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脂质开关:通过分子识别驱动的构象互变实现刺激响应的脂质体。

Lipid Switches: Stimuli-Responsive Liposomes through Conformational Isomerism Driven by Molecular Recognition.

机构信息

Department of Chemistry, University of Tennessee, 1420 Circle Drive, Knoxville, TN, 37996, USA.

出版信息

Chemistry. 2019 Jan 2;25(1):20-25. doi: 10.1002/chem.201803389. Epub 2018 Nov 26.

DOI:10.1002/chem.201803389
PMID:30133869
Abstract

Advancements in the field of liposomal drug carriers have culminated in greatly improved delivery properties. An important aspect of this work entails development of designer liposomes for release of contents triggered by environmental changes. The majority of these systems are driven by chemical reactions in the presence of different stimuli. However, a promising new paradigm instead focuses on molecular recognition events as the impetus for content release. In certain cases, these platforms exploit synthetic lipid switches designed to undergo conformational changes upon binding to target ions or molecules that perturb membrane assembly, thereby triggering cargo release. Examples of this approach reported thus far showcase how rational design of lipid switches can result in dramatic changes in lipid assembly properties. These strategies show great promise for opening up new pathophysiological stimuli that can be harnessed for programmed content release in drug delivery applications.

摘要

脂质体药物载体领域的进展最终导致了输送性能的极大改善。这项工作的一个重要方面是开发设计用于在环境变化触发时释放内容的脂质体。这些系统中的大多数是由不同刺激存在下的化学反应驱动的。然而,一个有前途的新范例则专注于分子识别事件作为内容释放的动力。在某些情况下,这些平台利用合成脂质开关,这些开关在与目标离子或分子结合时会发生构象变化,从而破坏膜组装,从而触发货物释放。迄今为止报道的此类方法的示例展示了如何通过合理设计脂质开关,从而导致脂质组装特性发生显著变化。这些策略为开辟新的病理生理学刺激提供了巨大的潜力,可用于药物输送应用中的程控内容释放。

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