Extracellular vesicles (EVs) are cell-derived membrane vesicles composed of a lipid bilayer. EVs contain biological molecules, such as nucleic acids, lipids, and proteins. As these molecules are transferred to cells that receive EVs, EVs function as intercellular communication tools. EV-mediated intercellular communication is involved in various diseases, such as cancer and neurodegenerative diseases, and biological events, such as immune reactions and inflammation. Therefore, EVs are suggested to be useful as therapeutic targets for various diseases. However, an EV-based drug delivery system (DDS) that utilizes its therapeutic properties has not yet been reported. The biological activities of EVs are derived from their endogenous components; hence, they can be directly applied as drugs. In this review, the basic aspects of EVs, such as their types, methods of isolation, and in vivo behavior, are briefly summarized. Moreover, the potential of using therapeutics targeting EVs has been discussed in cancer and neurodegenerative diseases. Various therapeutics using EVs, including DDSs, are listed and their associated advantages and challenges are discussed.