摘要
目的优化利福平聚乳酸-羟基乙酸共聚物纳米粒(RFP-PLGA-NPs)的制备工艺,并分析其制剂学性质。方法以PLGA为载体,采用改良的自乳化溶剂蒸发法(M-SESD)制备RFP-PLGA-NPs。以粒径、包封率、载药量为指标,采用正交设计法优化处方和制备工艺。结果制备RFP-PLGA-NPs的优化条件为PLGA 100 mg,poloxsmer 188质量分数1.0%,丙酮与乙醇体积比3:1,有机相体积15 mL。按优化条件所制备的RFP-PLGA-NPs的粒径为(128.73±4.07)nm,多分散系数(PDI)为0.046～0.105,包封率(65.84±0.69)%,载药量(3.78±0.14)%。结论该工艺简单、稳定性好,为后续RFP-PLGA-NPs的体内研究奠定了基础。
A/M To prepare rifampiein poly（lactic-co-glycolic acid）copolymer（PLGA） nanoparticles （RFP-PL- GA-NPs）with optimization. METHODS RFP-PLGA-NPs were prepared by modified spontaneous emulsification solvent diffusion（M-SESD）with the PLGA as its carrier. The orthogonal design was carried out to optimize the preparing technolo- gy according to particle size, entrapment efficiency and drug loading of RFP-PLGA-NPs. RESULTS The optimal condi- tiom for the preparation of RFP-PLGA-NPs were 100 mg PLGA, 1.0 % poloxamer 188（m/V） ,acetone/ethanol 3：1（ V/ V） and 15 mL organic phase. The mean particle size of the resulted RFP-PLGA-NPs was （128.73 ± 4.07）nm and the polydispersity index（PDI） was 0. 046 - 0. 105, the average entrapment efficiency and drug loading was （65.84 ± 0.69）% and （3.78±0.14）% , respectively. CONCLUSION An optimized nanoparticle drug delivery system is ob- tained by M-SESD and provides foundation for further pharmacokinetic research.
出处
《中国临床药学杂志》
CAS
2012年第4期210-213,共4页
Chinese Journal of Clinical Pharmacy
基金
杭州市卫生科技计划重点项目(编号2010Z007)
关键词
利福平
聚乳酸-羟基乙酸共聚物
纳米粒
正交设计
rifampicin
poly（lactic-co-glycolic acid） copolymer
nanoparticle
orthogonal design
