Cell transport compositions and uses thereof

A - Human Necessities – 61 – K

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A61K 9/12 (2006.01) A61K 9/14 (2006.01) A61K 9/16 (2006.01)

Patent

CA 2493478

Compositions and methods have been developed for transporting compounds across membranes with little or no toxicity and, when targeted through the appropriate routes of administration (i.e., lung, gastrointestinal (GI) tract), little or no immune stimulation. The compositions can mediate cellular delivery of compounds that would otherwise not enter cells and enhance the intracellular delivery of compounds that would otherwise enter cells inefficiently. The methods are carried out by contacting a proximal face of a lipid bilayer or membrane (e.g. the surface of an intact cell) with a complex containing a compound (e.g., a therapeutic agent) and a diketopiperazine (DKP). DKP and the compound are non-covalently associated with each other or covalently bound to each other .

L'invention concerne des compositions et des méthodes mises au point pour le transport de composés dans des membranes présentant peu ou pas de toxicité et, lorsque ciblées par les voies d'administration appropriées (c'est-à-dire par voie pulmonaire ou gastro-intestinale (GI)), peu ou pas de stimulation immunitaire. Ces compositions peuvent favoriser la distribution cellulaire de composés qui, autrement, n'entreraient pas dans les cellules, et améliorer la distribution intracellulaire de composés qui, autrement, n'entreraient pas efficacement dans les cellules. Les méthodes sont mises en oeuvre par mise en contact d'une face proximale d'une bicouche ou membrane lipidique (par exemple la surface d'une cellule intacte) avec un complexe contenant un composé (par exemple un agent thérapeutique) et une dicétopipérazine (DKP). La DKP et le composé sont associés l'un à l'autre de manière non covalente ou liés l'un à l'autre par covalence.

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