用毫微球增加体外小鼠腹腔巨噬细胞与大鼠肝细胞对庆大霉素的摄取

用³H-庆大霉素制备了聚氰基丙烯酸正丁酯毫微球。结果表明,毫微球可使小鼠腹腔巨噬细胞的cpm达³H-庆大霉素溶液对照组的6.34倍,使大鼠肝细胞的cpm在1,12和24h分别达到³H-庆大霉素溶液对照组的27.74,9.03和8.36倍。毫微球的粒径、使用的稳定剂种类、表面活性剂包裹以及庆大霉素的投药量等对摄取量均有明显影响。本研究为筛选细胞内给药系统提供了依据。

INCREASE OF GENTAMICIN UPTAKE IN CULTURED MOUSE PEKITONEAL MACROPHAGE AND RATHEPATOCYTES WHEN USED IN THE FORM OF NANOPARTICLES

The polybutylcyanoacrylate nanoparticles of 3H-labeled gentamicin were preparedin order to investigate the possi bili ty of gentamicin nanoparticles as an intracel l u lar dr ug de li ve rysystem for intracellular chemotherapy. The 3H-labeled gentamicin nanoparticles were incubated withmouse peritoneal macrophage(MPM)or rat hepatOcytes(RH)for some period,then the cells wereseparated from the nanoparticles, and finally the radiOactivity(cpm)of 3H in the cells were measuredby a liquid scintillation counter.By comparison with the solution of 3H-labeled gentamicin,a6.34times increase of cpm value in MPM after 30 min incubation , and 27. 74,9.03 and 8.36 timesincrease of MPM values in RH after 1,12, and 2 4 h incubation respectively l were observed bybinding gentamicin with polybutylcyanoacrylate nanoparticles,The particle size , surfactant coating,stabilizer and the gentamicin concentration were found to have some effect on the uptake ofnanoparticles by two kinds of cells.This study provided a basis for the screenning of intracellular drugdelivery system