Abstract

The main goal of this work is the design of a mucoadhesive system, based on three layers for the unidirectional release of dexamethasone sodium phosphate (DEX-F) for possible use in the oral mucosal cavity. The different layers were created by the electrospinning process, using polyvinylpyrrolidone (PVP) and poly(ε-caprolactone) (PCL)as polymeric base and polycarbophil (NOVEON^® AA-1, PCF) as adhesion enhancer. The system contains a drug-release layer, an adhesive layer and a backing layer. The nanofibers matrices were characterized morphologically by scanning electron microscopy (SEM), Fourier-transform infrared spectroscopy (FTIR), thermogravimetric analysis (TGA) and differential scanning calorimetry (DSC); in vitro drug content, degradation time and ex vivo mucoadhesive properties studies were performed. SEM images showed the formation of fibers with a variable diameter and porosity between the layers. Thermal studies TGA and DSC indicated an excellent thermal stability for materials. In vitro studies show a drug content release of 79.86% ±13.5% of the loaded drug in a 4 h release period. Mucoadhesive evaluation exhibit excellent characteristics for a mucosal adhesion. The produced electrospun mucoadhesive patch exhibited an excellent stability, thermal properties, mucoadhesive properties, and the appropriate amount of drug released, promising features for successful DEX-F delivery in a mucoadhesive system for oromucosal surface.

摘要

这项工作的主要目标是设计一个粘膜粘附系统，该系统基于三层单向释放地塞米松磷酸钠 (DEX-F)，可能用于口腔粘膜。不同的层是通过静电纺丝工艺创建的，使用聚乙烯吡咯烷酮 (PVP) 和聚（ε-己内酯）（PCL）作为聚合物基础和聚卡波非（NOVEON ^® AA-1，PCF）作为粘合增强剂。该系统包含药物释放层、粘合剂层和背衬层。通过扫描电子显微镜 (SEM)、傅里叶变换红外光谱 (FTIR)、热重分析 (TGA) 和差示扫描量热法 (DSC) 对纳米纤维基质进行形态学表征；体外药物含量、降解时间和离体进行了粘膜粘附特性​​研究。SEM 图像显示形成了具有可变直径和层间孔隙率的纤维。热研究 TGA 和 DSC 表明材料具有出色的热稳定性。体外研究表明，在 4 小时的释放期内，所载药物的药物含量释放率为 79.86% ±13.5%。粘膜粘附评价表现出优异的粘膜粘附特性​​。生产的电纺粘膜粘附贴剂表现出优异的稳定性、热性能、粘膜粘附特性​​和适当的药物释放量，在口腔粘膜表面的粘膜粘附系统中成功递送 DEX-F 的有希望的特征。