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用于药物控释的智能及pH敏感型硫酸软骨素/聚苯乙烯磺酸钠水凝胶的体外评价

In Vitro Evaluation of Smart and pH-Sensitive Chondroitin Sulfate/Sodium Polystyrene Sulfonate Hydrogels for Controlled Drug Delivery.

作者信息

Suhail Muhammad, Chiu I-Hui, Hung Ming-Chia, Vu Quoc Lam, Lin I-Ling, Wu Pao-Chu

机构信息

School of Pharmacy, Kaohsiung Medical University, 100 Shih-Chuan 1st Road, Kaohsiung 80708, Taiwan.

Department of Clinical Pharmacy, Thai Nguyen University of Medicine and Pharmacy, 284 Luong Ngoc Quyen Str., Thai Nguyen City 24000, Vietnam.

出版信息

Gels. 2022 Jun 25;8(7):406. doi: 10.3390/gels8070406.

DOI:10.3390/gels8070406
PMID:35877491
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9323728/
Abstract

Ibuprofen is an antipyretic and analgesic drug used for the management of different inflammatory diseases, such as rheumatoid arthritis and osteoarthritis. Due to a short half-life and rapid elimination, multiple doses of ibuprofen are required in a day to maintain pharmacological action for a long duration of time. Due to multiple intakes of ibuprofen, certain severe adverse effects, such as gastric irritation, bleeding, ulcers, and abdominal pain are produced. Therefore, a system is needed which not only prolongs the release of ibuprofen but also overcomes the drug's adverse effects. Hence, the authors have synthesized chondroitin sulfate/sodium polystyrene sulfonate-co-poly(acrylic acid) hydrogels by the free radical polymerization technique for the controlled release of ibuprofen. Sol-gel, porosity, swelling, and drug release studies were performed on the fabricated hydrogel. The pH-responsive behavior of the fabricated hydrogel was determined by both swelling and drug release studies in three different pH values, i.e., pH 1.2, 4.6, and 7.4. Maximum swelling and drug release were observed at pH 7.4, as compared to pH 4.6 and 1.2. Similarly, the structural arrangement and crosslinking of the hydrogel contents were confirmed by Fourier transform infrared spectroscopy (FTIR). Scanning electron microscopy (SEM) evaluated the hard and irregular surface with a few macrospores of the developed hydrogel, which may be correlated with the strong crosslinking of polymers with monomer content. Similarly, thermogravimetric analysis (TGA) and differential scanning calorimetry (DSC) demonstrated the high thermal stability of the formulated hydrogel, as compared to pure polymers. A decrease in the crystallinity of chondroitin sulfate and sodium polystyrene sulfonate after crosslinking was revealed by powder X-ray diffraction (PXRD). Thus, considering the results, we can demonstrate that a developed polymeric network of hydrogel could be used as a safe, stable, and efficient carrier for the controlled release of ibuprofen.

摘要

布洛芬是一种用于治疗不同炎症性疾病(如类风湿性关节炎和骨关节炎)的解热镇痛药。由于半衰期短且消除迅速,一天内需多次服用布洛芬以长时间维持药理作用。由于多次摄入布洛芬,会产生某些严重的不良反应,如胃刺激、出血、溃疡和腹痛。因此,需要一种既能延长布洛芬的释放时间又能克服药物不良反应的系统。因此,作者通过自由基聚合技术合成了硫酸软骨素/聚苯乙烯磺酸钠-共-聚丙烯酸水凝胶,用于布洛芬的控释。对制备的水凝胶进行了溶胶-凝胶、孔隙率、溶胀和药物释放研究。通过在三种不同pH值(即pH 1.2、4.6和7.4)下的溶胀和药物释放研究,确定了制备的水凝胶的pH响应行为。与pH 4.6和1.2相比,在pH 7.4时观察到最大溶胀和药物释放。同样,通过傅里叶变换红外光谱(FTIR)证实了水凝胶成分的结构排列和交联。扫描电子显微镜(SEM)评估了所制备水凝胶坚硬且不规则的表面以及一些大孔,这可能与聚合物与单体含量的强交联有关。同样,热重分析(TGA)和差示扫描量热法(DSC)表明,与纯聚合物相比,所制备的水凝胶具有较高的热稳定性。粉末X射线衍射(PXRD)显示交联后硫酸软骨素和聚苯乙烯磺酸钠的结晶度降低。因此,考虑到结果,我们可以证明所开发的水凝胶聚合物网络可作为一种安全、稳定且高效的载体用于布洛芬的控释。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/71e3/9323728/6d4341f57f5e/gels-08-00406-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/71e3/9323728/1236fe488478/gels-08-00406-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/71e3/9323728/315eadf768ab/gels-08-00406-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/71e3/9323728/548c287505c0/gels-08-00406-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/71e3/9323728/8fc11260f02e/gels-08-00406-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/71e3/9323728/7210f011cd8f/gels-08-00406-g005a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/71e3/9323728/c273dfd35fb9/gels-08-00406-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/71e3/9323728/67771d7a3e10/gels-08-00406-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/71e3/9323728/6d4341f57f5e/gels-08-00406-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/71e3/9323728/1236fe488478/gels-08-00406-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/71e3/9323728/315eadf768ab/gels-08-00406-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/71e3/9323728/548c287505c0/gels-08-00406-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/71e3/9323728/8fc11260f02e/gels-08-00406-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/71e3/9323728/7210f011cd8f/gels-08-00406-g005a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/71e3/9323728/c273dfd35fb9/gels-08-00406-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/71e3/9323728/67771d7a3e10/gels-08-00406-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/71e3/9323728/6d4341f57f5e/gels-08-00406-g008.jpg

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