Ullah Irshad, Alhodaib Aiyeshah, Naz Iffat, Ahmad Waqar, Ullah Hidayat, Amin Adnan, Nawaz Asif
Department of Pharmacy, University of Swabi, Swabi 23430, Pakistan.
Department of Physics, College of Science, Qassim University, Buraydah 51452, Saudi Arabia.
Polymers (Basel). 2023 Mar 4;15(5):1298. doi: 10.3390/polym15051298.
Infectious diseases remain inevitable factors for high mortality and morbidity rate in the modern world to date. Repurposing is a novel approach to drug development has become an intriguing research topic in the literature. Omeprazole is one of the top ten proton pump inhibitors prescribed in the USA. The literature suggests that no reports based on omeprazole anti-microbial actions have been discovered to date. This study entails the potential of omeprazole to treat skin and soft tissue infections based on the literature's evident anti-microbial effects. To get a skin-friendly formulation, a chitosan-coated omeprazole-loaded nanoemulgel formulation was fabricated using olive oil, carbopol 940, Tween 80, Span 80, and triethanolamine by high-speed homogenization technique. The optimized formulation was physicochemically characterized for zeta potential, size distribution, pH, drug content, entrapment efficiency, viscosity, spreadability, extrudability, in-vitro drug release, ex-vivo permeation analysis, and minimum inhibitory concentration determination. The FTIR analysis indicated that there was no incompatibility between the drug and formulation excipients. The optimized formulation exhibited particle size, PDI, zeta potential, drug content, and entrapment efficiency of 369.7 ± 8.77 nm, 0.316, -15.3 ± 6.7 mV, 90.92 ± 1.37% and 78.23 ± 3.76%, respectively. In-vitro release and ex-vivo permeation data of optimized formulation showed 82.16% and 72.21 ± 1.71 μg/cm, respectively. The results of minimum inhibitory concentration (1.25 mg/mL) against selected bacterial strains were satisfactory, suggesting a successful treatment approach for the topical application of omeprazole to treat microbial infections. Furthermore, chitosan coating synergistically increases the antibacterial activity of the drug.
迄今为止,传染病仍是现代世界高死亡率和高发病率的不可避免因素。药物重新利用是一种新型药物开发方法,已成为文献中一个引人关注的研究课题。奥美拉唑是美国处方量排名前十的质子泵抑制剂之一。文献表明,迄今为止尚未发现基于奥美拉唑抗菌作用的报告。本研究基于文献中明显的抗菌作用,探讨奥美拉唑治疗皮肤和软组织感染的潜力。为了获得对皮肤友好的制剂,采用高速均质技术,以橄榄油、卡波姆940、吐温80、司盘80和三乙醇胺制备了壳聚糖包衣的载奥美拉唑纳米乳凝胶制剂。对优化后的制剂进行了物理化学表征,包括zeta电位、粒径分布、pH值、药物含量、包封率、粘度、铺展性、挤出性、体外药物释放、离体渗透分析和最低抑菌浓度测定。傅里叶变换红外光谱(FTIR)分析表明,药物与制剂辅料之间不存在不相容性。优化后的制剂粒径、多分散指数(PDI)、zeta电位、药物含量和包封率分别为369.7±8.77nm、0.316、-15.3±6.7mV、90.92±1.37%和78.23±3.76%。优化制剂的体外释放和离体渗透数据分别为82.16%和72.21±1.71μg/cm。对所选细菌菌株的最低抑菌浓度(1.25mg/mL)结果令人满意,表明奥美拉唑局部应用治疗微生物感染是一种成功的治疗方法。此外,壳聚糖包衣协同增强了药物的抗菌活性。