This paper discusses the present status of, and future perspectives on, drug targeting through the bloodstream by describing the drug targeting concept, its methodologies, types of drug carriers, and recent clinical examples. This explanation and discussion is made from the viewpoint of possible correlations with studies on artificial organs, implants, and biomaterials. Two targeting methodologies (active and passive targeting), two targeting strategies (the magic bullet and the enhanced permeability and retention effect), and five types of drug carriers are explained. In addition, the clinical status of the five carrier systems is discussed.