Method for preparing vesicular nanocapsules

Details Method for preparing vesicular nanocapsules Method for preparing vesicular nanocapsules

A - Human Necessities

61

K

A61K 9/51 (2006.01) A61K 31/216 (2006.01) A61K 31/355 (2006.01) A61K 31/405 (2006.01)

Patent

CA 2297760

The invention concerns the preparation of nanoparticles for encapsulating active principles, and more precisely a method for obtaining vesicular nanoparticles dispersible in aqueous phase in colloidal form, which are non-toxic, biologically compatible, stable in colloidal suspension, protecting well the active principle and simply and inexpensively obtainable. The method consists in using two non-oily phases S¿1? (ethyl acetate) and S¿2? (water), non-miscible with each other and a third oily phase S¿3? (mygliol); in producing an oil-in-water emulsion whereof the dispersed phase comprises S¿3?, S¿1?, or a polymer PE dissolved in S¿1? and designed to form the nanocapsule envelope and optionally a dissolved active principle PA (S¿1? being brought by a solution saturated with S¿2? in S¿1?) and whereof the continuous phase is S¿2? = non-solvent of PE; and in extracting from the dispersed phase, ensuring that the conditions of the continuous phase are such that S¿1? is miscible in S¿2?, thereby obtaining a stable colloidal solution of nanocapsules with diameter of the order of 300 nanometers.

L'invention concerne la préparation de nanoparticules pour l'encapsulation de principes actifs. L'un des objectifs de l'invention est de fournir un procédé d'obtention de nanocapsules vésiculaires dispersibles en phase aqueuse sous forme colloïdale, non-toxiques bio-compatibles, stables en suspension colloïdale, protégeant bien le principe actif et obtenables de manière simple et économique. Le procédé consiste à faire intervenir deux phases non huileuses S1 (acétate d'éthyle) et S2 (eau), non miscibles l'une à l'autre et une troisième phase huileuse S3 (mygliol); à réaliser une émulsion huile dans l'eau dont la phase dispersée comprend S3, S1, ou un polymère PE dissous dans S1 et destiné à former l'enveloppe des nanocapsules et éventuellement un principe actif PA dissous (S1 étant apporté par une solution saturée de S2 dans S1) et dont la phase continue est S2 = non-solvant de PE; et à extraire S1 de la phase dispersée, en faisant en sorte que les conditions de la phase continue soient telles que S1 soit miscible dans S2. On obtient ainsi une solution colloïdale stable de nanocapsules de diamètre de l'ordre de 300 nanomètres.

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