Given the inherent nanoscale functional components of living cells, it was inevitable that nanotechnology would be applied in biotechnology giving rise to the term “nanobiotechnology,” which will be used in this chapter and indicates biotechnology as the main field. A less recognized and less frequently used term, almost synonymously, is “bionanotechnology,” which implies application in life sciences of nanotechnology as the main discipline. An up-to-date description of nanobiotechnologies and their applications in healthcare are given in a special report on this topic (1). The topic of this book is the nanoparticulate drug-delivery systems. This chapter will provide an integrated overview of application of nanobiotechnology-based molecular diagnostics, drug discovery, and drug delivery in the development of nanomedicine with the relationships as shown in Figure 1. Integration of nanobiotechnologies for the development of nanomedicine. https://s3-euw1-ap-pe-df-pch-content-public-u.s3.eu-west-1.amazonaws.com/9780429164613/85182e9d-7a80-46a9-bda0-17b3951ba029/content/fig12_1.tif"/>