This study investigated the performance of chitosan-graphene oxide nanocomposite for the controlled release of the Sumatriptan Succinate (SS) drug. Various analytical methods (i.e., SEM, TEM, AFM, TGA, XRD, and FT-IR) were used to characterize the crystalline structure, molecular structure, and morphology of the fabricated nanocomposites. The effective parameters, including pH, adsorbent amount, temperature, and contact time, on the adsorption of SS on nanocomposite, were optimized. The adsorption mechanism was determined as Langmuir isotherm (R2 = 0.9976), representing the monolayer adsorption with the highest adsorption capacity of 45.4 mg/g. The addition of GO resulted in a noticeable increase (100%–200%) in the swelling degree and a decrease in drug release rates (20%- 45%) of the fabricated nanocomposites compared with the chitosan hydrogel. As the percentage of GO in hydrogel beads increases, drug release occurs less rapidly and in a controlled manner. Eventually, antibacterial activity and cytotoxicity of the prepared nanocomposite beads were evaluated, which confirmed their antibacterial properties and biocompatibility.