This textbook explains the fundamental aspects of nanotechnology and fills the gap between bio-inspired nanotechnological systems and functionality of living organisms, introducing new insights to their physicochemical, biophysical and thermodynamic behaviour. Addressed to all those involved in recent advances in pharmaceutics, this book is divided in three major parts: Part A refers to the physicochemical and thermodynamics aspects of nanosystems, wherein their biophysical behaviour is correlated with that of the cells of living organisms; Part B refers to the application of nanotechnology in imaging, diagnostics and therapeutics; Part C is focused on issues regarding safety and nanotoxicity of nanosystems, and the regulatory framework that surrounds these. The text promotes the concept that biophysics, thermodynamics and nanotechnology are considered to be emerging tools that, when approached within regulatory boundaries, provide new and integrated knowledge for the production of new medicines. In 2018, Prof. Demetzos was honored with an award by the Order of Sciences of the Academy of Athens for his scientific contribution in Pharmaceutical Nanotechnology.