TY - JOUR
T1 - Formulation and Evaluation of Fenbendazole Extended-Release Extrudes Processed by Hot-Melt Extrusion
AU - Bezerra, Gilberto S.N.
AU - de Lima, Tielidy A.de M.
AU - Colbert, Declan M.
AU - Geever, Joseph
AU - Geever, Luke
N1 - Publisher Copyright:
© 2022 by the authors.
PY - 2022/10
Y1 - 2022/10
N2 - 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.
AB - 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.
KW - extended-release
KW - fenbendazole
KW - hot-melt extrusion
UR - http://www.scopus.com/inward/record.url?scp=85139821351&partnerID=8YFLogxK
U2 - 10.3390/polym14194188
DO - 10.3390/polym14194188
M3 - Article
AN - SCOPUS:85139821351
SN - 2073-4360
VL - 14
JO - Polymers
JF - Polymers
IS - 19
M1 - 4188
ER -