Prodrug approaches to reduce hyperexcitation in the CNS

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• 作者：Devaiah Vytla^a ; ^b ; Rosamund E. Combs-Bachmann^b ; Amanda M. Hussey^a ; ¹ ; Stephen T. McCarron^a ; ¹ ; Devon S. McCarthy^a ; James J. Chambers^a ; ^b ; ^{chambers@chem.umass.edu}
• 关键词：CNS prodrug ; Hyperexcitation prodrug ; Receptors ; Targeting ; Stroke ; Alzheimer's disease
• 刊名：Advanced Drug Delivery Reviews
• 出版年：2012
• 期刊代码：2_0169409x
• 类别：bio
• 出版时间：15 May, 2012
• 卷：64
• 期：7
• 页码：666-685
• 文件大小：1181 K

摘要

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.