Yenigun Vildan Betul, Yenigun Alper, Sagiroglu Ali Asram, Kocyigit Abdurrahim, Ozturan Orhan
Department of Medical Biochemistry, Faculty of Medicine, Bezmialem Vakif University, Istanbul, Turkey.
Vocational School of Health Sciences, Bezmialem Vakif University, Istanbul, Turkey.
Sci Prog. 2024 Oct-Dec;107(4):368504241304200. doi: 10.1177/00368504241304200.
Intranasal analgesic sprays represent a safe, efficacious method for pain relief, with a shorter working time compared to oral painkillers. This study aimed to develop nasal sprays using commonly available over-the-counter analgesics, providing an alternative treatment option that is more convenient and potentially more effective in managing pain, particularly in pediatric patients.
Three different nasal spray formulations with the contents of diclofenac sodium, ibuprofen, and paracetamol were created, and characterization studies were completed. The possible cytotoxic, genotoxic, and apoptotic effects of nasal sprays were studied on human normal skin fibroblastic cells (CCD-1079Sk) using WST cell viability test, alkaline single-cell gel electrophoresis analysis, and acridine orange/ethidium bromide staining, respectively.
The formulations' physical appearance and drug content were assessed, yielding nonsignificant results ( > 0.05). All formulations were determined at pH 5.5-6.2 so that the pH values of the prepared formulations were compatible with the pH value of the nasal mucosa. Selected nasal spray formulations were stable for 90 days, and the safe doses were chosen as 0.0625, 0.375, and 1.25 mg/mL for diclofenac, ibuprofen, and paracetamol, respectively, by not showing toxicity even at 24 h.
This study demonstrated that nasal sprays containing paracetamol, ibuprofen, and diclofenac sodium can be successfully formulated. These new formulations may provide alternative treatment and easier application for patients unable to swallow or refuse to take oral analgesics.
鼻内镇痛喷雾剂是一种安全、有效的止痛方法，与口服止痛药相比，起效时间更短。本研究旨在使用常见的非处方镇痛药开发鼻喷雾剂，提供一种更方便且可能在疼痛管理方面更有效的替代治疗选择，尤其是在儿科患者中。
制备了三种分别含有双氯芬酸钠、布洛芬和对乙酰氨基酚的不同鼻喷雾剂配方，并完成了特性研究。分别使用WST细胞活力测试、碱性单细胞凝胶电泳分析和吖啶橙/溴化乙锭染色，研究了鼻喷雾剂对人正常皮肤成纤维细胞（CCD-1079Sk）可能的细胞毒性、遗传毒性和凋亡作用。
评估了配方的外观和药物含量，结果无统计学意义（>0.05）。所有配方的pH值均测定为5.5 - 6.2，使得所制备配方的pH值与鼻黏膜的pH值相匹配。选定的鼻喷雾剂配方在90天内稳定，双氯芬酸、布洛芬和对乙酰氨基酚的安全剂量分别选择为0.0625、0.375和1.25 mg/mL，因为即使在24小时时也未显示出毒性。
本研究表明，含有对乙酰氨基酚、布洛芬和双氯芬酸钠的鼻喷雾剂可以成功配制。这些新配方可能为无法吞咽或拒绝服用口服镇痛药的患者提供替代治疗和更便捷的应用方式。
