星点设计-效应面法优化长春新碱长循环纳米粒的制备工艺  

Optimization of Vincristine Long-Circulation Nanoparticles Preparation by Central Composite Design-Response Surface Method

作　　者：封烨 周朝阳 刘芊芊 杨阳 李敏才[1] FENG Ye;ZHOU Chao-yang;LI Min-cai(Hubei University of Science and Technology,Xianning Hubei 437100,China)

机构地区：[1]湖北科技学院,湖北咸宁437100 [2]军事科学院军事医学研究院

出　　处：《湖北科技学院学报（医学版）》2020年第4期296-301,F0002,共7页Journal of Hubei University of Science and Technology(Medical Sciences)

基　　金：国家“重新药创制”科技重大专项资助项目(2018ZX09711003-008)。

摘　　要：目的制备载长春新碱(VCR)的聚乳酸-羟基乙酸共聚物(PLGA)纳米粒,采用星点设计-效应面法筛选优化制备工艺。方法通过纳米沉淀法制备PLGA,以粒径和包封率为评价指标,采用星点设计-效应面法对PLGA的处方进行筛选,优化载药纳米粒的制备工艺。结果VCR长循环纳米粒(VCR-NPs)的最佳处方和工艺条件为:用量为4.0mg,水相体积4.0mL,PLGA用量为20mg。该工艺制备的载药纳米粒平均粒径为177.9nm,包封率为81.39%,载药量为6.32%,Zeta电位为-30.7mV。结论沉淀法适用于制备长循环VCR-NPs,星点设计-效应面法可优化获得载药纳米粒的最佳制备工艺,所得的载药纳米粒包封率和载药量较高,稳定性好。Objective To prepare vincristine long-circulation nanoparticles and optimize preparation process of nanoparticles by central composite design-response surface method.Methods PLGA were prepared through nanoprecipitation method.To optimize the preparation process of nanoparticles,central composite design-response surface method were conducted to screen the prescription of PLGA taking particle size and encapsulation rate as evaluation parameters.Results The optimal formulation of vincristine PLGA nanoparticles was as follows:the dosage of vincritine was 4.0 mg,the volume of aqueous phase was 4.0 mL,and the dosage of PLGA was 20 mg.According to the preparation process of vincristine nanoparticles,the average particle size was 177.9 nm,the encapsulation rate was 81.39%,the drug loading was 6.32%,and the Zeta potential was-30.7 mV.Conclusion Nanoprecipitation method is suitable for the preparation of vincristine long-circulation nanoparticles.The encapsulation rate,drug loading and stability of drug loaded nanoparticles were higher after optimizing by the central composite design-response surface method.

关 键 词：长循环纳米粒 长春新碱 纳米沉淀法 星点设计-效应面法 

分 类 号：R943[医药卫生—药剂学]