Abstract:[Objective] The aim of this study is to synthesize aminated glycogen (NG) for loading of the photosensitizer TTVBA and construct a nano drug delivery system (NGT NPs) for photodynamic therapy (PDT) of tumors. [Method] Positively charged NG was synthesized through modification of glycogen with diethylenetriamine (DETA). Then, TTVBA was encapsulated by NG via electrostatic interaction to prepare NGT NPs. The prepared NGT NPs were characterized by infrared spectroscopy, dynamic light scattering (DLS), and transmission electron microscopy (TEM). The hemolysis assay was performed to evaluate the biocompatibility of NGT NPs. The reactive oxygen species (ROS) generation capability of cells treated with NGT NPs was detected with the DCFH-DA probe. The in vitro antitumor activity of NGT NPs was assessed by the CCK-8 assay and AM/PI staining. [Result] NGT NPs were spherical, with the diameter of 104.8 nm and the surface potential of 23.83 mV. The ROS generated by the cells treated with NGT NPs (20 μg/mL) under light was 12 folds of that in the dark. The NGT NPs group possessed a hemolysis rate below 0.41%, which indicated excellent biocompatibility. In B16 cells under light, NGT NPs raised the ROS level ( P<0.001) while reducing the cell survival rate in a mass concentration-dependent manner. AM/PI staining showed more cell death in the light group than in the control group. [Conclusion] NGT NPs possessed good biocompatibility, light-responsive induction of ROS generation, and antitumor activity. This work provides a novel and efficient nanocarrier for the PDT of tumors.