Kim S, Howell S B
Cancer Treat Rep. 1987 May;71(5):447-50.
Sc administration of cytarabine entrapped in multivesicular liposomes to BDF1 mice resulted in slow first-order release from skin, with a half-life of 4 days. The half-life was 10 minutes for unencapsulated free drug. A single-dose sc treatment of BDF1 mice, inoculated iv with 10(5) L1210 leukemia cells 24 hours previously, resulted in long-term survivors over a wide dose range. This study demonstrates that encapsulation of cytarabine in multivesicular liposomes results in slow release from skin and that a single sc dose is often curative for mice with systemic leukemia.
将包裹于多囊泡脂质体中的阿糖胞苷皮下注射给BDF1小鼠后，药物从皮肤缓慢释放，呈一级动力学过程，半衰期为4天。未包裹的游离药物半衰期为10分钟。对24小时前经静脉接种10(5)个L1210白血病细胞的BDF1小鼠进行单剂量皮下治疗，在很宽的剂量范围内都产生了长期存活者。本研究表明，阿糖胞苷包裹于多囊泡脂质体中可导致药物从皮肤缓慢释放，且单剂量皮下给药对患有全身性白血病的小鼠常常具有治愈作用。
