Baranauskaite Juste, Sefer Sedef, Zevzikoviene Augusta, Zevzikovas Andrejus, Ivanauskas Liudas
Department of Pharmaceutical Technology, Faculty of Pharmacy, Yeditepe University, Kayisdagi Cad., Atasehir, 34755 Istanbul, Türkiye.
Department of Analytical and Toxicological Chemistry, Lithuanian University of Health Sciences, Mickeviciaus Str. 9, 44307 Kaunas, Lithuania.
Pharmaceuticals (Basel). 2025 Jun 21;18(7):938. doi: 10.3390/ph18070938.
Enoxolon is widely recognized for its pharmacological potential, exhibiting antioxidant, anti-inflammatory, anticancer, and antiviral properties. : This study aimed to develop an enhanced formulation of enoxolone-loaded microsponges as a novel drug delivery system. A design of experiments (DoE) approach was employed for the optimization process. : The microsponges were produced using the -emulsion technique. The selected formulation was evaluated for yield, particle size, and entrapment efficiency. Furthermore, the microsponges were incorporated into a 1% MC solution matrix, and in vitro release studies were performed to assess their drug delivery performance. : The optimal formulation was determined through the DoE methodology, which involved varying the concentrations of methylcellulose (MC) (0.55-1.87%, /), polyvinyl alcohol (PVA) (0.5-1%, /), and Tween 80 (TW80) (1.5-2.5%, /). The results showed a particle size of 142.8 ± 10.02 µm and an entrapment efficiency of 80.3 ± 1.99%. When comparing the optimized microsponge formulation to pure enoxolon, a 1.29 times higher release rate was observed ( ≤ 0.05). : Following optimizationand physicochemical characterization studies were conducted to further assess the formulation. These findings suggest that microsponge-based delivery systems hold considerable potential as an alternative platform for the topical treatment of chronic periodontitis.
甘草次酸因其药理潜力而被广泛认可，具有抗氧化、抗炎、抗癌和抗病毒特性。本研究旨在开发一种增强型载甘草次酸微球制剂作为新型药物递送系统。优化过程采用了实验设计（DoE）方法。微球采用 - 乳液技术制备。对选定的制剂进行产率、粒径和包封率评估。此外，将微球掺入1%的甲基纤维素（MC）溶液基质中，并进行体外释放研究以评估其药物递送性能。通过DoE方法确定最佳制剂，该方法涉及改变甲基纤维素（MC）（0.55 - 1.87%，/）、聚乙烯醇（PVA）（0.5 - 1%，/）和吐温80（TW80）（1.5 - 2.5%，/）的浓度。结果显示粒径为142.8 ± 10.02 µm，包封率为80.3 ± 1.99%。将优化后的微球制剂与纯甘草次酸相比，观察到释放速率提高了1.29倍（≤ 0.05）。优化后进行了物理化学表征研究以进一步评估该制剂。这些发现表明基于微球的递送系统作为慢性牙周炎局部治疗的替代平台具有相当大的潜力。
