Phenylboronic-Acid-Modified Amphiphilic Polyether as a Neutral Gene Vector

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. An amphiphilic block polyether bearing pendant phenylboronic acid groups on the hydrophilic blocks can form sub‐µm polymer/DNA complex particles and greatly facilitate the cell uptake of DNA. It enhances the transfection efficiency of pGL3 to HeLa, COS‐7 and HepG2 cells by a factor of 100 to 1000. Notably, the transfection efficiency is not significantly affected by the presence of serum.