Stabilized microparticles and their use as ultrasound...

A - Human Necessities – 61 – K

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A61K 49/00 (2006.01) A61K 49/22 (2006.01)

Patent

CA 2268763

Microparticles useful for enhancing the ultrasound image of a tissue or organ consist of liquid and/or gas core material which is encapsulated by a biocompatible, tanned protein shell. These stabilized microparticles are useful as ultrasonic imaging agents, and are additionally useful in the further production of functionalized microparticles for in vivo imaging. In particular, targeting molecules such as antibodies or other ligands can be attached to the strengthened exterior surface of the stabilized microparticles to impart target-specificity to the microparticles. The targeting molecules may also provide hydrophilicity to the exterior surface, thus increasing the recirculation time of the microparticles. The targeting molecules may be attached directly to the exterior surface of the microparticles, or they may be attached via a bifunctional spacer arm, which may itself be hydrophilic. The target-specific microparticles are injected intravenously, allowed to accumulate at the target site, and used to enhance the ultrasound image of a target tissue or organ.

L'invention concerne des microparticules utiles pour améliorer l'image par ultrasons d'un tissu ou d'un organe, consistant en un matériau central liquide et/ou gazeux encapsulé dans une enveloppe protéique "tannée", biocompatible. Ces microparticules stabilisées sont utiles en tant qu'agents de contraste en imagerie à ultrasons, et, en outre, dans la production ultérieure de microparticules fonctionnalisées destinées à l'imagerie in vivo. En particulier, on peut associer des molécules d'acheminement vers la cible, telles que des anticorps ou d'autres ligands, à la surface externe renforcée des microparticules stabilisées en vue de donner une spécificité de ciblage aux microparticules. Les molécules d'acheminement vers la cible peuvent également donner à la surface externe un caractère hydrophile, augmentant ainsi le temps de recirculation des microparticules. On peut associer les molécules d'acheminement vers la cible directement à la surface externe des microparticules, ou les associer à l'aide d'un bras localisateur bifonctionnel, pouvant lui-même être hydrophile. On injecte les microparticules à spécificité de ciblage par intraveineuse, on les laisse s'accumuler à l'endroit cible, et on les utilise pour améliorer l'image par ultrasons d'un tissu ou d'un organe cible.

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