Liaqat Huma, Badshah Syed Faisal, Minhas Muhammad Usman, Barkat Kashif, Khan Saeed Ahmad, Hussain Muhammad Delwar, Kazi Mohsin
Faculty of Pharmacy, University of Lahore, Lahore 54590, Pakistan.
Department of Pharmacy, Faculty of Medical and Health Sciences, University of Poonch, Rawalakot, Azad Jammu and Kashmir 12350, Pakistan.
ACS Omega. 2024 Jun 21;9(26):28827-28840. doi: 10.1021/acsomega.4c03240. eCollection 2024 Jul 2.
Hydrogels with the main objective of releasing mesalamine (5-aminosalicylic acid) in the colon in a modified manner were formulated in the present work using a free-radical polymerization approach. Different ratios of hyaluronic acid were cross-linked with methacrylic and acrylic acids using methylenebis(acrylamide). The development of a new polymeric network and the successful loading of drug were revealed by Fourier transform infrared spectroscopy. Thermogravimetric analysis demonstrated that the hydrogel was more thermally stable than the pure polymer and drug. Scanning electron microscopy (SEM) revealed a rough and hard surface which was relatively suitable for efficient loading of drug and significant penetration of dissolution medium inside the polymeric system. Studies on swelling and drug release were conducted at 37 °C in acidic and basic conditions (pH 1.2, 4.5, 6.8, and 7.4, respectively). Significant swelling and drug release occurred at pH 7.4. Swelling, drug loading, drug release, and gel fraction of the hydrogels increased with increasing hyaluronic acid, methacrylic acid, and acrylic acid concentrations, while the sol fraction decreased. Results obtained from the toxicity study proved the formulated system to be safe for biological systems. The pH-sensitive hydrogels have the potential to be beneficial for colon targeting due to their pH sensitivity and biodegradability. Inflammatory bowel disease may respond better to hydrogel treatment as compared to conventional dosage forms. Specific amount of drug is released from hydrogels at specific intervals to maintain its therapeutic concentration at the required level.
在本研究中，采用自由基聚合方法制备了主要目的是以改良方式在结肠中释放美沙拉嗪（5-氨基水杨酸）的水凝胶。使用亚甲基双丙烯酰胺将不同比例的透明质酸与甲基丙烯酸和丙烯酸交联。通过傅里叶变换红外光谱揭示了新聚合物网络的形成以及药物的成功负载。热重分析表明，水凝胶比纯聚合物和药物具有更高的热稳定性。扫描电子显微镜（SEM）显示表面粗糙且坚硬，这相对有利于药物的有效负载以及溶解介质在聚合物体系内的显著渗透。在37°C下分别在酸性和碱性条件（pH 1.2、4.5、6.8和7.4）下进行了溶胀和药物释放研究。在pH 7.4时发生了显著的溶胀和药物释放。水凝胶的溶胀、药物负载、药物释放和凝胶分数随透明质酸、甲基丙烯酸和丙烯酸浓度的增加而增加，而溶胶分数则降低。毒性研究结果证明所制备的体系对生物系统是安全的。由于其pH敏感性和生物可降解性，pH敏感水凝胶具有结肠靶向的潜力。与传统剂型相比，炎症性肠病对水凝胶治疗可能反应更好。特定量的药物在特定间隔从水凝胶中释放，以将其治疗浓度维持在所需水平。
