Conventional anticancer drugs display significant shortcomings which limit their use in cancer therapy. For this reason, important progress has been achieved in the field of nanotechnology to solve these problems and offer a promising and effective alternative for cancer treatment. Nanoparticle drug delivery systems exploit the abnormal characteristics of tumour tissues to selectively target their payloads to cancer cells, either by passive, active or triggered targeting. Additionally, nanoparticles can be easily tuned to improve their properties, thereby increasing the therapeutic index of the drug. Liposomes, polymeric nanoparticles, polymeric micelles and polymer- or lipid-drug conjugate nanoparticles incorporating cytotoxic therapeutics have been developed; some of them are already on the market and others are under clinical and preclinical research. However, there is still much research to be done to be able to defeat the limitations of traditional anticancer therapy. This review focuses on the potential of nanoparticle delivery systems in cancer treatment and the current advances achieved.