Lipid-based drug delivery system containing phospholipase A2-degradable lipid that undergoes intramolecular cyclization during hydrolysis

摘要

The present invention relates to a lipid-based drug delivery system for administration of anti-cancer drugs in a prodrug form, said prodrug furthermore being a substrate for extracellular phospholipase A2 to the extent that an organic radical can be hydrolytically cleaved off, resulting in an intramolecular reaction, said system comprising lipopolymers and/or glycolipids so as to present hydrophilic chains on the surface of the system. In addition, the lipid prodrug and drug carries can be used in combination with incorporated drugs. Pharmaceutical compositions comprising the drug delivery system can be used in diagnosis and targeted treatment of various disorders, e.g. cancer, infectious, and inflammatory conditions, etc., i.e. disorders and diseases associated with or resulting from increased levels of extracellular PLASUB2/SUB activity in the diseased tissue.