To achieve tumor-specific delivery of doxorubicin, TiO@FeO/PEI/delivery of doxorubicin conjugates were designed and synthesized. FeO could act as magnetically responsive carriers and enhance the visible light photodynamic activities of TiO Delivery of doxorubicin was conjugated via coordination bond. The drug release rate at pH 5.2 was much faster than that at pH 7.4, due to pH-sensitive coordination bond. Besides, TiO@FeO/PEI/delivery of doxorubicin showed high antitumor efficacy combining with phototherapy, good bio-safety, higher cellular uptake with an external magnetic field, and less toxicity in vitro and in vivo. These results suggested that TiO@FeO/PEI/delivery of doxorubicin may be promising for high tumor treatment efficacy with minimal side effects in future.