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巯基化纤维素:一种具有双重作用的黏附性和渗透增强聚合物。

Thiolated Cellulose: A Dual-Acting Mucoadhesive and Permeation-Enhancing Polymer.

机构信息

Center for Chemistry and Biomedicine, Department of Pharmaceutical Technology, Institute of Pharmacy, University of Innsbruck, Innrain 80-82, A-6020 Innsbruck, Austria.

Department of Polymer Materials, Faculty of Engineering, Hitit University, 19030 Corum, Turkey.

出版信息

Biomacromolecules. 2023 Nov 13;24(11):4880-4889. doi: 10.1021/acs.biomac.3c00577. Epub 2023 Oct 5.

Abstract

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 -acetylmercaptosuccinic anhydride. The chemical structure of the target compound was confirmed by FTIR and H NMR spectroscopy. The thiol content was determined by Ellman's test. The conjugate exhibited 215.5 ± 25 μmol/g of thiol groups and 84 ± 16 μmol/g of disulfide bonds. Because of thiolation, mucoadhesion on porcine intestinal mucosa was 9.6-fold enhanced. The apparent permeability () 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. 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.

摘要

本研究旨在设计一种阴离子型、巯基化的纤维素衍生物,并利用依诺肝素作为模型药物来评估其黏膜黏附性和渗透增强特性。通过纤维素与乙酰巯基丁二酸酐的反应合成了 2-巯基琥珀酸改性纤维素(纤维素巯基琥珀酸盐)。目标化合物的化学结构通过傅里叶变换红外光谱(FTIR)和核磁共振光谱(H NMR)得到确认。通过 Ellman 试验测定了巯基含量。该缀合物的巯基含量为 215.5 ± 25 μmol/g,二硫键含量为 84 ± 16 μmol/g。由于巯基化,其对猪肠黏膜的黏膜黏附性增强了 9.6 倍。在 Caco-2 细胞单层上,0.5%纤维素巯基琥珀酸盐使模型染料 Lucifer yellow 的表观渗透系数()提高了 2.2 倍。与仅在缓冲液中给药相比,在 0.5%纤维素巯基琥珀酸盐存在下,依诺肝素通过大鼠肠黏膜的渗透增加了 2.4 倍。在大鼠中的研究表明,使用纤维素巯基琥珀酸盐的口服生物利用度为 8.98%,是药物水溶液的 12.5 倍。本研究结果表明,用 2-巯基琥珀酸对纤维素进行修饰提供了黏膜黏附性和渗透增强特性,使这种巯基化聚合物成为口服药物递送的有吸引力的赋形剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a7b1/10646989/1f558449f623/bm3c00577_0001.jpg

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