Ionophore-mediated liposome loading of weakly basic drug

A - Human Necessities – 61 – K

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A61K 9/127 (2006.01)

Patent

CA 2269921

Novel methods are provided for loading a weakly basic drug into liposomes utilizing an electroneutral 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.

L'invention porte sur de nouvelles méthodes de chargement de médicaments faiblement basiques dans des liposomes recourant à un système de transport électoneutre. On utilise dans ces méthodes des ionophores et des liposomes présentant un gradient d'ions métalliques favorisant l'échange des ions métalliques contre des protons. Dans certains modes de réalisation, l'ion métal transporté est complexé avec un chélateur présent dans le milieu extérieur.

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