Sulfonated aluminum phthalocyanine (AlPcS), a widely used photosensitizer for photodynamic therapy of cancer, was conjugated to doxorubicin (Dox), a chemotherapy drug, through electrostatic binding. The fluorescence resonance energy transfer from Dox to AlPcS showed the formation of AlPcS-Dox conjugates, as the fluorescence intensity of conjugated Dox was decreased and that of the AlPcS moiety was enhanced. This AlPcS-Dox conjugation was further confirmed by electrophoresis. The AlPcS-Dox conjugates enhanced the cellular uptake of AlPcS three times more than unconjugated AlPcS in both human hepatocellular carcinoma cell line 7701 and rat basophilic leukemia cell line. Moreover, the photodynamic killing effect of the conjugates was markedly increased as compared with that of AlPcS alone or the cytotoxicity of Dox alone, showing an enhanced effect of the AlPcS-Dox conjugates. These results indicate that the conjugation of a photosensitizer with a chemotherapy drug may improve photodynamic cancer therapy.