Drug Delivery and Cosmetic Lab (DDCL), Faculty of Pharmacy, Gomal University, Dera Ismail Khan, Pakistan.
Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia.
Drug Deliv. 2022 Dec;29(1):52-61. doi: 10.1080/10717544.2021.2015483.
Urticaria affects all age groups of a population. It is triggered by allergens in foods, insect bites, medications, and environmental conditions. Urticaria is characterized by itching, a burning sensation, wheals and flares, erythema, and localized edema. The aim of this study was to develop a polymeric dosage form of ebastine using Carbopol 940 and mixture of span and tween. The emulsion was prepared, the gelling agent was added and the desired emulgel loaded with active drug was formulated. The formulations were subjected to physical stability, pH, viscosity, spreadability, drug content analysis, thermal analysis, drug release, and anti-allergic activity in animal model. The formulated emulgel exhibited good physical stability. The pH of the formulation was in the range of 5.2 ± 0.17 to 5.5 ± 0.20 which is suitable for topical application. Insignificant changes ( > .05) were observed in viscosity and spreadability of stored emulgels. The drug content was in the official limit of Pharmacopeia (i.e. 100 ± 10%). DSC measurements predicted that there is no interaction between the active moiety and excipients in emulgel formulation. The optimized formulation (ES3) released 74.25 ± 1.8% of ebastine after 12 h. The ebastine emulgel showed significant ( < .05; ANOVA) anti-allergic activity as compared to commercial product Benadryl in histamine-induced allergy in rabbits. This study concluded that a topical drug delivery of ebastine-loaded emulgel could be well tolerated and safe for the treatment of urticaria/hives.
荨麻疹影响人群的所有年龄段。它是由食物、昆虫叮咬、药物和环境条件中的过敏原引起的。荨麻疹的特征是瘙痒、烧灼感、风团和潮红、红斑和局部水肿。本研究旨在开发一种使用 Carbopol 940 和 Span 和吐温混合物的埃巴斯汀聚合物剂型。制备乳液,加入凝胶剂,并将含有活性药物的所需乳凝胶制剂化。对制剂进行物理稳定性、pH 值、粘度、铺展性、药物含量分析、热分析、药物释放和动物模型中的抗过敏活性测试。所制备的乳凝胶表现出良好的物理稳定性。制剂的 pH 值在 5.2±0.17 至 5.5±0.20 范围内,适用于局部应用。储存的乳凝胶的粘度和铺展性没有明显变化(>.05)。药物含量在药典的规定范围内(即 100±10%)。DSC 测量预测活性成分和乳凝胶制剂中的赋形剂之间没有相互作用。优化的配方(ES3)在 12 小时后释放了 74.25±1.8%的埃巴斯汀。与组胺诱导的兔过敏症中的商业产品苯海拉明相比,埃巴斯汀乳凝胶显示出显著(<.05;ANOVA)的抗过敏活性。本研究得出结论,埃巴斯汀负载的乳凝胶的局部药物递送可以很好地耐受且安全,可用于治疗荨麻疹/风团。