Nanomaterials have a prominent role in new methods of diagnosis and treatment of cancer, so the development of smart nanocarriers constitutes a competent strategy against cancer. Graphene oxide (GO) has a hydrophilic character, which gives it stability in the physiological environment, thanks to which graphene oxide can be used in biomedical applications. GO, due to its large surface area, mechanical resistance and oxygenated groups on the surface and/or edges, can support and transport drugs. In addition, its functionalization with COOH has shown better efficiency in transporting drugs and other compounds, also facilitating their dispersion. Curcumin (Cur), which possesses anti-inflammatory, antioxidant and anticancer properties, but has a hydrophobic character and low bioavailability, was used as a model drug. GO was chemically modified with sodium chloroacetate (ClCH2COONa). Then the carboxylated graphene oxide (GO-COOH) was left in agitation with Cur overnight. By means of UV-Vis spectroscopy, RAMAN spectroscopy, FTIR and electron microscopy (TEM and SEM), the functionalization of GO and its interaction with curcumin were confirmed, obtaining 85.35% of curcumin adsorption. Likewise, in vitro release assays in tumor microenvironment conditions were performed. And in order to determine the selective cytotoxic potential of the system, its cell viability was evaluated in healthy and cancerous cell lines.