The present invention provides a bufalin liposome comprising a liposome bilayer and bufalin. The liposome bilayer comprises phospholipid, sterol and polyethylene glycol (PEG)-derived compound. The liposome of the present invention can be used to treat cancer, especially a cancer chosen from liver cancer, lung cancer, ovarian cancer, prostate cancer, colon cancer, pancreas cancer, gastric cancer, and leukemia. The preparation method of the present invention is simple, and the bufalin liposome can increase an effect of antitumor, reduce a toxicity compared with bufalin monomer, and has wide applications.
