Formulation and Evaluation of Topical Nano-Lipid-Based Delivery of Butenafine: In Vitro Characterization and Antifungal Activity
The present research work was designed to prepare butenafine (BN)-loaded bilosomes (BSs) by the thin-film hydration method. BN is a sparingly water-soluble drug having low permeability and bioavailability. BSs are lipid-based nanovesicles used to entrap water-insoluble drugs for enhanced permeation...
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MDPI AG
2022-02-01
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| Online Access: | https://www.mdpi.com/2310-2861/8/2/133 |
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| author | Ameeduzzafar Zafar Syed Sarim Imam Nabil K. Alruwaili Mohd Yasir Omar Awad Alsaidan Sultan Alshehri Mohammed M. Ghoneim Mohammad Khalid Ali Alquraini Salman S. Alharthi |
| author_facet | Ameeduzzafar Zafar Syed Sarim Imam Nabil K. Alruwaili Mohd Yasir Omar Awad Alsaidan Sultan Alshehri Mohammed M. Ghoneim Mohammad Khalid Ali Alquraini Salman S. Alharthi |
| author_sort | Ameeduzzafar Zafar |
| collection | DOAJ |
| description | The present research work was designed to prepare butenafine (BN)-loaded bilosomes (BSs) by the thin-film hydration method. BN is a sparingly water-soluble drug having low permeability and bioavailability. BSs are lipid-based nanovesicles used to entrap water-insoluble drugs for enhanced permeation across the skin. BSs were prepared by the thin-film hydration method and optimized by the Box–Behnken design (BBD) using lipid (A), span 60 (B), and sodium deoxycholate (C) as independent variables. The selected formulation (BN-BSo) was converted into the gel using Carbopol 940 as a gelling agent. The prepared optimized gel (BN-BS-og) was further evaluated for the gel characterization, drug release, drug permeation, irritation, and anti-fungal study. The optimized bilosomes (BN-BSo) showed a mean vesicle size of 215 ± 6.5 nm and an entrapment efficiency of 89.2 ± 1.5%. The DSC study showed that BN was completely encapsulated in the BS lipid matrix. BN-BSog showed good viscosity, consistency, spreadability, and pH. A significantly (<i>p</i> < 0.05) high release (81.09 ± 4.01%) was achieved from BN-BSo compared to BN-BSog (65.85 ± 4.87%) and pure BN (17.54 ± 1.37 %). The permeation study results revealed that BN-BSo, BN-BSog, and pure BN exhibited 56.2 ± 2.7%, 39.2 ± 2.9%, and 16.6 ± 2.3%. The enhancement ratio of permeation flux was found to be 1.4-fold and 3.4-fold for the BN-BS-og and pure BN dispersion. The HET-CAM study showed that BN-BSog was found to be nonirritant as the score was found within the limit. The antifungal study revealed a significant (<i>p</i> < 0.05) enhanced antifungal activity against <i>C. albicans</i> and <i>A. niger</i>. The findings of the study revealed that BS is an important drug delivery system for transdermal delivery. |
| first_indexed | 2024-03-09T21:53:55Z |
| format | Article |
| id | doaj.art-90c96e8381f94832bacfd0fac405d7c6 |
| institution | Directory Open Access Journal |
| issn | 2310-2861 |
| language | English |
| last_indexed | 2024-03-09T21:53:55Z |
| publishDate | 2022-02-01 |
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| record_format | Article |
| series | Gels |
| spelling | doaj.art-90c96e8381f94832bacfd0fac405d7c62023-11-23T20:02:22ZengMDPI AGGels2310-28612022-02-018213310.3390/gels8020133Formulation and Evaluation of Topical Nano-Lipid-Based Delivery of Butenafine: In Vitro Characterization and Antifungal ActivityAmeeduzzafar Zafar0Syed Sarim Imam1Nabil K. Alruwaili2Mohd Yasir3Omar Awad Alsaidan4Sultan Alshehri5Mohammed M. Ghoneim6Mohammad Khalid7Ali Alquraini8Salman S. Alharthi9Department of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka 72341, Al-Jouf, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka 72341, Al-Jouf, Saudi ArabiaDepartment of Pharmacy, College of Health Science, Arsi University, Asella 