Drug Delivery by an Enzyme-Mediated Cyclization of a Lipid Prodrug with Unique Bilayer-Formation Properties

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 (...

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Veröffentlicht in:Angewandte Chemie (International ed.) 2009-01, Vol.48 (10), p.1823-1826
Hauptverfasser: Linderoth, Lars, Peters, Günther H, Madsen, Robert, Andresen, Thomas L
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Sprache:eng
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Zusammenfassung: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.
ISSN:1433-7851
1521-3773
DOI:10.1002/anie.200805241