The applications of nanoparticulate drug delivery have received significant attention in the field of cancer diagnosis and treatment. Owing to their unique features and design, nanomedicines have made remarkable progress in eliminating dreadful tumors. Research in cancer nanomedicine has spanned multitudes of drug-delivery systems that possess 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 a wide range of 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, targetted drug delivery, and clinical implications in a concise and informative way. It presents simple and reader-friendly representations of nanomaterials' cellular targets to assist readers in understanding the mechanisms of action and highlights the challenges in targeted drug delivery with ongoing antibiotics and chemotherapeutic drugs.