Multi-arm block copolymers as drug delivery vehicles

Details Multi-arm block copolymers as drug delivery vehicles Multi-arm block copolymers as drug delivery vehicles

C - Chemistry, Metallurgy

08

G

C08G 81/00 (2006.01) A61K 31/724 (2006.01) A61K 31/77 (2006.01) A61K 47/48 (2006.01) C08G 65/26 (2006.01) C08L 71/02 (2006.01)

Patent

CA 2435301

The invention provides multi-arm block copolymers useful as drug delivery vehicles comprising a central core molecule, such as a residue of a polyol, and at least three copolymer arms covalently attached to the central core molecule, each copolymer arm comprising an inner hydrophobic polymer segment covalently attached to the central core molecule and an outer hydrophilic polymer segment covalently attached to the hydrophobic polymer segment, wherein the central core molecule and the hydrophobic polymer segment define a hydrophobic core region. The solubility of hydrophobic biologically active agents can be improved by entrapment within the hydrophobic core region of the block copolymer. The invention further includes pharmaceutical compositions including such block copolymers, methods of making such copolymers and pharmaceutical compositions, and methods of using the block copolymers as drug delivery vehicles.

L'invention concerne des copolymères séquencés à bras multiples utiles en tant que véhicules pour l'administration de médicaments. Ces copolymères comprennent une molécule formant un noyau central, telle qu'un résidu d'un polyol, et au moins trois bras copolymères liés de manière covalente avec cette molécule de noyau central, chaque bras copolymère comprenant un segment polymère hydrophobe interne lié de manière covalente avec la molécule du noyau central, et un segment polymère hydrophile externe lié de manière covalente avec le segment polymère hydrophobe, la molécule du noyau central et le segment polymère hydrophobe définissant une région centrale hydrophobe. La capture des agents biologiquement actifs hydrophobes dans la région du noyau hydrophobe du copolymère séquencé permet d'améliorer la solubilité de ceux-ci. L'invention concerne en outre des compositions pharmaceutiques comprenant de tels copolymères séquencés, et des procédés permettant de préparer de tels copolymères et compositions pharmaceutiques, ainsi que des procédés comprenant l'utilisation de ces copolymères séquencés en tant que véhicules d'administration de médicaments.

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