肝靶向米托蒽醌聚乳酸毫微粒冻干针剂抗肝癌活性及毒性研究  

Study on the anti-hepatocellular tumour activity of the liver targeted mitoxantrone polylactic acid extended-release nanoparticles

作　　者：徐超群[1] 张志荣[2] 廖工铁[2] 牛洁[3] 荣祖元[3] 

机构地区：[1]四川省中药研究所,成都610041 [2]四川大学华西药学院,成都610041 [3]四川抗菌素工业研究所,成都610041

出　　处：《四川生理科学杂志》2002年第1期30-32,共3页Sichuan Journal of Physiological Sciences

摘　　要：目的 :观察对米托蒽醌聚乳酸毫微粒肝靶向制剂 (DHAQ PLA NP)的抗肝癌活性及毒理。方法 :采用常位移植鼠肝癌瘤株的小鼠肝癌模型 ,(DHAQ PLA NP)的抗肝癌活性进行了研究。结果 :显示DHAQ PLA NP对H2 2 实体型肝癌的抑瘤率高于DHAQ水针剂。用免疫组化 (HIC)SP法染色显示肿瘤增殖细胞 ,计算阳性百分率 ,DHAQ PLA NP组增殖细胞阳性率低于DHAQ水针剂组 ,说明靶向制剂具有良好的抗增殖细胞活性。测定靶向制剂的LD50 为 1 5 7mg·kg 1,与水针剂LD50 文献值 1 3 6mg·kg 1比较[1] ,表明靶向制剂毒性与水针剂接近。结论 :DHAQ PLA NP有良好的肝靶向性 。The anti hepatocellular tumour activity of the liver targeted mitoxantrone polylactic acid extended release nanoparticles (DHAQ PLA NP) was tested by using orthtopic transplanting hepatocellular carcinoma model in mice. The rrate of tumour inhibition of DHAQ PLA NP is 12.8% higher than that of the DHAQ injection. The anti proliferating cell activity of DHAQ PLA NP was also higher than that of the DHAQ injection. The acute toxicity test showed the LD 50 of DHAQ PLA NP is 15.7mg·kg 1 . It is higher than the LD 50 (13.6mg·kg 1 ) of DHAQ injection. This result indicates the toxicity of DHAQ PLA NP is lower of not higher than that of DHAQ injection.

关 键 词：米托蒽醌 聚乳酸毫微粒 肝靶向制剂 抗肝癌活性 

分 类 号：R735.7[医药卫生—肿瘤]