Design, synthesis and transfection efficiency of a novel redox-sensitive polycationic amphiphile

Abstract

A novel redox-sensitive polycationic amphiphile (2S3) with disulphide linkers for nucleic acid delivery was developed. Cationic liposomes formed by 2S3 and the helper lipid DOPE demonstrated effective DNA delivery into HEK293 cells with a maximal transfection activity that is superior than both nonredox-sensitive cationic liposomes and Lipofectamine® 2000 at an N/P ratio of 6/1. Redox-sensitivity was tested by experiments with extracellular glutathione which shown the ability of disulphide linker degradation. Our results suggest that polycationic amphiphile 2S3 is a promising candidate for nucleic acid delivery.

Keywords: Cationic liposomes; Disulphide linker; Gemini amphiphiles; Gene therapy; Redox-sensitive.