Fabrication and Evaluation of Voriconazole Loaded Transethosomal Gel for Enhanced Antifungal and Antileishmanial Activity
Voriconazole (VRC) is a broad-spectrum antifungal agent belonging to BCS class II (biopharmaceutical classification system). Despite many efforts to enhance its solubility, this primary issue still remains challenging for formulation scientists. Transethosomes (TELs) are one of the potential innovat...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-05-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/27/10/3347 |
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| author | Mudassir Farooq Faisal Usman Sumera Zaib Hamid Saeed Shah Qazi Adnan Jamil Fatima Akbar Sheikh Ajmal Khan Sameh Rabea Soheir A. A. Hagras Gaber El-Saber Batiha Imtiaz Khan |
| author_facet | Mudassir Farooq Faisal Usman Sumera Zaib Hamid Saeed Shah Qazi Adnan Jamil Fatima Akbar Sheikh Ajmal Khan Sameh Rabea Soheir A. A. Hagras Gaber El-Saber Batiha Imtiaz Khan |
| author_sort | Mudassir Farooq |
| collection | DOAJ |
| description | Voriconazole (VRC) is a broad-spectrum antifungal agent belonging to BCS class II (biopharmaceutical classification system). Despite many efforts to enhance its solubility, this primary issue still remains challenging for formulation scientists. Transethosomes (TELs) are one of the potential innovative nano-carriers for improving the solubility and permeation of poorly soluble and permeable drugs. We herein report voriconazole-loaded transethosomes (VRCT) fabricated by the cold method and followed by their incorporation into carbopol 940 as a gel. The prepared VRCT were evaluated for % yield, % entrapment efficiency (EE), surface morphology, possible chemical interaction, particle size, zeta potential, and polydispersity index (PDI). The optimized formulation had a particle size of 228.2 nm, a zeta potential of −26.5 mV, and a PDI of 0.45 with enhanced % EE. Rheology, spreadability, extrudability, in vitro release, skin permeation, molecular docking, antifungal, and antileishmanial activity were also assessed for VRCT and VRC loaded transethosomal gel (VTEG). Ex-vivo permeation using rat skin depicted a transdermal flux of 22.8 µg/cm<sup>2</sup>/h with enhanced efficiency up to 4-fold. A two-fold reduction in inhibitory as well as fungicidal concentration was observed against various fungal strains by VRCT and VTEG besides similar results against L-donovani. The development of transethosomal formulation can serve as an efficient drug delivery system through a topical route with enhanced efficacy and better patient compliance. |
| first_indexed | 2024-03-10T03:17:53Z |
| format | Article |
| id | doaj.art-5ade3ba0fc0d4563962978b632564f38 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T03:17:53Z |
| publishDate | 2022-05-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-5ade3ba0fc0d4563962978b632564f382023-11-23T12:25:01ZengMDPI AGMolecules1420-30492022-05-012710334710.3390/molecules27103347Fabrication and Evaluation of Voriconazole Loaded Transethosomal Gel for Enhanced Antifungal and Antileishmanial ActivityMudassir Farooq0Faisal Usman1Sumera Zaib2Hamid Saeed Shah3Qazi Adnan Jamil4Fatima Akbar Sheikh5Ajmal Khan6Sameh Rabea7Soheir A. A. Hagras8Gaber El-Saber Batiha9Imtiaz Khan10Department of Pharmaceutics, Faculty of Pharmacy, Bahauddin Zakariya University, Multan 66000, PakistanDepartment of Pharmaceutics, Faculty of Pharmacy, Bahauddin Zakariya University, Multan 66000, PakistanDepartment of Biochemistry, Faculty of Life Sciences, University of Central Punjab, Lahore 54590, PakistanInstitute of Pharmaceutical Sciences, University of Veterinary and Animal Sciences, Lahore 54000, PakistanDepartment of Pharmaceutics, Faculty of Pharmacy, The Islamia University of Bahawapur, Bahawalpur 