Uster P S, Allen T M, Daniel B E, Mendez C J, Newman M S, Zhu G Z
SEQUUS Pharmaceuticals, Inc., Menlo Park, CA 94025, USA.
FEBS Lett. 1996 May 20;386(2-3):243-6. doi: 10.1016/0014-5793(96)00452-8.
Transfer of MPEG(1900)-DSPE from micellar phase to pre-formed liposomes imparts long in vivo circulation half-life to an otherwise rapidly cleared lipid composition. MPEG(1900)-DSPE transfers efficiently and quickly in a time and temperature dependent manner. There is negligible content leakage and a strong correlation between assayed mol% MPEG(1900)-DSPE, liposome diameter increase, and pharmacokinetic parameters such as distribution phase half-life. Since a biological attribute (liposome clearance rate) can be modified by the insertion process, it suggests a simple and economical way to impart site-specific targeting to a variety of liposome delivery systems. This method is also a convenient way to measure the 'brush' thickness of such conjugates directly.
将MPEG(1900)-DSPE从胶束相转移至预先形成的脂质体，可赋予原本会迅速清除的脂质组合物较长的体内循环半衰期。MPEG(1900)-DSPE以时间和温度依赖性方式高效且快速地转移。内容物泄漏可忽略不计，且测定的MPEG(1900)-DSPE摩尔百分比、脂质体直径增加与药代动力学参数（如分布相半衰期）之间存在强相关性。由于生物属性（脂质体清除率）可通过插入过程进行修饰，这提示了一种简单且经济的方法，可为多种脂质体递送系统赋予位点特异性靶向性。该方法也是直接测量此类缀合物“刷状”厚度的便捷方式。
