Abstract: Carboxymethyl chitosan-graft-polycaprolactone (CMCS-g-PCL) was selected as the carrier of Apatinib and drug-loaded micelles were prepared to reduce Apatinib's side effects. Emulsion-evaporation method, dialysis method and film hydration method were used to prepare drug-loaded micelles and UV-Vis spectrophotometry was used to test drug loading contents and encapsulation efficiency of micelles. Then the stability, release and cytotoxicity of micelles were studied. Research showed that emulsion-evaporation method was the best method for preparing drug-loaded micelles and the particle sizes of the prepared micelles were approximately 100~150 nm. The micelles could be stable for more than 21 d in aqueous solution while maintained 7 d in PBS solution. The micelles had a good sustained-release effect and the release rate decreased with the increase of grafting ratio of carrier. Cell proliferation inhibition test showed that the inhibitory effect of drug-loaded micelles on human umbilical vein endothelial cells (HUVECs) gradually increased with the increase of culture time, which was beneficial to long-term treatment.