Cationic nanoparticles of CS were developed according to ionotropic gelation process as potential cancer cell targeting agent. CS nanoparticies (CSNP) (F1 and F2) diameters varied between ranges of 100 -800 nm. Particle size, polydispersity index and zeta potential values of formulations were measured by photon correlation spectroscopy. The morphological analysis for CSNPs was provided with scanning electron microscopy. For cell incorporation study, F1 and F2 were directly labeled by Technetium-99m (Tc-99m), radiochemical purity and stability of the complex were analyzed by radioactive thin layer chromatography and radioactive high performance liquid chromatography studies. After that, incorporation of Tc-99m labeled F1 and F2 were evaluated in U2OS and NCl-H209 cell lines. The six well plates were used for all experiments and the integrity of each cell monolayer was checked by measuring its TEER values with an epithelial voltammeter. Results confirmed that Fl and F2 formulations were successfully radiolabeled with Tc-99m. The incorporation percentages of Tc-99m labeled Fl and F2 in NCI-H209 and U2OS cell lines were found different when they compared to Tc-99m solution. Since Tc-99m labeled Fl and F2 highly uptake in cancer cell line. The results demonstrated that radiolabeled CSNPs may be a promising agent for cancer diagnosis. (C) 2015 Elsevier B.V. All rights reserved.