Multimodular assembly useful for intracellular delivery

摘要

A stabilized multimodular assembly for intracellular delivery comprising a complex of at least one cationic transfection agent and of at least one negatively charged macromolecule, wherein the complex has a theoretical charge ratio ranging from about 0 to about 4, and an efficient amount of at least one amphiphilic block co-polymer acting as a steric colloidal stabilizer with respect to the complex, the block co-polymer having hydrophilic and hydrophobic blocks wherein at least one hydrophilic block is conjugated with at least one targeting ligand.

主权项

1. A stabilized multimodular assembly useful for intracellular delivery comprising:
a complex of at least one cationic transfection agent and of at least one negatively charged macromolecule, wherein said complex has a theoretical charge ratio ranging from about 0 to about 4, the theoretical charge ratio being defined as a number of moles of positive charges per mole of negative charges, and an efficient amount of at least one amphiphilic block co-polymer acting as a steric colloidal stabilizer with respect to said complex, said amphiphilic block co-polymer comprising hydrophilic and hydrophobic blocks wherein at least one hydrophilic block is conjugated with at least one targeting ligand, and wherein said amphiphilic block co-polymer is an A-B-A type linear block co-polymer of the following formula (III) or formula (IV): in which x and z have, independently of each other, a value from about 100 to about 200, and y has a value from 35 to about 80.