Abstract: OBJECTIVE To investigate the anti-tumor activity of PEG-modified liposomes combined with sorafenib nuclear transcription factor NF-κB inhibitors PDTC in vivo and in vitro. METHODS The PEG-Sora-LPs were prepared by using thin-film methods. Cytotoxicity assays in vitro were applied to investigate the anti-tumor effect of free drug and liposomes. The in vivo tumor model was established based on the 5-7 weeks old SPF nudes. The weight of the nudes, the weight and size of tumors were measured to assess the anti-tumor effects. And Western blot detection means were applied to evaluate the pro-apoptotic and anti-tumor effects PEG-Sora-LPs combined with varying concentrations of PDTC. RESULTS The optimal prescription of PEG-Sora-LPs were prepared with high encapsulation efficiency and were evenly distributed. The anti-tumor effects of PEG-Sora-LPs were stronger than free drug in SW480 cells in vitro. In vivo animal studies showed that in combination with PEG-Sora-LPs, PDTC could significantly reduce the rate of tumor growth, with higher tumor inhibition and induce apoptosis functions. Western blot analysis also confirmed the joint application of these two had stronger effects to promote tumor cell apoptosis. CONCLUSION PEG-modified liposomes combined with sorafenib nuclear transcription factor NF-κB inhibitor PDTC can significantly increase the anti-tumor and pro-apoptotic effects by in vivo and in vitro experiments. This study can provide a reference for the investigation of sorafenib new drug system.