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用于富马酸替诺福韦二吡呋酯控释给药的pH敏感壳聚糖-聚（丙烯酰胺-丙烯酸）水凝胶的研制

Development of pH-Sensitive Chitosan--poly(acrylamide--acrylic acid) Hydrogel for Controlled Drug Delivery of Tenofovir Disoproxil Fumarate.

作者信息

Safari Justin B, Bapolisi Alain M, Krause Rui W M

机构信息

Department of Chemistry, Faculty of Science, Rhodes University, Makhana 6140, South Africa.

Department of Pharmacy, Faculty of Pharmaceutical Sciences and Public Health, Official University of Bukavu, Bukavu 570, Democratic Republic of the Congo.

出版信息

Polymers (Basel). 2021 Oct 16;13(20):3571. doi: 10.3390/polym13203571.

DOI:10.3390/polym13203571
PMID:34685332
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8541207/
Abstract

The present study aimed to develop a pH-sensitive chitosan-based hydrogel for controlled delivery of an anti-hepatitis B drug, tenofovir disoproxil fumarate (TDF). Free radical polymerization was utilized to graft acrylamide and acrylic acid using ,-methylene bisacrylamide as the crosslinker. Physicochemical characterization confirmed the synthesis of thermally stable chitosan-g-poly(acrylamide-co-acrylic acid) hydrogels with well-defined pores within a fibrous surface. The prepared hydrogels exhibited pH and ionic strength sensitivity, with the swelling significantly lower under acidic and strong ionic strength conditions but higher in neutral and basic solutions. In addition, cytotoxicity studies on HeLa cell lines proved the cytocompatibility of the drug delivery material and its readiness for physiological applications. The encapsulation of TDF in the hydrogels was optimized and an encapsulation efficiency and a drug loading percentage of 96% and 10% were achieved, respectively. More interestingly, in vitro release studies demonstrated a pH-dependent release of TDF from hydrogels. The release at pH 7.4 was found to be up to five times higher than at pH 1.2 within 96 h. This further suggested that the newly developed hydrogel-loaded TDF could be proposed as a smart delivery system for oral delivery of anti-hepatitis B drugs.

摘要

本研究旨在开发一种基于壳聚糖的pH敏感水凝胶，用于抗乙肝药物替诺福韦酯富马酸盐（TDF）的控释。利用自由基聚合反应，以N,N'-亚甲基双丙烯酰胺为交联剂接枝丙烯酰胺和丙烯酸。物理化学表征证实合成了具有热稳定性的壳聚糖接枝聚（丙烯酰胺-共-丙烯酸）水凝胶，其纤维表面具有明确的孔隙。制备的水凝胶表现出pH和离子强度敏感性，在酸性和强离子强度条件下溶胀显著较低，而在中性和碱性溶液中较高。此外，对HeLa细胞系的细胞毒性研究证明了药物递送材料的细胞相容性及其在生理应用中的适用性。优化了TDF在水凝胶中的包封，包封效率和载药率分别达到96%和10%。更有趣的是，体外释放研究表明TDF从水凝胶中的释放具有pH依赖性。发现在96小时内，pH 7.4时的释放量比pH 1.2时高多达五倍。这进一步表明，新开发的载TDF水凝胶可作为抗乙肝药物口服递送的智能递送系统。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c120/8541207/86da8795ac10/polymers-13-03571-g012.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c120/8541207/e0c73731f1f1/polymers-13-03571-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c120/8541207/86da8795ac10/polymers-13-03571-g012.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c120/8541207/e0760a619742/polymers-13-03571-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c120/8541207/9df77dae3d69/polymers-13-03571-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c120/8541207/c68b0ab90cbd/polymers-13-03571-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c120/8541207/f3f3e71aa1e2/polymers-13-03571-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c120/8541207/a6223cb1448f/polymers-13-03571-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c120/8541207/e365adffe56c/polymers-13-03571-g006a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c120/8541207/d6482b76bc6d/polymers-13-03571-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c120/8541207/718053fdbaad/polymers-13-03571-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c120/8541207/25566f234e8d/polymers-13-03571-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c120/8541207/8899c1c812e2/polymers-13-03571-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c120/8541207/e0c73731f1f1/polymers-13-03571-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c120/8541207/86da8795ac10/polymers-13-03571-g012.jpg

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