Oligoarginine-linked polymers-induced penetration enhancement of poorly membrane-permeable molecules via cell membranes

Abstract

Cationic oligopeptides, which are mainly composed of basic amino acids such as arginine, are internalized into cells via macropinocytosis. We designed a novel polymer: cationic oligopeptide-linked polymer, with the expectation that the polymers will remain on the cell membrane and poorly membrane-permeable molecules are continuously internalized into cells mainly via macropinocytosis repeated for the individual peptidyl branches in the polymer backbone without the concomitant cellular uptake of the polymers. Here, we report the potential of oligoarginine-linked polymers, mainly poly(N-vinylacetamide-co-acrylic acid) modified with D-octaarginine, as a new class of penetration enhancers.