Fabrication and characterization of electrospun nanofibers using biocompatible polymers for the sustained release of venlafaxine

Abstract Recently, drug-controlled release nanotechnology has gained special attention in biomedicine. This work focuses on developing novel electrospun polymeric nanofibers (NFs) for buccal delivery of VEN to avoid the hepatic metabolism and enzymatic degradation in the GIT and develop an effective...

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Main Authors: Heba M. Hashem, Amira Motawea, Ayman H. Kamel, E. M. Abdel Bary, Saad S. M. Hassan
Format: Article
Language:English
Published: Nature Portfolio 2022-10-01
Series:Scientific Reports
Online Access:https://doi.org/10.1038/s41598-022-22878-7
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author Heba M. Hashem
Amira Motawea
Ayman H. Kamel
E. M. Abdel Bary
Saad S. M. Hassan
author_facet Heba M. Hashem
Amira Motawea
Ayman H. Kamel
E. M. Abdel Bary
Saad S. M. Hassan
author_sort Heba M. Hashem
collection DOAJ
description Abstract Recently, drug-controlled release nanotechnology has gained special attention in biomedicine. This work focuses on developing novel electrospun polymeric nanofibers (NFs) for buccal delivery of VEN to avoid the hepatic metabolism and enzymatic degradation in the GIT and develop an effective control of drug release. The optimized NFs were obtained by blending polylactic acid (PLA), and poly (ɛ-caprolactone) (PCL) fixed at a ratio of 1:1. It was characterized for morphology, drug-loading, FTIR, XRD, DSC, and in vitro drug release. Ex vivo permeability of the blend NFs was assessed using chicken pouch mucosa compared to VEN suspension, followed by histopathological examination. Further, the cytotoxic effect in three different cell lines using WST-1 assay. SEM morphologies refer to defect-free uniform NFs of PLA, PCL, and PLA/PCL mats. These fibers had a diameter ranging from 200 to 500 nm. The physico-thermal characterization of NFs depicted that the drug was successfully loaded and in an amorphous state in the PLA/PCL NFs. In vitro release of NFs substantiated a bi-phasic profile with an initial burst release of about 30% in the initial 0.5 h and a prolonged cumulative release pattern that reached 80% over 96 h following a non-Fickian diffusion mechanism. Ex vivo permeation emphasizes the major enhancement of the sustained drug release and the noticeable decrease in the permeability of the drug from NFs. Cytotoxicity data found that IC50 of VEN alone was 217.55 μg/mL, then VEN-NFs recorded an IC50 value of 250.62 μg/mL, and plain NFs showed the lowest toxicity and IC50 440.48 μg/mL in oral epithelial cells (OEC). Histopathology and cell toxicity studies demonstrated the preserved mucosal architecture and the preclinical safety. The developed PLA/PCL NFs can be promising drug carriers to introduce a step-change in improved psychiatric treatment healthcare.
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spelling doaj.art-1abcf925b08843599ba5a25ad452e5652022-12-22T03:22:31ZengNature PortfolioScientific Reports2045-23222022-10-0112111610.1038/s41598-022-22878-7Fabrication and characterization of electrospun nanofibers using biocompatible polymers for the sustained release of venlafaxineHeba M. Hashem0Amira Motawea1Ayman H. Kamel2E. M. Abdel Bary3Saad S. M. Hassan4Pharmaceutical Analytical Chemistry Department, Faculty of Pharmacy, Mansoura UniversityPharmaceutics Department, Faculty of Pharmacy, Mansoura UniversityChemistry Department, Faculty of Science, Ain Shams UniversityChemistry Department, Faculty of Science, Mansoura UniversityChemistry Department, Faculty of Science, Ain Shams UniversityAbstract Recently, drug-controlled release nanotechnology has gained special attention in biomedicine. This work focuses on developing novel electrospun polymeric nanofibers (NFs) for buccal delivery of VEN to avoid the hepatic metabolism and enzymatic degradation in the GIT and develop an effective control of drug release. The optimized NFs were obtained by blending polylactic acid (PLA), and poly (ɛ-caprolactone) (PCL) fixed at a ratio of 1:1. It was characterized for morphology, drug-loading, FTIR, XRD, DSC, and in vitro drug release. Ex vivo permeability of the blend NFs was assessed using chicken pouch mucosa compared to VEN suspension, followed by histopathological examination. Further, the cytotoxic effect in three different cell lines using WST-1 assay. SEM morphologies refer to defect-free uniform NFs of PLA, PCL, and PLA/PCL mats. These fibers had a diameter ranging from 200 to 500 nm. The physico-thermal characterization of NFs depicted that the drug was successfully loaded and in an amorphous state in the PLA/PCL NFs. In vitro release of NFs substantiated a bi-phasic profile with an initial burst release of about 30% in the initial 0.5 h and a prolonged cumulative release pattern that reached 80% over 96 h following a non-Fickian diffusion mechanism. Ex vivo permeation emphasizes the major enhancement of the sustained drug release and the noticeable decrease in the permeability of the drug from NFs. Cytotoxicity data found that IC50 of VEN alone was 217.55 μg/mL, then VEN-NFs recorded an IC50 value of 250.62 μg/mL, and plain NFs showed the lowest toxicity and IC50 440.48 μg/mL in oral epithelial cells (OEC). Histopathology and cell toxicity studies demonstrated the preserved mucosal architecture and the preclinical safety. The developed PLA/PCL NFs can be promising drug carriers to introduce a step-change in improved psychiatric treatment healthcare.https://doi.org/10.1038/s41598-022-22878-7
spellingShingle Heba M. Hashem
Amira Motawea
Ayman H. Kamel
E. M. Abdel Bary
Saad S. M. Hassan
Fabrication and characterization of electrospun nanofibers using biocompatible polymers for the sustained release of venlafaxine
Scientific Reports
title Fabrication and characterization of electrospun nanofibers using biocompatible polymers for the sustained release of venlafaxine
title_full Fabrication and characterization of electrospun nanofibers using biocompatible polymers for the sustained release of venlafaxine
title_fullStr Fabrication and characterization of electrospun nanofibers using biocompatible polymers for the sustained release of venlafaxine
title_full_unstemmed Fabrication and characterization of electrospun nanofibers using biocompatible polymers for the sustained release of venlafaxine
title_short Fabrication and characterization of electrospun nanofibers using biocompatible polymers for the sustained release of venlafaxine
title_sort fabrication and characterization of electrospun nanofibers using biocompatible polymers for the sustained release of venlafaxine
url https://doi.org/10.1038/s41598-022-22878-7
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