Faculty of Pharmacy, "Grigore T. Popa", University of Medicine and Pharmacy of Iași, Iași 700115, Romania.
Faculty of Pharmacy, University of Medicine and Pharmacy of Tîrgu Mureș, Târgu Mureş 540001, Romania.
Molecules. 2018 Jul 5;23(7):1640. doi: 10.3390/molecules23071640.
This study aims to develop new antifungal dermal films based on their mechanical properties (elongation, adhesion, behaviour towards vapour moisture) and the in vitro availability of miconazole nitrate, used as a pharmaceutical active ingredient in various concentrations. The three polymeric films prepared were translucent or shiny, with the surface of 63.585 cm², 0.20⁻0.30 mm thickness, and content of miconazole nitrate of 3.931 or 15.726 mg·cm². The mechanical resistance and elongation tests demonstrated that the two films based on hydroxyethyl cellulose (HEC) polymer were more elastic than the one prepared with hydroxypropyl methylcellulose (HPMC). The vapour water absorption and vapour water loss capacity of the films revealed that the HPMC film did not dry very well in the process of preparation by the evaporation of the solvent technique, unlike the HEC films that jellified more evenly in water and had higher drying capacity at 40 °C. The in vitro availability of miconazole nitrate from dermal films was evaluated using the Franz diffusion cell method, through a synthetic membrane (Ø 25 mm × 0.45 µm) and acceptor media with pH 7.4 (phosphate buffer and sodium lauryl sulphate 0.045%), resulting a release rate of up to 70%.
本研究旨在基于机械性能（伸长率、附着力、对蒸汽湿度的行为）以及硝酸咪康唑的体外可用性，开发新的抗真菌皮肤贴剂。硝酸咪康唑用作不同浓度的药物活性成分。所制备的三种聚合物膜为半透明或有光泽，表面积为 63.585cm²，厚度为 0.20⁻0.30mm，硝酸咪康唑含量为 3.931 或 15.726mg·cm²。机械阻力和伸长率测试表明，基于羟乙基纤维素（HEC）聚合物的两种薄膜比基于羟丙基甲基纤维素（HPMC）的薄膜更具弹性。薄膜的蒸汽水吸收和蒸汽水损失能力表明，在溶剂蒸发技术制备过程中，HPMC 薄膜不能很好地干燥，而 HEC 薄膜在水中更均匀地胶凝，在 40°C 时具有更高的干燥能力。通过Franz 扩散池法，使用合成膜（Ø 25mm×0.45µm）和 pH 7.4 的接受介质（磷酸盐缓冲液和 0.045%十二烷基硫酸钠）评估硝酸咪康唑从皮肤贴剂中的体外可用性，结果释放率高达 70%。
