Altuntaş Ebru, Yener Gülgün, Doğan Remzi, Aksoy Fadlullah, Şerif Aydın Mehmet, Karataş Ersin
1 Department of Pharmaceutical Technology, Faculty of Pharmacy, Istanbul University, Fatih, Istanbul, Turkey.
2 Department of Otorhinolaryngology, Bezmialem Vakif University, Fatih, Istanbul, Turkey.
Am J Rhinol Allergy. 2018 May;32(3):132-138. doi: 10.1177/1945892418764951. Epub 2018 Apr 12.
Background Mometasone furoate, one of the second generation intranasal corticosteroids, is currently used in suspension form due to its poor solubility. However, this is not favorable for nasal application because of the rapid elimination of the instilled drug from the nasal cavity by mucociliary clearance and delayed onset of action due to the slow dissolution of drug in suspension. Objective The aim of this study was to determine the antiallergic effects of mucoadhesive thermosensitive in situ gel containing mometasone furoate that we developed previously to prolong the contact between the drug and nasal mucosa and to prevent drainage of the formulation in an ovalbumin-induced rat model of allergic rhinitis. Methods An experimental allergic rhinitis model was developed in female Wistar albino rats by intraperitoneal injection of ovalbumin every 2 days for 14 days followed by its repeated intranasal instillation for 7 consecutive days. Intranasal instillation of ovalbumin was continued every other day for 14 days. Mometasone furoate in situ gel (5 μg/10 µl), mometasone furoate suspension (5 μg/10 µl), and physiological saline (10 µl) were administered into the bilateral nasal cavities from day 22 to day 35. Antiallergic effects were evaluated through histopathological evaluation, analysis of ovalbumin-specific serum immunoglobulin E, and a symptom score. Results Mometasone furoate in situ gel significantly decreased the nasal symptoms and ovalbumin-specific serum immunoglobulin E level as compared with mometasone furoate suspension and physiological saline. Additionally, inflammatory histological symptoms such as mucosal edema, vascular dilatation, eosinophil infiltration, and loss of cilia within the nasal mucosa of allergic rhinitis model rats were remarkably improved with the treatment of mometasone furoate in situ gel. Conclusion These results suggest that mometasone furoate in situ gel has a better therapeutic potential for the treatment of allergic rhinitis compared to mometasone furoate suspension.
背景 糠酸莫米松是第二代鼻用皮质类固醇药物之一，由于其溶解度差，目前以混悬液形式使用。然而，这对于鼻腔给药并不有利，因为滴鼻药物会通过黏液纤毛清除作用迅速从鼻腔清除，且由于药物在混悬液中溶解缓慢，起效延迟。目的 本研究旨在确定我们之前研发的含糠酸莫米松的黏膜黏附热敏原位凝胶的抗过敏作用，该凝胶可延长药物与鼻黏膜的接触时间，并防止制剂在卵清蛋白诱导的大鼠变应性鼻炎模型中排出。方法 通过每2天腹腔注射卵清蛋白，连续注射14天，随后连续7天反复滴鼻，建立雌性Wistar白化大鼠实验性变应性鼻炎模型。每隔一天继续滴鼻卵清蛋白，持续14天。从第22天至第35天，将糠酸莫米松原位凝胶（5μg/10μl）、糠酸莫米松混悬液（5μg/10μl）和生理盐水（10μl）分别滴入双侧鼻腔。通过组织病理学评估、卵清蛋白特异性血清免疫球蛋白E分析和症状评分来评估抗过敏作用。结果 与糠酸莫米松混悬液和生理盐水相比，糠酸莫米松原位凝胶显著减轻了鼻部症状，降低了卵清蛋白特异性血清免疫球蛋白E水平。此外，糠酸莫米松原位凝胶治疗可显著改善变应性鼻炎模型大鼠鼻黏膜的炎症组织学症状，如黏膜水肿、血管扩张、嗜酸性粒细胞浸润和纤毛缺失。结论 这些结果表明，与糠酸莫米松混悬液相比，糠酸莫米松原位凝胶在治疗变应性鼻炎方面具有更好的治疗潜力。
