Ultra-deformable liposomes containing terpenes (terpesomes) loaded fenticonazole nitrate for treatment of vaginal candidiasis: Box-Behnken design optimization, comparative ex vivo and in vivo studies
Fenticonazole nitrate (FTN) is a potent antifungal drug adopted in the treatment of vaginal candidiasis. It has inadequate aqueous solubility hence, novel ultra-deformable liposomes ‘Terpesomes’ (TPs) were developed that might prevail over FTN poor solubility besides TPs might abstain the obstacles...
| Main Authors: | , , , , |
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2020-01-01
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| Series: | Drug Delivery |
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| Online Access: | http://dx.doi.org/10.1080/10717544.2020.1837295 |
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| author | Rofida Albash Yasmina Elmahboub Kholoud Baraka Menna M. Abdellatif Ahmed Adel Alaa-Eldin |
| author_facet | Rofida Albash Yasmina Elmahboub Kholoud Baraka Menna M. Abdellatif Ahmed Adel Alaa-Eldin |
| author_sort | Rofida Albash |
| collection | DOAJ |
| description | Fenticonazole nitrate (FTN) is a potent antifungal drug adopted in the treatment of vaginal candidiasis. It has inadequate aqueous solubility hence, novel ultra-deformable liposomes ‘Terpesomes’ (TPs) were developed that might prevail over FTN poor solubility besides TPs might abstain the obstacles of mucus invasion. TPs were assembled by thin-film hydration then optimized by Box Behnken design utilizing terpenes ratio (X1), sodium deoxycholate amount (X2), and ethanol concentration (X3) as independent variable, whereas their impact was inspected for entrapment efficiency (Y1), particle size (Y2), and polydispersity index (Y3). Design Expert® was bestowed to select the optimal TP for more studies. The optimal TP had entrapment efficiency of 62.18 ± 1.39%, particle size of 310.00 ± 8.16 nm, polydispersity index of 0.20 ± 0.10, and zeta potential of −10.19 ± 0.2.00 mV. Elasticity results were greater in the optimal TP related to classical bilosomes. Further, ex vivo permeation illustrated tremendous permeability from the optimal TP correlated to classical bilosomes, and FTN suspension. Besides, in vivo assessment displayed significant inhibition effect in rats from FTN-TPs gel compared to FTN gel. The antifungal potency with undermost histopathological variation was detected in rats treated with FTN-TPs gel. Overall, the acquired findings verified the potency of utilizing FTN-TPs gel for treatment of vaginal candidiasis. |
| first_indexed | 2024-12-14T17:08:07Z |
| format | Article |
| id | doaj.art-10cb8c5028de4dfb9d596b46de153737 |
| institution | Directory Open Access Journal |
| issn | 1071-7544 1521-0464 |
| language | English |
| last_indexed | 2024-12-14T17:08:07Z |
| publishDate | 2020-01-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Drug Delivery |
| spelling | doaj.art-10cb8c5028de4dfb9d596b46de1537372022-12-21T22:53:40ZengTaylor & Francis GroupDrug Delivery1071-75441521-04642020-01-012711514152310.1080/10717544.2020.18372951837295Ultra-deformable liposomes containing terpenes (terpesomes) loaded fenticonazole nitrate for treatment of vaginal candidiasis: Box-Behnken design optimization, comparative ex vivo and in vivo studiesRofida Albash0Yasmina Elmahboub1Kholoud Baraka2Menna M. Abdellatif3Ahmed Adel Alaa-Eldin4Department of Pharmaceutics, College of Pharmaceutical Sciences and Drug Manufacturing, Misr University for Science and TechnologyCollege of Pharmaceutical Sciences and Drug Manufacturing, Misr University for Science and TechnologyMicrobiology and Immunology Department, Faculty of Pharmacy, Damanhour UniversityDepartment of Industrial Pharmacy, College of Pharmaceutical Sciences and Drug Manufacturing, Misr University for Science and TechnologyDepartment of Pharmaceutics, Faculty of Pharmacy, Fayoum universityFenticonazole nitrate (FTN) is a potent antifungal drug adopted in the treatment of vaginal candidiasis. It has inadequate aqueous solubility hence, novel ultra-deformable liposomes ‘Terpesomes’ (TPs) were developed that might prevail over FTN poor solubility besides TPs might abstain the obstacles of mucus invasion. TPs were assembled by thin-film hydration then optimized by Box Behnken design utilizing terpenes ratio (X1), sodium deoxycholate amount (X2), and ethanol concentration (X3) as independent variable, whereas their impact was inspected for entrapment efficiency (Y1), particle size (Y2), and polydispersity index (Y3). Design Expert® was bestowed to select the optimal TP for more studies. The optimal TP had entrapment efficiency of 62.18 ± 1.39%, particle size of 310.00 ± 8.16 nm, polydispersity index of 0.20 ± 0.10, and zeta potential of −10.19 ± 0.2.00 mV. Elasticity results were greater in the optimal TP related to classical bilosomes. Further, ex vivo permeation illustrated tremendous permeability from the optimal TP correlated to classical bilosomes, and FTN suspension. Besides, in vivo assessment displayed significant inhibition effect in rats from FTN-TPs gel compared to FTN gel. The antifungal potency with undermost histopathological variation was detected in rats treated with FTN-TPs gel. Overall, the acquired findings verified the potency of utilizing FTN-TPs gel for treatment of vaginal candidiasis.http://dx.doi.org/10.1080/10717544.2020.1837295box behnken designfenticonazole nitratemicrobiological studyultra-deformable liposomesterpesomesvaginal drug delivery |
| spellingShingle | Rofida Albash Yasmina Elmahboub Kholoud Baraka Menna M. Abdellatif Ahmed Adel Alaa-Eldin Ultra-deformable liposomes containing terpenes (terpesomes) loaded fenticonazole nitrate for treatment of vaginal candidiasis: Box-Behnken design optimization, comparative ex vivo and in vivo studies Drug Delivery box behnken design fenticonazole nitrate microbiological study ultra-deformable liposomes terpesomes vaginal drug delivery |
| title | Ultra-deformable liposomes containing terpenes (terpesomes) loaded fenticonazole nitrate for treatment of vaginal candidiasis: Box-Behnken design optimization, comparative ex vivo and in vivo studies |
| title_full | Ultra-deformable liposomes containing terpenes (terpesomes) loaded fenticonazole nitrate for treatment of vaginal candidiasis: Box-Behnken design optimization, comparative ex vivo and in vivo studies |
| title_fullStr | Ultra-deformable liposomes containing terpenes (terpesomes) loaded fenticonazole nitrate for treatment of vaginal candidiasis: Box-Behnken design optimization, comparative ex vivo and in vivo studies |
| title_full_unstemmed | Ultra-deformable liposomes containing terpenes (terpesomes) loaded fenticonazole nitrate for treatment of vaginal candidiasis: Box-Behnken design optimization, comparative ex vivo and in vivo studies |
| title_short | Ultra-deformable liposomes containing terpenes (terpesomes) loaded fenticonazole nitrate for treatment of vaginal candidiasis: Box-Behnken design optimization, comparative ex vivo and in vivo studies |
| title_sort | ultra deformable liposomes containing terpenes terpesomes loaded fenticonazole nitrate for treatment of vaginal candidiasis box behnken design optimization comparative ex vivo and in vivo studies |
| topic | box behnken design fenticonazole nitrate microbiological study ultra-deformable liposomes terpesomes vaginal drug delivery |
| url | http://dx.doi.org/10.1080/10717544.2020.1837295 |
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