Cancer is a serious threat to human health. Graphene oxide (GO) is a good carrier for cancer treatment due to its large surface area and high drug loading, while it & rsquo;s unstable under physiological conditions with a high tendency to be uptaken by macrophages in the body. This paper constructs a red blood cell (RBC) membrane modified GO nanocarrier system for cancer chemotherapy. After the modification of RBC, the stability and hemolysis performance of GO were greatly improved, which is beneficial to the biological application. Moreover, DOX-loaded RBC-GO still able to maintain good stability with a pH-dependent DOX release profile. RBC-GO can be uptaken by MCF-7 cells and DOX-loaded RBC-GO nanocomposites have strong concentration-dependent cytotoxicity. More importantly, in vivo study showed that RBCGO can accumulate at the tumor site in a large quantity, and among all the experimental groups, RBCGO-DOX had the best anti-tumor effect after tail vein injection in mice and the lowest systemic toxicity. Experiments have proved that RBC-GO can be used as a drug carrier to achieve targeted drug delivery. (c) 2021 Elsevier Inc. All rights reserved.