[载药Ⅲ型免疫脂质体及其体内外靶向性研究]

[Study on third-type immunoliposomes loaded drugs and the targeting in vitro and in vivo].

作者信息

Hou X P, Zhang Y F, Xie S S, Hu X

机构信息

School of Pharmaceutical Science, Peking University, Beijing 100083, China.

出版信息

Yao Xue Xue Bao. 2001 Jul;36(7):539-42.

PMID:12585089

Abstract

AIM

To study the preparation, targeting and pharmacodynamics of third-type immunoliposome loaded anticancer drugs.

METHODS

The monoclonal antibody of human bladder cancer was combined with the terminal of PEG-COOH (polyethyleneglycol carboxylic acid) that make the liposomes not only prolong circulation by the membrane protection of PEG, but also target by spreading the antibody on the liposomes surface. That was the third type immunoliposomes. According to this scheme, the IML-ADM (immunoliposome carried adriamycin) wes prepared in which ADM entrapment was efficient and stability was high and the antibody activity was kept.

RESULTS

The % survival of the targeting EJ cells treated with IML-ADM (ADM = 45.45 micrograms.mL-1) was 4.3% +/- 1.0%, but 72% +/- 6% for non-targeting LOVO cells in vitro; the tumor weight in nude mice which were implanted by EJ cells after 27 days were (39 +/- 25) mg, (135 +/- 32) mg, (598 +/- 240) mg treated by IML-ADM, SSL-ADM (steric stable lipsomes carried Adriamycin) and normal saline, respectively, in vivo.

CONCLUSION

The results confirmed that the immunoliposme-mediated targeting anticancer drug is a feasible way.

摘要

目的

研究负载抗癌药物的Ⅲ型免疫脂质体的制备、靶向性及药效学。

方法

将人膀胱癌单克隆抗体与聚乙二醇羧酸（PEG - COOH）末端相连，使脂质体不仅通过PEG的膜保护作用延长循环时间，还通过抗体在脂质体表面的分布实现靶向性，此即Ⅲ型免疫脂质体。按此方案制备了阿霉素免疫脂质体（IML - ADM），其阿霉素包封率高、稳定性好且保留抗体活性。

结果

体外实验中，用IML - ADM（阿霉素浓度为45.45微克·毫升⁻¹）处理的靶向EJ细胞存活率为4.3%±1.0%，而非靶向LOVO细胞为72%±6%；体内实验中，接种EJ细胞的裸鼠在27天后，分别用IML - ADM、阿霉素立体稳定脂质体（SSL - ADM）和生理盐水处理，肿瘤重量分别为（39±25）毫克、（135±32）毫克、（598±240）毫克。