Unimolecular polymeric micelles with an ionizable inner core

Details Unimolecular polymeric micelles with an ionizable inner core Unimolecular polymeric micelles with an ionizable inner core

B - Operations, Transporting

01

J

B01J 13/02 (2006.01) A61K 9/107 (2006.01) A61K 47/48 (2006.01)

Patent

CA 2452813

The present invention describes the preparation of unimolecular polymeric micelles (UPM) that bear a hydrophilic shell and a potentially ionizable and relatively hydrophobic core at a determined pH value. The core becomes electrostatically charged as the pH is changed. Such micelles can be made from either biodegradable or non-biodegradable polymers. Loaded drugs can be physically retained in the micelles when the pH of the surrounding medium favors interactions with the core. Upon a change in pH, modification in the ionization state of the core will decrease the interactions between the drug and the inner core and facilitate the release of the micellar contents.

La présente invention concerne la préparation de micelles polymères monomoléculaires (UPM) qui portent une enveloppe hydrophile et un coeur potentiellement ionisable et relativement hydrophobe à un pH déterminé. Le coeur se charge d'un point de vue électrostatique lorsque le pH varie. Des micelles de ce type peuvent être réalisées à partir de polymères biodégradables ou non biodégradables. Des substances pharmaceutiques chargées peuvent être retenues d'un point de vue physique dans les micelles lorsque le pH du milieu environnant favorise les interactions avec le coeur. Lorsque le pH varie, la modification de l'état d'ionisation du coeur provoque une diminution des interactions entre la substance pharmaceutique et le coeur interne, et facilite la libération des contenus micellaires.

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