摘要
阿克拉霉素Ａ聚氰基丙烯酸异丁酯毫微粒的冻干针剂，能明显抑制体外培养人肝癌细胞株７７０３的生长，ＩＣ５０为０．２８μｇ·ｍｌ－１。在０．８μｇ·ｍｌ－１浓度时，克隆形成抑制率为９０％，抑制作用有明显剂量依赖关系而未见明显时间依赖关系。静脉给药后，对常位移植人肝癌模型裸小鼠的抑瘤率为８６．８４％，肿瘤细胞增殖活性阳性率为２０．８３％。体内外均显示明显的抗肝癌活性，且体内抗肝癌活性比阿克拉霉素Ａ冻干针剂强。
This paper reports the results of experiments on the
antihepatoma effects of live targeted drug delivery system
lyophilized aclacinomycin A polyisobutylcyanoacrylate
nanoparticle(ACM-IBC-NP )in vitro and in vivo. The median inhibition
concentration were found to be 0.28 μg·ml-1 and 0.34μg·ml-1 of
lyophilized ACM-IBC-NP and ACM respectively in vitro. The
inhibition ratio of colony formation were found to be 99%and 88%of
lyophilized ACM-IBC-NP and ACM respectively in vitro,The antihepatoma
activity was shown to be significantly concentration dependent.The
results showed that lyophilized ACM-IBC-NP and ACM possess strong
cytotoxicity on human hepatoma cell 7703,and the cytotoxicity was
not significantly different between lyophilized ACM-IBC-NP and ACM
in vitro. The model of orthotopic transplantation of human hepatoma
in nude mice were used for evaluation of the activity of lyophilized
ACM-IBC-NP against hepatoma. The tumor inhibition rate were found
to be 86.84%for lyophilized ACM-IBC-NP and 46.69%for ACM. The cell
proliferative activity of hepatoma were found to be 20.83%by
lyophilized ACM-IBC-NP and 72.50%by ACM;All the results indicate
that lyophilized ACM-IBC-NP and ACM have clinical application
potential and the antihepatoma activity of lyophilized ACM-IBC-NP was
obviously higher than that of ACM.
出处
《药学学报》
CAS
CSCD
北大核心
1995年第3期179-183,共5页
Acta Pharmaceutica Sinica
基金
国家自然科学基金
卫生部青年科学基金
