This chapter discusses the rationale of targeted nanomedicines, different approaches to achieve this goal, current challenges, and considerations for their future development. Here, nanomedicines refer to particulate materials with a diameter in nanometer scale, prepared with natural or synthetic polymers, lipids, or inorganic solids, in the form of polymer‐drug conjugates, liposomes, polymeric nanoparticles (NPs) or micelles, dendrimers, nanotubes, nanocrystals, nanorods, nanoshells, or nanocages. Nanomedicines used as a carrier of a drug are often called nanocarriers. Nanoparticles and nanocarriers are also interchangeably used. Throughout this chapter, the term “nanoparticles” will represent various types of nanocarriers.