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为了提高化疗药物的治疗指数和降低其毒性,制备了柔红霉素-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治疗。Dau-HA~MS在生理盐水中能有效释放Dau,但无爆发释放的缺点。释放的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S180腹水癌小鼠活存超过6个月,而肿瘤对照组及Dau治疗肿瘤组均分别在21d和14d全部死亡,说明Dau-HA-MS有较好的疗效及较低的毒性,提示Dau-HA-MS有可能用于人肝癌的导管动脉栓塞治疗,有进一步研究的价值。
In order to improve the therapeutic index of chemotherapy drugs and reduce their toxicity, daunorubicin-human serum albumin microspheres (Dau-HA-MS) were prepared, the majority of them were monodisperse phase microspheres with an average diameter of 56 ± 16μm, 29 ─ 194μm, suitable for catheter arterial embolization. Dau-HA-MS can effectively release Dau in normal saline without the defect of burst release. The spectral characteristics of the released Dau and in vitro cytotoxicity showed no change compared with the original drug, indicating that Dau still retains the original physicochemical and biological properties by microsphere preparation. The results showed that 30% of S180 ascites tumor mice survived by intraperitoneal injection of Dau-HA-MS for more than 6 months, while the tumor control group and the Dau-treated tumor group all died on 21d and 14d respectively, indicating that Dau-HA-MS Have better curative effect and lower toxicity, suggesting that Dau-HA-MS may be used for the treatment of catheterization of human hepatocellular carcinoma and has further research value.