Liposomes as targeted drug delivery systems are an emerging strategy in the treatment of cancer to selectively target tumors or genes. In this study, we generated the recombinant protein, EC1-GLuc, by fusing the EC1 peptide, an artificial ligand of ErbB2, with Gaussia luciferase (GLuc). The purified EC1-GLuc was conjugated with a nickel-chelating liposome to construct the EC1-GLuc-liposome. In vitro experiments revealed that the EC1-GLuc-liposome selectively targeted and internalized into ErbB2-overexpressing SKOv3 cells for bioluminescence imaging. A cell-impermeable fluorescence dye (HPTS) encapsulated in the EC-GLuc-liposome was efficiently delivered into the SKOv3 cells. In addition, the EC1-GLuc-liposome also targeted metastatic SKOv3 tumors for bioluminescence imaging and effectively delivered HPTS into metastatic tumors in vivo. Therefore, the present study demonstrates the novel EC1-GLuc-liposome to be an effective theranostic system for monitoring and treating ErbB2-overexpressing metastatic ovarian carcinoma through a combination of targeted molecular imaging and DDS.