Prodrug approaches to reduce hyperexcitation in the CNS.
Prodrug approaches to reduce hyperexcitation in the CNS.
复制标题
减少中枢神经系统过度兴奋的前药方法。
DOI：
10.1016/j.addr.2011.11.007
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发表时间：
2012
影响因子：
16.1
通讯作者：
Chambers,JamesJ
中科院分区：
文献类型：
--
作者：
Vytla,Devaiah;Combs-Bachmann,RosamundE;Hussey,AmandaM;McCarron,StephenT;McCarthy,DevonS;Chambers,JamesJ
中枢神经系统中的过度兴奋是从急性损伤到慢性和进行性疾病的许多脑疾病的根本原因。治疗这些疾病的主要限制是微小但强大的血脑屏障。为了将治疗剂递送至所需作用部位，已经开发了许多生物医学工程策略，包括允许被动扩散或主动转运穿过该屏障的前药制剂。在前药的情况下，一旦在脑区室中，活性治疗剂被释放。在这篇综述中，我们详细讨论了一些与治疗中枢神经系统兴奋过度相关的因素，包括分子靶点、疾病、前药策略，以及处于临床开发各个阶段的一些治疗方法的重点病例研究。
Hyperexcitation in the central nervous system is the root cause of a number of disorders of the brain ranging from acute injury to chronic and progressive diseases. The major limitation to treatment of these ailments is the miniscule, yet formidable blood–brain barrier. To deliver therapeutic agents to the site of desired action, a number of biomedical engineering strategies have been developed including prodrug formulations that allow for either passive diffusion or active transport across this barrier. In the case of prodrugs, once in the brain compartment, the active therapeutic agent is released. In this review, we discuss in some detail a number of factors related to treatment of central nervous system hyperexcitation including molecular targets, disorders, prodrug strategies, and focused case studies of a number of therapeutics that are at a variety of stages of clinical development.