Nanotechnology has the potential to impact the treatment of cancer significantly. This review will explore how this potential is beginning to be realized through the design of polymeric nanoparticle delivery systems. Current research is focused on developing biocompatible nanoparticles capable of targeting specific cancer markers and delivering imaging and therapeutic agents for the detection and treatment of cancer, resulting in a number of preclinical and clinical applications. More sophisticated nanoparticle designs are now in development, including particles able to release multiple drugs for enhanced treatment efficacy and targeted, multifunctional particles capable of combining imaging and drug release.