Binary ethosomes for the enhanced topical delivery and antifungal efficacy of ketoconazole
This work aimed to prepare ketoconazole-loaded ethosomes and binary ethosomes to improve its skin delivery and antifungal efficacy. A 32 factorial design was used to optimize the ethosomes and formulate ketoconazole-loaded binary ethosomes. Ethosomes and binary ethosomes were evaluated for particle...
| Main Authors: | , , , , , , |
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| Format: | Article |
| Language: | English |
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Elsevier
2023-05-01
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| Series: | OpenNano |
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S2352952023000245 |
| _version_ | 1797837778437799936 |
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| author | Alhanouf A. Aljohani Maryam A. Alanazi Lujain A. Munahhi Jawaher D. Hamroon Yasmin Mortagi Mona Qushawy Ghareb M. Soliman |
| author_facet | Alhanouf A. Aljohani Maryam A. Alanazi Lujain A. Munahhi Jawaher D. Hamroon Yasmin Mortagi Mona Qushawy Ghareb M. Soliman |
| author_sort | Alhanouf A. Aljohani |
| collection | DOAJ |
| description | This work aimed to prepare ketoconazole-loaded ethosomes and binary ethosomes to improve its skin delivery and antifungal efficacy. A 32 factorial design was used to optimize the ethosomes and formulate ketoconazole-loaded binary ethosomes. Ethosomes and binary ethosomes were evaluated for particle size, polydispersity index, zeta potential, percent drug entrapment efficiency, drug release, skin permeation and deposition and antifungal efficacy. The ethosomes particle size ranged from 78.99±16.72 to 321.53±10.41 nm and decreased by increasing phospholipid and ethanol concentrations. The polydispersity index values were in the range of 0.17±0.01 to 0.49 ± 0.04. The percent drug entrapment efficiency ranged from 36.09±2.66 to 95.89±0.19 and increased by increasing phospholipid concentration while ethanol concentration had the opposite effect. The binary ethosomes had smaller size but similar drug entrapment efficiency and zeta potential compared with the ethosomes. They had significantly higher percent drug release (∼96%) and permeation (∼95%) through rat skin compared with the ethosomes (93% and 90%, respectively). Binary ethosomes and ethosomes had, respectively 1.9 and 1.8-fold higher drug skin permeation and 5.3- and 5.6-fold higher drug deposition in the epidermis/dermis compared with the drug suspension. The antifungal efficacy of the drug-loaded ethosomes and binary ethosomes were similar to the drug hydroalcoholic solution. Collectively, these results confirm the potential of these nanocarriers to enhance drug efficacy given their small size, sustained drug release and enhanced skin permeability. |
| first_indexed | 2024-04-09T15:30:10Z |
| format | Article |
| id | doaj.art-712d7df4cce142b38568960f9cb63a20 |
| institution | Directory Open Access Journal |
| issn | 2352-9520 |
| language | English |
| last_indexed | 2024-04-09T15:30:10Z |
| publishDate | 2023-05-01 |
| publisher | Elsevier |
| record_format | Article |
| series | OpenNano |
| spelling | doaj.art-712d7df4cce142b38568960f9cb63a202023-04-28T08:55:51ZengElsevierOpenNano2352-95202023-05-0111100145Binary ethosomes for the enhanced topical delivery and antifungal efficacy of ketoconazoleAlhanouf A. Aljohani0Maryam A. Alanazi1Lujain A. Munahhi2Jawaher D. Hamroon3Yasmin Mortagi4Mona Qushawy5Ghareb M. Soliman6PharmD Program, Faculty of Pharmacy, University of Tabuk, Tabuk, Saudi ArabiaPharmD Program, Faculty of Pharmacy, University of Tabuk, Tabuk, Saudi ArabiaPharmD Program, Faculty of Pharmacy, University of Tabuk, Tabuk, Saudi ArabiaPharmD Program, Faculty of Pharmacy, University of Tabuk, Tabuk, Saudi ArabiaDepartment of Pharmaceutics, Faculty of Pharmacy, Sinai University, Alarish, North Sinai, EgyptDepartment of Pharmaceutics, Faculty of Pharmacy, Sinai University, Alarish, North Sinai, Egypt; Department of Pharmaceutics, Faculty of Pharmacy, University of Tabuk, Tabuk, Saudi ArabiaDepartment of Pharmaceutics, Faculty of Pharmacy, University of Tabuk, Tabuk, Saudi Arabia; Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt; Corresponding author.This work aimed to prepare ketoconazole-loaded ethosomes and binary ethosomes to improve its skin delivery and antifungal efficacy. A 32 factorial design was used to optimize the ethosomes and formulate ketoconazole-loaded binary ethosomes. Ethosomes and binary ethosomes were evaluated for particle size, polydispersity index, zeta potential, percent drug entrapment efficiency, drug release, skin permeation and deposition and antifungal efficacy. The ethosomes particle size ranged from 78.99±16.72 to 321.53±10.41 nm and decreased by increasing phospholipid and ethanol concentrations. The polydispersity index values were in the range of 0.17±0.01 to 0.49 ± 0.04. The percent drug entrapment efficiency ranged from 36.09±2.66 to 95.89±0.19 and increased by increasing phospholipid concentration while ethanol concentration had the opposite effect. The binary ethosomes had smaller size but similar drug entrapment efficiency and zeta potential compared with the ethosomes. They had significantly higher percent drug release (∼96%) and permeation (∼95%) through rat skin compared with the ethosomes (93% and 90%, respectively). Binary ethosomes and ethosomes had, respectively 1.9 and 1.8-fold higher drug skin permeation and 5.3- and 5.6-fold higher drug deposition in the epidermis/dermis compared with the drug suspension. The antifungal efficacy of the drug-loaded ethosomes and binary ethosomes were similar to the drug hydroalcoholic solution. Collectively, these results confirm the potential of these nanocarriers to enhance drug efficacy given their small size, sustained drug release and enhanced skin permeability.http://www.sciencedirect.com/science/article/pii/S2352952023000245KetoconazoleFungal infectionsBinary ethosomesEthosomesTopical drug delivery |
| spellingShingle | Alhanouf A. Aljohani Maryam A. Alanazi Lujain A. Munahhi Jawaher D. Hamroon Yasmin Mortagi Mona Qushawy Ghareb M. Soliman Binary ethosomes for the enhanced topical delivery and antifungal efficacy of ketoconazole OpenNano Ketoconazole Fungal infections Binary ethosomes Ethosomes Topical drug delivery |
| title | Binary ethosomes for the enhanced topical delivery and antifungal efficacy of ketoconazole |
| title_full | Binary ethosomes for the enhanced topical delivery and antifungal efficacy of ketoconazole |
| title_fullStr | Binary ethosomes for the enhanced topical delivery and antifungal efficacy of ketoconazole |
| title_full_unstemmed | Binary ethosomes for the enhanced topical delivery and antifungal efficacy of ketoconazole |
| title_short | Binary ethosomes for the enhanced topical delivery and antifungal efficacy of ketoconazole |
| title_sort | binary ethosomes for the enhanced topical delivery and antifungal efficacy of ketoconazole |
| topic | Ketoconazole Fungal infections Binary ethosomes Ethosomes Topical drug delivery |
| url | http://www.sciencedirect.com/science/article/pii/S2352952023000245 |
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