Lipid-based drug delivery system containing non-natural phospholipase A2 degradable lipid derivative and therapeutic use thereof

摘要

The present invention relates to a lipid-based drug delivery system for administration of a lysolipid derivative present in a prodrug from, said prodrug furthermore being a substrate for extracellular phospholipase A2 to the extent that an organic radical can be hydrolytically cleaved off, whereas the aliphatic group of the lysolipid derivative remains substantially unaffected, said system having included therein lipopolymers or glycolipids so as to present hydrophilic chains on the surface of the system. Particularly interesting lipid derivatives are lipids in which the head group is linked to the C-2 position and the organic radical (a drug substance) is covalently attached to the C-3 position of the glycerol moiety. 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 extracel lular PLASUB2 /SUBactivity in the diseased tissue.