Ajaz Nyla, Bukhsh Munnaza, Kamal Yousaf, Rehman Fauzia, Irfan Muhammad, Khalid Syed Haroon, Asghar Sajid, Rizg Waleed Y, Bukhary Sahar M, Hosny Khaled M, Alissa Mohammed, Safhi Awaji Y, Sabei Fahad Y, Khan Ikram Ullah
Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Government College University Faisalabad, Faisalabad, Pakistan.
Department of Pharmacy, The University of Faisalabad, Faisalabad, Pakistan.
Front Bioeng Biotechnol. 2023 May 9;11:1173883. doi: 10.3389/fbioe.2023.1173883. eCollection 2023.
Hydrogels are crosslinked three-dimensional networks, and their properties can be easily tuned to target the various segments of the gastrointestinal tract (GIT). Cetirizine HCl (CTZ HCl) is an antihistaminic drug, which when given orally can upset the stomach. Moreover, this molecule has shown maximum absorption in the intestine. To address these issues, we developed a pH-responsive semi-interpenetrating polymer network (semi-IPN) for the delivery of CTZ HCl to the lower part of the GIT. Initially, 10 different formulations of itaconic acid-grafted-poly (acrylamide)/aloe vera [IA-g-poly (AAm)/aloe vera] semi-IPN were developed by varying the concentration of IA and aloe vera using the free radical polymerization technique. Based on swelling and sol-gel analysis, formulation F5 containing 0.3%w/w aloe vera and 6%w/w IA was chosen as the optimum formulation. The solid-state characterization of the optimized formulation (F5) revealed a successful incorporation of CTZ HCl in semi-IPN without any drug-destabilizing interaction. The drug release from F5 showed limited release in acidic media followed by a controlled release in the intestinal environment for over 72 h. Furthermore, during the evaluation, formulation F5 did not affect the hematological parameters, kidney, and liver functions. Clinical observations did not reveal any signs of illness in rabbits treated with hydrogels. Histopathological images of vital organs of treated animals showed normal cellular architecture. Thus, the results suggest a non-toxic nature and overall potential of the developed formulation as a targeted drug carrier.
水凝胶是交联的三维网络结构，其性质可以很容易地进行调整，以针对胃肠道（GIT）的不同部位。盐酸西替利嗪（CTZ HCl）是一种抗组胺药物，口服时会引起胃部不适。此外，该分子在肠道中显示出最大吸收。为了解决这些问题，我们开发了一种pH响应性半互穿聚合物网络（半IPN），用于将CTZ HCl递送至GIT的下部。最初，使用自由基聚合技术，通过改变衣康酸（IA）和芦荟的浓度，制备了10种不同配方的衣康酸接枝聚（丙烯酰胺）/芦荟[IA-g-聚（AAm）/芦荟]半IPN。基于溶胀和溶胶-凝胶分析，选择含有0.3%w/w芦荟和6%w/w IA的F5配方作为最佳配方。优化配方（F5）的固态表征表明，CTZ HCl成功地掺入了半IPN中，没有任何药物稳定性相互作用。F5的药物释放在酸性介质中显示出有限释放，随后在肠道环境中持续释放超过72小时。此外，在评估过程中，F5配方对血液学参数、肾脏和肝脏功能没有影响。临床观察未发现用水凝胶治疗的兔子有任何疾病迹象。治疗动物重要器官的组织病理学图像显示细胞结构正常。因此，结果表明所开发的配方具有无毒性质和作为靶向药物载体的整体潜力。
