【Objective】To investigate the safety and efficacy of phosphorylcholine oligomer grafted graphene oxide as a drug carrier for transcatheter arterial chemoembolization in the treatment of liver cancer.【Methods】Doxorubicin loaded folic acid labeled phosphorylcholine oligomer grafted graphene oxide（DOX@GO-PCn-FA）was prepared. Graphene ox? ide（GO）and DOX@GO-PCn-FA were injected intravenously via marginal ear vein in New Zealand white rabbits respec? tively to assess their safety and biodistribution for intravenous administration. Ten male New Zealand rabbits were used to establishe the VX2 liver cancer model and the tumor characteristics were confirmed by dynamic contrast enhanced CT scan. Catheter was inserted via femoral artery and advanced into hepatic lobar or segmental artery. Digital subtraction angi? ography（DSA）was performed to validate the tumor feeding vessels. DOX@GO-PCn-FA was injected through the cathe? ter to carry out selective transcatheter arterial chemoembolization（TACE）. Dynamic enhanced CT scan and pathological examinations of major tissues and organs were implemented 7 days post TACE to evaluate the efficacy of embolizationeffect of DOX@GO-PCn-FA against liver tumor as well as the biodistribution and safety.【Results】Intravenous injection of GO resulted in significant thrombosis and pulmonary embolism whereas DOX@GO-PCn-FA of same dosage did not. DOX@GO-PCn-FA was capable of effectively diminishing the blood supply of liver tumors when applied in TACE. Pathologic exploration revealed that DOX@ GO-PCn-FA mainly deposited in the tumor，and no obvious complications were observed. 【Conclusions】GO- PCn presented superior biocompatibility and exerted effective chemoembolization against liver cancer.