In this study, a novel magnetic nanoadsorbent was synthesized by grafting β-cyclodextrin onto the modified surface of Fe O nanoparticles for the sorption and extraction of sertraline hydrochloride from human biological fluids. The extracted sertraline hydrochloride was measured by high-performance liquid chromatography. The grafted nanosorbent was confirmed by Fourier transform infrared spectroscopy, transmission electron microscopy, thermogravimetric analysis, and elemental analysis. The kinetic sorption of sertraline hydrochloride by magnetic nanosorbent was 1 h. The best temperature for sorption of sertraline hydrochloride was at 25°C at an optimum pH of 5. The adsorbed sertraline hydrochloride can be desorbed by using methanol solution containing acetic acid (5%) and trifluoroacetic acid (1%).