A budding interest in nanopharmaceuticals has generated a number of advancements throughout recent years with a focus on engineering novel applications. Nanotechnology also offers the ability to detect diseases at much earlier stages, such as finding hidden or overt metastatic colonies often seen in patients diagnosed with breast, lung, colon, prostate, and ovarian cancer. Diagnostic applications could build upon conventional procedures using nanoparticles, such as colloidal gold, iron oxide crystals, and quantum dots. Additionally, diseases may be managed by multifunctional agents encompassing both imaging and therapeutic capabilities, thus allowing simultaneous monitoring and treatment. A detailed evaluation of each formulation is essential to expand our current nanopharmaceutical repertoire. However, the safety and long-term effects of nanoformulations must not be overlooked. This review will provide a brief discussion of the major nanopharmaceutical formulations as well as the impact of nanotechnology into the future.