Suhail Muhammad, Hsieh Yi-Han, Shao Yu-Fang, Minhas Muhammad Usman, Wu Pao-Chu
School of Pharmacy, Kaohsiung Medical University, Kaohsiung City 80708, Taiwan.
Department of Biomedical Science and Environmental Biology, Kaohsiung Medical University, Kaohsiung City 80708, Taiwan.
Gels. 2021 Oct 13;7(4):167. doi: 10.3390/gels7040167.
Ketorolac tromethamine is a non-steroidal anti-inflammatory drug used in the management of severe pain. The half-life of Ketorolac tromethamine is within the range of 2.5-4 h. Hence, repeated doses of Ketorolac tromethamine are needed in a day to maintain the therapeutic level. However, taking several doses of Ketorolac tromethamine in a day generates certain complications, such as acute renal failure and gastrointestinal ulceration. Therefore, a polymeric-controlled drug delivery system is needed that could prolong the release of Ketorolac tromethamine. Therefore, in the current study, pH-responsive carbopol 934/sodium polystyrene sulfonate-co-poly(acrylic acid) (CP/SpScPAA) hydrogels were developed by the free radical polymerization technique for the controlled release of Ketorolac tromethamine. Monomer acrylic acid was crosslinked with the polymers carbopol 934 and sodium polystyrene sulfonate by the cross-linker ','-methylene bisacrylamide. Various studies were conducted to evaluate and assess the various parameters of the fabricated hydrogels. The compatibility of the constituents used in the preparation of hydrogels was confirmed by FTIR analysis, whereas the thermal stability of the unreacted polymers and developed hydrogels was analyzed by TGA and DSC, respectively. A smooth and porous surface was indicated by SEM. The crystallinity of carbopol 934, sodium polystyrene sulfonate, and the prepared hydrogels was evaluated by PXRD, which revealed a reduction in the crystallinity of reactants for the developed hydrogels. The pH sensitivity of the polymeric hydrogel networks was confirmed by dynamic swelling and in vitro release studies with two different pH media i.e., pH 1.2 and 7.4, respectively. Maximum swelling was exhibited at pH 7.4 compared to pH 1.2 and, likewise, a greater percent drug release was perceived at pH 7.4. Conclusively, we can demonstrate that the developed pH-sensitive hydrogel network could be employed as a suitable carrier for the controlled delivery of Ketorolac tromethamine.
酮咯酸氨丁三醇是一种用于管理严重疼痛的非甾体抗炎药。酮咯酸氨丁三醇的半衰期在2.5 - 4小时范围内。因此,一天内需要重复给药酮咯酸氨丁三醇以维持治疗水平。然而,一天内服用几次酮咯酸氨丁三醇会产生某些并发症,如急性肾衰竭和胃肠道溃疡。因此,需要一种聚合物控释给药系统来延长酮咯酸氨丁三醇的释放。因此,在当前研究中,通过自由基聚合技术开发了pH响应性卡波姆934/聚苯乙烯磺酸钠 - 共聚(丙烯酸)(CP/SpScPAA)水凝胶,用于酮咯酸氨丁三醇的控释。单体丙烯酸通过交联剂N, N'-亚甲基双丙烯酰胺与聚合物卡波姆934和聚苯乙烯磺酸钠交联。进行了各种研究以评估和评价所制备水凝胶的各种参数。通过FTIR分析确认了制备水凝胶所用成分的相容性,而未反应聚合物和所开发水凝胶的热稳定性分别通过TGA和DSC进行分析。SEM表明表面光滑且多孔。通过PXRD评估了卡波姆934、聚苯乙烯磺酸钠和所制备水凝胶的结晶度,结果显示所开发水凝胶的反应物结晶度降低。通过在两种不同pH介质即pH 1.2和7.4下的动态溶胀和体外释放研究,证实了聚合物水凝胶网络的pH敏感性。与pH 1.2相比,在pH 7.4时表现出最大溶胀,同样,在pH 7.4时药物释放百分比更高。总之,我们可以证明所开发的pH敏感水凝胶网络可作为酮咯酸氨丁三醇控释的合适载体。