THE INCREASED EFFICACY AND DECREASED NEPHROTOXICITY OF A CYCLOSPORINE LIPOSOME1,2
THE INCREASED EFFICACY AND DECREASED NEPHROTOXICITY OF A CYCLOSPORINE LIPOSOME1,2
复制标题
环孢素脂质体提高疗效并降低肾毒性1,2
作者：
C. Freise;Tao Liu;K. Hong;R. Osorio;D. Papahadjopoulos;L. Ferrell;N. Ascher;J. Roberts
避免全身免疫抑制并发症的一种可能的方法是将免疫抑制药物局部输送到同种异体移植物的部位。脂质体是一种磷脂颗粒，可以优先将药物输送到网状内皮系统。由于肝脏是RES的主要组成部分，我们假设可以利用脂质体技术将免疫抑制药物局部输送到移植肝脏，从而避免系统输送免疫抑制的并发症。我们在大鼠模型中用原型环孢素脂质体对这一假设进行了评估。药代动力学研究表明，与标准静脉给药形式相比，这种脂质体更早地从体循环中清除，并增加了肝脏摄取。
A potential approach to avoid the complications of systemic immunosuppression is to deliver immunosuppressive agents locally to the site of the allograft. Liposomes are phospholipid particles that allow delivery of drugs preferentially to the reticuloendothelial system. Since the liver is a primary component of the RES, we hypothesized that liposome technology could be utilized to deliver immunosuppressive agents locally to a transplanted liver, thereby avoiding the complications of systemically delivered immunosuppression.We evaluated this hypothesis with a prototypic cyclosporine liposome in a rat model. Pharmacokinetic studies of this liposome indicated earlier clearance from the systemic circulation and increased hepatic uptake relative to the standard intravenous form of