Okur Mehmet Evren, Ayla Şule, Yozgatlı Vildan, Aksu Neşe Buket, Yoltaş Ayşegül, Orak Duygu, Sipahi Hande, Üstündağ Okur Neslihan
University of Health Sciences, Faculty of Pharmacy, Department of Pharmacology, İstanbul, Turkey.
Istanbul Medipol University, School of Medicine, Department of Histology and Embryology, Beykoz, 34810 Istanbul, Turkey.
Saudi Pharm J. 2020 Mar;28(3):338-348. doi: 10.1016/j.jsps.2020.01.015. Epub 2020 Feb 3.
The objective of the present research was to examine the possible usage of microemulsion based gel for fusidic acid (FA) dermal application as burn wound treatment. During the preparation of microemulsion, ethyl oleate as oil phase, tween 80 as a surfactant, ethanol as co-surfactant, water as aqueous phase were used. The prepared microemulsions were evaluated for clarity, pH, viscosity and FA content. Moreover, stability, sterility, antibacterial activity, release of the formulations were also evaluated. The results showed that the FA loaded microemulsion and microemulsion based gel formation and characteristics were related to many parameters of the components. The performed optimized microemulsion-based gel showed good stability over a period of 3 months. The antibacterial activity of microemulsion-based gel was found to be comparable with marketed cream. RAW 264.7 macrophages were used to determine cell viability (MTT assay) and nitric oxide production. MBG and FA-MBG significantly inhibit the production of the inflammatory mediator NO in LPS-stimulated RAW 264.7 cells in a concentration-dependent manner. The wound healing property was evaluated by histopathological examination and by measuring the wound contraction. The % of wound area in rats treated with FA (2%) loaded microemulsion based gel ranged from 69.30% to 41.39% in the period from 3 to 10 days. In conclusion, FA loaded microemulsion based gel could be offered as encouraging strategy as dermal systems for the burn wound treatment.
本研究的目的是考察基于微乳的凝胶用于夫西地酸（FA）皮肤给药治疗烧伤创面的可能性。在微乳制备过程中，使用油酸乙酯作为油相，吐温80作为表面活性剂，乙醇作为助表面活性剂，水作为水相。对制备的微乳进行澄清度、pH值、粘度和FA含量的评估。此外，还评估了制剂的稳定性、无菌性、抗菌活性和释放情况。结果表明，载FA微乳及基于微乳的凝胶的形成和特性与各组分的许多参数有关。所制备的优化的基于微乳的凝胶在3个月内显示出良好的稳定性。发现基于微乳的凝胶的抗菌活性与市售乳膏相当。使用RAW 264.7巨噬细胞来测定细胞活力（MTT法）和一氧化氮的产生。MBG和FA-MBG以浓度依赖性方式显著抑制LPS刺激的RAW 264.7细胞中炎性介质NO的产生。通过组织病理学检查和测量伤口收缩来评估伤口愈合性能。在3至10天期间，用载有FA（2%）的基于微乳的凝胶治疗的大鼠的伤口面积百分比范围为69.30%至41.39%。总之，载FA的基于微乳的凝胶可作为一种用于烧伤创面治疗的皮肤给药系统的令人鼓舞的策略。
