The University of British Columbia

Inex Pharmaceuticals Corporation

Nancy L Boman

Pieter Rutter Cullis

Marcel B Bally

Lawrence D Mayer

Elisabeth Maurer

Kim F Wong

David B Fenske

Maurer Norbert

Johanna M Leenhouts

Novel methods are provided for loading a weakly basic drug into liposomes utilizing an electoneutral transport system. In these methods, ionophores are utilized with liposomes having a metal ion gradient to facilitate the exchange of metal ions for protons. The transported metal ion will, in some embodiments, be complexed with a chelating agent which is present in the external media.

Ionophore-mediated liposome loading

Liposomal compositions encapsulating bioactive agents and having improved circulation longevity of the agents are disclosed. Such liposomes combine a low pH of the solution in which a bioactive agent is entrapped and a sugar-modified lipid or an amine-bearing lipid, the combination of which enhances the retention of the encapsulated bioactive agent and thereby promotes circulation longevity. The present invention also discloses methods of making and using such compositions.

Liposomal compositions for enhanced retention of bioactive agents

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Richmond, Canada

Nancy L Boman