Citation: Sajid Hussain, Omer M.A. Dagah, Essam A.M.S Obaid, Peng Jin, Ovas Ahmed Dar, Muhammd Irfan, Yiming Qi, Qinghua Wu, Ming Jin, Tengli Zhang, Lei Luo. Chitosan as oral absorption enhancer and inhibitor: A comprehensive review[J]. Chinese Chemical Letters, ;2026, 37(1): 111273. doi: 10.1016/j.cclet.2025.111273 shu

Chitosan as oral absorption enhancer and inhibitor: A comprehensive review

a.
College of Pharmaceutical Sciences, Southwest University, Chongqing 400715, China
b.
School of Life Sciences, Southwest University, Chongqing 400715, China

drluolei@swu.edu.cn

Received Date: 1 November 2024
Revised Date: 25 April 2025
Accepted Date: 28 April 2025
Available Online: 29 April 2025

Figures(6)

Chitosan (CS), a natural polymer derived from chitin found in the exoskeletons of crustaceans, has garnered significant interest in the pharmaceutical field due to its unique properties, including biocompatibility and biodegradability. In recent years, various studies have reported that CS can affect drug bioavailability, and interestingly, it works as an oral absorption enhancer and inhibitor. This review offers an in-depth analysis of the mechanisms underlying such a phenomenon and supports its application as a pharmaceutical excipient. CS enhances oral drug absorption through various mechanisms, such as interaction with the intestinal mucosa, tight junction modulation, inhibition of efflux transporters, enzyme inhibition, solubility and stability enhancement, and complexation. On the other side, CS exhibits the ability to inhibit the absorption of certain drugs by adsorbing to lipids and sterols, modulating bile acids and gut microbiota, altering drug-cell interaction at the polar interface, and mucus-mediated entrapment and interference. Future potential pharmaceutical research in this field includes elucidating the underneath absorption relevant mechanisms, rational use in formulations as excipient, exploring functional CS derivatives, and developing CS-based drug delivery systems. This comprehensive review highlights CS’s versatile and significant role in enhancing and inhibiting oral drug absorption, providing insights into the complexities of drug delivery and the potential of CS to improve therapeutic outcomes.
- Oral absorption,
- Excipients,
- Chitosan,
- Enhancer,
- Inhibitor
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