In the last decade, nanobiotechnology research has emerged as a revolutionising new approach to the 21st century pharmaceutical challenges, offering valuable gains in a vast set of biomedical applications. In the field of bone tissue engineering, a broad range of nanotechnology-based delivery systems have been researched and the most recent developments in high-throughput technology and in silico approaches are creating very high expectations. This review presents a comprehensive overview of the emergent nanotechnology-based materials, processing techniques and research strategies for the delivery of pharmaceutics to bone including the materials general characteristics and the available drug delivery systems to distribute agents systemically or locally. Complementary to what was stated above, it also reviews the latest high-throughput processing techniques and the existent in silico tools (mathematical and computational models) used to help on the design of delivery systems.