This book is a collection of the major publications of the authors in the emerging area of chemotherapeutic engineering. It describes and demonstrates the concept, feasibility, safety and prospect of chemotherapeutic engineering through a full spectrum of proof-of-concept experiments from design, characterization, in vitro cellular uptake, cytotoxicity, to in vivo pharmacokinetics, biodistribution, and xenograft tumor model of the various nanocarriers, such as prodrugs, micelles, liposomes, and nanoparticles of biodegradable polymers.