The invention discloses nanoparticles containing apatinib and SN38-polylactic acid coupled medicament as well as a preparation method and application of the nanoparticles. According to the invention,the specific EPR effect of the nanoparticles is utilized, and according to the nanoparticles, controlled release of the two drugs and action on tumor blood vessels and tumor cells at different time sequences can be realized. The anti-vascular drug apatinib is firstly released to act on tumor blood vessels to block local blood vessels on a tumor part, and then the tumor cell killing drug SN38 is released to act on tumor cells locally and efficiently. Moreover, the invention discloses that the apatinib also has a certain inhibition effect on metastasis of liver cancer cells, and the possibilityof drug resistance of tumors to the anti-vascular drug apatinib is reduced to a certain extent. Moreover, the nano drug improves the water solubility of the prodrug apatinib and SN38-polylactic acid,and can be directly injected intravenously.