This book covers various cancer chemotherapeutics, offering research-oriented overviews of phytochemical-based cancer treatments. It contrasts nano-formulated phytochemical delivery with conventional chemotherapy, introducing nanocarriers or bioengineering for poly-chemotherapy and phytochemicals as alternative treatments to reduce resistance. The text elaborates on the nano-formulation techniques and synthesis approaches of phytochemicals as drugs, the targeted drug delivery facilitated by nanocarriers, and subsequent mechanisms of drug release. Additionally, it examines the implications of nano-formulated phytochemicals in cancer therapeutics and their impact on cancer treatment and prevention. By enhancing bioavailability and improving functional qualities through nanoencapsulation, this innovative approach promises significant advancements in cancer therapy. Key concepts include dietary phytochemicals' role in various types of cancer chemotherapeutics, the pharmacological mechanisms of action in prevention and treatment, and strategies to enhance chemotherapy and radiotherapy efficacy. The book also presents preclinical and clinical studies on the efficacy of phytochemicals in cancer treatment. Additionally, it highlights improvements in drug delivery systems using nanotechnology-based dosage forms for herbal drugs. The content is designed for professionals involved in drug development, including chemists, pharmacists, biologists, biotechnologists, industrialists, nanotechnologists, microbiologists, economists, and all disciplines related to cancer treatment and phytochemical-based drug development. Academic students, scientists, and researchers at universities, institutes, hospitals, botanical institutes, pharmaceutical industries, government organizations, and NGOs will find invaluable insights into the application of phytochemical drugs in cancer treatment. By providing a detailed examination of cutting-edge research on nano-formulated phytochemicals for cancer therapy, this book invites readers to rethink traditional approaches to chemotherapy and explore innovative solutions that promise better outcomes for patients worldwide.