The conjugation of bioactive molecules to polymeric nanocarriers has the potential to revolutionize current methods of cancer therapy. These nanocarriers can also reduce the undesirable adverse effects of small molecule therapeutic agents. In the present study, the LC-g-PEI (lauryl chitosan graft polyethyleneimine) polymer was synthesized and evaluated as a potential carrier of therapeutic molecules, such as the p53 gene and doxorubicin. The study was designed to investigate the cytotoxicity, drug uptake and transfection efficiency of LC-g-PEI. This polymer had lower interactions with blood components than the unmodified PEI. LC-g-PEI buffered protons, protected DNA from nuclease attack and induced effective gene transfer in the C6 cell line. LC-g-PEI that had incorporated doxorubicin exhibited an enhanced release of this compound at pH 5. LC-g-PEI demonstrated its efficacy in the enhancement of drug uptake and the promotion of gene expression in the C6 cell line. Therefore, LC-g-PEI shows promise as a drug/gene carrier with potential applications in cancer therapy. (c) 2012 Elsevier Ltd. All rights reserved.