Abstract
The discovery of sulfhydryl-modified polymers named thiomers in the late twentieth century resulted in a reframing conceptualization of polymers and their pharmaceutical use. As it is well known, the mucosal barrier in the body has a high influence in drug delivery, leading to loss of drug or low bioavailability. Chitosan is a wide known polymer commonly used in the pharmaceutical and medical field due to its great properties. However, thiolated chitosan, as first generation, presents improvement in its mucoadhesive, as well as other properties compared to the native chitosan. S-protected or second generation of chitosan overcomes stability and oxidation problems. However, recent development of a third generation, less-reactive, chitosan changes the recent drug delivery field completely.
Hence, second and third generation thiomers present enhanced mucoadhesive, efflux pump inhibitory and controlled drug release properties, without (or with a very small, almost non-notable) cell toxicity. In this article, the syntheses of thiolated, S-protected and less reactive chitosan are elucidated. Furthermore, its properties, more in detail, the cell viability and toxicity, permeation enhancement, efflux pump inhibition, mucoadhesive properties and controlled drug release, are stated. Finally, an overview of in vivo studies for buccal, nasal, ocular, oral and vaginal drug delivery is given within this work as a proof of the concept.
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Sanchez Armengol, E., Laffleur, F. (2021). Generations of Chitosan: The Progress in Drug Delivery. In: Jayakumar, R., Prabaharan, M. (eds) Chitosan for Biomaterials IV. Advances in Polymer Science, vol 288. Springer, Cham. https://doi.org/10.1007/12_2021_97
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