Frontiers in drug delivery
Design and optimization of mucoadhesive chitosan microspheres for oesophageal delivery of fluconazole
By Shivakumar HN, Parmar A, Shinde R and 1 others.
Abstract
Background
Oesophageal candidiasis remains challenging to treat owing to rapid transit of conventional oral formulations through the oesophagus, resulting in inadequate local drug delivery and reduced therapeutic efficacy. To address these limitations, the present study aimed to develop fluconazole-loaded chitosan microspheres (FCZ-CMs)-based orodispersible tablets (ODTs) that rapidly disintegrate in the oral cavity while releasing mucoadhesive microspheres capable of adhering to oesophageal mucosa, enabling sustained localized drug delivery.
Methods
FCZ-CMs were developed by the emulsion cross-linking method using a 23 full factorial design to optimize particle size (PS), entrapment efficiency (EE), drug release (DR), and ex vivo oesophageal retention (ORT). Optimised FCZ-CMs (F9) were extensively characterized by Infrared spectroscopy (FTIR), scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X-ray diffractometry (XRD), and in vitro drug release studies. Further, the ODTs developed by direct compression of F9 were evaluated for wetting time (WT), disintegration time (DT), drug content (DC), % drug release at 60 min (%DR), similarity (f 1 /f 2 ), and stability under real-time and accelerated conditions.