Composition and method for enhancing transport across...

A - Human Necessities – 61 – K

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A61K 47/48 (2006.01)

Patent

CA 2291074

Methods and compositions for transporting drugs and macromolecules across biological membranes are disclosed. In one embodiment, the invention includes a method for enhancing transport of a selected compound across a biological membrane, wherein a biological membrane is contacted with a conjugate containing a biologically active agent that is covalently attached to a transport polymer. In one embodiment, the polymer consists of from 6 to 25 subunits, at least 50 % of which contain a guanidino or amidino sidechain moiety. The polymer is effective to impart to the attached agent a rate of trans-membrane transport across a biological membrane that is greater than the rate of trans-membrane transport of the agent in non-conjugated form.

L'invention concerne des procédés et des compositions permettant de transporter des médicaments et des macromolécules à travers des membranes biologiques. Dans une forme de réalisation, l'invention concerne un procédé qui améliore le transport d'un composé sélectionné à travers une membrane biologique. Ce procédé consiste à mettre en contact une membrane biologique avec un conjugué contenant un agent biologiquement actif qui est lié de manière covalente à un polymère transporteur. Dans une forme de réalisation, le polymère est constitué de 6 à 25 sous-unités, dont au moins 50 % contiennent une fraction de chaîne latérale guanidino ou amidino. Le polymère est efficace pour conférer à l'agent attaché une vitesse de transport transmembranaire à travers une membrane biologique qui est supérieure à la vitesse de transport transmembranaire de l'agent se présentant sous une forme non conjuguée.

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