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 (see picture). Activation of the prodrug vesicles by the enzyme sPLA(2) initiates a cyclization reaction, which leads to the release of the drug.
Linderoth
Lars
L
Department of Chemistry, Technical University of Denmark, 2800 Lyngby, Denmark.
Peters
Günther H
GH
Madsen
Robert
R
Andresen
Thomas L
TL
D002211:Capsaicin / Q000008:administration & dosage / Q000138:chemical synthesis / Q000737:chemistry; D003500:Cyclization; D016503:Drug Delivery Systems; D006801:Humans; D008051:Lipid Bilayers / Q000737:chemistry*; D008081:Liposomes / Q000737:chemistry; D054497:Phospholipases A2, Secretory / Q000378:metabolism*; D011355:Prodrugs / Q000008:administration & dosage* / Q000138:chemical synthesis / Q000737:chemistry*; D019032:Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization
D008051:Lipid Bilayers; D008081:Liposomes; D011355:Prodrugs; D054497:Phospholipases A2, Secretory; D002211:Capsaicin