OBJECTIVE Nanotechnology provides a novel strategy for the delivery of anticancer drugs. In this study, titanium dioxide coated gold nanorod (GNR/TiO2) nanostructures were used as the drug carrier for gambogic acid in order to improve its anticancer effect. METHODS Biocompatibility and cellular uptake of GNR/TiO2 nanostructures were studied in human glioblastoma U-87 MG cells. Cell viability was evaluated by ATP assay and calcein AM staining. LysoSensor Green DND-189 and Hoechst 33342 were used to analyze the intracellular location of GNR/TiO2 nanostructures. The in vitro anti-cancer effect of gambogic acid loaded nanoparticles was compared with free drug. RESULTS The results showed that GNR/TiO2 nanostructures are biocompatible, and they are localized at the intracel?lular acidic compartments of endosomes and lysosomes. The intracellular drug content delivered via GNR/TiO2 nanostructures was 6 fold higher than the free form, thus dramatically enhancing the anticancer effect of gambogic acid. Furthermore, mild photothermal therapy also showed synergistic effect with the drug. CONCLUSION Our study suggested that GNR/TiO2 nanostructures can be considered as a promising anticancer drug carrier.