Abstract An effective dose at specific sites is of paramount importance for disease therapy. While therapeutic reagents such as small molecule drugs, nucleic acids, peptides, and proteins are suffered from degradation or clearance by physiological environment, nanomedicine has emerged to improve drug delivery efficiency due to their superior targeting ability. By tailoring the properties of nanoparticle, including size, shape, surface chemistry, site‐specific drug delivery in organ, cellular, and subcellular level could be achieved. This minireview highlights recent advances in the development of targeted drug delivery system for disease therapy.
