In an era wherein nanotechnology has sparked a huge research interest, brain drug delivery is not an exception. Aiming at fighting several central nervous system (CNS) conditions, tailored nanoparticles open new avenues to address several challenges in the fields of drug delivery and brain targeting. This book gathers contributions from experts in different, complementary fields, having in common their interest in developing new strategies for brain delivery based on nanotechnologies. The book encompasses general aspects pertaining to fundamental development, including tripartite in silico–in vitro–in vivo approaches. It also covers a diversity of nanomedicines applied in treatment and/or diagnosis and monitoring of CNS disorders. Aspects concerning their translation from the bench to clinical practice are also seamlessly discussed. This book will inspire readers to discover possible approaches to holistically delivering drugs into the brain. Edited by Carla Vitorino, Andreia Jorge and Alberto Pais, this book will appeal to anyone involved in nanomedicine, pharmaceutics, neurological and cancer therapies, drug delivery research and computational and regulatory sciences.