Liposome allowing liposome-entrapped substance to escape...

A - Human Necessities – 61 – K

Patent

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Details

A61K 9/127 (2006.01) A61K 47/34 (2006.01) A61K 47/42 (2006.01)

Patent

CA 2573696

It is intended to provide a liposome, wherein a hydrophilic polymer has been introduced into the outer face of the liposome membrane, allowing the discharge of a substance entrapped in the liposome from an endosome thereby releasing it into the cytoplasm. This object is achieved by providing a liposome containing a liposome membrane-constituting substance bonded to the following peptide (a) or (b) and a liposome membrane-constituting substance bonded to one end of a hydrophilic polymer to the other end of which the following peptide (a) or (b) is bonded: (a) a peptide comprising the amino acid sequence represented by SEQ ID NO:1; and (b) a peptide having an amino acid sequence derived from the amino acid sequence represented by SEQ ID NO:1 by deletion, substitution or addition of one or more amino acids and being capable of fusing lipid membranes together under acidic conditions.

L'invention concerne un liposome, dans la face externe de la membrane duquel on a introduit un polymère hydrophile, permettant ainsi la libération d'une substance piégée dans le liposome à partir d'un endosome pour de cette manière la libérer dans le cytoplasme. On parvient à réaliser cet objet avec un liposome contenant une substance constituant la membrane du liposome liée au peptide (a) ou (b) suivant et une substance constituant la membrane du liposome liée à une extrémité d'un polymère hydrophile dont l'autre extrémité est liée au peptide (a) ou (b) suivant : (a) un peptide comprenant la séquence d'acides aminés représentée par la SEQ ID n° : 1 ; et (b) un peptide ayant une séquence d'acides aminés dérivée de la séquence d'acides aminés représentée par la SEQ ID n° : 1 par délétion, substitution ou addition d'un ou plusieurs acides aminées et qui est capable de fusionner ensemble des membranes de lipides dans des conditions acides.

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