Cancer treatment suffers with the failure of chemotherapeutic agents because of multi drug resistance. Investigation of new molecules involves huge expenditure and time. Present investigation aims at the dual loading of anticancer agent Imatinib Mesylate along with Piperine on to bovine serum albumin nanoparticles in order to overcome multi drug resistance and to achieve the maximum therapeutic effect. Desolvation method with the addition of acetone is used to prepare the nanoparticles. Drugs and polymer are subjected to differential scanning calorimetry. Nanoparticles are evaluated for encapsulation efficiency, particle size, zeta potential and drug release studies. In-vitro anticancer activity of the nanoparticles against Human Glioblastoma Multiforme (GBM) cell line T98G is determined. Results indicated compatibility in DSC, an encapsulation efficiency of 52.456%-88.254%, particle size of 208.3nm -497.3nm, zetapotential of -16.5mV to -63.2mV and drug release of 86.256% to 94.56% in 24H. In in-vitro anticancer activity % of cell death is 68.257% to 79.658%. Results suggest increased anticancer activity with the nanoparticles dual loaded with Imatinib mesylate and Piperine.