66000, PakistanAl-Raziq College of Pharmacy, Sargodha 40100, PakistanNatural and Medical Sciences Research Center, University of Nizwa, Nizwa 616, OmanDepartment of Pharmaceutical Sciences, College of Pharmacy, AlMaarefa University, Diriyah, Riyadh 13713, Saudi ArabiaDepartment of Clinical Laboratory Sciences, Inaya Medical Colleges, Riyadh 11352, Saudi ArabiaDepartment of Pharmacology and Therapeutics, Faculty of Veterinary Medicine, Damanhour University, Damanhour 22511, Albeheira, EgyptDepartment of Chemistry and Manchester Institute of Biotechnology, The University of Manchester, 131 Princess Street, Manchester M1 7DN, UKVoriconazole (VRC) is a broad-spectrum antifungal agent belonging to BCS class II (biopharmaceutical classification system). Despite many efforts to enhance its solubility, this primary issue still remains challenging for formulation scientists. Transethosomes (TELs) are one of the potential innovative nano-carriers for improving the solubility and permeation of poorly soluble and permeable drugs. We herein report voriconazole-loaded transethosomes (VRCT) fabricated by the cold method and followed by their incorporation into carbopol 940 as a gel. The prepared VRCT were evaluated for % yield, % entrapment efficiency (EE), surface morphology, possible chemical interaction, particle size, zeta potential, and polydispersity index (PDI). The optimized formulation had a particle size of 228.2 nm, a zeta potential of −26.5 mV, and a PDI of 0.45 with enhanced % EE. Rheology, spreadability, extrudability, in vitro release, skin permeation, molecular docking, antifungal, and antileishmanial activity were also assessed for VRCT and VRC loaded transethosomal gel (VTEG). Ex-vivo permeation using rat skin depicted a transdermal flux of 22.8 µg/cm<sup>2</sup>/h with enhanced efficiency up to 4-fold. A two-fold reduction in inhibitory as well as fungicidal concentration was observed against various fungal strains by VRCT and VTEG besides similar results against L-donovani. The development of transethosomal formulation can serve as an efficient drug delivery system through a topical route with enhanced efficacy and better patient compliance.https://www.mdpi.com/1420-3049/27/10/3347fungal infectionleishmaniasisphospholipidstransethosomestransethosomal gelvoriconazole |
| spellingShingle | Mudassir Farooq Faisal Usman Sumera Zaib Hamid Saeed Shah Qazi Adnan Jamil Fatima Akbar Sheikh Ajmal Khan Sameh Rabea Soheir A. A. Hagras Gaber El-Saber Batiha Imtiaz Khan Fabrication and Evaluation of Voriconazole Loaded Transethosomal Gel for Enhanced Antifungal and Antileishmanial Activity Molecules fungal infection leishmaniasis phospholipids transethosomes transethosomal gel voriconazole |
| title | Fabrication and Evaluation of Voriconazole Loaded Transethosomal Gel for Enhanced Antifungal and Antileishmanial Activity |
| title_full | Fabrication and Evaluation of Voriconazole Loaded Transethosomal Gel for Enhanced Antifungal and Antileishmanial Activity |
| title_fullStr | Fabrication and Evaluation of Voriconazole Loaded Transethosomal Gel for Enhanced Antifungal and Antileishmanial Activity |
| title_full_unstemmed | Fabrication and Evaluation of Voriconazole Loaded Transethosomal Gel for Enhanced Antifungal and Antileishmanial Activity |
| title_short | Fabrication and Evaluation of Voriconazole Loaded Transethosomal Gel for Enhanced Antifungal and Antileishmanial Activity |
| title_sort | fabrication and evaluation of voriconazole loaded transethosomal gel for enhanced antifungal and antileishmanial activity |
| topic | fungal infection leishmaniasis phospholipids transethosomes transethosomal gel voriconazole |
| url | https://www.mdpi.com/1420-3049/27/10/3347 |
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