Liposome composition for improved intracellular delivery of...

A - Human Necessities – 61 – K

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A61K 9/127 (2006.01) A61K 9/133 (2006.01) A61K 47/48 (2006.01)

Patent

CA 2442261

A liposomal composition and a method of using the same for achieving intracellular delivery of a liposome-entrapped agent is described. The liposomes are composed of a pH sensitive lipid and include a targeting ligand to direct the liposomes to a target cell. The liposomes also include a stabilizing component, such a polymer-derivatized lipid, where the polymer is attached to the lipid by a releasable linkage. Administration of the liposomes results in cellular internalization and destabilization of the liposome for intracellular delivery of the entrapped agent.

L'invention concerne une composition de liposome et un procédé d'utilisation de cette composition destinés à réaliser une administration intracellulaire d'un agent inclus dans un liposome. Les liposomes sont composés d'un lipide sensible au pH et comprennent un ligand de ciblage permettant de diriger le liposome vers une cellule cible. Les liposomes comprennent aussi un composant stabilisant, tel qu'un lipide à dérivatisation polymérique, dans lequel le polymère est attaché au lipide par une liaison lâche. L'administration de ces liposomes conduit à une internalisation cellulaire et à une déstabilisation du liposome menant à la libération intracellulaire de l'agent inclus.

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