Preparation and physicochemical characterization of modafinil nanoparticles prepared via electrospraying method

Abstract

Introduction: Modafinil (MDF) is a novel wake-promoting agent approved by FDA for the treatment of excessive daytime sleepiness caused by narcolepsy, shift work sleep disorder and obstructive sleep apnea. Regarding its low solubility and high permeability, improving the dissolution properties of the drug by preparing nanoformulations can be a promising approach to improve the bioavailability of the drug. Aim: The aim of the present study was to prepare and characterize modafinil–Eudragit® RS100 nanoparticles. Methods: The modafinil-Eudragit® RS100 nanobeads and nanofibers with the different drug:polymer ratios and solution concentrations were prepared using electrospraying technique. The physicochemical characteristics of the nanobeads and nanofibers were evaluated using scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD) and Fourier-transform infrared spectroscopy (FTIR). In vitro dissolution tests were carried out using USP apparatus II at a pH of 6.8. Drug release profiles were compared by the use of two model-independent parameters: percent drug dissolved within 45 min (Q45min) and dissolution efficiency within 120 min (DE120min). Results: Increasing the concentration of the injected solution resulted in more nanofibers and less nanobeads production with the particle size ranged from 40–150 nm. DSC and XRPD studies indicated that the drug crystallinity was notably reduced. FIIR analysis revealed no chemical interaction between drug and polymer during the preparation process. Nanoformulations exhibited biphasic release profiles with improved release profiles compared to pure drug. Conclusions: Findings from the research suggest that MDF-EUD nanofibers and nanobeads with improved physicochemical characteristics are possible to be formulated through optimizing the preparation parameters. Simplicity of the electrospraying process makes it an excellent choice for being scaled up.