生物素化壳聚糖微球的体外抗癌活性

目的　研究一套有预定位及肿瘤导向作用的药物载体系统。方法　以生物素化无唾液酸胎球蛋白为分子识别系统，与肝癌细胞特异性结合，将包封有5-Fu的壳聚糖微球生物素化，作为药物载体，通过生物素-亲和素系统将二者桥连，用“三步法”研究微球体外抗肿瘤作用。结果　亲和素-生物素化受体介导的生物素化壳聚糖微球能与体外培养的肝癌细胞特异结合并有显著的抗癌作用。结论　生物素化微球-亲和素-生物素化受体(或单克隆抗体)系统可望在体内有预定位及肿瘤靶向作用，有广泛的应用前景。

ANTICANCER ACTIVITY OF BIOTINYLATED 5-FU-LOADED CHITOSAN MICROSPHERES IN VITRO

AIM　To study a novel microspheres system pre-located and targeted to tumor. METHODS　Biotinylated asialofetuin was used as a pretargeting agent. Biotinylated 5-Fu chitosan microspheres were bridged to it by avidin-biotin system. The antitumor activity was evaluated against SMMC-7721 in vitro by “three-step” method. RESULTS　Biotinylated chitosan microspheres displayed targetability to specific cells, and showed higher growth-inhibiting effect against SMMC-7721. CONCLUSION　The system of biotinylated receptor (or monoclonal antibody)-avidin-biotinylated microspheres may be used for targeted therapy of tumor.