Chitin is the most important natural polysaccharide after cellulose, found in crustaceous shell or in cell walls of fungi. Chitosan, one of the natural multifunctional polymers, due to its unique and versatile biological properties is regarded as a useful compound in medical and pharmaceutical technology. In recent times chitosan has been far and wide used as a popular formulation excipient due to its inimitable characteristics in the field of pharmaceutical sciences as binding, disintegrating, stabilizing, suspending, tablet coating, and film forming material. Recently, considerable research effort has been made in order to develop safe and efficient chitosan products. Chitosan has been comprehensively investigated for its suitability for its controlled release characteristics in various studies. Oral delivery of genes and peptides by means of different formulations based on chitosan is also investigated in various examinations by the capability of its absorption and penetration enhancing properties. It is possessing tremendous mucoadhesive and inherent anti-microbial properties, so that it can be used as a carrier for novel drug delivery. In addition to the above mentioned reasons, tailoring the controlled release and to improve the therapeutic efficacy of the low molecular weight drug compounds can also be achieved by this polymer and moreover in combination with various polymers is feasible due its compatibility i.e. low chemical reactivity. This brief editorial epitomizes the potential applications of chitosan in novel drug delivery systems.