This course describes the emerging role of nanostructures in drug development activities. It covers the most current nanotechniques applied by the pharmaceutical industry to engineer shuttling mechanisms for delivering previously failed drug molecules. Throughout the course, students learn the basic principles of drug likeness, the rule of five for drug design, and the effect of these principles on excluding a wide range of chemical structures. The course focuses on methods of nanostructures' surface functionalization, immobilization, engineering of stealth nanovehicles for cellular delivery, as well as the use of quantum dots for nuclear and cytoplasmic visualization. Examples of FDA-approved nanodrugs in addition to nanoformulations at the pre-clinical and clinical stages are discussed.