Liposomal delivery system with photoactivatable triggered...

A - Human Necessities – 61 – K

Patent

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A61K 47/24 (2006.01) A61N 5/06 (2006.01)

Patent

CA 2050971

A triggered release liposomal delivery system is disclosed that selectively releases its contents in response to illumination or reduction in pH. The liposomes contain an amphipathic lipid, such as a phospholipid, having two chains derived from fatty acid that allow the lipid to pack into a bilayer structure. One or both of the alkyl chains contains a vinyl ether functionality that is cleaved by reactive oxygen species (ROS) or acid. A photosensitizer is incorporated into the liposomal cavity or membrane, and produces ROS or acid when illuminated to cleave the vinyl ether functionality and disrupt the liposomal membrane to release the vesicle contents. The lipid is preferably a plasmalogen, for example (see formula I) wherein R1 and R2 are each long chain hydrocarbons containing 12-24 carbons.

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