STERICALLY STABILIZED LIPOSOMES - IMPROVEMENTS IN PHARMACOKINETICS AND ANTITUMOR THERAPEUTIC EFFICACY
STERICALLY STABILIZED LIPOSOMES - IMPROVEMENTS IN PHARMACOKINETICS AND ANTITUMOR THERAPEUTIC EFFICACY
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DOI：
10.1073/pnas.88.24.11460
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发表时间：
1991-12-01
影响因子：
11.1
通讯作者：
MARTIN, FJ
中科院分区：
文献类型：
--
作者：
PAPAHADJOPOULOS, D;ALLEN, TM;MARTIN, FJ
本研究中获得的结果表明，掺入合成聚乙二醇衍生化磷脂的脂质体制剂对脂质体组织分布具有显著影响，并可大幅增加包封抗肿瘤药物的药理学疗效。这种作用显著大于先前用常规脂质体观察到的作用，并且与脂质体在血液中的循环时间延长超过5倍、组织如肝和脾的摄取显著减少以及植入肿瘤中相应的蓄积增加相关。本文所述的这些和其他性质大大扩展了脂质体作为各种药物活性大分子的有效载体系统的前景。
The results obtained in this study establish that liposome formulations incorporating a synthetic polyethylene glycol-derivatized phospholipid have a pronounced effect on liposome tissue distribution and can produce a large increase in the pharmacological efficacy of encapsulated antitumor drugs. This effect is substantially greater than that observed previously with conventional liposomes and is associated with a more than 5-fold prolongation of liposome circulation time in blood, a marked decrease in uptake by tissues such as liver and spleen, and a corresponding increased accumulation in implanted tumors. These and other properties described here have expanded considerably the prospects of liposomes as an effective carrier system for a variety of pharmacologically active macromolecules.