Relationship between phosphorylamine-modification and molecular weight on transfection efficiency of chitosan

Abstract The aim of this study is both to design the chitosan (Chi) nanoparticles with different Mw containing the phosphoester bonds and increase their amino function for the transfection. The phosphorylamine-modification of Chi and depolymerized Chi (DChi) was realized using o-phosphorylethanolamine (o-PEA) and characterized, for the first time. The nanoparticles (nMChi and nMDChi) were prepared by ionic gelation and their particle size, polydispersity index (PDI), zeta potential, stability, gene binding capacity and cytotoxicity were examined. The effects of the Mw of Chi on the cytotoxicity, gene binding capacity, and in vitro transfection efficiency of the nanoparticles on Human Embryonic Kidney 293 (HEK293) cells were also examined. Green Fluorescent Protein Circular Plasmid DNA (pEGFN1) loaded nanoparticles (gnMChi and gnMDChi) were used in the transfection. This study showed that the Mw of phosphorylamine-modified Chi significantly affected the characteristics, cytotoxicity, gene binding capacity and transfection efficiency of the nanoparticles.