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This chapter summarizes the types of nano drugs, their synthesis, formulation, characterization, and applications, with the most important administration routes. To achieve safer, more effective, and affordable therapies, various polymers have been used in the nanoparticle formulations, e.g., polymeric nanoparticles, as well as liposome vesicles, cyclodextrins, dendrimers, etc. The main purposes in nanoparticles design as a delivery system are to control particle size, surface features, and drug release to achieve the site-specific action of the drug at the therapeutically optimal rate and dose regimen. Different administration routes for nano drug delivery systems, e.g., oral, nasal, ophthalmic, parenteral, dermal, transdermal, pulmonary, and others, were reviewed in this chapter. They provide more localized and better drug use by increasing bioavailability, biodistribution, and minimizing undesirable side effects …