单抗导向阿霉素免疫毫微粒的~(131)I标记及其体内抗肝癌作用
The Labeling of Adriamycin-loaded Human Serum Albumin Immunonanoparticles Led by Monoclonal Antibodies With ~(131)I and Its Anti-hepatoma Effect in Vivo
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摘要: 将HAb18-ADR-HSA-NP和ADR-HSA-NP或其131I标记物进行荷肝癌裸鼠实验,观察其在动物体内对肝癌细胞的靶向性及其抑瘤作用。结果表明:HAb18-ADR-HSA-NP的有效载药量为1.44%,比ADR-HSA-NP(1.69%)有所降低;呈缓慢释药状,其最大释药量(41%)明显低于ADR-HSA-NP(65%)(P<0.05)。正常裸鼠显像显示,131I-HAb18-ADR-HSA-NP在体内的趋肝性和稳定性均优于131I-ADR-HSA-NP,肝脏清除较131I-ADR-HSA-NP慢。HAb18-ADR-HSA-NP主要滞留于瘤体,随时间延长,其滞留量明显多于ADR-HSA-NP(P<0.05);它能明显抑制癌细胞生长,其抑癌率显著高于ADR-HSA-NP(P<0.05)。因此,HAb18-ADR-HSA-NP在体内能和肝癌细胞结合并抑制其生长。Abstract: The pharmaceutics character, targeting to hepatoma and anticancer activity in nude mice of adriamycinloaded human serum albumin immunonanoparticles (ADRHSANP) against hepatoma led by antihuman hepatoma monoclonal antibodies HAb18 are studied. The results show that effective loaded drug dose of HAb18ADRHSANP is 1.44%, which is lower than ADRHSANP(1.69%); HAb18ADRHSANP slowly releases drug ADR and its maximum releasing drug dose(41%)is obviously lower than ADRHSANP(65%) (P<0.05); nowever, 131IHAb18ADRHSANP mainly accumulates in liver and its liertaxis and stability are better than 131IADRHSANP in nude mice by intravenous injection; HAb18ADRHSANP mainly accumulates in tumor and its accumulation amount of tumor is higher than ADRHSANP(P<0.05), and has obvious inhibiting cancer action and its inhibitory rate of cancer is also higher than ADRHSANP(P<0.05) by tumor injection. So, HAb18ADRHSANP can bind and inhibit hepatoma cell from growing in vivo.