Polynucleotide formulation for enhanced intracellular transfer

A - Human Necessities – 61 – K

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A61K 47/10 (2006.01) A61K 48/00 (2006.01) C12N 15/87 (2006.01)

Patent

CA 2438696

The invention relates to a pharmaceutical composition comprising a polynucleotide and at least 2 % (weight/volume), preferably 2 to 10 %, of a nonionic copolymer of formula (I) OH(CH2CH2O)a(CH(CH3)CH2O)b(CH2CH2O)cH, in which a, b, and c are such that the polyoxypropylene portion has a molecular weight of between 1450 and 2050, and the polyoxyethylene portions constitute between 75 and 85 % (weight : weight) of the copolymer. The composition is preferably free of cationic lipid or of sodium phosphate. The copolymer is intended to improve the transfer of the polynucleotide into, or the expression of the polynucleotide in, eukaryotic cells. A typical example of a copolymer corresponding to formula (I) is F68. A composition according to the invention is in particular useful in the gene therapy, vaccination and immunotherapy fields.

La présente invention concerne une composition pharmaceutique qui comprend un polynucléotide et au moins 2 % (poids/volume), de préférence de 2 à 10 % d'un copolymère non ionique représenté par la formule (I) : OH(CH2CH2O)a(CH(CH3)CH2O)b(CH2CH2O)cH, dans laquelle a, b et c sont tels que la partie polyoxypropylène ait un poids moléculaire compris entre 1450 et 2050, lesdites parties polyoxyéthylène constituant entre 75 et 85 % (poids: poids) du copolymère. La composition est de préférence dépourvue de lipide cationique ou de phosphate de sodium. Le copolymère est prévu pour améliorer le transfert du polynucléotide dans des cellules eucaryotes ou bien l'expression du polynucléotide dans ces dernières. F68 est un exemple typique d'un copolymère correspondant à la formule (I). Une composition selon l'invention est tout particulièrement utile dans les domaines de la thérapie génique, de la vaccination et de l'immunothérapie.

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