顺铂聚乳酸微球的药物释放特性及肝动脉栓塞研究

对顺铂聚乳酸微球进行了体外药物释放和家犬肝动脉栓塞研究。该微球粒径范围为50～200μm,平均粒径为115.76±35.94μm,顺铂含量为37.16%(W/W);体外药物释放机制符合Higuchi方程;肝动脉栓塞后8h,肝组织顺铂浓度高达21.55±12.18μg/g,明显高于肝动脉灌注顺铂组:3.16±0.09μg/g(P<0.05);肝动脉栓塞组的顺铂血浓峰值、各取血点浓度及曲线下面积AUC皆低于肝动脉灌注顺铂组。可望达到提高栓塞部位的药物疗效,降低全身毒副反应的作用。

CHARACTERISTICS OF CDDP—PLA MICROSPHERES IN VITRO AND IN VIVO

Studies on the drug release in vitro and hepatic arterial chemoembolization in rivo were carried out with the newly developed CDDP—PLA microspheres. The mechanism of the in vitro release was shown to conform to Higuchi equation. After chemoembolization the CDDP—PLA microspheres showed remarkably lower CDDP concentrations in the general circulation and much higher concentrations in the hepatic tissue e. g. up to 21.55±12. 18 μg/g at 8 h, which is much higher than that (3. 16±0. 09 μg/g) of the CDDP in hepatic arterial infusions. Thus, the CDDPPLA microspheres may improve the curative effects and lower the side effects, especially the kidney toxicity, of the anticancer drug cisplatin.