紫杉醇PLGA纳米粒的处方优化与评价  

Preparation and Formulation Optimization of Paclitaxel PLGA Nanoparticles

作　　者：王俊[1] 刘哲鹏[1] WANG Jun;LIU Zhepeng(University of Shanghai for Science and Technology,Shanghai,200093,China)

机构地区：[1]上海理工大学,上海200093

出　　处：《肿瘤药学》2021年第1期52-57,共6页Anti-Tumor Pharmacy

摘　　要：目的采用生物可降解材料乳酸-羟基乙酸共聚物(PLGA)为载体,比较不同的制备方法和工艺对紫杉醇(PTX)PLGA纳米粒(PTX-PLGA NPs)粒径的影响,筛选出最优制备工艺,并考察所制备纳米粒的体外表征以及对人源胃癌细胞SGC-7901的抗肿瘤效果,为紫杉醇缓释制剂在胃癌中的开发提供一定的实验基础。方法采用单因素实验法优化PTXPLGA NPs的制备处方及工艺,对粒径、Zeta电位、形态、稳定性、包封率和载药量及体外释放进行表征,在SGC-7901细胞中考察PTX-PLGA NPs的体外抗肿瘤效果。结果制得的PTX-PLGA NPs平均粒径为(219.9±4.5)nm,表面电位为(-21.7±1.81)mV,载药量为(4.42±1.33)%,包封率为(80.73±2.66)%,外观圆整,在37℃下PTX-PLGA NPs能够在含有血清的PBS中保持稳定72 h。24 h时,PTX-PLGA NPs的体外释放率仅24%。PTX-PLGA NPs对人胃癌细胞SGC-7901的IC_(50)为1.56×10^(-10)mol·L^(-1),是游离PTX IC_(50)的44.4%,具有较好的抗肿瘤效果。结论所制备的PTX-PLGA NPs粒径分布均一、稳定性好、载药量高、具有缓释效果,且对胃癌细胞SGC-7901有明显的抗肿瘤作用。Objective Using biodegradable material lactic acid-glycolic acid copolymer[poly(lactic-co-glycolic acid),PLGA]as carrier,to compare the effects of different preparation methods and formulations on the particle size of paclitaxel(PTX)PLGA nanoparticles(PTX-PLG A NPs),to select the optimized formulation,and to investigate the in vitro characterizations and anti-tumor effects of PTX-PLGA NPs on human gastric cancer cell line SGC-7901,so as to provide an experimental basis for a new paclitaxel formulation in the treatment of gastric cancer.Methods The formulations and methods of PTX-PLGA NPs were optimized by single factor experimental method.The particle size,zeta potential,morphology,stability,entrapment efficiency,drug loading and in vitro release of PTX-PLGA NPs were characterized.The anti-tumor effects of PTX-PLGA NPs in vitro were investigated in SGC-7901 cells.Results The average particle size of the PTXPLGA NPs was(219.9±4.5)nm,zeta potential(-21.7±1.81)mV,drug loading(4.42±1.33)%,and entrapment efficiency(80.73±2.66)%.It showed a nearly sphere appearance.It was stable in PBS containing serum for at least 72 h at 37℃,and 24%was released in vitro within 24 h.On human gastric cancer cell SGC-7901,the IC_(50) of PTX-PLG A NPs was 1.56×10^(-10) mol·L^(-1),which was 44.4%of free PTX IC_(50).It showed good anti-tumor effects.Conclusion The optimized PTX-PLGA NPs has uniform particle size distribution,good stability,high drug loading and sustained release effect,and has obvious anti-tumor effects on gastric cancer cell line SGC-7901.

关 键 词：紫杉醇 乳酸-羟基乙酸共聚物 纳米粒 复乳法 缓释 胃癌 

分 类 号：R944.15[医药卫生—药剂学] R735.2[医药卫生—药学]