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Adv Drug Deliv Rev. 2012 May 15;64(7):666-85. doi: 10.1016/j.addr.2011.11.007. Epub 2011 Nov 27.

Prodrug approaches to reduce hyperexcitation in the CNS.

Author information

1
Department of Chemistry, University of Massachusetts, Amherst, MA 01003, United States.

Abstract

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.

PMID:
22138074
DOI:
10.1016/j.addr.2011.11.007
[Indexed for MEDLINE]

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