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Nowadays, a novel thiolated chitosan and its S-protected derivative have attracted broad attention for their permeation enhancing and efflux pump inhibitory properties.Similar to chitosan, the permeation enhancing properties of thiolated chitosan is related to its effect on tight junctions, and the mechanism has been elucidated.However, the efflux pump inhibitory mechanism that is related to its effect on P-glycoprotein (P-gp) remains unclear.