Enhancing drug delivery across and into epithelial tissues...

A - Human Necessities – 61 – K

Patent

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A61K 47/48 (2006.01) C07K 7/06 (2006.01) C07K 7/64 (2006.01)

Patent

CA 2381425

This invention provides compositions and methods for enhancing delivery of drugs and other agents across epithelial tissues, including the skin, gastrointestinal tract, pulmonary epithelium, and the like. The compositions and methods are also useful for delivery across endothelial tissues, including the blood brain barrier. The compositions and methods employ a delivery enhancing transport that has sufficient guanidino or amidino sidechain moieties to enhance delivery of a compound conjugated to the reagent across one or more layers of the tissue, compared to the non-conjugated compound. The delivery enhancing polymers include, for example, poly-arginine molecules that are preferably between about 6 and 25 residues in length.

L'invention porte sur des compositions et procédés améliorant la diffusion à travers des tissus épithéliaux (dont la peau, le tube digestif, ou l'épithélium pulmonaire) de médicaments et analogues, et à travers des tissus endothéliaux dont la barrière hématoencéphalique. Ces compositions et procédés recourent à un transporteur activant la diffusion présentant assez de fragments de chaînes latérales guanidino ou amidino pour améliorer la diffusion d'un composé conjugué au réactif à travers une ou plusieurs couches de tissu par rapport à celle d'un composé non conjugué. Les polymères activant la diffusion comportent par exemple des molécules de polyarginine d'une longueur préférée comprise entre environ 6 et 25 résidus.

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