AbstractTransdermal drug delivery systems have received a lot of attention due to their noninvasive nature and possible advantages over standard drug administration methods. Because transdermal administration systems skip the gastrointestinal tract and hence avoid hepatic first pass metabolism, also the chance of adverse effects such as liver malfunction and gastrointestinal tract discomfort is low. This comprehensive review explores the various aspects of polymeric advancements in transdermal drug delivery, encompassing their roles as matrix and microreservoir formers, microneedles, pressure sensitive adhesives, rate controlling membranes, and many other components. The article emphasizes the importance of biocompatibility, chemical compatibility, and stability of polymers within the transdermal delivery system. Furthermore, it delves into the recent advancements in synthetic and natural polymer‐based transdermal drug delivery systems. Thus, a comprehensive search strategy is conducted in electronic databases such as PubMed, Scopus, and Web of Science to write this review paper. The scope of this investigation involves an in‐depth study of the various polymeric materials used, their formulations, and the mechanisms that support their efficacy in delivering medications over the skin barrier. Additionally, it explores the challenges associated with stability and safety concerns, while highlighting novel approaches to overcome these problems. Furthermore, the review discusses the biocompatibility of polymeric materials, crucial for ensuring minimal adverse effects and maximum therapeutic efficacy.