Nanotechnology is a cutting edge and rapidly evolving technology in medicine. The potential of nanomedicine in cancer therapy is infinitely promising due to the fact that novel developments are constantly being explored. This is particularly the case in the use of nanoparticles in both tumor diagnosis, as well as treatment. This article will attempt to describe some recent advances using nanoparticle drug delivery system in cancer therapy. The evolution history, the challenges and the role of nanoparticles in cancer drug delivery will briefly be discussed together with additional opportunities in cancer therapy. An overall understanding of these issues will help with further advancement of designing better drug delivery system that can be applied clinically.