In this work, we reported a facile method to produce stable aqueous graphene dispersion through direct exfoliation of graphite by modified hyperbranched polyglycerol. Size of graphene sheets was manipulated by simultaneous exfoliation and sonication of graphite, and functionalized graphene sheets with narrow size distribution were obtained. The polyglycerol-functionalized graphene sheets exhibited highly efficient cellular uptake and photothermal conversion, enabling it to serve as a photothermal agent for cancer therapy.