In order to improve its biological properties, graphene oxide can be modified with hydrophilic polymers. Therefore, in this study, the surface of graphene oxide was modified with polyethylene glycol and albumin by covalent methods. In the subsequent step, paclitaxel which is a hydrophobic anticancer drug was loaded onto the surface of the functionalized graphene by π–π interactions. The synthesis of the nanocarrier and its interaction with paclitaxel were evaluated by FT-IR, CD, TEM, UV, AFM, DLS and fluorescence experiments. Release of the loaded drug from albumin–graphene conjugate was investigated at pH 5.4, 6.8 and 7.4.