Zn(ii)-Dipicolylamine analogues with amphiphilic side chains endow low molecular weight PEI with high transfection performance

Abstract

To investigate the effect of amphiphilic balance of Zn(II)-dipicolylamine analogues on the transfection process, we fabricated a series of Zn(II)-dipicolylamine functional modules (DDAC-Rs) with different hydrophilic-phobic side chains to modify low molecular weight PEI (Zn-DP-Rs) by the Michael addition reaction. Zn-DP-Rs with hydrophilic terminal hydroxy group side chains demonstrate superior overall performance compared to those of hydrophobic alkyl side chains. In terms of the influence of the chain lengths in DDAC-Rs, from Zn-DP-A/OH-3 to Zn-DP-A/OH-5, the corresponding transfection efficiency shows an upward trend as the lengths increase. However, decreasing efficacy is observed with further increase in the length of side chains. In addition, the Zn-DP-Rs with amphiphilic side chains show prominent performance in every respect, highlighting the significance of balance in the amphipathy of side chains in DDAC-Rs. This work is of great significance for the development of polycationic gene carrier materials with excellent performance.