快速膜乳化法制备荧光探针PLGA纳米粒及体内外研究  

In vitro and in vivo study of fluorescent probe PLGA particles prepared by premix membrane emulsification method

作　　者：胡涛[1,2] 石飞燕[1,2] 潘林梅[1,2] 朱华旭[1,2] 郭立玮[1,2] 

机构地区：[1]南京中医药大学江苏省中药资源产业化过程协同创新中心,江苏南京210023 [2]南京中医药大学药学院江苏省植物药深加工工程研究中心,江苏南京210023

出　　处：《中国中药杂志》2014年第23期4583-4589,共7页China Journal of Chinese Materia Medica

基　　金：国家自然科学基金项目(81072749;81303230;30873450;30873449);江苏省抗肿瘤验方研究与产业化工程实验室开放课题;南京中医药大学校级创新团队项目;江苏省高校优势学科建设工程项目

摘　　要：采用快速膜乳化法制备了粒径均一的聚乳酸-羟基乙酸共聚物(PLGA)纳米粒,对其载药特性和体内分布进行研究。以平均粒径和PDI为指标,通过单因素实验考察了膜孔径、过膜次数、过膜压力、油水比和聚乙烯醇(PVA)浓度对快速膜乳化法制备纳米粒的影响,空白纳米粒的优化条件为膜孔径1μm,过膜压力1 150 k Pa,油水比1∶5,PVA质量浓度20 g·L-1,过膜3次,得到空白纳米粒的平均粒径为332.6 nm,PDI为0.010。采用激光共聚焦技术对其结构特点进行模拟研究,在此基础之上,将荧光探针包载于纳米粒中,采用小动物活体成像技术研究纳米粒的体内靶向性。体外模拟研究表明,荧光物质均匀分布于微球内,体内研究表明该粒子具有较好的肝、脾靶向性。Relatively uniform-sized nanoparticles made of poly （lactic-co-glycolic acid） （PLGA） were prepared by premix membrane emulsification method. After the drug loading property was completed, the dynamic tissue distribution of uanoparticles was recorded. With the average particle size and span as indexes, membrane pore size, number of passing membrane times, membrane pressure, volume ratio of oil-water phase and the concentration of poly（vinyl alcohol） （PVA） in external water phase were investigated by single factor test, the optimum preparation technology of blank PLGA nanlparticles was as following： pore size of SPG membrane was 1μm, membrane pressure was 1.15 MPa, the number of passing membrane time was 3, the mass fraction of PVA of 2%, volume ratio of oil-water phase of 1： 5. Prepared nanoparticles were round with smooth surface, the mean diameter was 332. 6 nm, span was 0. 010, the confocal laser scanning microscope （CLSM） concluded that fluorescent substance is uniform composizion in PLGA nanoparticle, and the in vivo imaging technology in mice include that the nanoparticles show good liver and spleen targeting property.

关 键 词：快速膜乳化 聚乳酸-羟基乙酸共聚物 纳米粒 工艺优选 荧光探针 靶向 

分 类 号：TQ460.1[化学工程—制药化工]