Book excerpt: This book discusses the recent progress and advances in nanochemoprevention. Chemoprevention utilizes natural dietary compounds and has regained interest due to larger safety window and proven efficacy of such molecules in cancer treatments. Nanotechnology has revolutionized drug delivery through passive as well as active targeting. This book provides a comprehensive overview of phytochemical bioactives that are used in chemoprevention. It gives a comprehensive overview of the variety of natural molecules and types of nanoparticles as well as mechanistic aspects of their superior efficacy over plain drug molecules. The book concludes with summarizing the progress of pre-clinical results of developed formulations for cancer treatment using nano-chemoprevention.