The application of nanotechnology to medicine, commonly referred to as 'nanomedicine', has the potential to transform our approach to human health and disease. Research at the nanoscale level affords the opportunity to address some of the most confounding human diseases at the molecular level, with the potential for significant improvements in disease prevention, diagnosis and treatment. Rapid advances and emerging technologies in nanoscale systems, particularly nanoparticles, are having a profound impact on cancer diagnosis, treatment and monitoring. The development of nanoparticulate systems that offer improved chemotherapeutic delivery through increased solubility and sustained retention times is an area of intense focus in nanomedicine. In addition, active targeting of nanoparticles through conjugation of tumor-specific cell surface markers such as tumor-specific antibodies or ligands can enhance the efficacy of nanoparticle drug delivery systems while significantly reducing toxicity. Perhaps some of the most exciting advances in nanomedicine are multifunctional nanoparticulate systems for simultaneous imaging of tumor mass and drug delivery. In a relatively short period of time, nanomedicine has already begun to have a strong presence in the global market. This review provides a comprehensive summary of recent progress in nanomedicine as it relates specifically to nanoparticles and anticancer drug delivery. Research into different nanoprobes for cancer detection/imaging will also be discussed. Lastly, the future of this growing and dynamic field and its potential impact will be discussed.