载异烟肼、利福平白蛋白纳米粒的制备及其体外释药研究  

Preparation and in vitro release of albumin nanoparticles loaded with isoniazid and rifampicin

作　　者：马荣[1] 陈振[1] 张惠勇[1] 杨小英[2] 王文萍[3] 戈朝晖[4] 

机构地区：[1]宁夏医科大学研究生院,银川750004 [2]宁夏医科大学总医院药剂科,银川750004 [3]宁夏医科大学药学院,银川750004 [4]宁夏医科大学总医院骨科,银川750004

出　　处：《第三军医大学学报》2013年第21期2336-2339,共4页Journal of Third Military Medical University

基　　金：国家自然科学基金(30960391);宁夏自然科学基金(NZ13144)~~

摘　　要：目的研究载异烟肼(isoniazid,INH)、利福平(rifampicin,RFP)牛血清白蛋白(bovine serum albumin,BSA)纳米粒的制备及体外释药特性。方法以白蛋白为载体聚乳酸为骨架,采用改良自乳化-溶剂扩散法制备纳米粒。采用透射电镜观察纳米粒形态;激光粒度衍射分析仪测定纳米粒粒径分布;高效液相色谱法测定纳米粒的载药量和包封率;动态膜透析法观察载药纳米粒的体外释药特性。结果制备的INH-RFP-BSA-NPs电镜下观察外观圆整,大小均匀、分散性好,粒径为(60.5±4.6)nm。异烟肼、利福平的载药量分别为19.8%、20.1%,包封率分别为87.8%、98%。INH至6 d时累计释放97.02%,RFP至5d时完全释放。结论以白蛋白和聚乳酸为载药基质,采用改良自乳化-溶剂扩散法可制备出粒径小、载药量和包封率较高的载异烟肼、利福平白蛋白纳米粒,体外释药显示载异烟肼、利福平白蛋白纳米粒具有良好的缓释作用。Objective To prepare of bovine serum albumin nanoparticles loaded with isoniazid and rifampicin（INH-RFP-BSA-NPs） and investigate its in vitro release characteristics.Methods INH-RFP-BSANPs were prepared by modified self-emulsion solvent diffusion method.Albumin and polylactic acid was used as a carrier as well as skeleton structure.Transmission electron microscopy was used to observe the morphology of INH-RFP-BSA-NPs.The nanoparticle＇s size and distribution of INH-RFP-BSA-NPs were performed by submicron particle size analyzer.High performance liquid chromatography（HPLC） was used to measure the drug loadings and the coating rate of INH-RFP-BSA-NPs.Dynamic membrane dialysis was used to study the in vitro release characteristics of INH-RFP-BSA-NPs.Results The INH-RFP-BSA-NPs were smooth,sphere-like,relatively uniform in size and good dispersion.The submicron particle size analyzer showed the diameter was60.5±4.6 nm.The drug loading and entrapment efficiency of isoniazid were 19.8% and 87.8% respectively,and those of rifampicin were 20.1% and 98% respectively,INH cumulative release of 97.02% to 6 d,RFP to5 d fully released.Conclusion INH-RFP-BSA-NPs can be prepared by drug-loading with albumin and polylactic acid,matrix modified self-emulsion solvent diffusion,with higher encapsulation efficiency,higher drug loading,and smaller particle size.In vitro drug release shows INH-RFP-BSA-NPs has good slow release effect.

关 键 词：白蛋白 异烟肼 利福平 纳米粒 体外释药 

分 类 号：R912[医药卫生—药学] R944.9