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Prodrug Approaches for CNS Delivery

  • Research Article/Themed Issue: Current Advances in CNS Delivery of Therapeutic Molecules Guest Editors: Jean-Michel Scherrmann a
  • Themed Issue: Current Advances in CNS Delivery of Therapeutic Molecules Guest Editors: Jean-Michel Scherrmann and Craig K. Svens
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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.

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Acknowledgements

Authors thank Dr. Jace Callaway for his valuable comments and the Academy of Finland (KL,108569) for financial support.

Author information

Authors and Affiliations

  1. Department of Pharmaceutical Chemistry, University of Kuopio, PO Box 1627, FI-70211, Kuopio, Finland

    Jarkko Rautio, Krista Laine & Mikko Gynther

  2. Fennopharma, Ltd., Microkatu 1, FI-70210, Kuopio, Finland

    Jouko Savolainen

Authors
  1. Jarkko Rautio
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  2. Krista Laine
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  3. Mikko Gynther
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  4. Jouko Savolainen
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Correspondence to Jarkko Rautio.

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Rautio, J., Laine, K., Gynther, M. et al. Prodrug Approaches for CNS Delivery. AAPS J 10, 92–102 (2008). https://doi.org/10.1208/s12248-008-9009-8

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  • DOI: https://doi.org/10.1208/s12248-008-9009-8

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