396, EthiopiaDepartment of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka 72341, Al-Jouf, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaDepartment of Pharmacy Practice, College of Pharmacy, Almaarefa University, Ad Diriyah 13713, Saudi ArabiaDepartment of Pharmacognosy, College of Pharmacy, Prince Sattam Bin Abdulaziz University, P.O. Box 173, Al-Kharj 11942, Saudi ArabiaDepartment of Pharmaceutical Chemistry, Faculty of Clinical Pharmacy, Al Baha University, Al Baha 65779, Saudi ArabiaDepartment of Pharmacy, Security Forces Hospital Program, Riyadh 11481, Saudi ArabiaThe present research work was designed to prepare butenafine (BN)-loaded bilosomes (BSs) by the thin-film hydration method. BN is a sparingly water-soluble drug having low permeability and bioavailability. BSs are lipid-based nanovesicles used to entrap water-insoluble drugs for enhanced permeation across the skin. BSs were prepared by the thin-film hydration method and optimized by the Box–Behnken design (BBD) using lipid (A), span 60 (B), and sodium deoxycholate (C) as independent variables. The selected formulation (BN-BSo) was converted into the gel using Carbopol 940 as a gelling agent. The prepared optimized gel (BN-BS-og) was further evaluated for the gel characterization, drug release, drug permeation, irritation, and anti-fungal study. The optimized bilosomes (BN-BSo) showed a mean vesicle size of 215 ± 6.5 nm and an entrapment efficiency of 89.2 ± 1.5%. The DSC study showed that BN was completely encapsulated in the BS lipid matrix. BN-BSog showed good viscosity, consistency, spreadability, and pH. A significantly (<i>p</i> < 0.05) high release (81.09 ± 4.01%) was achieved from BN-BSo compared to BN-BSog (65.85 ± 4.87%) and pure BN (17.54 ± 1.37 %). The permeation study results revealed that BN-BSo, BN-BSog, and pure BN exhibited 56.2 ± 2.7%, 39.2 ± 2.9%, and 16.6 ± 2.3%. The enhancement ratio of permeation flux was found to be 1.4-fold and 3.4-fold for the BN-BS-og and pure BN dispersion. The HET-CAM study showed that BN-BSog was found to be nonirritant as the score was found within the limit. The antifungal study revealed a significant (<i>p</i> < 0.05) enhanced antifungal activity against <i>C. albicans</i> and <i>A. niger</i>. The findings of the study revealed that BS is an important drug delivery system for transdermal delivery.https://www.mdpi.com/2310-2861/8/2/133butenafinebilosomespermeationirritation studyantifungal activity |
| spellingShingle | Ameeduzzafar Zafar Syed Sarim Imam Nabil K. Alruwaili Mohd Yasir Omar Awad Alsaidan Sultan Alshehri Mohammed M. Ghoneim Mohammad Khalid Ali Alquraini Salman S. Alharthi Formulation and Evaluation of Topical Nano-Lipid-Based Delivery of Butenafine: In Vitro Characterization and Antifungal Activity Gels butenafine bilosomes permeation irritation study antifungal activity |
| title | Formulation and Evaluation of Topical Nano-Lipid-Based Delivery of Butenafine: In Vitro Characterization and Antifungal Activity |
| title_full | Formulation and Evaluation of Topical Nano-Lipid-Based Delivery of Butenafine: In Vitro Characterization and Antifungal Activity |
| title_fullStr | Formulation and Evaluation of Topical Nano-Lipid-Based Delivery of Butenafine: In Vitro Characterization and Antifungal Activity |
| title_full_unstemmed | Formulation and Evaluation of Topical Nano-Lipid-Based Delivery of Butenafine: In Vitro Characterization and Antifungal Activity |
| title_short | Formulation and Evaluation of Topical Nano-Lipid-Based Delivery of Butenafine: In Vitro Characterization and Antifungal Activity |
| title_sort | formulation and evaluation of topical nano lipid based delivery of butenafine in vitro characterization and antifungal activity |
| topic | butenafine bilosomes permeation irritation study antifungal activity |
| url | https://www.mdpi.com/2310-2861/8/2/133 |
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