阿克拉霉素A聚氰基丙烯酸异丁酯毫微粒动物体内分布研究

 分别对￣３Ｈ－阿克霉素Ａ聚氰基丙烯酸异丁酯毫微粒尾静脉ｉｖ给药和ｐｏ给药后小鼠体内分布特点及其与￣３Ｈ－阿克拉霉素Ａ水溶液的比较进行了研究。毫微粒制剂在小鼠各脏器中相对放射性强度以肝脏最高，尾静脉ｉｖ与ｐｏ给药分别达给予量的７１．２１％与５３．７６％，分别是￣３Ｈ－阿克拉霉素Ａ水溶液分布量的３．６２倍和３．９５倍。常位移植人肝癌模型裸小鼠尾静脉ｉｖ￣３Ｈ－阿克拉霉素Ａ聚氰基丙烯酸异丁酯毫微粒后各脏器分布特点与正常小鼠相似，肝癌组织中相对放射性强度达给予量的８．７９％，是￣３Ｈ－阿克拉霉素Ａ水溶液的９．３９倍。电镜观察发现载药毫微粒可进入肝脏实质细胞浆与肝脏枯否氏细胞浆中，也可进入肝脏瘤组织中。

Distribution of aclacinomycin A loaded nanoparticles in mice and humanhepatocellular carcinoma bearing nude mice

The distribution characteristics of aclacinomycin A polyisobutylcyanoacrylatenanoparticle(ACM- IBC- NP)in mice and human hepatocellular carcinoma bearing nude mice werestudied.￣3H as a tracer isotope was labelled in aclacinomycin A(ACM),and ￣3H-ACM-IBC-NP wasprepared with a diameter of 85 ± 31 nm。 The relative radioactivity of various organs and bloodwere detected by liquid scintillation counting technique。 The relative radioactivity of liver was thehighest in various organs after ￣3H-ACM-IBC-NP was injected via mice tail vein and orally admin-istered,and it was obviously different from ￣3H-ACM solution。The distribution of ￣3H-ACM-IBCNP in human hepatocellular carcinoma bearing nude mice after iv administration was also studiedand the radioactivity of carcinoma in situ was higher than ￣3H-ACM solution。The ￣3H-ACM-IBC-NP was discovered in cytoplasm of Kupffer’s cells and parenchyma cells,and in liver tumor tissueby TEM method:The results demonstrated that ￣3H-ACM-IBC-NP not only concentrated in liverbut also targets in liver tumor,and two administration routes can be used for liver targeting。