白蛋白微球作为肝靶向给药载体的研究

用均匀设计方法和计算机技术筛选了乳化化学交联法制备白蛋白微球的六个因素,十二个水平。优化出最佳制备工艺,制备了平均粒径0.41～0.47μm的白蛋白微球。将此工艺制备的¹²⁵I-白蛋白微球做动物体内研究,结果表明微球iv后主要浓集在肝脏,可达注入总剂量的68%,此微球在靶组织肝脏的变化规律可用二室模型契合。

STUDY ON ALBUMIN MICROSPHERES AS DRUG CARRIER FOR LIVER TARGETING

In this paper 6 factors and 12 levels of each variable were selected by Uniform Design Method and computer for preparing albumin microspheres with emulsion- chemical crosslinking. An optimal procedure for preparing albumin microspheres was established and the mean diameter of albumin microspheres is 0. 41～0. 47μm. Albumin was labelled with ¹²⁵Ⅰ-isotope and ¹²⁵Ⅰ-albumin microspheres were prepared according to the optimal procedure. The suspension of ¹²⁵Ⅰ-albumin microspheres with 0. 1% Tween-80 saline was injected Via mice tail vein. The animals were sequentially killed and the radioactivity of blood, spleen, liver, kidney, stomach, heart, lung, thyroid and brain were measured. The results showed that albumin microspheres were accumulated mainly in the liver, about 68% of the injected dose at the peak concentration. The pharmacokinetics of albumin microspheres in liver was also studied and twe--compartmental model can be used to describe the regulation.