Liposome formulations of boronic acid compounds

Details Liposome formulations of boronic acid compounds Liposome formulations of boronic acid compounds

A - Human Necessities

61

K

A61K 9/127 (2006.01) A61K 31/69 (2006.01) A61K 41/00 (2006.01) A61K 47/48 (2006.01)

Patent

CA 2697044

A liposome composition comprised of liposomes having a pep-tide boronic acid proteasome inhibitor compound entrapped in the liposomes is described. More specifically, liposomes having a compound of Formula I or II entrapped in the interior aqueous compartment are loaded with a peptide boronic acid compound, to form a boronate ester compound inside the liposo-mal aqueous compartment. In one embodiment, the liposomes have an outer coating of hydrophilic polymer chains and are used to treat a solid tumor in a subject.

Cette invention se rapporte à une composition liposomale constituée de liposomes ayant un inhibiteur du protéasome d'acide boronique peptidique piégé dans les liposomes. Plus spécifiquement, les liposomes ayant un composé de formule I ou II piégé dans le compartiment aqueux intérieur sont chargés avec un composé d'acide boronique peptidique, et forment un composé d'ester de boronate à l'intérieur du compartiment aqueux du liposome. Dans un mode de réalisation, les liposomes ont un enrobage externe constitué de chaînes polymères hydrophiles et sont utilisés pour traiter une tumeur solide chez un sujet.

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