The conventional chemotherapeutic agents used in the treatment of human malignancies are directed nonspecifically against both malignant and nonmalignant cells, often limiting their efficacy with having serious side effects. Recent development of drug delivery vehicles has opened up the possibility of targeted drug delivery systems with the potential of achieving maximum efficacy with minimal toxicity. The possibility of using a nanomaterial as a combinational drug component is intuitively evident as it would compensate the toxicity level by enhancing drug delivery efficiency. Additionally, cell-specific cytotoxicity (reported earlier by our group) of the nanovehicle itself may potentiate a more effective targeted cell killing. In this paper, we explore the possibility of using gold nanoparticles playing the dual role of an anticancer agent and a carrier of a chemotherapeutic drug. This is demonstrated using vincristine sulfate (VS), salt of an alkaloid often used in the treatment of multiple myeloma (MM), and U266 as a test MM cell line. The drug VS shows the expected G2-M-phase arrest of cells. Notably, bare gold nanoparticle shows arrest of the S phase cells that may be particularly important in case of slow-growing malignancies like MM where most of the cells remain in G1 phase of the cell cycle. The VS conjugated gold retains the activity of both gold nanoparticle and VS leading to a synergistic rise of the apoptotic cell population.