Compositions and methods for enhancing receptor-mediated...

A - Human Necessities – 61 – K

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A61K 9/00 (2006.01) A61K 9/06 (2006.01) A61K 47/28 (2006.01) A61P 5/00 (2006.01) A61P 15/08 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2346539

Compositions and methods for improving cellular internalization of one or more compounds are disclosed. The compositions include a compound to be delivered and a biocompatible viscous material, such as a hydrogel, lipogel, or highly viscous sol. The compositions also include, or are administered in conjunction with, an enhancer in an amount effective to maximize expression of or binding to receptors and enhance RME of the compound into the cells. This leads to high transport rates of compounds to be delivered across cell membranes, facilitating more efficient delivery of drugs and diagnostic agents. Compositions are applied topically orally, nasally, vaginally, rectally, and ocularly. The enhancer is administered with the composition or separately, either systemically or preferably locally. The compound to be delivered can also be the enhancer.

La présente invention concerne des compositions et des procédés permettant d'augmenter l'internalisation cellulaire d'au moins un composé. Ces compositions comportent un composé à livrer et un matériau visqueux biocompatible tel qu'un hydrogel, un lipogel ou un sol hautement visqueux. Les compositions incluent également, ou sont administrées en relation avec, un potentialisateur en quantité suffisante pour maximiser l'expression ou la liaison à des récepteurs et renforcer la RME du composé pénétrant dans les cellules. Cela conduit à des taux élevés de transport des composés à livrer dans l'ensemble des membranes cellulaires, ce qui favorise une livraison plus efficace des médicaments et agents de diagnostic. Ces compositions s'administrent en application locale, par voie orale, nasale, vaginale, rectale et oculaire. Le potentialisateur s'administre avec la composition, ou séparément, soit systémiquement, soit de préférence localement. Le composé à livrer peut également être le potentialisateur.

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