The applications of nanoparticulate drug delivery have gained significant attention in cancer diagnosis and treatment. Owing to their unique features and design, nanomedicines have made remarkable progress in eliminating dreadful tumors. Research in cancer nanomedicine spans multitudes of drug-delivery systems that include high tumor-targeting ability, sensitivity toward tumor microenvironments, and improved efficacy. Various nanocarriers have been developed and approved for anti-tumor drug targeting. These nanocarriers, such as liposomes, micelles, nanotubes, dendrimers, and peptides, offer several advantages including high selectivity, multifunctionality, specificity, biocompatibility, and precise control of drug release. This book provides complete information about each aspect of nanomaterials and nanotherapeutics, including synthesis, analysis, disease diagnosis, mechanistic insight, targeted drug delivery, and clinical implications in a concise and informative way. It presents simple and reader-friendly representations of the mechanisms of action of nanomaterials on cellular targets and highlights the challenges in targeted drug delivery with ongoing chemotherapeutic drugs.