Histidylated cationic polyorganophosphazene/DNA self-assembled nanoparticles for gene delivery

摘要

Cationic polyorganophosphazene has shown the ability to deliver gene. To obtain more efficient transfection, His (Boc)-OMe bearing histidine moiety was introduced to synthesize a new derivative of canonic polyphosphazenes with another side group of 2-dimethylaminoethylamine (DMAEA). The poly (DMAEA/His (Boc)-OMe) phosphazene (PDHP) and DNA could self-assembled into nanoparticles with a size around 110nm and zeta potential of+15mV at the PDHP/DNA ratio of 10:1 (w/w). The maximum transfection efficiency of PDHP/DNA self-assembled nanoparticles (PHSNs) against 293 T cells at the polymer/DNA ratio of 10:1 was much higher than that of control group, poly (di-2-dimethylaminoethylamine) phosphazenes (PDAP)/DNA self-assembled nanoparticles (PASNs), but the cytotoxicity of PDHP assayed by MTT was much lower than that of PDAP. These results suggested that PDHP could be a good candidate with high transfection efficiency and low cytotoxicity for gene delivery.