Universidad Nacional Autónoma de México (UNAM), Facultad de Estudios Superiores Cuautitlán (FES-Cuautitlán), Laboratorio de Sistemas Farmacéuticos de Liberación Modificada, Km. 2.5 Carretera Cuautitlán-Teoloyucan, San Sebastián Xhala, C.P. 54714 Cuautitlán Izcalli, Edo. de México, Mexico.
UNAM, FES-Cuautitlán, Laboratorio de Posgrado en Tecnología Farmacéutica, Av. 1o de mayo s/n, C.P. 54740 Cuautitlán Izcalli, Edo. de México, Mexico.
Eur J Pharm Sci. 2018 Mar 30;115:185-195. doi: 10.1016/j.ejps.2017.11.029. Epub 2017 Dec 5.
This study aimed to prepare poly (d,l-lactide-co-glycolide) (PLGA) nanoparticles (NPs) with chitosan (CTS) surface modification to be used as a vaginal delivery system for antimycotic drugs. Clotrimazole was encapsulated with entrapment efficiencies of 86.1 and 68.9% into Clotrimazole-PLGA-NPs (CLT-PLGA-NPs) and PLGA-NPs with CTS-modified surface (CLT-PLGA-CTS-NPs), respectively. The later NPs exhibited a larger size and higher positive zeta potential (Z potential) in comparison to unmodified NPs. In vitro release kinetic studies indicated that Clotrimazole was released in percentages of >98% from both nanoparticulate systems after 18days. Antifungal activity and mucoadhesive properties of NPs were enhanced when CTS was added onto the surface. In summary, these results suggested that Clotrimazole loaded into PLGA-CTS-NPs has great potential for vaginal applications in treating vaginal infections generated by Candida albicans.
本研究旨在制备壳聚糖（CTS）表面修饰的聚（丙交酯-共-乙交酯）（PLGA）纳米粒子（NPs），用作抗真菌药物的阴道递药系统。克霉唑的包封效率分别为 86.1%和 68.9%，包裹到克霉唑-PLGA-NPs（CLT-PLGA-NPs）和表面经 CTS 修饰的 PLGA-NPs（CLT-PLGA-CTS-NPs）中。与未修饰的 NPs 相比，后者的 NPs 具有更大的粒径和更高的正 Zeta 电位（Z 电位）。体外释放动力学研究表明，18 天后，两种纳米颗粒系统中克霉唑的释放百分比均超过 98%。当在表面添加 CTS 时，NPs 的抗真菌活性和粘膜粘附性能得到增强。总之，这些结果表明，负载到 PLGA-CTS-NPs 中的克霉唑具有治疗白色念珠菌引起的阴道感染的阴道应用的巨大潜力。
