Bioconjugates and delivery of bioactive agents

C - Chemistry – Metallurgy – 07 – H

Patent

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Details

C07H 21/02 (2006.01) A61K 31/525 (2006.01) A61K 35/00 (2006.01) A61K 39/00 (2006.01) A61K 39/44 (2006.01) A61K 41/00 (2006.01) A61K 47/48 (2006.01) A61K 49/00 (2006.01) C07H 21/00 (2006.01) C07H 21/04 (2006.01) C07H 23/00 (2006.01) G01N 33/15 (2006.01)

Patent

CA 2264592

The present invention relates to bioconjugates and the delivery of bioactive agents which are preferably targeted for site-specific release in cells, tissues or organs. More particularly, this invention relates to bioconjugates which comprise of bioactive agent and an organocobalt complex. The bioactive agent is covalently bonded directly or indirectly to the cobalt atom of the oragnocobalt complex. The bioactive agent is released from the bioconjugate by the cleavage of the covalent bond between the bioactive agent and the cobalt atom in the oragnocobalt complex. The cleavage may occur as a result of normal displacment by cellular nucleophiles or enzymatic action, but is preferably caused to occur selectively at a predetermined release site by application of an external signal. The external signal may be light or photoexcitation, i.e. photolysis, or it may be ultrasound, i.e. sonolysis. Further, if the photolysis takes places in the presence of a magnetic field surrounding the release site, the release of the bioactive agent into surrounding healthy tissue is minimized.

Bioconjugués et administration d'agents bioactifs qui sont de préférence ciblés pour la libération spécifique à des sites au sein des cellules, tissus ou organes. Plus particulièrement, la présente invention concerne des bioconjugués qui comportent un agent bioactif et un complexe organocobalt. L'agent bioactif est lié de manière covalente directement ou indirectement à l'atome de cobalt du complexe organocobalt. L'agent bioactif est libéré du bioconjugué par le clivage de la liaison covalente entre l'agent bioactif et l'atome de cobalt du complexe organocobalt. Ledit clivage peut se produire en résultat d'un déplacement normal de nucléophiles cellulaires ou par action enzymatique, mais il est de préférence provoqué de manière à se produire de façon sélective à un site de libération prédéterminé par application d'un signal externe. Le signal externe peut être de la lumière ou la photoexcitation, par ex. la photolyse, ou peut être ultrasonique, par ex. la sonolyse. De plus, si la photolyse a lieu en présence d'un champ magnétique qui entoure le site de libération, la libération de l'agent bioactif dans les tissus sains environnants est maintenue à un minimum.

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