Sustained‐release properties of microencapsulated mitomycin C with ethylcellulose infused into the renal artery of the dog
Sustained‐release properties of microencapsulated mitomycin C with ethylcellulose infused into the renal artery of the dog
复制标题
乙基纤维素微囊丝裂霉素 C 注入犬肾动脉的缓释特性
作者：
Tetsuro Kato;R. Nemoto;H. Mori;I. Kumagai
用乙基纤维素对丝裂霉素C(MMC)进行微胶囊化。该微胶囊平均含有80%的生物活性MMC，并具有缓释性能。微囊的平均粒径为224μm，通过动脉插管可以很容易地将微囊注入犬肾脏。体外输注表明，微囊滞留在小动脉内，主要位于皮质-髓质交界处，并将浓缩的MMC释放到周围组织中。体内实验表明，注入微囊的犬肾脏在注射后5天内保持活性的MMC超过6小时，并出现广泛的坏死。注入无囊化MMC的肾脏可迅速排泄MMC，组织学改变较轻。肾内微囊释放的MMC血药浓度明显低于对照组。结果提示，动脉内注入MMC微囊的潜在治疗作用是一种栓塞和延长药效的作用，选择性地将MMC微囊注入肿瘤供血动脉可促进局部强化化疗，且全身副作用最小。癌症46：14-21,1980。
Mitomycin C (MMC) was microencapsulated with ethylcellulose. The microcapsules contained, on average, 80% of biologically active MMC and had a sustained‐release property. The mean particle size was 224 μm so that the microcapsules were readily infused into a canine kidney through arterial catheterization. Ex vivo infusion demonstrated that the microcapsules lodged in the small arteries, mainly at the cortico‐medullary junction, and released concentrated MMC into the surrounding tissue. In vivo experiments revealed that the canine kidneys infused with the microcapsules retained active MMC for more than 6 hours and showed extensive necrosis five days after the infusion. The kidneys infused with nonencapsulated MMC rapidly excreted MMC and showed mild histologic changes. The blood level of MMC released from the intrarenal microcapsules was markedly reduced as compared with control levels. The results suggest that the potential therapeutic effect of intraarterial infusion of MMC microcapsules is a function of embolization and prolonged drug action, and that selective infusion of MMC microcapsules into tumor‐supplying arteries could facilitate intensive topical chemotherapy with minimum systemic side‐effects. Cancer 46:14–21, 1980.