The mechanisms and applications of chitosan and its derivatives in transdermal drug delivery to promote drug permeation were reviewed in this paper. Specifically, we summarized the permeation-promoting mechanisms of chitosan and several of its derivatives, including changing the structure of stratum corneum proteins, acting on the tight junction of granular layers, affecting intercellular lipids, and increasing the water content of stratum corneum. These mechanisms are the reason why chitosan and its derivatives can increase the transdermal permeation of drugs. In addition, various transdermal preparations containing chitosan and its derivatives were summarized, and their respective advantages were expounded, including nanoparticles, emulsions, transdermal microneedles, nanocapsules, transdermal patches, transdermal membranes, hydrogels, liposomes, and nano-stents. The purpose of this review is to provide a theoretical basis for the further and wider application of chitosan in transdermal drug delivery systems. In the future, research results of chitosan and its derivatives in transdermal drug delivery need more support from in vivo experiments, as well as good correlation between in vitro and in vivo experiments. In conclusion, the excellent permeability-promoting property, good biocompatibility, and biodegradability of chitosan and its derivatives make them ideal materials for local transdermal drug delivery.
Keywords: application; chitosan and its derivatives; mechanism; permeation promotion; transdermal administration.