There is a worldwide need to design new and intelligent vehicles for drug delivery in order to improve the effectiveness of therapy. Graphene oxide presents structural and chemical properties, as well as biocompatibility that can be considered for biomedical applications including the design of drug delivery systems for therapy. The aim of this work was to target graphene oxide functionalized with lactose to the tumoral cell HepG2 that presents the asialoglicoprotein receptor. In order to accomplish this Graphene Oxide (GO) was synthesized by modified Hummer s method. The Hummers method consists in the oxidation of graphite. The GO was modified with lactose by a chemical procedure resulting in a product lactocylated. Afterward, blades of GO lactocylated were synthesized. The GO characterization was done by the following techniques Raman Spectroscopy, Fourier Transform Infrared Spectroscopy (FT-IR), Atomic Force Microscopy (AFM), and X-ray Photoelectron Spectroscopy (XPS). The results show that GO lactocylated is specifically recognized by HepG2 cell indicating that this product could be useful as vehicle tissue-specific for antitumor drug delivery or probe for cell and biological imaging.