This review summarises the recent efforts to engineer macromolecular prodrugs (MPDs) based on polysaccharidal materials. Polysaccharidal materials are of utmost importance to design and develop MPDs of non-steroidal anti-inflammatory drugs, antibiotics, anti-viral and anti-cancer drugs, etc. Covalent drug loading capabilities of the polysaccharidal materials are thoroughly discussed. In order to successfully transform drugs into prodrugs using polysaccharidal materials, present review details different syntheses strategies which are being applied to design pharmaceutically viable MPDs. Herein, we also reported the collection of polysaccharidal materials which are being widely spun in to MPDs of several classes of drugs and their applications. Merits and demerits of polysaccharide biomaterials for MPDs are critically discussed. Cellulose ether derivatives are newly introduced materials attracting the vigil eye of researchers working in MPD design for potential therapeutic applications. Special emphasis will be given to amphiphilic materials, i.e. MPDs, which self-assemble at solvent interfaces into nanorods, nanoparticles (NPs), nanowires, etc. Furthermore, the stability of MPDs at elevated conditions of temperature is discussed to gain information about their storage properties. We highlighted thrust areas in polysaccharidal materials-based research and development of MPDs.