Thiolated Cellulose: A Dual-Acting Mucoadhesive and Permeation-Enhancing Polymer
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Tarih
2023
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
AMER CHEMICAL SOC
Erişim Hakkı
info:eu-repo/semantics/openAccess
Özet
This study aims to design an anionic, thiolated cellulose derivative and to evaluate its mucoadhesive and permeation-enhancing properties utilizing enoxaparin as a model drug. 2-Mercaptosuccinic acid-modified cellulose (cellulose–mercaptosuccinate) was synthesized by the reaction of cellulose with S-acetylmercaptosuccinic anhydride. The chemical structure of the target compound was confirmed by FTIR and 1H NMR spectroscopy. The thiol content was determined by Ellman’s test. The conjugate exhibited 215.5 ± 25 ?mol/g of thiol groups and 84 ± 16 ?mol/g of disulfide bonds. Because of thiolation, mucoadhesion on porcine intestinal mucosa was 9.6-fold enhanced. The apparent permeability (Papp) of the model dye Lucifer yellow was up to 2.2-fold improved by 0.5% cellulose–mercaptosuccinate on a Caco-2 cell monolayer. Enoxaparin permeation through rat intestinal mucosa increased 2.4-fold in the presence of 0.5% cellulose–mercaptosuccinate compared with the drug in buffer only. In vivo studies in rats showed an oral bioavailability of 8.98% using cellulose–mercaptosuccinate, which was 12.5-fold higher than that of the aqueous solution of the drug. Results of this study show that the modification of cellulose with 2-mercaptosuccinic acid provides mucoadhesive and permeation-enhancing properties, making this thiolated polymer an attractive excipient for oral drug delivery.
Açıklama
Anahtar Kelimeler
Cells, Cellulose, Dyes and pigments, Interface engineering, Thiols
Kaynak
BIOMACROMOLECULES
WoS Q Değeri
Q1
Scopus Q Değeri
Q1
Cilt
24
Sayı
11
Künye
Kali, G., O?zkahraman, B., Laffleur, F., Knoll, P., Wibel, R., Zo?ller, K., & Bernkop-Schnu?rch, A. (2023). Thiolated Cellulose: A Dual-Acting Mucoadhesive and Permeation-Enhancing Polymer. Biomacromolecules, 24(11), 4880-4889.
