Considerable research exercises have been directed towards the development of efficient and safe drug delivery systems. Various materials are used in different pharmaceutical formulations for the development of efficient drug delivery systems in the treatment of disease. Biopolymers are a choice of research as an excipient delivery system due to their biodegradability, low toxicity, safe, stable, and renewable nature. Biopolymers are naturally occurring polymers or polymer matrix composites, that are extracted from animals, bacteria, fungi, and plants. Cellulose, starches are carbohydrate-based polymers, and wool, silk, gelatin, and collagen are protein-based biopolymers. Biopolymers are obtained from various sources but biopolymers, that belong to the carbohydrate origin, have been found very promising in drug delivery through various routes. The review mainly focuses on the biopolymers currently in use for buccal-mediated pharmaceutical drug delivery systems because the buccal route is an efficient drug delivery system that allows direct systemic circulation of drugs. It also prevents the hydrolysis of the drug molecule in the gastrointestinal tract and thus increases the bioavailability of the drug. The present review discusses the overview of other drug delivery routes, challenges with conventional drug delivery systems, pharmaceutical applications of some biopolymers used in buccal drug delivery systems, that are published recently, currently in use, or used over the past decade.