AbstractGraphene nanoribbons are thin sheets of graphene showing exclusive characteristics such as better drug‐loading capacity, adsorption on mammalian cells, greater surface area, and light‐absorbing ability. The current research work is to develop metformin‐adsorbed carboxyl‐functionalized oxidized graphene nanoribbons and utilize drug repurposing for the treatment of oral cancer by activating photo‐thermal radiation therapy. The nanoribbons are formulated by Hummer's method and evaluated for several characterization parameters like ATR‐ Fourier Transform Infrared (FTIR), Differential scanning calorimetry (DSC), topology, in vitro efficacy, ex vivo and in vitro cell line studies. The ATR‐FTIR spectrum of formulated nanoribbons shows distinctive peak at 3370 cm−1 (NH group) of metformin. The DSC specifies the incidence of steep endothermic crests at 235 °C (CNH3). The in vitro and ex vivo drug release studies show enhanced drug release in acidic pH (6.4) than physiological pH (7.4) with photothermal radiation. The in vitro cell line studies are processed via two‐way ANOVA that exhibits 67.74 ± 0.03% of % inhibition in presence of photothermal radiation. The study demonstrates higher inhibition of cancerous cells at lower concentration of drug and photothermal therapy in comparison to plain drug. The characteristic feature of graphene is used to develop targeted drug delivery system against the oral cancerous cells.