Abstract: Gene therapy holds great promise in providing new approaches for the treatment of a large number of inherited and acquired diseases, such as cancer. Yet its widespread application has been restricted by naked genes vulnerable to enzyme degradation, the rapid clearance by renal filtration, the poor cellular uptake and the inefficient escape out of endosome into cytosol. A successful gene therapy mainly relies on the development of an efficient gene delivery system. The safe and efficient delivery of therapeutic genes to host cells and subsequent release in the target compartment in a therapeutic way represents a fundamental obstacle to the clinical success of gene therapy. Here, we summarize the recent researches concerning biocompatible polymers such as chitosan, poly(amino ester)s and their derivatives as non-viral vectors for cancer gene therapy.