Cargando…

Investigation of Molecular Weight, Polymer Concentration and Process Parameters Factors on the Sustained Release of the Anti-Multiple-Sclerosis Agent Teriflunomide from Poly(ε-caprolactone) Electrospun Nanofibrous Matrices

In the current work, a series of PCL polyesters with different molecular weights was synthesized and used for the fabrication of nanofibrous patches via electrospinning, as sustained release matrices for leflunomide’s active metabolite, teriflunomide (TFL). The electrospinning conditions for each sa...

Descripción completa

Detalles Bibliográficos
Autores principales: Bikiaris, Nikolaos D., Koumentakou, Ioanna, Michailidou, Georgia, Kostoglou, Margaritis, Vlachou, Marilena, Barmpalexis, Panagiotis, Karavas, Evangelos, Papageorgiou, George Z.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9412398/
https://www.ncbi.nlm.nih.gov/pubmed/36015319
http://dx.doi.org/10.3390/pharmaceutics14081693
_version_ 1784775484376088576
author Bikiaris, Nikolaos D.
Koumentakou, Ioanna
Michailidou, Georgia
Kostoglou, Margaritis
Vlachou, Marilena
Barmpalexis, Panagiotis
Karavas, Evangelos
Papageorgiou, George Z.
author_facet Bikiaris, Nikolaos D.
Koumentakou, Ioanna
Michailidou, Georgia
Kostoglou, Margaritis
Vlachou, Marilena
Barmpalexis, Panagiotis
Karavas, Evangelos
Papageorgiou, George Z.
author_sort Bikiaris, Nikolaos D.
collection PubMed
description In the current work, a series of PCL polyesters with different molecular weights was synthesized and used for the fabrication of nanofibrous patches via electrospinning, as sustained release matrices for leflunomide’s active metabolite, teriflunomide (TFL). The electrospinning conditions for each sample were optimized and it was found that only one material with high Mn (71,000) was able to produce structures with distinct fibers devoid of the presence of beads. The successful preparation of the fibers was determined by scanning electron microscopy (SEM).TFL (10, 20 and 30 wt%) in three different concentrations was incorporated into the prepared nanofibers, which were used in in vitro drug release experiments. The drug-loaded nanofibrous formulations were further characterized by Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and powder X-ray diffractometry (XRD).It was found that TFL was incorporated in an amorphous form inside the polymeric nanofibers and that significant molecular interactions were formed between the drug and the polyester. Additionally, in vitro dissolution studies showed that the PCL/TFL-loaded nanofibers exhibit a biphasic release profile, having an initial burst release phase, followed by a sustained release until 250 h. Finally, a kinetic analysis of the obtained profiles revealed that the drug release was directly dependent on the amount TFL incorporated into the nanofibers.
format Online
Article
Text
id pubmed-9412398
institution National Center for Biotechnology Information
language English
publishDate 2022
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-94123982022-08-27 Investigation of Molecular Weight, Polymer Concentration and Process Parameters Factors on the Sustained Release of the Anti-Multiple-Sclerosis Agent Teriflunomide from Poly(ε-caprolactone) Electrospun Nanofibrous Matrices Bikiaris, Nikolaos D. Koumentakou, Ioanna Michailidou, Georgia Kostoglou, Margaritis Vlachou, Marilena Barmpalexis, Panagiotis Karavas, Evangelos Papageorgiou, George Z. Pharmaceutics Article In the current work, a series of PCL polyesters with different molecular weights was synthesized and used for the fabrication of nanofibrous patches via electrospinning, as sustained release matrices for leflunomide’s active metabolite, teriflunomide (TFL). The electrospinning conditions for each sample were optimized and it was found that only one material with high Mn (71,000) was able to produce structures with distinct fibers devoid of the presence of beads. The successful preparation of the fibers was determined by scanning electron microscopy (SEM).TFL (10, 20 and 30 wt%) in three different concentrations was incorporated into the prepared nanofibers, which were used in in vitro drug release experiments. The drug-loaded nanofibrous formulations were further characterized by Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and powder X-ray diffractometry (XRD).It was found that TFL was incorporated in