Motivated by the enhanced cytotoxicity of some chemotherapeutic agents at temperature rise, multifunctional chitosan nanospheres which co-carried gold nanorods and cisplatin were prepared. These hybrid nanospheres were characterized by dynamic light scattering, zeta potential, UV-Vis absorption spectra and transmission electron microscopy. It was demonstrated that these 120 nm-sized hybrid nanospheres could be selectively accumulated at the tumor site with about 11% injection dose per g of tumor, and produced local hyperthermia to an average temperature of 49 °C in tumor tissue after near-IR irradiation for 10 min. Due to the enhanced cytotoxicity of cisplatin at elevated temperatures, cisplatin-loaded hybrid nanospheres showed about one-second lower IC50 values than hybrid nanospheres alone in vitro and almost complete tumor growth inhibition in vivo. Compared with chemotherapy or photothermal treatment alone, the combined photothermal therapy and chemotherapy had a significantly synergistic effect and improved the therapeutic efficacy, which was supported by immunofluorescence staining and in vivo apoptosis imaging.
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