A stimulatable asymmetrical polymersome

A - Human Necessities – 61 – K

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A61K 8/11 (2006.01) A61K 8/90 (2006.01) A61K 9/127 (2006.01)

Patent

CA 2737421

The invention relates to a polymer vesicle with an asymmetrical unilamellar membrane, said membrane being constituted by two distinct layers, a layer (A) and a layer (B), said layers comprising respective amphiphilic block copolymers with layer (A) comprising, in contrast to said layer (B), an effective quantity of amphiphilic block copolymer comprising at least one stimulatable hydrophobic polymer block, said block polymers provided by said copolymers being capable of adopting a new steric configuration in response to an exogenous stimulus, conditioning the rupture of said unilamellar membrane. The invention also provides a method of producing said vesicle, a method of encapsulating an active ingredient in said vesicles, and a method of controlled release of the active ingredient.

La présente invention concerne une vésicule polymère comportant une membrane unilamellaire asymétrique, ladite membrane étant constituée de deux couches distinctes, une couche (A) et une couche (B), comprenant respectivement des copolymères séquencés amphiphiles. La couche (A) comporte, à la différence de la couche (B), une quantité efficace de copolymères séquencés amphiphiles comprenant au moins un polymère séquencé hydrophobe stimulable, lesdits polymères séquencés apportés par lesdits copolymères étant capables d'adopter une nouvelle configuration stérique en réponse à un stimulus exogène, ce qui conditionne la rupture de ladite membrane unilamellaire. L'invention concerne également un procédé de production de ladite vésicule, un procédé d'encapsulation d'un principe actif dans ladite vésicule et un procédé de libération contrôlée dudit principe actif.

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