Dendritic polymers have gained significant attention in the last two decades due to their size, shape, and multifunctionality. They have emerged as potential scaffolds for drug delivery applications. This chapter deals with the many recently developed applications of dendritic polymers in targeted drug delivery. The general properties of the dendritic polymers as drug delivery systems are discussed with special focus on active or passive delivery of conjugated or encapsulated drugs in targeting tumors, brain, skin, and inflammation. Some in vivo studies are discussed where dendrimer–drug conjugates were not only found to be active against aggressive tumor models but also showed better antitumor efficacy over the free drug. We also describe targeted gene delivery for the treatment of different disorders and diseases. Cellular penetration properties of the dendritic polymers without any targeting ligands, specifically in the inflammatory tissues, are highlighted as well. The extreme versatility of dendritic polymers with extensive research efforts is underway, leading to the development of targeted drug delivery systems for wide clinical use.