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Artemisinin or its derivatives possess a remarkable capacity to exert anti-colorectal cancer (CRC) effects depending on higher Fe concentration in tumor tissue than healthy tissues. However, it can lead to severe bone marrow suppression and the liver is the primary site of iron storage. So the therapeutic concentration could not be reached at the lesion sites of hepatic metastases.Therefore, Artemether (ARM) is incorporated in docosahexaenoic acid-modified BSA nanoparticles (DBNs), and the activities of ARM@DBNs in inhibiting colorectal cancer liver metastases (CRLM) were investigated. The in vitroand in vivostudies indicated that the docosahexaenoic acid (DHA)-modified nanoparticles targeted the CRC cell effectively. The in vitrodrug release of ARM@DBNs showed that nanoparticles released in a sustained and controlled manner against CRC cells. Notably, results also showed that the ARM@DBNs had higher inhibition of CRLM than the ARM in vivo. The mean survival of ARM@DBNs (31.4 ± 3.09 d) was longer than that of ARM (20.3 ± 2.49 d), P＜0.05. In consideration of the activities in inhibiting CRLM, the ARM@DBNs might hold potential in CRLM treatment.