Production, Characterization, and In Vitro Antifungal Evaluation of Itraconazole-Loaded Fibrous Sheets Prepared by Electrospinning with a Factorial Design

Itraconazole (ITZ) is a broad-spectrum triazole antifungal agent suitable for the treatment of superficial and systemic mycoses. This study aimed to formulate, characterize, and evaluate the in vitro antifungal performance of single-jet electrospun itraconazole-loaded polyvinylpyrrolidone-based fibe...

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Main Authors: Emőke-Margit Rédai, Orsolya Péterfi, Attila Levente Gergely, Enikő Barabás, Andrada Pintea, Paula Antonoaea, Robert-Alexandru Vlad, Nicoleta Todoran, Cornelia-Titiana Cotoi, Adriana Ciurba, Emese Sipos
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Language:English
Published: MDPI AG 2025-01-01
Series:Applied Sciences
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Online Access:https://www.mdpi.com/2076-3417/15/2/710
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author Emőke-Margit Rédai
Orsolya Péterfi
Attila Levente Gergely
Enikő Barabás
Andrada Pintea
Paula Antonoaea
Robert-Alexandru Vlad
Nicoleta Todoran
Cornelia-Titiana Cotoi
Adriana Ciurba
Emese Sipos
author_facet Emőke-Margit Rédai
Orsolya Péterfi
Attila Levente Gergely
Enikő Barabás
Andrada Pintea
Paula Antonoaea
Robert-Alexandru Vlad
Nicoleta Todoran
Cornelia-Titiana Cotoi
Adriana Ciurba
Emese Sipos
author_sort Emőke-Margit Rédai
collection DOAJ
description Itraconazole (ITZ) is a broad-spectrum triazole antifungal agent suitable for the treatment of superficial and systemic mycoses. This study aimed to formulate, characterize, and evaluate the in vitro antifungal performance of single-jet electrospun itraconazole-loaded polyvinylpyrrolidone-based fibers. Fibrous mats were prepared under the following experimental conditions: 10, 12.5, and 15 cm needle–collector distance, 20 kV tension, and 1, 1.5, and 2 mL/hour flow rate. The fibers were characterized by SEM, DSC, FTIR, assays, disintegration tests, dissolution tests, and in vitro antifungal activity. Using a 2<sup>2</sup> factorial design, the effects of preparation variables on the characteristics of the fibrous sheets were described. The electrospinning process led to smooth-surfaced, randomly oriented, and bead-free fibers. The average fiber diameter ranged from 887 nm to 1175 nm. The scanning calorimetry of pure ITZ revealed a sharp endothermic melting point at a temperature of 170 °C, not present in the curves of the fibers. After 60 min, between 70 and 100% of ITZ was released. The antifungal assay revealed that the fibers inhibited the growth of <i>Candida albicans</i> and <i>Candida parapyilosis</i>. The obtained fiber mats prepared from the hydrophilic polymer presented almost instantaneous disintegration, with potential applications for rapid antifungal delivery in oral or topical pharmaceutical form.
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spelling doaj-art-e928f95fd5024a8d8122cbbae525937e2025-01-24T13:20:33ZengMDPI AGApplied Sciences2076-34172025-01-0115271010.3390/app15020710Production, Characterization, and In Vitro Antifungal Evaluation of Itraconazole-Loaded Fibrous Sheets Prepared by Electrospinning with a Factorial DesignEmőke-Margit Rédai0Orsolya Péterfi1Attila Levente Gergely2Enikő Barabás3Andrada Pintea4Paula Antonoaea5Robert-Alexandru Vlad6Nicoleta Todoran7Cornelia-Titiana Cotoi8Adriana Ciurba9Emese Sipos10Department of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, George Emil Palade University of Medicine, Pharmacy, Science, and Technology of Targu Mures, 540142 Targu Mures, RomaniaDepartment of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, George Emil Palade University of Medicine, Pharmacy, Science, and Technology of Targu Mures, 540142 Targu Mures, RomaniaDepartment of Mechanical Engineering, Faculty of Technical and Human Sciences, Sapientia Hungarian University of Transylvania, Calea Sighisoarei nr. 2., 540485 Targu Mures, RomaniaDepartment of Cellular Biology and Microbiology, Faculty of Pharmacy, George Emil Palade University of Medicine, Pharmacy, Science, and Technology of Targu Mures, 540142 Targu Mures, RomaniaDepartment of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, George Emil Palade University of Medicine, Pharmacy, Science, and Technology