Inulin, as a unique and flexible structure, has been one of the most popular biodegradable polymers for the development of drug delivery systems due to its stabilization and protective effects and organ-targeting ability, including improved bioavailability, better cellular uptake, and sustained and controlled release of drugs and biomolecules. Inulin belongs to the fructan group of polysaccharides and has recently gained attention as a potential coating material, especially in studies of colon-targeted nanosized drug delivery systems, because of its rapid water solubility, low friability, and stability against gastric and intestinal enzymes. This chapter presents a comprehensive overview of the fundamentals and application of inulin as a coating agent for the delivery of therapeutic agents. Furthermore, chemical behavior, challenges, and future perspectives related to the use of inulin coatings for drug delivery purposes are discussed here.