The PDT treatment in vivo was carried out on 30 tumorbearing BALB/c mice, and divided into 6 groups: PBS + light, SAC4A + light, TPA-H, TPA-H + light, TPA-H⊂SAC4A, TPA-H⊂SAC4A + light groups. After intratumoral injection of PBS, TPA-H and TPA-H⊂SAC4A, the tumor sites of PBS + light, TPA-H + light, TPA-H⊂SAC4A + light groups were exposed under white light for 30 min, and other groups without light irradiation were served as a control. The tumor size in volume and body weight were monitored every 2 days during the treatment. As illustrated in Figure and 6D, the mice in the group PBS + light, SAC4A + light, TPA-H, TPA-H⊂SAC4A, showed similar tumor growth trend, implying that PBS and SAC4A with light irradiation, TPA-H and TPA-H⊂SAC4A without light irradiation, had no antitumor activity. However, the group of TPA-H + light showed outstanding PDT efficacy. As a hypoxia-sensitive PDT model, TPA-H⊂SAC4A + light group also afforded good antitumor activity. The stable body weights of all mice indicated good biocompatibility of TPA-H and TPA-H⊂SAC4A (Figure ). Hematoxylin and eosin (H&E) staining of tumors and major organs were conducted in each group to explore systemic toxicity. As shown in Figure , no obvious damage and inflammatory lesion were obtained in the heart, liver, spleen, lung and kidney, but TPA-H + light and TPA-H⊂SAC4A + light groups showed remarkable necrosis of the cell nucleus. Additionally, blood routine assays of above all groups were implemented after 14 days' treatment, and few variations of the hematological indexes were detected in Table , further illustrating excellent antitumor activity and low systematic toxicity.