Otto Filip, Froelich Anna
Poznan University of Medical Sciences, Chair and Department of Pharmaceutical Technology, 3 Rokietnicka Street, 60-806 Poznań, Poland.
Poznan University of Medical Sciences, Chair and Department of Pharmaceutical Technology, 3D Printing Division, 3 Rokietnicka Street, 60-806 Poznań, Poland.
Gels. 2024 Jun 29;10(7):435. doi: 10.3390/gels10070435.
Ketoprofen is a non-steroidal, anti-inflammatory drug frequently incorporated in topical dosage forms which are an interesting alternatives for oral formulations. However, due to the physiological barrier function of skin, topical formulations may require some approaches to improve drug permeation across the skin. In this study, ketoprofen-loaded microemulsion-based gels with the addition of menthol, commonly known for absorption-enhancing activity in dermal products, were investigated. The main objective of this study was to analyze the physicochemical properties of the obtained gels in terms of topical application and to investigate the correlation between the gel composition and its mechanical properties and the drug release process. Microemulsion composition was selected with the use of a pseudoternary plot and the selected systems were tested for electrical conductivity, viscosity, pH, and particle diameter. The polymer gels obtained with Carbopol EZ-3 were subjected to rheological and textural studies, as well as the drug release experiment. The obtained results indicate that the presence of ketoprofen slightly decreased yield stress values. A stronger effect was exerted by menthol presence, even though it was independent of menthol concentration. A similar tendency was seen for hardness and adhesiveness, as tested in texture profile analysis. Sample cohesiveness and the drug release rate were independent of the gel composition.
酮洛芬是一种非甾体抗炎药,常用于局部剂型,是口服制剂的一种有趣替代方案。然而,由于皮肤的生理屏障功能,局部制剂可能需要一些方法来改善药物透过皮肤的渗透。在本研究中,研究了添加薄荷醇的载酮洛芬微乳凝胶,薄荷醇在皮肤产品中通常具有吸收增强活性。本研究的主要目的是从局部应用角度分析所得凝胶的物理化学性质,并研究凝胶组成与其机械性能和药物释放过程之间的相关性。使用拟三元相图选择微乳组成,并对所选体系进行电导率、粘度、pH值和粒径测试。用卡波姆EZ-3制备的聚合物凝胶进行了流变学和质地研究以及药物释放实验。所得结果表明,酮洛芬的存在略微降低了屈服应力值。薄荷醇的存在产生了更强的影响,尽管这与薄荷醇浓度无关。在质地剖面分析中测试的硬度和粘性也有类似趋势。样品内聚性和药物释放速率与凝胶组成无关。