Self-nanoemulsifying drug delivery system to improve transcorneal permeability of voriconazole : in-vivo studies
© 2020 Royal Pharmaceutical Society..
OBJECTIVE: This study investigates the effectiveness of self-nanoemulsifying drug delivery system (SNEDDS) in improving voriconazole transcorneal permeability.
METHODS: Voriconazole-SNEDDS was prepared with isopropyl myristate, PEG 400, Tween 80® and Span 80® and was subjected for physicochemical characterization after reconstitution with NaCl 0.9% (1/9; v/v). In-vitro antifungal activity was assessed and compared with the marketed formulation. In-vivo studies, namely ocular irritation test via modified Draize test and pharmacokinetic study, were investigated using rabbit as animal model.
KEY FINDINGS: Voriconazole-SNEDDS presented a droplet size of 21.353 ± 0.065 nm, a polydispersity index of 0.123 ± 0.003, a pH of 7.205 ± 0.006 and an osmolarity of 342.667 ± 2.517 mOsmol/l after reconstitution with NaCl 0.9%. Voriconazole-SNEDDS minimum inhibitory concentration (MIC90 ) was similar to the one of marketed formulation for Candida species while it was significantly lower (P < 0.001) for Aspergillus fumigatus. Draize test revealed that Voriconazole-SNEDDS was safe for ocular administration. Voriconazole maximum concentration (5.577 ± 0.852 µg/ml) from SNEDDS was higher than marketed formulation (Cmax = 4.307 ± 0.623 µg/ml), and the Tmax was delayed to 2 h. The area under the concentration-time curve value of Voriconazole-SNEDDS was improved by 2.419-fold.
CONCLUSION: Our results suggest that SNEDDS is a promising carrier for voriconazole ocular delivery and this encourages further clinical studies.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2020 |
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| Erschienen: |
2020 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:72 |
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| Enthalten in: |
The Journal of pharmacy and pharmacology - 72(2020), 7 vom: 01. Juli, Seite 889-896 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Rasoanirina, Bakoliarisoa Nivomalala Voahangy [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 29.03.2021 Date Revised 29.03.2021 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1111/jphp.13265 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM308797086 |
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| 500 | |a Date Completed 29.03.2021 | ||
| 500 | |a Date Revised 29.03.2021 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a © 2020 Royal Pharmaceutical Society. | ||
| 520 | |a OBJECTIVE: This study investigates the effectiveness of self-nanoemulsifying drug delivery system (SNEDDS) in improving voriconazole transcorneal permeability | ||
| 520 | |a METHODS: Voriconazole-SNEDDS was prepared with isopropyl myristate, PEG 400, Tween 80® and Span 80® and was subjected for physicochemical characterization after reconstitution with NaCl 0.9% (1/9; v/v). In-vitro antifungal activity was assessed and compared with the marketed formulation. In-vivo studies, namely ocular irritation test via modified Draize test and pharmacokinetic study, were investigated using rabbit as animal model | ||
| 520 | |a KEY FINDINGS: Voriconazole-SNEDDS presented a droplet size of 21.353 ± 0.065 nm, a polydispersity index of 0.123 ± 0.003, a pH of 7.205 ± 0.006 and an osmolarity of 342.667 ± 2.517 mOsmol/l after reconstitution with NaCl 0.9%. Voriconazole-SNEDDS minimum inhibitory concentration (MIC90 ) was similar to the one of marketed formulation for Candida species while it was significantly lower (P < 0.001) for Aspergillus fumigatus. Draize test revealed that Voriconazole-SNEDDS was safe for ocular administration. Voriconazole maximum concentration (5.577 ± 0.852 µg/ml) from SNEDDS was higher than marketed formulation (Cmax = 4.307 ± 0.623 µg/ml), and the Tmax was delayed to 2 h. The area under the concentration-time curve value of Voriconazole-SNEDDS was improved by 2.419-fold | ||
| 520 | |a CONCLUSION: Our results suggest that SNEDDS is a promising carrier for voriconazole ocular delivery and this encourages further clinical studies | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a minimum inhibitory concentration aqueous humour | |
| 650 | 4 | |a mycotic keratitis | |
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| 650 | 4 | |a self-nanoemulsifying drug delivery system | |
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| 700 | 1 | |a Lassoued, Mohamed Ali |e verfasserin |4 aut | |
| 700 | 1 | |a Miladi, Karim |e verfasserin |4 aut | |
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| 700 | 1 | |a Ramanitrahasimbola, David |e verfasserin |4 aut | |
| 700 | 1 | |a Cornet, Muriel |e verfasserin |4 aut | |
| 700 | 1 | |a Sfar, Souad |e verfasserin |4 aut | |
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