Prodrug Approaches for CNS Delivery
Journal Title: The AAPS Journal - Year 2008, Vol 10, Issue 1
Abstract
Central nervous system (CNS) drug delivery remains a major challenge, despite extensive efforts that have been made to develop novel strategies to overcome obstacles. Prodrugs are bioreversible derivatives of drug molecules that must undergo an enzymatic and/or chemical transformation in vivo to release the active parent drug, which subsequently exerts the desired pharmacological effect. In both drug discovery and drug development, prodrugs have become an established tool for improving physicochemical, biopharmaceutical or pharmacokinetic properties of pharmacologically active agents that overcome barriers to a drug’s usefulness. This review provides insight into various prodrug strategies explored to date for CNS drug delivery, including lipophilic prodrugs, carrier- and receptor-mediated prodrug delivery systems, and gene-directed enzyme prodrug therapy.
Authors and Affiliations
Jarkko Rautio, Krista Laine, Mikko Gynther, Jouko Savolainen
Keywords
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- EP ID EP681537
- DOI 10.1208/s12248-008-9009-8
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