In the present study, we prepared magnetite nanoparticles (MNPs) loaded with natural () herb and Epilim (Ep) drug to evaluate the anti-cancerous activity against brain cancer cells. All the samples were prepared via co-precipitation approach modified with different concentrations of and Ep drug at room temperature. The MNPs loaded with drug and natural herb were studied in terms of crystal structure, morphology, colloidal stability, size distribution, and magnetic properties. Field emission scanning electron microscopy (FESEM) images exhibited the morphologies of samples with spherical shape as well as the particles size of 9 nm for MNPs and up to 23 nm for its composites. The results of vibrating sample magnetometer (VSM) indicated the magnetization saturation (Ms) of 42.510 emu/g for MNPs. This value reduced to 16-35 emu/g upon loading MNPs with different concentrations of and Ep. Fourier transform infrared spectroscopy (FTIR) indicated the chemical interaction between the Ep, and MNPs. Brunauer-Emmett-Teller (BET) analysis confirmed the largest surface area for MNPs (422.61 m/g) which gradually reduced on addition of and Ep indicating the successful loading. The zeta potential measurements indicated that the MNPs and MNPs loaded with and Ep are negatively charged and can be dispersed in the suspension. Furthermore, U87 human glioblastoma cell line was used for the cellular studies to determine the efficacy of synthesized MNPs against cancer cells. The results confirmed the anti-proliferative activity of the MNPs loaded with and Ep.