Pharmaceutical companies are turning to miniaturisation and nanotechnology to enhance drug target discovery and drug development. In fact, nanomedicine – the application of nanotechnology to healthcare – is already influencing the pharmaceutical industry, especially in the design, formulation and delivery of ‘nanopharmaceuticals’. Nanopharmaceuticals are a relatively new class of ‘therapeutic-containing nanomaterials’ that often have unique ‘nanoproperties’ (physiochemical properties) due to their small size (compared with their bulk-phase counterparts), a high surface-to-volume ratio and the possibility of modulating their properties. They are, in essence, nanoparticles intended for a broad spectrum of clinical therapeutic applications. They have the potential to target a particular organ or tissue site, either passively or actively. Nanopharmaceuticals present novel reformulation opportunities for active agents (e.g. small-molecule drugs, proteins, nucleic acids, etc.) that were previously insoluble or could not be targeted to the specific site of the body where they were needed.