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影响脂质体药物释放的因素。

Factors affecting drug release from liposomes.

作者信息

Lindner Lars H, Hossann Martin

机构信息

CCG-Hyperthermia, Helmholtz Zentrum München, German Research Center for Environmental Health, Munich, Germany.

出版信息

Curr Opin Drug Discov Devel. 2010 Jan;13(1):111-23.

Abstract

Liposomes are the most widely used nanocarrier systems in medicine. Common strategies for tumor-specific drug delivery using liposomes include the passive accumulation of liposomes that have an increased circulation half-life, which is possible as a result of the leakiness of tumor neovasculature, as well as the active targeting of liposomes using surface-bound ligands. However, such targeting of the nanocarrier is not effective if the encapsulated drug within the liposome is not released at the intended site. Drug release can be influenced by both the membrane composition of the liposome and the choice of drug. In addition to environmental triggers, such as low pH and the presence of particular enzymes, external stimuli such as heat or ultrasound have gained attention in the clinic. This review provides a summary of the various approaches to modifying drug release from liposomes.

摘要

脂质体是医学上应用最广泛的纳米载体系统。使用脂质体进行肿瘤特异性药物递送的常见策略包括:利用肿瘤新生血管的渗漏性使脂质体循环半衰期延长,从而实现脂质体的被动蓄积;以及使用表面结合配体对脂质体进行主动靶向。然而,如果脂质体内包裹的药物不能在预期部位释放,那么这种纳米载体的靶向作用就无效。药物释放会受到脂质体膜组成和药物选择的影响。除了低pH值和特定酶的存在等环境触发因素外,热或超声等外部刺激在临床上也受到了关注。本综述总结了修饰脂质体药物释放的各种方法。

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