an amorphous form inside the polymeric nanofibers and that significant molecular interactions were formed between the drug and the polyester. Additionally, in vitro dissolution studies showed that the PCL/TFL-loaded nanofibers exhibit a biphasic release profile, having an initial burst release phase, followed by a sustained release until 250 h. Finally, a kinetic analysis of the obtained profiles revealed that the drug release was directly dependent on the amount TFL incorporated into the nanofibers. MDPI 2022-08-14 /pmc/articles/PMC9412398/ /pubmed/36015319 http://dx.doi.org/10.3390/pharmaceutics14081693 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Bikiaris, Nikolaos D.
Koumentakou, Ioanna
Michailidou, Georgia
Kostoglou, Margaritis
Vlachou, Marilena
Barmpalexis, Panagiotis
Karavas, Evangelos
Papageorgiou, George Z.
Investigation of Molecular Weight, Polymer Concentration and Process Parameters Factors on the Sustained Release of the Anti-Multiple-Sclerosis Agent Teriflunomide from Poly(ε-caprolactone) Electrospun Nanofibrous Matrices
title Investigation of Molecular Weight, Polymer Concentration and Process Parameters Factors on the Sustained Release of the Anti-Multiple-Sclerosis Agent Teriflunomide from Poly(ε-caprolactone) Electrospun Nanofibrous Matrices
title_full Investigation of Molecular Weight, Polymer Concentration and Process Parameters Factors on the Sustained Release of the Anti-Multiple-Sclerosis Agent Teriflunomide from Poly(ε-caprolactone) Electrospun Nanofibrous Matrices
title_fullStr Investigation of Molecular Weight, Polymer Concentration and Process Parameters Factors on the Sustained Release of the Anti-Multiple-Sclerosis Agent Teriflunomide from Poly(ε-caprolactone) Electrospun Nanofibrous Matrices
title_full_unstemmed Investigation of Molecular Weight, Polymer Concentration and Process Parameters Factors on the Sustained Release of the Anti-Multiple-Sclerosis Agent Teriflunomide from Poly(ε-caprolactone) Electrospun Nanofibrous Matrices
title_short Investigation of Molecular Weight, Polymer Concentration and Process Parameters Factors on the Sustained Release of the Anti-Multiple-Sclerosis Agent Teriflunomide from Poly(ε-caprolactone) Electrospun Nanofibrous Matrices
title_sort investigation of molecular weight, polymer concentration and process parameters factors on the sustained release of the anti-multiple-sclerosis agent teriflunomide from poly(ε-caprolactone) electrospun nanofibrous matrices
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9412398/
https://www.ncbi.nlm.nih.gov/pubmed/36015319
http://dx.doi.org/10.3390/pharmaceutics14081693
work_keys_str_mv AT bikiarisnikolaosd investigationofmolecularweightpolymerconcentrationandprocessparametersfactorsonthesustainedreleaseoftheantimultiplesclerosisagentteriflunomidefrompolyecaprolactoneelectrospunnanofibrousmatrices
AT koumentakouioanna investigationofmolecularweightpolymerconcentrationandprocessparametersfactorsonthesustainedreleaseoftheantimultiplesclerosisagentteriflunomidefrompolyecaprolactoneelectrospunnanofibrousmatrices
AT michailidougeorgia investigationofmolecularweightpolymerconcentrationandprocessparametersfactorsonthesustainedreleaseoftheantimultiplesclerosisagentteriflunomidefrompolyecaprolactoneelectrospunnanofibrousmatrices
AT kostogloumargaritis investigationofmolecularweightpolymerconcentrationandprocessparametersfactorsonthesustainedreleaseoftheantimultiplesclerosisagentteriflunomidefrompolyecaprolactoneelectrospunnanofibrousmatrices
AT vlachoumarilena investigationofmolecularweightpolymerconcentrationandprocessparametersfactorsonthesustainedreleaseoftheantimultiplesclerosisagentteriflunomidefrompolyecaprolactoneelectrospunnanofibrousmatrices
AT barmpalexispanagiotis investigationofmolecularweightpolymerconcentrationandprocessparametersfactorsonthesustainedreleaseoftheantimultiplesclerosisagentteriflunomidefrompolyecaprolactoneelectrospunnanofibrousmatrices
AT karavasevangelos investigationofmolecularweightpolymerconcentrationandprocessparametersfactorsonthesustainedreleaseoftheantimultiplesclerosisagentteriflunomidefrompolyecaprolactoneelectrospunnanofibrousmatrices
AT papageorgiougeorgez investigationofmolecularweightpolymerconcentrationandprocessparametersfactorsonthesustainedreleaseoftheantimultiplesclerosisagentteriflunomidefrompolyecaprolactoneelectrospunnanofibrousmatrices