Gunnel Karlsson (Biomicroscopy Unit, Polymer and Materials Chemistry, Lund, Sweden) is gratefully acknowledged for valuable assistance with cryo-TEM, and Prof. Rolf H. Berg for valuable discussions. Financial support from DTU, the Danish National Cancer Agency, and LiPlasome Pharma is gratefully acknowledged. The Center for Biomembrane Physics and the Center for Sustainable and Green Chemistry are supported by the Danish National Research Foundation.
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Communication
Drug Delivery by an Enzyme-Mediated Cyclization of a Lipid Prodrug with Unique Bilayer-Formation Properties†
Article first published online: 28 JAN 2009
DOI: 10.1002/anie.200805241
Copyright © 2009 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Issue
Angewandte Chemie International Edition
Volume 48, Issue 10, pages 1823–1826, February 23, 2009
Additional Information
How to Cite
Linderoth, L., Peters, Günther H., Madsen, R. and Andresen, Thomas L. (2009), Drug Delivery by an Enzyme-Mediated Cyclization of a Lipid Prodrug with Unique Bilayer-Formation Properties. Angew. Chem. Int. Ed., 48: 1823–1826. doi: 10.1002/anie.200805241
- †
Publication History
- Issue published online: 17 FEB 2009
- Article first published online: 28 JAN 2009
- Manuscript Revised: 1 DEC 2008
- Manuscript Received: 27 OCT 2008
Funded by
- DTU
- Danish National Cancer Agency
- LiPlasome Pharma
Keywords:
- cyclization;
- drug delivery;
- liposomes;
- phospholipase;
- prodrugs
Abstract
Special delivery: Liposomal drug-delivery systems in which prodrugs are activated specifically by disease-associated enzymes have great potential for the treatment of severe diseases, such as cancer. A new type of phospholipid-based prodrug has the ability to form stable small unilamellar vesicles (see picture). Activation of the prodrug vesicles by the enzyme sPLA2 initiates a cyclization reaction, which leads to the release of the drug.