Abstract: OBJECTIVE To prepare doxorubicin(DOX)-loaded titanium dioxide(TiO₂) nanoparticles and evaluate in vitro release and cytotoxicity. METHODS The TiO₂ nanoparticles were sythesized using solvothermal reaction and then characterized with TEM and X-ray diffraction (XRD). The drug loading capacity and release profile were determined using UV-Vis spectrophotometer. The cytotoxicity against MCF-7 and Hela cells was evaluated by MTT method. RESULTS The obtained TiO₂ nanoparticles with the length about 200 nm were well dispersed in water. The drug loading capacity in water was 10.85%. The release of DOX in vitro was pH sensitive. No obvious cytotoxicity of TiO₂ nanoparticles was observed. The drug-loaded nanoparticles showed equivalent cytotoxicity against MCF-7 and Hela cells with free DOX. CONCLUSION TiO₂ nanoparticles which show high drug loading capacity and controllable drug release can be used as a novel carrier for the antitumor drug doxorubicin.