The application of nanotechnology in life sciences, nanobiotechnology, is already having an impact on diagnostics and drug delivery. Now, researchers are starting to use nanotechnology in the field of drug discovery. This review explains how several technologies, including nanoparticles and nanodevices such as nanobiosensors and nanobiochips, are used to improve drug discovery and development. Nanoscale assays can contribute significantly to cost-saving in screening campaigns. In addition, some nanosubstances (such as fullerenes) could be potential drugs for the future. Although there might be some safety concerns with respect to the in vivo use of nanoparticles, studies are in place to determine the nature and extent of adverse events. Future prospects for the application of nanotechnology in healthcare and for the development of personalized medicine appear to be excellent.