侯新朴, 张宇锋, 谢蜀生, 胡新. 第三代载药免疫脂质体及体内外寻靶研究J. 药学学报, 2001, 36(7): 539-542.
引用本文: 侯新朴, 张宇锋, 谢蜀生, 胡新. 第三代载药免疫脂质体及体内外寻靶研究J. 药学学报, 2001, 36(7): 539-542.
HOU Xin-pu, ZHANG Yu-feng, XIE Shu-sheng, HU Xin. STUDY ON THIRD TYPE IMMUNOLIPOSOMES LOADED DRUGS AND THE TARGETING IN VITRO AND IN VIVOJ. Acta Pharmaceutica Sinica, 2001, 36(7): 539-542.
Citation: HOU Xin-pu, ZHANG Yu-feng, XIE Shu-sheng, HU Xin. STUDY ON THIRD TYPE IMMUNOLIPOSOMES LOADED DRUGS AND THE TARGETING IN VITRO AND IN VIVOJ. Acta Pharmaceutica Sinica, 2001, 36(7): 539-542.

第三代载药免疫脂质体及体内外寻靶研究

STUDY ON THIRD TYPE IMMUNOLIPOSOMES LOADED DRUGS AND THE TARGETING IN VITRO AND IN VIVO

  • 摘要: 目的 研究载阿霉素第三代免疫脂质体的制备及体内外寻靶、抑瘤效果。方法 设计将人膀胱癌单抗与聚乙二醇羧酸(PEG-COOH)端相联,使构成的脂质体既充分发挥PEG的保护功能,延长药物血循环时间,又使单抗伸展在外部充分发挥其寻靶作用,即第三代免疫脂质体(IML)。进而研究载抗癌药的免疫脂质体的制备方案,制备出阿霉素免疫脂质体(IML-ADM)使达到对药物高包封、高稳定,又不降低单抗活性的目的。以人膀胱癌靶细胞EJ和人直肠癌非靶细胞LOVO进行体外杀伤和体内肿瘤的抑瘤实验。结果 IML-ADM对EJ细胞和LOVO细胞杀伤,及对EJ细胞移植瘤体的抑制与对照组比较均有显著性差异。结论 证实脂质体载药以单抗制导达到主动靶向给药是可行的

     

    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 μg·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.

     

/

返回文章
返回