Herein, the magnetic graphene oxide/β-cyclodextrin–chitosan (MGO/β-CD-CS) nanocomposite was prepared via a two-step reaction and characterized by 1H NMR, FT-IR, BET, VSM, TGA, EDX-MAP, CHN, SEM, TEM, and XRD analyses. To graft the CS on β-CD, epichlorohydrin (ECH) was used as the crosslinking agent to prepare β-CD-CS. Then β-CD-CS was covalently attached to MGO through an amidation reaction. By using isotherm models, thermodynamic analyses, and kinetic modeling, this work aimed to encapsulate Omeprazole as a drug model and study its plausible in-vitro release mechanism. Also, a cytotoxicity assessment has been performed on MGO/β-CD-CS nanocomposite against HK2 cell lines. Our next research project will be focused on imaging drug-loaded nanocarriers in-vivo.