Optimized D-α-tocopherol polyethylene glycol succinate/phospholipid self-assembled mixed micelles: A promising lipid-based nanoplatform for augmenting the antifungal activity of fluconazole
Fluconazole (FLZ) is the most widely used antifungal agent for treating cutaneous candidiasis. Although oral FLZ has been proved to be effective, the incidence of side effects necessitates the development of an effective formulation that could surpass the pitfalls associated with systemic availabili...
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| Format: | Article |
| Language: | English |
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Sciendo
2022-12-01
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| Series: | Acta Pharmaceutica |
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| Online Access: | https://doi.org/10.2478/acph-2022-0028 |
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| author | Badr-Eldin Shaimaa M. Aldawsari Hibah M. Fahmy Usama A. Ahmed Osama A. A. Alhakamy Nabil A. Elfaky Mahmoud A. Sirwi Alaa Hawsawi Salman A. Alzahrani Ali H. Yaseen Abdulrahman Y. Qassim Mohannad Kotta Sabna |
| author_facet | Badr-Eldin Shaimaa M. Aldawsari Hibah M. Fahmy Usama A. Ahmed Osama A. A. Alhakamy Nabil A. Elfaky Mahmoud A. Sirwi Alaa Hawsawi Salman A. Alzahrani Ali H. Yaseen Abdulrahman Y. Qassim Mohannad Kotta Sabna |
| author_sort | Badr-Eldin Shaimaa M. |
| collection | DOAJ |
| description | Fluconazole (FLZ) is the most widely used antifungal agent for treating cutaneous candidiasis. Although oral FLZ has been proved to be effective, the incidence of side effects necessitates the development of an effective formulation that could surpass the pitfalls associated with systemic availability. Accordingly, this research aimed at developing a self-assembled mixed micelles topical delivery system to enhance the topical delivery of the drug. Self-assembled mixed micelles were developed using D-α-tocopheryl polyethylene glycol 1000 succinate and phospholipids and optimized using Box-Behnken design. The optimized formulation with minimized size was then tested in vivo for the antifungal activity against C. albicans in immunocompromised mice. Treatment with the optimized formulation led to decreased peripheral erythema as well as lesions due to fungal infection in comparison to raw FLZ loaded gel. Therefore, the developed formulation was found to be a promising vehicle for the treatment of cutaneous candidiasis. |
| format | Article |
| id | doaj-art-d723f4a6618046b5b43dded3e99b0600 |
| institution | Kabale University |
| issn | 1846-9558 |
| language | English |
| publishDate | 2022-12-01 |
| publisher | Sciendo |
| record_format | Article |
| series | Acta Pharmaceutica |
| spelling | doaj-art-d723f4a6618046b5b43dded3e99b06002025-02-03T10:46:36ZengSciendoActa Pharmaceutica1846-95582022-12-0172454756010.2478/acph-2022-0028Optimized D-α-tocopherol polyethylene glycol succinate/phospholipid self-assembled mixed micelles: A promising lipid-based nanoplatform for augmenting the antifungal activity of fluconazoleBadr-Eldin Shaimaa M.0Aldawsari Hibah M.1Fahmy Usama A.2Ahmed Osama A. A.3Alhakamy Nabil A.4Elfaky Mahmoud A.5Sirwi Alaa6Hawsawi Salman A.7Alzahrani Ali H.8Yaseen Abdulrahman Y.9Qassim Mohannad10Kotta Sabna11Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah21589, Saudi ArabiaDepartment of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah21589, Saudi ArabiaDepartment of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah21589, Saudi ArabiaDepartment of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah21589, Saudi ArabiaDepartment of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah21589, Saudi ArabiaDepartment of Natural Products, Faculty of Pharmacy, King Abdulaziz University, Jeddah21589, Saudi ArabiaDepartment of Natural Products, Faculty of Pharmacy, King Abdulaziz University, Jeddah21589, Saudi ArabiaFaculty of Pharmacy, King Abdulaziz University, Jeddah21589, Saudi ArabiaFaculty of Pharmacy, King Abdulaziz University, Jeddah21589, Saudi ArabiaFaculty of Pharmacy, King Abdulaziz University, Jeddah21589, Saudi ArabiaFaculty of Pharmacy, King Abdulaziz University, Jeddah21589, Saudi ArabiaDepartment of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah21589, Saudi ArabiaFluconazole (FLZ) is the most widely used antifungal agent for treating cutaneous candidiasis. Although oral FLZ has been proved to be effective, the incidence of side effects necessitates the development of an effective formulation that could surpass the pitfalls associated with systemic availability. Accordingly, this research aimed at developing a self-assembled mixed micelles topical delivery system to enhance the topical delivery of the drug. Self-assembled mixed micelles were developed using D-α-tocopheryl polyethylene glycol 1000 succinate and phospholipids and optimized using Box-Behnken design. The optimized formulation with minimized size was then tested in vivo for the antifungal activity against C. albicans in immunocompromised mice. Treatment with the optimized formulation led to decreased peripheral erythema as well as lesions due to fungal infection in comparison to raw FLZ loaded gel. Therefore, the developed formulation was found to be a promising vehicle for the treatment of cutaneous candidiasis.https://doi.org/10.2478/acph-2022-0028fluconazolefungal infectionscandida albi-cansself-assembled mixed micellesd-α-tocopheryl polyethylene glycol 1000 succinatephospholipids |
| spellingShingle | Badr-Eldin Shaimaa M. Aldawsari Hibah M. Fahmy Usama A. Ahmed Osama A. A. Alhakamy Nabil A. Elfaky Mahmoud A. Sirwi Alaa Hawsawi Salman A. Alzahrani Ali H. Yaseen Abdulrahman Y. Qassim Mohannad Kotta Sabna Optimized D-α-tocopherol polyethylene glycol succinate/phospholipid self-assembled mixed micelles: A promising lipid-based nanoplatform for augmenting the antifungal activity of fluconazole Acta Pharmaceutica fluconazole fungal infections candida albi-cans self-assembled mixed micelles d-α-tocopheryl polyethylene glycol 1000 succinate phospholipids |
| title | Optimized D-α-tocopherol polyethylene glycol succinate/phospholipid self-assembled mixed micelles: A promising lipid-based nanoplatform for augmenting the antifungal activity of fluconazole |
| title_full | Optimized D-α-tocopherol polyethylene glycol succinate/phospholipid self-assembled mixed micelles: A promising lipid-based nanoplatform for augmenting the antifungal activity of fluconazole |
| title_fullStr | Optimized D-α-tocopherol polyethylene glycol succinate/phospholipid self-assembled mixed micelles: A promising lipid-based nanoplatform for augmenting the antifungal activity of fluconazole |
| title_full_unstemmed | Optimized D-α-tocopherol polyethylene glycol succinate/phospholipid self-assembled mixed micelles: A promising lipid-based nanoplatform for augmenting the antifungal activity of fluconazole |
| title_short | Optimized D-α-tocopherol polyethylene glycol succinate/phospholipid self-assembled mixed micelles: A promising lipid-based nanoplatform for augmenting the antifungal activity of fluconazole |
| title_sort | optimized d α tocopherol polyethylene glycol succinate phospholipid self assembled mixed micelles a promising lipid based nanoplatform for augmenting the antifungal activity of fluconazole |
| topic | fluconazole fungal infections candida albi-cans self-assembled mixed micelles d-α-tocopheryl polyethylene glycol 1000 succinate phospholipids |
| url | https://doi.org/10.2478/acph-2022-0028 |
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