In recent years, the application of polymeric materials for a targeted drug-delivery system has been greatly advanced. Since polymeric materials played a crucial role in the targeted drug-delivery technology, the selection of such materials is very important in formulation and development. Polymeric materials used as components of the drug-delivery system should not be toxic and must have the desired essential properties required for such developments. Nowadays, research is much focused on the targeted drug-delivery system as it will deliver a medication to the patient with increase in the concentration in some parts of the body relative to others. Thus, such a drug-delivery system is largely founded on polymer-mediated drug delivery in order to combat the downfalls of conventional drug delivery. The selected polymeric material will bind with drugs and target specific parts of the body where there is solely diseased tissue, thereby avoiding interaction with healthy tissue. The aim of a targeted drug-delivery system is to prolong, localize, target, and have a protected drug interaction with the diseased tissue. However, for optimization in the formulation and development of a targeted drug-delivery system, selection of polymeric materials plays a significant role. Various types of polymeric materials were used for the same. Such polymeric materials will be classified as per site of targeting and properties of the polymeric materials. The present chapter intends to focus on various polymeric materials used for targeted delivery of bioactive agents and drugs.