Pitolisant nanofibers: A promising frontier in drug delivery for narcolepsy - Formulation, optimisation, and characterization insights

Abstract

The study focuses on developing a new way to deliver the narcolepsy medication pitolisant. Electrospinning was used to make polyvinyl alcohol (PVA) and hyperbranched polyglycerol (HPG) polymers into pitolisant nanofibers (PT-NF). A design expert created the best formulation to optimise the process variables like applied voltage, distance, and feed rate. The nanofibers were characterised using scanning electron microscopy, X-ray diffraction, FT-IR, entrapment efficiency, and in-vitro drug release studies. Results showed that the optimal PT-NF formulation had an average diameter of 172 ​nm with an entrapment efficacy of 95 ​% and 92 ​% drug release within 45 ​min. HPG polymer was included in the optimised formulation, whose average fibre diameter was 118 ​nm with 98 ​% entrapment efficacy and 98 ​± ​2 ​% drug release within 30 ​min. These findings strongly suggest that PT nanofibers hold substantial promise as a viable alternative to conventional solid dosage forms for brain-targeted administration, especially when administered via a transdermal patch to a patient during sleep.

Keywords

• Pitolisant
• Design expert
• Electrospinning
• Nanofibers
• PVA
• HPG