Development and Optimization of Luliconazole Spanlastics to Augment the Antifungal Activity against <i>Candida albicans</i>
Luliconazole is a new topical imidazole antifungal drug for the treatment of skin infections. It has low solubility and poor skin penetration which limits its therapeutic applications. In order to improve its therapeutic efficacy, spanlastics nanoformulation was developed and optimized using a combi...
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MDPI AG
2021-06-01
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| Online Access: | https://www.mdpi.com/1999-4923/13/7/977 |
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| author | Nabil A. Alhakamy Mohammed W. Al-Rabia Shadab Md Alaa Sirwi Selwan Saud Khayat Sahar Saad AlOtaibi Raghad Abkar Hakami Hadeel Al Sadoun Basmah Medhat Eldakhakhny Wesam H. Abdulaal Hibah M. Aldawsari Shaimaa M. Badr-Eldin Mahmoud A. Elfaky |
| author_facet | Nabil A. Alhakamy Mohammed W. Al-Rabia Shadab Md Alaa Sirwi Selwan Saud Khayat Sahar Saad AlOtaibi Raghad Abkar Hakami Hadeel Al Sadoun Basmah Medhat Eldakhakhny Wesam H. Abdulaal Hibah M. Aldawsari Shaimaa M. Badr-Eldin Mahmoud A. Elfaky |
| author_sort | Nabil A. Alhakamy |
| collection | DOAJ |
| description | Luliconazole is a new topical imidazole antifungal drug for the treatment of skin infections. It has low solubility and poor skin penetration which limits its therapeutic applications. In order to improve its therapeutic efficacy, spanlastics nanoformulation was developed and optimized using a combined mixture-process variable design (CMPV). The optimized formulation was converted into a hydrogel formula to enhance skin penetration and increase the efficacy in experimental cutaneous <i>Candida albicans</i> infections in Swiss mice wounds. The optimized formulation was generated at percentages of Span and Tween of 48% and 52%, respectively, and a sonication time of 6.6 min. The software predicted that the proposed formulation would achieve a particle size of 50 nm with a desirability of 0.997. The entrapment of luliconazole within the spanlastics carrier showed significant (<i>p</i> < 0.0001) antifungal efficacy in the immunocompromised Candida-infected Swiss mice without causing any irritation, when compared to the luliconazole treated groups. The microscopic observation showed almost complete removal of the fungal colonies on the skin of the infected animals (0.2 ± 0.05 log CFU), whereas the control animals had 0.2 ± 0.05 log CFU. Therefore, luliconazole spanlastics could be an effective formulation with improved topical delivery for antifungal activity against <i>C. albicans</i>. |
| first_indexed | 2024-03-09T04:46:33Z |
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| id | doaj.art-10eecbfbfb1840cba618ff57c6a4f676 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-09T04:46:33Z |
| publishDate | 2021-06-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-10eecbfbfb1840cba618ff57c6a4f6762023-12-03T13:14:56ZengMDPI AGPharmaceutics1999-49232021-06-0113797710.3390/pharmaceutics13070977Development and Optimization of Luliconazole Spanlastics to Augment the Antifungal Activity against <i>Candida albicans</i>Nabil A. Alhakamy0Mohammed W. Al-Rabia1Shadab Md2Alaa Sirwi3Selwan Saud Khayat4Sahar Saad AlOtaibi5Raghad Abkar Hakami6Hadeel Al Sadoun7Basmah Medhat Eldakhakhny8Wesam H. Abdulaal9Hibah M. Aldawsari10Shaimaa M. Badr-Eldin11Mahmoud A. Elfaky12Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi ArabiaDepartment of Medical Microbiology and Parasitology, Faculty of Medicine, King Abdulaziz Universit, Jeddah 21589, Saudi ArabiaDepartment of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi ArabiaDepartment of Natural Products and Alternative, Medicine, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi ArabiaDepartment of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi ArabiaDepartment of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi ArabiaDepartment of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi ArabiaDepartment of Medical Laboratory Technology, Faculty of Applied Medical Sciences, King Fahd Medical Research Center, King Abdulaziz University, Jeddah 21589, Saudi ArabiaDepartment of Clinical Biochemistry, Faculty of Medicine, King Abdulaziz University, Jeddah 21589, Saudi ArabiaDepartment of Biochemistry, Faculty of Science, Cancer and Mutagenesis Unit, King Fahd Medical Research Center, King Abdulaziz University, Jeddah 21589, Saudi ArabiaDepartment of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi ArabiaDepartment of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi ArabiaDepartment of Natural Products and Alternative, Medicine, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi ArabiaLuliconazole is a new topical imidazole antifungal drug for the treatment of skin infections. It has low solubility and poor skin penetration which limits its therapeutic applications. In order to improve its therapeutic efficacy, spanlastics nanoformulation was developed and optimized using a combined mixture-process variable design (CMPV). The optimized formulation was converted into a hydrogel formula to enhance skin penetration and increase the efficacy in experimental cutaneous <i>Candida albicans</i> infections in Swiss mice wounds. The optimized formulation was generated at percentages of Span and Tween of 48% and 52%, respectively, and a sonication time of 6.6 min. The software predicted that the proposed formulation would achieve a particle size of 50 nm with a desirability of 0.997. The entrapment of luliconazole within the spanlastics carrier showed significant (<i>p</i> < 0.0001) antifungal efficacy in the immunocompromised Candida-infected Swiss mice without causing any irritation, when compared to the luliconazole treated groups. The microscopic observation showed almost complete removal of the fungal colonies on the skin of the infected animals (0.2 ± 0.05 log CFU), whereas the control animals had 0.2 ± 0.05 log CFU. Therefore, luliconazole spanlastics could be an effective formulation with improved topical delivery for antifungal activity against <i>C. albicans</i>.https://www.mdpi.com/1999-4923/13/7/977luliconazolespanlasticsparticle size<i>Candida albicans</i> infectionslesion score |
| spellingShingle | Nabil A. Alhakamy Mohammed W. Al-Rabia Shadab Md Alaa Sirwi Selwan Saud Khayat Sahar Saad AlOtaibi Raghad Abkar Hakami Hadeel Al Sadoun Basmah Medhat Eldakhakhny Wesam H. Abdulaal Hibah M. Aldawsari Shaimaa M. Badr-Eldin Mahmoud A. Elfaky Development and Optimization of Luliconazole Spanlastics to Augment the Antifungal Activity against <i>Candida albicans</i> Pharmaceutics luliconazole spanlastics particle size <i>Candida albicans</i> infections lesion score |
| title | Development and Optimization of Luliconazole Spanlastics to Augment the Antifungal Activity against <i>Candida albicans</i> |
| title_full | Development and Optimization of Luliconazole Spanlastics to Augment the Antifungal Activity against <i>Candida albicans</i> |
| title_fullStr | Development and Optimization of Luliconazole Spanlastics to Augment the Antifungal Activity against <i>Candida albicans</i> |
| title_full_unstemmed | Development and Optimization of Luliconazole Spanlastics to Augment the Antifungal Activity against <i>Candida albicans</i> |
| title_short | Development and Optimization of Luliconazole Spanlastics to Augment the Antifungal Activity against <i>Candida albicans</i> |
| title_sort | development and optimization of luliconazole spanlastics to augment the antifungal activity against i candida albicans i |
| topic | luliconazole spanlastics particle size <i>Candida albicans</i> infections lesion score |
| url | https://www.mdpi.com/1999-4923/13/7/977 |
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