PLGA/TiO_2纳米药物缓释载体的研究  

PREPARATION AND CHARACTERIZATION OF PLGA/TiO_2 NANO DRUG DELIBERY CARRIERS

作　　者：张秀梅[1] 蔡静[2] 杨亚楠[2,3] 陈学思[4] 谢续明[3] 

机构地区：[1]吉林大学第一医院放射线科,长春130021 [2]长春工业大学化工学院,长春130012 [3]清华大学化工系高分子研究所,北京100084 [4]中国科学院长春应用化学研究所高分子物理与化学重点实验室,长春130022

出　　处：《高分子学报》2011年第6期653-660,共8页Acta Polymerica Sinica

摘　　要：首先利用硅烷偶联剂(KH550)对纳米二氧化钛表面进行预处理,得到氨基改性的二氧化钛,然后与带有高活性端基的丙交酯-乙交酯共聚物(PLGA)反应,制备纳米药物缓释载体PLGA/TiO2有机-无机杂化材料.通过核磁(1H-NMR)、傅里叶变换红外光谱仪(FTIR)、热重分析(TGA)、扫描电子显微镜(SEM)、透射电子显微镜(TEM)等测试方法对杂化材料的结构与形貌进行表征.结果表明,PLGA成功接枝到了TiO2纳米粒子的表面,平均接枝量为14%左右,与纯纳米TiO2粒子相比,杂化材料的分散性得到较好的改善,无明显团聚现象,并对模型药牛血清蛋白(BSA)表现出较好的吸附能力,吸附量由43.3%提高到81.3%.然后采用水包油包固体(S/O/W)乳化法以PLGA为载体分别包裹上述含药纳米TiO2粒子和杂化粒子,比较两者的载药量和包封率,发现后者的载药量和包封率显著提高分别为14.6%和96%,且微球表面光滑,体外释放中突释较小.A novel biodegradable PLGA/TiO2 organic-inorganic hybrid nano-material was prepared by the reaction between activated carboxyl-terminated PLGA,which was synthesized by PLGA and succinic anhydride with TEA as catalyzer,and amino-terminated TiO2 nano-particles which were modified by amino propyltriethoxysilane（KH550）.The structure and morphology of the materials were characterized by Fourier transform infrared spectroscopy（FTIR）,1H nuclear magnetic resonance（1H-NMR）,thermogravimetic analysis（TGA）,environmental scanning electron microscopy（ESEM） and transmission electron microscopy（TEM） methods.The results showed that the PLGA was grafted successfully on the surface of nano scale TiO2 particles with 14% average grafting;PLGA/TiO2 hybrid nano-material dispersed uniformly in BSA aqueous solution without obvious aggregation and showed a better adsorptivity（81.3%） to model drug BSA as compared with that（43.3%） of pure TiO2 nanoparticles.Different kinds of the nanopaticles containing proteins BSA（TiO2-BSA and PLGA/TiO2-BSA） were loaded into polymer microspheres with PLGA as carrier by the solid-in-oil-in-water emulsion method.The drug loading content,entrapment efficiency and drug release in vitro of different drug containing microspheres were tested.The results indicated that the microspheres of PTB/P showed smooth morphologies,high entrapment efficiency 96% and drug loading content 14.6% and decreased burst effect of drug,compared with TB/P microspheres.

关 键 词：纳米二氧化钛 PLGA 有机-无机杂化 药物缓释 

分 类 号：TQ460.1[化学工程—制药化工]