Application of nanoparticles based on hydrophilic polymers...

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A61K 9/51 (2006.01) A61K 31/715 (2006.01) A61K 38/16 (2006.01) A61K 47/36 (2006.01)

Patent

CA 2233501

Application of nanoparticles based on hydrophilic polymers as, pharmaceutical forms for the administration of active macromolecules. The nanoparticles (having a nanometric size and a hydrophilic character), also called nanospheres or latex, are colloidal systems comprised of the combination of hydrophilic polymers and an active ingredient having a high molecular weight (active macromolecule, molecular weight higher than 1000 daltons). The hydrophilic polymers are the chitosane (an aminopolysaccharide) or its derivatives and the polyoxyethylene or its derivatives. The association of the active macromolecule to said nanoparticles takes place in an aqueous phase without having to use organic solvents or auxiliary toxic substances. The active ingredient charge capacity of the nanoparticles is extremely high and additionally said charge is released in a controlled and time extended way. Additionally, said nanoparticles have a positive surface electric charge which the intensity may vary in relation to its composition.

Application de nanoparticules à base de polymères hydrophiles en tant que formes pharmaceutiques pour l'administration de macromolécules actives. Les nanoparticules (de taille nanométrique et de caractères hydrophile), également appelées nanosphères ou latex, sont des systèmes colloïdaux formés par la combinaison de polymères hydrophiles et d'un ingrédient actif de poids moléculaire élevé (macromolécule active, poids moléculaire supérieur à 1000 daltons). Les polymères hydrophiles sont le chitosane (un aminopolysaccharide) ou ses dérivés et le polyoxyéthylène ou ses dérivés. L'association de la macromolécule active avec lesdites nanoparticules se fait en phase aqueuse sans avoir besoin d'utiliser des solvants organiques ou des substances auxiliaires de nature toxique. La capacité de charge d'ingrédients actifs des nanoparticules est extrêmement élevée et de plus cette charge est libérée de façon contrôlée et prolongée dans le temps. En outre, lesdites nanoparticules ont une charge électrique superficielle positive dont l'intensité peut varier en fonction de leur composition.

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