Intracellular uptake study of radiolabeled anticancer drug and impedimetric detection of its interaction with DNA

Topoisomerase I inhibitor topotecan (TPT) is the only single-agent therapy certified for the remedy of repetitive small cell lung cancer (SCLC). In this study, TPT was labeled with I-131 via iodogen method and its quality control was determined using thin layer radiochromatography and paper electrophoresis methods. Intracellular uptake study was carried out with human lung adenocarcinoma cell line (A-549) and human lung fibroblast cell line (WI-38). The interaction of I-131-TPT with healthy DNA and cancer DNA was also investigated using single-use sensor technology combined with electrochemical impedance spectroscopy (EIS). The change at the charge transfer resistance (R-ct) obtained before/after interaction was evaluated. Similar to the results of intracellular uptake study, it was found that I-131-TPT could more interact with the cancer DNA than healthy DNA according to the impedimetric results. I-131-TPT is promising in terms of a new nuclear imaging agent for lung cancer. (C) 2016 Elsevier B.V. All rights reserved.