Compositions and methods for enhancing drug delivery across...

Details Compositions and methods for enhancing drug delivery across... Compositions and methods for enhancing drug delivery across...

A - Human Necessities

61

K

A61K 47/42 (2006.01) A61K 47/34 (2006.01) A61K 47/48 (2006.01)

Patent

CA 2400099

This invention provides compositions and methods for enhancing delivery of drugs and other agents across a biological barrier, including epithelial tissues such as 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 transporter that has sufficient guanidino or amidino sidechain moieties to enhance delivery of a compound 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 50 residues in length.

L'invention concerne des compositions et des procédés destinés à augmenter l'apport de médicaments ou d'autres agents à travers une barrière biologique, y compris de tissus épithéliaux tels que la peau, le tractus gastro-intestinal, l'épithélium pulmonaire, et d'autres du même type. Les compositions et les procédés sont aussi utiles pour un apport à travers des tissus endothéliaux, y compris la barrière hémato-encéphalique. Ces compositions et ces procédés utilisent un agent de transport permettant d'augmenter un apport, cet agent comportant suffisamment d'entités guanidino ou amidino sous forme de chaînes latérales pour permettre une augmentation d'apport d'un composé à travers une ou plusieurs couches de tissu, en comparaison au composé non conjugué. Les polymères permettant un apport comprennent, par exemple, des molécules de poly-arginine qui comportent de préférence environ de 6 à 50 résidus en longueur.

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