Limón David, Amirthalingam Ezhil, Rodrigues Mafalda, Halbaut Lyda, Andrade Berenice, Garduño-Ramírez María Luisa, Amabilino David B, Pérez-García Lluïsa, Calpena Ana C
Departament de Farmacologia i Química Terapèutica, Universitat de Barcelona, Av. Joan XXIII, s/n, 08028 Barcelona, Spain; Institut de Nanociència i Nanotecnologia IN2UB, Universitat de Barcelona, 08028 Barcelona, Spain.
Departament de Farmàcia i Tecnologia Farmacèutica, Universitat de Barcelona, Av. Joan XXI, s/n, 08028 Barcelona, Spain.
Eur J Pharm Biopharm. 2015 Oct;96:421-36. doi: 10.1016/j.ejpb.2015.09.007. Epub 2015 Sep 25.
A bis-imidazolium-based amphiphilic molecule was used to form novel supramolecular gels in ethanol-water mixtures. The proportion of solvents, the concentration of gellant and the temperature are factors that strongly influence the gelling process. The physical gels that are formed comprise entangled fibers of around 100nm in diameter, able to incorporate anionic drugs, whose morphology varies depending on the drug they incorporate. These hydrogels are soft and therefore optimum for skin application. They show good stability when compared to previously reported gels. Suitable drug release and skin permeation profiles were obtained, and, moreover, they seem to promote the retention of the drug inside the skin. Finally, effective in vivo anti-inflammatory activity was observed, especially with the indomethacin-incorporated gel, which indicates that these supramolecular hydrogels are a good option for the delivery of poor water soluble drugs for the treatment of acute inflammation or other skin diseases.
一种基于双咪唑鎓的两亲分子被用于在乙醇 - 水混合物中形成新型超分子凝胶。溶剂比例、胶凝剂浓度和温度是强烈影响胶凝过程的因素。形成的物理凝胶由直径约100nm的缠结纤维组成，能够包载阴离子药物，其形态取决于所包载的药物。这些水凝胶质地柔软，因此最适合用于皮肤给药。与先前报道的凝胶相比，它们表现出良好的稳定性。获得了合适的药物释放和皮肤渗透曲线，此外，它们似乎能促进药物在皮肤内的滞留。最后，观察到了有效的体内抗炎活性，尤其是含吲哚美辛的凝胶，这表明这些超分子水凝胶是递送难溶性药物用于治疗急性炎症或其他皮肤病的良好选择。
