Drug release from nanoparticle-coated capsules

A - Human Necessities – 61 – K

Patent

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Details

A61K 9/107 (2006.01) A61K 9/22 (2006.01) A61K 9/54 (2006.01)

Patent

CA 2649870

Methods of producing a controlled release formulation for an active substance are disclosed, wherein the methods involve dispersing a discontinuous phase comprising an active substance into a continuous phase so as to form a two-phase liquid system comprising droplets of said discontinuous phase, and allowing nanoparticles provided to the two-phase liquid system to congregate at the phase interface to thereby coat the surface of the droplets in at least one layer of said nanoparticles. The methods utilise a concentration of a suitable electrolyte which enhances the nanoparticle congregation such that the coating of nanoparticles on the surface of the droplets presents a semi- permeable barrier to the active substance, or otherwise utilise a amount of the active substance that is greater than the solubility limit of that active substance in the discontinous phase. Formulations comprising vitamin A (retinol) as the active substance for dermal delivery are specifically exemplified.

L'invention concerne des procédés de fabrication d'une préparation à libération contrôlée pour une substance active, lesdits procédés consistant à disperser une phase discontinue comprenant une substance active dans une phase continue de façon à former un système liquide à deux phases comprenant des gouttelettes de ladite phase discontinue et à permettre aux nanoparticules introduites dans le système liquide à deux phases de s'agglomérer à l'interface entre les phases et recouvrir ainsi la surface des gouttelettes d'au moins une couche desdites nanoparticules. Les procédés reposent sur l'emploi d'une concentration d'un électrolyte approprié qui accroît l'agglomération des nanoparticules de façon à ce que le revêtement de nanoparticules sur la surface des gouttelettes présente une barrière semi-perméable pour la substance active, ou bien sur une quantité de la substance active qui est supérieure à la limite de solubilité de cette substance active dans la phase discontinue. Un exemple de l'invention concerne des préparations comprenant de la vitamine (A) (du rétinol) en tant que substance active pour une administration cutanée.

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