Compatibility Study Between Fenbendazole and Poly(Ethylene Oxide) with Application in Solid Dispersion Formulations Using Hot-Melt Extrusion

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5 Citations (Scopus)

Abstract

Fenbendazole (fen) or methyl N-(6-phenylsulfanyl-1H-benzimidazol-2-yl)carbamate is a broad-spectrum anthelmintic from the class of organic compounds known as benzimidazoles. Despite its pharmacological potential, fen has a limited application in oral pharmaceutical dosage forms due to its low aqueous solubility leading to an unsatisfactory bioavailability. This work aims to evaluate the compatibility between fen and poly(ethylene oxide) (PEO) applying differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR), followed by the processing of solid dispersions using hot-melt extrusion (HME) with thermal evaluation by DSC, drug dispersion assessment by scanning electron microscopy (SEM) with electron-dispersive X-ray spectroscopy (EDX), and drug release profile by ultraviolet–visible spectroscopy (UV–Vis). The results obtained from the compatibility study using thermal and non-thermal techniques proved that fen and PEO are compatible. The thermal analysis of solid dispersions showed that the extrusion process increases the polymer’s crystalline content when compared to powder mixtures. It also demonstrated that PEO dissolves fen crystalline structure, thus converting it to an amorphous state. SEM with EDX showed that solid dispersions had a homogeneous distribution of fen in the polymeric matrix with the presence of voids, pores, and ducts. Dissolution testing proved that solid dispersions of fen 5% and PEO 95% processed at 50 rpm was able to improve significantly the drug solubility in water-based media. Thus, this work brings a new solution to improving the poor-water solubility of fen using PEO to develop solid dispersion formulations processed by HME.

Original languageEnglish
Pages (from-to)262-274
Number of pages13
JournalJournal of Pharmaceutical Innovation
Volume18
Issue number1
DOIs
Publication statusPublished - Mar 2023

Keywords

  • Compatibility study
  • Fenbendazole
  • Hot-melt extrusion
  • Poly(ethylene oxide)
  • Solid dispersion formulation

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