Phenylboronic-acid-modified amphiphilic polyether as a neutral gene vector.

ABSTRACT

A phenylboronic-acid-modified amphiphilic block polyether is prepared via reaction of polyglycidol-block-poly(ethylene oxide)-block-poly(propylene oxide)-block-poly(ethylene oxide)-block-polyglycidol (Pluronic-PG) with 2-(N,N-dimethylaminomethyl)-5-aminomethyl phenylboronic acid using phosgene as a coupling reagent. The boronic-acid-modified non-cationic polymer binds plasmid pGL3 effectively, forms sub-µm polymer/DNA complex particles, and greatly facilitates the cell uptake of the plasmid. The efficiency of the polymer as a gene vector is evaluated in vitro by transfection of pGL3 to HeLa, COS-7 and HepG2 cells. Pluronic-PG-BA enhances the transfection efficiency by 100 to 1000 times compared with Pluronic-PG. The presence of serum does not significantly affect the transfection efficiency.