Linoleic acid (LA) and β-CD-NH2 molecule are covalently conjugated to form a β-CD-LA molecule. The β-CD-LA molecule can self-assemble into spherical micelles with an average particle size of about 50.75±13.58 nm, which is beneficial for blood circulation. The micelles has a high drug loading rate (84.78%±6.78), and in vitro release experiments show that the Dox release from the β-CD-LA-Dox nanomedicine has the characteristics of pH-responsive and slow-release. Cell experiments show that the cytotoxicity of β-CD-LA micelles is relatively low, and β-CD-LA-Dox nanomedicine can enter the cytoplasm well and eventually enter the nucleus, which induce cancer cells apoptosis. In vivo experiments show that β-CD-LA-Dox nanomedicine had a good inhibitory effect on tumor growth without affecting the body weight of mice, and tumor tissue sections proved that β-CD-LA-Dox nanomedicine could induce effectively cancer cell apoptosis which resulted in tumor tissue necrosis, and it showed has a good therapeutic effect on the tumor. [ABSTRACT FROM AUTHOR]