Design and Pharmaceutical Applications of Prodrugs

Järvinen, Tomi; Rautio, Jarkko; Másson, Már; Loftsson, Þorsteinn

doi:10.1002/9780470571224.pse018

Cited by 1 publication

(1 citation statement)

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“…The choice of promoiety should be considered with respect to the disease state, dose, and the duration of therapy. The prodrug approach can be exploited for almost all administration routes and dosage forms, and it can be applied to a wide variety of existing medicines on the market, as well as to novel drug molecules in the lead optimization step early in the drug discovery process (20,26,27). Prodrug approaches are used to improve drug delivery and targeting in the CNS, and utilize passive drug uptake processes into CNS by chemically modifying a drug to become more lipophilic.…”

Section: Prodrug Conceptmentioning

confidence: 99%

Prodrug Approaches for CNS Delivery

Rautio

Laine

Gynther

et al. 2008

AAPS J

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149

106

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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.

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Section: Prodrug Conceptmentioning

confidence: 99%