The present invention discloses a gene delivery system containing a reduction-sensitive shielding system having a targeting function, a preparation method and an application in the field of gene therapy thereof. The gene delivery system is composed of a reduction-sensitive shielding system having a targeting function, cationic polymer material and plasmid DNA; the cationic polymer material and the plasmid DNA complexed to form complex particles, the reduction-sensitive shielding system having a targeting function is shielded on the complex surface by means of electrostatic interaction, so as to reduce the toxicity of the delivery system and successfully transfer the loaded genetic material into cells, thereby achieving expression of genetic material and completing the transfection process, and moreover, improving the targeting and the efficiency of gene transfection.