Hazard-free microencapsulation for structurally delicate...

A - Human Necessities – 61 – K

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A61K 9/66 (2006.01) A61K 9/107 (2006.01) A61K 9/48 (2006.01) A61K 9/50 (2006.01) A61K 31/7088 (2006.01) A61K 35/76 (2006.01) A61K 38/17 (2006.01) A61K 47/30 (2006.01) A61K 47/36 (2006.01) B01J 13/02 (2006.01) A61K 9/16 (2006.01)

Patent

CA 2487867

This invention provides method for sustained release delivery of structurally delicate agents such as proteins and peptides. Using a unique emulsion system (Stable polymer aqueous-aqueous emulsion), proteins and peptides can be microencapsulated in polysacchride glassy particles under a condition free of any chemical or physical hazard such as organic solvents, strong interfacial tension, strong shears, elevated temperature, large amount of surfactants, and cross-linking agents. Proteins loaded in these glassy particles showed strong resistance to organic solvents, prolonged activity in hydrated state, and an excellent sustained release profile with minimal burst and incomplete release when being further loaded in degradable polymer microspheres. This invention provides a simple yet effective approach to address all the technical challenges raised in sustained release delivery of proteins.

L'invention concerne un procédé de libération prolongée d'agents de structure délicate tels que des protéines et des peptides. Grâce à un système unique d'émulsion (émulsion aqueuse-aqueuse stable de polymère), il est possible de microencapsuler des protéines et des peptides dans des particules de polysaccharides vitreux dans des conditions ne comportant aucun danger chimique ou physique, tel que solvant organique, tension interfaciale importante, cisaillement élevé, température élevée, quantité importante de tensioactif et agent de réticulation. Les protéines chargées dans ces particules vitreuses montrent une grande résistance aux solvants organiques, une activité prolongée à l'état hydraté, et un très bon profil de libération prolongée avec éclatement et libération incomplète minimums lorsqu'elles sont chargées dans des microsphère de polymère dégradable. Cette invention concerne donc une approche simple mais efficace de résolution des challenges techniques posés par l'administration sous forme de libération prolongée de protéines.

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