PGMA-based starlike polycations with flanking phenylboronic acid groups for highly efficient multifunctional gene delivery systems

Phenylboronic acid (PBA) possesses good affinities to glycoproteins on cell surfaces, as well as stable fluorescence properties. Recently, it was found that ethanolamine (EA)-decorated poly(glycidyl methacrylate) (PGMA), namely PGEA, exhibited promising applications as effective gene vectors. In this work, a strategy to prepare series of starlike PGEA vectors (s-PGEA-B) with flanking PBA groups was proposed for the development of highly efficient multifunctional gene delivery systems. Compared with the s-PGEA vectors without PBA groups, the corresponding s-PGEA-B counterparts showed a greater ability to bind pDNA. The sizes of the formed s-PGEA-B/pDNA nanoparticles were similar to 100 nm at higher N/P ratios. The s-PGEA-B/pDNA complexes exhibited enhanced cellular internalization and transfection efficiencies, particularly in the cell lines with abundant cell surface glycoproteins. The cellular internalization mediated by s-PGEA-B with 30% of PBA content was about 85% in HepG2 cells, much higher than that of the corresponding s-PGEA (about 53%). In addition, the simultaneous fluorescence emitted from s-PGEA-B provided convenient observation for locating gene vectors during the transfection processes. This present work provides new useful information for the design of multifunctional gene delivery systems.