Formulation and Evaluation of Fenbendazole Extended-Release Extrudes Processed by Hot-Melt Extrusion

This study aimed to demonstrate the feasibility of hot-melt extrusion in the development of extended-release formulations of Fenbendazole (Fen) dispersed in PEO/PCL blend-based matrices. Their thermal, physical, chemical and viscosity properties were assessed by differential scanning calorimetry, th...

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Bibliographic Details
Published in:Polymers 2022-10, Vol.14 (19), p.4188
Main Authors: Bezerra, Gilberto S. N., de Lima, Tielidy A. de M., Colbert, Declan M., Geever, Joseph, Geever, Luke
Format: Article
Language:English
Subjects:
Calorimetry
Diffraction
Dispersion
Drug delivery systems
Drug dosages
Evaluation
Extrusion rate
Formulations
Fourier transforms
Infrared analysis
Infrared spectroscopy
Melt flow index
Polymers
Scanning electron microscopy
Spectrum analysis
Thermal analysis
Thermogravimetric analysis
Thermogravimetry
Viscosity
X-ray spectroscopy
X-rays
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Summary:This study aimed to demonstrate the feasibility of hot-melt extrusion in the development of extended-release formulations of Fenbendazole (Fen) dispersed in PEO/PCL blend-based matrices. Their thermal, physical, chemical and viscosity properties were assessed by differential scanning calorimetry, thermogravimetric analysis/derivative thermogravimetry, Fourier transform infrared spectroscopy, X-ray diffraction spectroscopy, and melt flow index. Drug dispersion was analyzed by scanning electron microscopy with electron dispersive X-ray spectroscopy, and drug release was evaluated by ultraviolet-visible spectroscopy. A thermal analysis indicated the conversion of the drug to its amorphous state. FTIR analysis endorsed the thermal studies pointing to a decrease in the drug’s crystallinity with the establishment of intermolecular interactions. XRD analysis confirmed the amorphous nature of Fen. MFI test revealed that PCL acts as a plasticizer when melt-processed with PEO. SEM images displayed irregular surfaces with voids and pores, while EDX spectra demonstrated a homogeneous drug distribution throughout the polymeric carrier. Dissolution testing revealed that PCL retards the drug release proportionally to the content of such polymer incorporated. These melt-extruded matrices showed that the drug release rate in a PEO/PCL blend can easily be tailored by altering the ratio of PCL to address the issues related to the multiple-dosing regimen of Fen in ruminants.
ISSN:2073-4360
2073-4360
DOI:10.3390/polym14194188