RVG peptide tethered bioreducible polyethylenimine for gene delivery to brain.

The work demonstrated the successful delivery of gene to mouse brain overcoming the blood-brain barrier (BBB) through expedient vector construct having RVG peptide as targeting ligand for neuronal cells. The newly developed delivery vector was designed to impart bioreducibility for greater intracellular pDNA release, higher serum stability and efficient complexing ability by incorporating disulfide linkage, PEG and low molecular weight polyethylenimine, respectively. The physiochemical properties of the polyplex, its cytotoxicity and the in vitro transfection efficiency on Neuro2a cell were studied prior to the successful in vivo study. In vivo fluorescence assay substantiated the permeation of the pDNA loaded polymeric vector through the BBB. The RVG-mediated target-specific cellular uptake of polymeric vector was established conclusively by competitive assay.