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为了提高化疗药物的治疗指数和降低其毒性,制备成柔红霉素-人血清白蛋白微球(Dau-HA-MS)。绝大多数为单分散相微球,平均直径56±16μm,范围为29~194μm,适用于导管动脉栓塞(TAE)治疗。Dau-HA-MS在生理盐水中能有效的释放Dau,但无爆发释放的缺点。释放Dau的光谱特性和体外细胞毒效应与原药相比无变化,表明Dau通过微球制备仍保留原有的理化及生物学特性。实验表明,经腹腔注射Dau-HA-MS使30%的S-180腹水癌小鼠活存超过6个月,而肿瘤对照组及Dau治疗组均分别在21天和14天全部死亡,说明Cau-HA-MS有较好的疗效及较低的毒性。本结果提示,Dau-HA-MS有可能用于人肝癌的TAE治疗。
In order to increase the therapeutic index and reduce the toxicity of chemotherapeutic drugs, daunorubicin-human serum albumin microspheres (Dau-HA-MS) were prepared. The vast majority of monodisperse phase microspheres, the average diameter of 56 ± 16μm, the range of 29 ~ 194μm, suitable for catheter arterial embolization (TAE) treatment. Dau-HA-MS can effectively release Dau in normal saline, but has no disadvantage of burst release. The spectral characteristics and in vitro cytotoxicity of released Dau showed no change compared with the original drug, indicating that Dau still retains its original physicochemical and biological properties through microsphere preparation. Experiments showed that 30% of S-180 ascites carcinoma mice lived for more than 6 months after intraperitoneal injection of Dau-HA-MS, while tumor control group and Dau treatment group all died at 21 days and 14 days respectively, indicating that Cau - HA-MS has better efficacy and lower toxicity. This result suggests that Dau-HA-MS may be used for TAE treatment of human liver cancer.