This book presents the essential aspects of formulation design, drug targeting, barriers present in cell level and clinical trial requirements to approve a drug delivery system. It teaches the fundamentals, practical issues, and integration of pharmaceutics and molecular biology for developing drug delivery systems. An opening section reviews basics related to physiologic barriers, transporters, and biomaterials. Then, it moves on to discuss different strategies to target both synthetic small molecules and macromolecules, and further emphasizes advanced approaches to deliver the drug in different critical and life threatening diseases such as cardiovascular, cancer, sexual transmitted, and ophthalmic diseases. The book ends by evaluating drug delivery parameters in context to present current research as well as propel the reader to consider emerging research fields like stem cell research, cell-based therapeutics, tissue engineering, and imaging. In addition, each chapter contains objectives and assessment questions.