Lipid based drug delivery systems comprising phospholipase...

A - Human Necessities – 61 – K

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Details

A61K 47/48 (2006.01) A61K 31/665 (2006.01) A61P 29/00 (2006.01) A61P 31/00 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2647779

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 PLA2 activity in the diseased tissue.

La présente invention concerne un système d'administration de médicaments à base de lipides qui permet l'administration de médicaments anticancéreux sous forme de promédicament, ledit promédicament constituant en outre un substrat pour la phospholipase A2 extracellulaire dans la mesure où un radical organique peut en être clivé par hydrolyse, le résultat étant une réaction intramoléculaire. Ledit système comprend des lipopolymères et/ou des glycolipides de sorte que des chaînes hydrophiles soient présentes à la surface du système. De plus, les véhicules des promédicaments et médicaments à base de lipides peuvent être utilisés conjointement avec des médicaments incorporés. Les compositions pharmaceutiques renfermant le système d'administration de médicaments précité peuvent être utilisées dans le diagnostic et le traitement ciblé de divers troubles tels que le cancer, les états infectieux et inflammatoires entre autres, c'est-à-dire les troubles et maladies associés à, ou induits par l'accroissement de l'activité de la PLA2 extracellulaire dans les tissus malades.

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