.7）nm.Conclusion NEF-loaded PLGA nanoparticles prepared by the optical formulation method have higher encapsulation efficiency,higher drug loading,and smaller particle size.