of Targu Mures, 540142 Targu Mures, RomaniaDepartment of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, George Emil Palade University of Medicine, Pharmacy, Science, and Technology of Targu Mures, 540142 Targu Mures, RomaniaDepartment of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, George Emil Palade University of Medicine, Pharmacy, Science, and Technology of Targu Mures, 540142 Targu Mures, RomaniaDepartment of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, George Emil Palade University of Medicine, Pharmacy, Science, and Technology of Targu Mures, 540142 Targu Mures, RomaniaDepartment of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, George Emil Palade University of Medicine, Pharmacy, Science, and Technology of Targu Mures, 540142 Targu Mures, RomaniaDepartment of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, George Emil Palade University of Medicine, Pharmacy, Science, and Technology of Targu Mures, 540142 Targu Mures, RomaniaDepartment of Industrial Pharmacy and Management, Faculty of Pharmacy, George Emil Palade University of Medicine, Pharmacy, Science, and Technology of Targu Mures, 540142 Targu Mures, RomaniaItraconazole (ITZ) is a broad-spectrum triazole antifungal agent suitable for the treatment of superficial and systemic mycoses. This study aimed to formulate, characterize, and evaluate the in vitro antifungal performance of single-jet electrospun itraconazole-loaded polyvinylpyrrolidone-based fibers. Fibrous mats were prepared under the following experimental conditions: 10, 12.5, and 15 cm needle–collector distance, 20 kV tension, and 1, 1.5, and 2 mL/hour flow rate. The fibers were characterized by SEM, DSC, FTIR, assays, disintegration tests, dissolution tests, and in vitro antifungal activity. Using a 2<sup>2</sup> factorial design, the effects of preparation variables on the characteristics of the fibrous sheets were described. The electrospinning process led to smooth-surfaced, randomly oriented, and bead-free fibers. The average fiber diameter ranged from 887 nm to 1175 nm. The scanning calorimetry of pure ITZ revealed a sharp endothermic melting point at a temperature of 170 °C, not present in the curves of the fibers. After 60 min, between 70 and 100% of ITZ was released. The antifungal assay revealed that the fibers inhibited the growth of <i>Candida albicans</i> and <i>Candida parapyilosis</i>. The obtained fiber mats prepared from the hydrophilic polymer presented almost instantaneous disintegration, with potential applications for rapid antifungal delivery in oral or topical pharmaceutical form.https://www.mdpi.com/2076-3417/15/2/710polyvinylpyrrolidoneitraconazolefibrous sheetsantifungaldissolution
spellingShingle Emőke-Margit Rédai
Orsolya Péterfi
Attila Levente Gergely
Enikő Barabás
Andrada Pintea
Paula Antonoaea
Robert-Alexandru Vlad
Nicoleta Todoran
Cornelia-Titiana Cotoi
Adriana Ciurba
Emese Sipos
Production, Characterization, and In Vitro Antifungal Evaluation of Itraconazole-Loaded Fibrous Sheets Prepared by Electrospinning with a Factorial Design
Applied Sciences
polyvinylpyrrolidone
itraconazole
fibrous sheets
antifungal
dissolution
title Production, Characterization, and In Vitro Antifungal Evaluation of Itraconazole-Loaded Fibrous Sheets Prepared by Electrospinning with a Factorial Design
title_full Production, Characterization, and In Vitro Antifungal Evaluation of Itraconazole-Loaded Fibrous Sheets Prepared by Electrospinning with a Factorial Design
title_fullStr Production, Characterization, and In Vitro Antifungal Evaluation of Itraconazole-Loaded Fibrous Sheets Prepared by Electrospinning with a Factorial Design
title_full_unstemmed Production, Characterization, and In Vitro Antifungal Evaluation of Itraconazole-Loaded Fibrous Sheets Prepared by Electrospinning with a Factorial Design
title_short Production, Characterization, and In Vitro Antifungal Evaluation of Itraconazole-Loaded Fibrous Sheets Prepared by Electrospinning with a Factorial Design
title_sort production characterization and in vitro antifungal evaluation of itraconazole loaded fibrous sheets prepared by electrospinning with a factorial design
topic polyvinylpyrrolidone
itraconazole
fibrous sheets
antifungal
dissolution
url https://www.mdpi.com/2076-3417/15/2/710
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