Stimuli-responsive self-assembled polyethylenimine nanocomposites useful for colon-targeted gene and drug delivery
摘要
In order to enhance the transfection efficiency of a non-toxic-branched polyethylenimine (bPEI 1.8 kDa), a series of amphiphilic azo-conjugates has been prepared from the reaction of PEI with varying amounts of Dab-CETU. The resulting PEI-Dabsyl (P-Dab) conjugates, in an aqueous medium, self-assembled to form core/shell nanocomposites, which, on complexation with pDNA, exhibited excellent transfection efficiency. Among these complexes, P-Dab-1/pDNA complex displayed ~ 12-fold higher transfection efficacy vs. the PEI/pDNA complex. Further, these nanocomposites showed stimuli-responsiveness under the influence of UV-Vis light and azoreductase enzyme. Drug-entrapped nanocomposites showed faster in vitro release in response to human endogenous enzyme DT-diaphorase (azoreductase).
Graphical abstract