文献类型：期刊文献

中文题名：^(99)Tc^m-Cl_2MDP-明胶微粒的制备及其肝脾靶向性研究

英文题名：Preparation of 99Tcm-Cl_2MDP-loaded gelatin particles and its liver and spleen targeting study

作者：谭忠华[1];李培勇[1];朱以华[2]

机构：[1]上海第二医科大学附属瑞金医院核医学科;[2]华东理工大学超细材料制备与应用教育部重点实验室

年份：2005

卷号：25

期号：3

起止页码：181

中文期刊名：中华核医学杂志

外文期刊名：Chinese Journal of Nuclear Medicine

收录：北大核心:【北大核心2004】；CSCD:【CSCD2011_2012】；

语种：中文

中文关键词：靶向性研究;微粒;明胶;肝脾;^99Tc^m标记;亚甲基二膦酸盐;放射性核素显像;生物学分布;制备;药物包封;网状内皮系统;SD大鼠;静电吸附;脾巨噬细胞;包封技术;靶向输送;作用靶点;载药量;吸附法;连接;实验

外文关键词：Dichloromethylene diphosphonate; Gelatin particles; Pharmacokinetics; Radionuclide imaging; Rats

摘要：目的研究粒径300～500nm、表面带正电荷的明胶微粒对二氯亚甲基二膦酸盐(Cl2MDP)的包封技术,并观察明胶微粒和载药明胶微粒在SD大鼠体内的分布。方法通过静电吸附将Cl2MDP连接到明胶微粒表面完成药物包封。用99Tcm标记,进行SD大鼠生物学分布实验和显像,观察明胶微粒和Cl2MDP明胶微粒的组织靶向特性。结果通过静电吸附法可将Cl2MDP连接到明胶微粒表面,其药物包封效率约为20%,最大载药量达6mgmg明胶微粒;生物学分布实验和放射性核素显像示其具有较好的肝脾靶向性,可将Cl2MDP定向输送到巨噬细胞,肝脾的摄取超过注射量的60%。结论该明胶微粒具有良好的肝脾网状内皮系统靶向性,是较理想的以肝脾巨噬细胞为作用靶点的药物靶向输送载体;明胶微粒通过静电吸附的方法包封Cl2MDP简便可行,具有较高的药物包封效率和载药量。
Objective To investigate the coating technology of 300～500 nm, positive charged gelatin particles, encapsulate with dichloromethylene diphosphonate (Cl_2MDP), and to study the biodistribution of gelatin particles and drug-loaded gelatin particles. Methods Cl_2MDP was encapsulated on the surface of gelatin particles by static adsorption, and then labeled with 99Tcm. Biodistribution and radionuclide imaging were used to observe their tissue targeting characteristics in rats. Results Cl_2MDP can be facilely encapsulated to surface of gelatin particles with coating efficiency reached about 20%, and the maximal Cl_2MDP drug-loading amount was 6 mg/mg gelatin particles. Biodistribution and gamma imaging showed that more than 60% of injected particles were concentrated in macrophages of the liver and spleen. Conclusions The method of encapsulating Cl_2MDP is simple, convenient and highly efficient. Gelatin particles with diameter 300～500 nm and positive charged on their surface, have favorable targeting reticuloendothelial system characteristics in liver and spleen, and is a perfect carrier for those drug acting on macrophages.