Marcos Xelhua, Pérez-Casas Silvia, Llovo José, Concheiro Angel, Alvarez-Lorenzo Carmen
Laboratorio de Biofisicoquímica, Departamento de Fisicoquímica, Facultad de Química, Universidad Nacional Autónoma de México, México D.F. 04510, Mexico.
Servicio de Microbiología y Parasitología, Complejo Hospitalario Universitario de Santiago de Compostela, 15782 Santiago de Compostela, Spain.
Int J Pharm. 2016 Mar 16;500(1-2):11-9. doi: 10.1016/j.ijpharm.2016.01.015. Epub 2016 Jan 12.
Supramolecular gels of poloxamer-hydroxyethyl cellulose (HEC)-α-cyclodextrin (αCD) were developed aiming to obtain synergisms regarding solubilization and sustained release of griseofulvin for topical application. The effects of αCD concentration (0-10%w/w) on the phase behavior of aqueous dispersions of Pluronic(®) P123 (14%w/w) mixed with HEC (2%w/w) were evaluated at 4, 20 and 37°C. The cooperative effects of the inclusion complex formation between poly(ethylene oxide) (PEO) blocks and HEC with αCD prevented phase separation and led to supramolecular networks that solubilize the antifungal drug. Rheological and bioadhesive properties of gels with and without griseofulvin could be easily tuned modulating the polymers proportions. Supramolecular gels underwent sol-gel transition at lower temperature than P123 solely dispersions and enabled drug sustained release for at least three weeks. All gels demonstrated good biocompatibility in the HET-CAM test. Furthermore, the drug-loaded gels showed activity against Trichophyton rubrum and Trichophyton mentagrophytes and thus may be useful for the treatment of tinea capitis and other cutaneous fungal infections.
开发了泊洛沙姆 - 羟乙基纤维素（HEC）-α-环糊精（αCD）超分子凝胶，旨在获得关于灰黄霉素增溶和持续释放的协同作用，用于局部应用。在4、20和37°C下评估了αCD浓度（0 - 10%w/w）对与HEC（2%w/w）混合的普朗尼克（®）P123（14%w/w）水分散体相行为的影响。聚环氧乙烷（PEO）嵌段与HEC和αCD之间形成包合物的协同作用防止了相分离，并导致了能够增溶抗真菌药物的超分子网络。含和不含灰黄霉素的凝胶的流变学和生物粘附特性可以通过调节聚合物比例轻松调整。超分子凝胶在比单独的P123分散体更低的温度下经历溶胶 - 凝胶转变，并能够使药物持续释放至少三周。所有凝胶在HET - CAM试验中均表现出良好的生物相容性。此外，载药凝胶对红色毛癣菌和须癣毛癣菌具有活性，因此可能对治疗头癣和其他皮肤真菌感染有用。
