(32c) Preparation and Characterization of Modafinil Nanofibers By Electrospinning

Modafinil is an anti-narcoleptic drug used to treat excessive daytime sleepiness associated with sleep apnea and shift-work disorder.¹ It has been approved by the Food and Drug Administration (FDA) and is being marketed in the form of tablets with a trade name, ‘Provigil’.¹ Modafinil tablet forms suffer from disadvantages of susceptibility of reduced solid-state stability and drug loading. As nanofibers possess exceptional mechanical, physical and chemical properties, these formulations have gained tremendous attention in the scientific community.² For the first time, in this work, we report the formulation of polymeric nanofibers loaded with modafinil at dosage recommended by FDA (100 mg) via electrospinning. The modafinil-loaded polymer nanofibers were prepared by electrospinning polymer solutions with suspended modafinil crystals at a voltage of 12 kV and a flow rate of 5 mL/h. Polymers used were Poly Vinyl Pyrrolidone (PVP), Poly Vinyl Alcohol (PVA), Poly Ethylene Glycol (PEG), and Poly L-Lactide (PLLA). The obtained electrospun nanofiber formulations were characterized for their morphological, vibrational, structural, and thermal properties by Scanning Electron Microscopy (SEM), Raman spectroscopy, Powder X-Ray Diffraction (PXRD), Differential Scanning Calorimetric (DSC) and Thermogravimetric Analysis (TGA). The modafinil loading in the nanofibers and the dissolution of the electrospun modafinil nanofibres were determined using UV-Vis spectrophotometer at 220 nm.³ The morphological analysis revealed the encapsulation of circular-shaped modafinil particles within the nanofibers further evidenced by the broader stretching of the Raman spectral region around the wave numbers ranging between 1425 cm^-1 – 1225 cm^-1, 1050 cm^-1-1000 cm^-1 and 650 cm^-1 – 620 cm^-1 representative for C-H stretching, presence of a polystyrene peak and a S=O stretching in modafinil. The PXRD analysis confirmed the presence of modafinil in the nanofibers and the crystalline nature of the formulation. The melting point of the modafinil-loaded nanofibers was found to be higher than the melting point of commercial modafinil indicating that the modafinil-nanofiber formulation possesses a good thermal stability characteristic than the commercial modafinil. The unoptimized loading of modafinil into the nanofibers was determined to be 65%. The modafinil-loaded nanofibers illustrate that electrospinning can serve as a less laborious and an easily adoptable continuous method for the formulation of modafinil according to the desired dosage needs. Consequently, this study might be used as a rationale for necessary further analytical and regulatory studies.

Keywords: Modafinil, electrospinning, loading.

References

(1) Minzenberg, M. J.; Carter, C. S. Modafinil: A Review of Neurochemical Actions and Effects on Cognition, Neuropsychopharmacology 2008, 33, 1477-1502.

(2) Morie, A.; Garg, T.; Goyal, A. K.; Rath, G. Nanofibers as novel drug carrier, Artificial Cells, Nanomedicine, and Biotechnology 2014, 44(1), 135-143.

(3) Adibika, K.; Selselehjonban, S.; Emami, S.; Osouli-Bostanabad, K.; Barzegar-Jalali, M. Electrosprayed polymeric nanobeads and nanofibers of modafinil: preparation, characterization, and drug release studies, Bioimpacts 2019, 9(3), 179-188.