The importance of nanotechnology in human health care is unquestionable. There is a growing interest to apply nanotechnology in cancer therapy, as an example. In this report, we have fabricated gold nanoparticle (AuNP), the delivery vehicle of interest, with an anti-cancer drug (Velcade) and a targeting agent (folic acid) for potential therapeutic application in multiple myeloma. Physico-chemical characterization of the nanoconjugates were carried out by UV-Visble spectroscopy exploiting the surface plasmon resonance band of AuNP, transmission electron microscopy (TEM) and studying release of radio-labeled tritiated folic acid (3FA) in a scintillation counter. The evidence of the attachment of velcade to AuNP was confirmed by UV-Vis spectroscopy and studying the release of3FA from gold-velcade-FA conjugates (Au-Vel-FA). Furthermore, the stability of Au-Vel-FA tested in PBS (phosphate buffer saline) by monitoring the release of3FA suggested significant stability of the nanoconjugate. Functional activity of the nanoconjugate was tested by studying the apoptosis of different multiple myeloma cell lines by annexin/PI method. Apoptosis data suggested that Velcade retained its functional activity in Au-Vel-FA. In future, this strategy may be potentially utilized as an alternative approach for the treatment of multiple myeloma.