以聚乳酸为载体的药物释放及动物疗效学的研究

STUDIES OF THE IN VITRO AND IN VIVO RELEASE OF5-FLUOROURACIL FROM POLYLACTIC ACID COMPOSITE

本文采用熔融共混的方法，以可生物降解的聚乳酸为载体，制成合抗癌药５－Ｆｕ（五氟尿嘧啶）的复合针，对该针进行了体外药物释放测定，表明（１）复合针可缓慢释放药物，（２）复合针的药含量越大，体外释药速度越快，（３）聚乳酸分子量越大，体外释药越慢，释药期越长。此外研究了该复合针的动物疗效学，结果表明载体分子量ＭＷ＝２５ｘ１０４、药物含量为４０％或５０％的复合针抑瘤率明显提高，且毒性明显降低。

The polymer-drug composite was prepared by incorporating an antican-cer drug(5-fluorouracil)in the melted polylactic acid and shaping into aform of needles.The in vitro release of 5-Fu from the ncedles wasinvestigated- The results show that the needles could gradually releasedrug for sixmonths or more.The release rate. of 5-Fu was acceleratedwith increase in drug loading and decrease in the molecular weight ofpolylactic acid. In in vivo, experiments the needles were impianted su-bcutaneously in mice for anticancer effect during the 14 days test peri-od. In the case of anticancer rates,all test groups showed higher antic-ancer effect than control ones according to both the death rate andweight loss of mice, and the test groups showed lower toxic reactionthan control ones.These results assurcd that the 5-Fu needles withpolylactic acid conld keep prolonged drug releasein mice for anticancerpurpose.