High-resolution continuum source atomic absorption spectroscopy (HR-CS AAS) is a valuable analytical technique for metal quantification because of its high sensitivity and selectivity for metal atoms as well as its improved background correction mode. However, the quantification of metals in biological materials, e.g. cell lysates, is still challenging because of matrix effects and other experimental complications. A method to quantify the titanium content of tumor cells exposed to titanium-based drugs was developed using HR-CS AAS. This method allows the quantification of titanium in cell suspensions in the low µg L-1 range with a detection limit of 48.8 µg L-1. The procedure was applied to the study of the cellular uptake of novel titanium metallodrugs (namely titanium (IV) salan complexes) and results showed a higher accumulation of these complexes in cancer cells compared to the titanium lead compound, titanocene dichloride. The improved cellular uptake of the studied complexes indicates a target located inside the cells and this could possibly lead to a higher antitumor effect of this novel class of metallodrugs. The antiproliferative potential of the complexes was confirmed in two different cancer cell lines, in which the titanium complexes showed good to moderate activity.