FORMULATION OF ELECTROSPUN MICROSCOPIC THREAD STRUCTURES OF POSACONAZOLE: AMPLIFYING DISSOLUTION AND SKIN PERMEABILITY

Fungal infections pose a significant global health threat, especially for individuals with compromised immune systems1. Posaconazole, a class II drug, presents challenges due to its high permeability and low water solubility2. Innovative formulations are crucial for effective delivery. This research explores an electrospun nanofiber formulation of posaconazole, aiming to improve solubility and optimize drug release profiles. Additionally, the study focuses on developing transdermal patches as a non-invasive alternative to oral formulations, addressing potential gastrointestinal side effects. Posaconazole, generously provided by Rachem Pharma Ltd, was encapsulated in polyvinyl pyrrolidone (PVP) using an electrospinning technique. Characterization involved UV spectrophotometry, SEM, DSC, XRD, and FTIR. Laboratory experiments mimicked drug movement and penetration through skin to evaluate release patterns and absorption. The electrospun microscopic thread structures3 exhibited successful encapsulation of posaconazole, with SEM confirming nanofiber formation. XRD and DSC analyses indicated amorphization of posaconazole in the nanofiber formulation, enhancing solubility. FTIR showed compatibility between posaconazole and PVP. In vitro studies revealed higher and faster drug release from microscopic thread structures compared to solvent-solidified sheets. Ex vivo skin permeation studies demonstrated superior performance of microscopic thread structures, with increased flux and permeability coefficient. The study demonstrates the successful preparation of posaconazole-loaded microscopic thread structures with improved drug delivery kinetics compared to as-solidified sheets. The amorphization of posaconazole, molecular dispersion within PVP, and increased dissolution area contribute to enhanced performance. The findings suggest the potential of transdermal patches using microscopic thread structures as a promising alternative for optimizing posaconazole delivery and improving biopharmaceutical properties.