Posaconazole loaded bilosomes as a novel vesicular carrier for topical treatment of fungal infections: Formulation, optimization, ex-vivo permeation and antifungal assay
Posaconazole (PSZ) is potent drug used in infections caused by Candida, Aspergillus species and many other fungal species. However PSZ belongs to BCS class II limiting its in vivo performance. The objective of current work was to mitigate the difficulties in topical delivery of PSZ overcoming its sh...
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Elsevier
2025-01-01
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S2949829525000907 |
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| author | Shital Bahadure Sharvil Patil Shubham Patil |
| author_facet | Shital Bahadure Sharvil Patil Shubham Patil |
| author_sort | Shital Bahadure |
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| description | Posaconazole (PSZ) is potent drug used in infections caused by Candida, Aspergillus species and many other fungal species. However PSZ belongs to BCS class II limiting its in vivo performance. The objective of current work was to mitigate the difficulties in topical delivery of PSZ overcoming its shortcomings such as aqueous solubility. PSZ loaded bilosomes were prepared and optimized using Box-Behnken design. The optimized bilosomes were characterized by TEM, DSC, FTIR, in vitro PSZ release, ex-vivo skin permeation and antifungal activity against Candida albicans and Aspergillus niger. The optimized spherical, unilamellar batch (PSZ_BIL) of bilosomes had vesicle size of 264.40 ± 5.17 nm and encapsulation efficiency of 97.54 ± 3.5 %. DSC studies revealed solubilization of PSZ in the molten mixture of cholesterol, poloxamer and sodium deoxycholate. FTIR spectra of PSZ_BIL suggested hydrogen bonding between PSZ and poloxamer in bilosomes responsible for greater entrapment efficiency. Further PSZ_BIL showed 2 fold increase in PSZ release when formulated into bilosomes. Ex vivo skin permeation studies showed 2.5 fold higher PSZ retention in rat skin when compared to PSZ gel. Additionally, local accumulation efficiency of PSZ was found to be 2.01 for PSZ_BIL gel formulation. The PSZ_BIL showed 2.33-fold and 1.8 fold increase in zone of inhibition for Candida albicans and Aspergillus niger respectively when compared to PSZ gel. Thus the prepared posaconazole loaded bilosomal gel could be an alternative to the existing formulation demonstrating the antifungal activity at much lower dose of the drug alone. |
| format | Article |
| id | doaj-art-405526daddc142f6a2a443a6bc861efa |
| institution | Kabale University |
| issn | 2949-8295 |
| language | English |
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| series | Next Nanotechnology |
| spelling | doaj-art-405526daddc142f6a2a443a6bc861efa2025-08-20T03:50:49ZengElsevierNext Nanotechnology2949-82952025-01-01810022110.1016/j.nxnano.2025.100221Posaconazole loaded bilosomes as a novel vesicular carrier for topical treatment of fungal infections: Formulation, optimization, ex-vivo permeation and antifungal assayShital Bahadure0Sharvil Patil1Shubham Patil2Department of Drug Regulatory Affairs, Bharati Vidyapeeth Deemed University, Poona College of Pharmacy, Erandwane, Pune 411038, IndiaDepartment of Pharmaceutics, Bharati Vidyapeeth Deemed University, Poona College of Pharmacy, Erandwane, Pune 411038, India; Correspondence to: Department of Pharmaceutics,Bharati Vidyapeeth (Deemed to be University)Poona College of Pharmacy, Eranwane, Pune, India.Department of Pharmaceutics, Bharati Vidyapeeth Deemed University, Poona College of Pharmacy, Erandwane, Pune 411038, IndiaPosaconazole (PSZ) is potent drug used in infections caused by Candida, Aspergillus species and many other fungal species. However PSZ belongs to BCS class II limiting its in vivo performance. The objective of current work was to mitigate the difficulties in topical delivery of PSZ overcoming its shortcomings such as aqueous solubility. PSZ loaded bilosomes were prepared and optimized using Box-Behnken design. The optimized bilosomes were characterized by TEM, DSC, FTIR, in vitro PSZ release, ex-vivo skin permeation and antifungal activity against Candida albicans and Aspergillus niger. The optimized spherical, unilamellar batch (PSZ_BIL) of bilosomes had vesicle size of 264.40 ± 5.17 nm and encapsulation efficiency of 97.54 ± 3.5 %. DSC studies revealed solubilization of PSZ in the molten mixture of cholesterol, poloxamer and sodium deoxycholate. FTIR spectra of PSZ_BIL suggested hydrogen bonding between PSZ and poloxamer in bilosomes responsible for greater entrapment efficiency. Further PSZ_BIL showed 2 fold increase in PSZ release when formulated into bilosomes. Ex vivo skin permeation studies showed 2.5 fold higher PSZ retention in rat skin when compared to PSZ gel. Additionally, local accumulation efficiency of PSZ was found to be 2.01 for PSZ_BIL gel formulation. The PSZ_BIL showed 2.33-fold and 1.8 fold increase in zone of inhibition for Candida albicans and Aspergillus niger respectively when compared to PSZ gel. Thus the prepared posaconazole loaded bilosomal gel could be an alternative to the existing formulation demonstrating the antifungal activity at much lower dose of the drug alone.http://www.sciencedirect.com/science/article/pii/S2949829525000907PosaconazoleBilosomesQuality by designAntifungal activityBile salts |
| spellingShingle | Shital Bahadure Sharvil Patil Shubham Patil Posaconazole loaded bilosomes as a novel vesicular carrier for topical treatment of fungal infections: Formulation, optimization, ex-vivo permeation and antifungal assay Next Nanotechnology Posaconazole Bilosomes Quality by design Antifungal activity Bile salts |
| title | Posaconazole loaded bilosomes as a novel vesicular carrier for topical treatment of fungal infections: Formulation, optimization, ex-vivo permeation and antifungal assay |
| title_full | Posaconazole loaded bilosomes as a novel vesicular carrier for topical treatment of fungal infections: Formulation, optimization, ex-vivo permeation and antifungal assay |
| title_fullStr | Posaconazole loaded bilosomes as a novel vesicular carrier for topical treatment of fungal infections: Formulation, optimization, ex-vivo permeation and antifungal assay |
| title_full_unstemmed | Posaconazole loaded bilosomes as a novel vesicular carrier for topical treatment of fungal infections: Formulation, optimization, ex-vivo permeation and antifungal assay |
| title_short | Posaconazole loaded bilosomes as a novel vesicular carrier for topical treatment of fungal infections: Formulation, optimization, ex-vivo permeation and antifungal assay |
| title_sort | posaconazole loaded bilosomes as a novel vesicular carrier for topical treatment of fungal infections formulation optimization ex vivo permeation and antifungal assay |
| topic | Posaconazole Bilosomes Quality by design Antifungal activity Bile salts |
| url | http://www.sciencedirect.com/science/article/pii/S2949829525000907 |
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