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

  • 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 adriamycinloaded human serum albumin immunonanoparticles (ADRHSANP) against hepatoma led by antihuman hepatoma monoclonal antibodies HAb18 are studied. The results show that effective loaded drug dose of HAb18ADRHSANP is 1.44%, which is lower than ADRHSANP(1.69%); HAb18ADRHSANP slowly releases drug ADR and its maximum releasing drug dose(41%)is obviously lower than ADRHSANP(65%) (P<0.05); nowever, 131IHAb18ADRHSANP mainly accumulates in liver and its liertaxis and stability are better than 131IADRHSANP in nude mice by intravenous injection; HAb18ADRHSANP mainly accumulates in tumor and its accumulation amount of tumor is higher than ADRHSANP(P<0.05), and has obvious inhibiting cancer action and its inhibitory rate of cancer is also higher than ADRHSANP(P<0.05) by tumor injection. So, HAb18ADRHSANP can bind and inhibit hepatoma cell from growing in vivo.

     

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