Ocular Inserts of Voriconazole-Loaded Proniosomal Gels: Formulation, Evaluation and Microbiological Studies

Ghada Ahmed El-Emam,1 Germeen NS Girgis,1 Mohamed M Adel El-Sokkary,2 Osama Abd El-Azeem Soliman,1 Abd El Gawad H Abd El Gawad1 1Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura, Egypt; 2Department of Microbiology, Faculty of Pharmacy, Mansoura University, Mansoura 355...

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Autores principales:	El-Emam GA, Girgis GNS, El-Sokkary MMA, El-Azeem Soliman OA, Abd El Gawad AEGH
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2020
Materias:	voriconazole proniosomes coacervation ocusert antifungal activity. Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/699c807c72c84970beac81f2188071c3
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spelling	oai:doaj.org-article:699c807c72c84970beac81f2188071c32021-12-02T11:05:25ZOcular Inserts of Voriconazole-Loaded Proniosomal Gels: Formulation, Evaluation and Microbiological Studies1178-2013https://doaj.org/article/699c807c72c84970beac81f2188071c32020-10-01T00:00:00Zhttps://www.dovepress.com/ocular-inserts-of-voriconazole-loaded-proniosomal-gels-formulation-eva-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Ghada Ahmed El-Emam,1 Germeen NS Girgis,1 Mohamed M Adel El-Sokkary,2 Osama Abd El-Azeem Soliman,1 Abd El Gawad H Abd El Gawad1 1Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura, Egypt; 2Department of Microbiology, Faculty of Pharmacy, Mansoura University, Mansoura 35516, EgyptCorrespondence: Germeen NS GirgisDepartment of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura 35516, EgyptTel +2 01200960016Fax +20 (50) 239733Email g.girgis2012@yahoo.comBackground: Voriconazole (VRC) is a triazole broad spectrum antifungal drug, used in the management of versatile fungal infections, particularly fungal keratitis. The obligatory use of niosomal delivery of VRC may reduce the frequency of dosing intervals resulting from its short biological half time and consequently improve patient compliance.Methods: VRC loaded proniosomes (VRC-PNs) were set by the coacervation technique and completely characterized. The developed formula was comprehensively assessed concerning in- vitro release behavior, kinetic investigation, and its conflict against refrigerated and room temperature conditions. A selected noisomal formula was incorporated into ocusert (VRC-PNs Ocu) formulated by 1% w/w hydroxypropyl methyl cellulose HPMC and 0.1% w/w carbopol 940. Eventually, in vitro antifungal activity against Candida albicans and Aspergillus nidulans was assessed by the cup diffusion method.Results: The optimized VRC-PNs (Pluronic F127: cholesterol weight ratio 1:1 w/w) exhibited the highest entrapment efficiency (87.4± 2.55%) with a spherical shape, proper size in nano range and a suitable Zeta potential of 209.7± 8.13 nm and − 33.5± 1.85 mV, respectively. Assurance of drug encapsulation in nanovesicles was accomplished by several means such as attenuated total reflection Fourier-transform infrared spectroscopy, differential scanning calorimetry in addition to powder X-ray diffraction investigations. It displayed a biphasic in vitro release pattern and after 6 months of storage at a refrigerated temperature, the optimized formula preserved its stability. VRC-PNs Ocu proved a very highly significant antifungal activity matched with the free drug or nanosuspension which was extra assured by comparing its mean inhibition zone with that of 5% natamycin market eye drops.Conclusion: In conclusion, VRC-PNs Ocu could be considered as a promising stable sustained release topical ocular nanoparticulate system for the management of fungal infections.Keywords: voriconazole, proniosomes, coacervation, ocusert, antifungal activityEl-Emam GAGirgis GNSEl-Sokkary MMAEl-Azeem Soliman OAAbd El Gawad AEGHDove Medical Pressarticlevoriconazoleproniosomescoacervationocusertantifungal activity.Medicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 15, Pp 7825-7840 (2020)
institution	DOAJ
collection	DOAJ
language	EN
topic	voriconazole proniosomes coacervation ocusert antifungal activity. Medicine (General) R5-920
spellingShingle	voriconazole proniosomes coacervation ocusert antifungal activity. Medicine (General) R5-920 El-Emam GA Girgis GNS El-Sokkary MMA El-Azeem Soliman OA Abd El Gawad AEGH Ocular Inserts of Voriconazole-Loaded Proniosomal Gels: Formulation, Evaluation and Microbiological Studies
description	Ghada Ahmed El-Emam,1 Germeen NS Girgis,1 Mohamed M Adel El-Sokkary,2 Osama Abd El-Azeem Soliman,1 Abd El Gawad H Abd El Gawad1 1Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura, Egypt; 2Department of Microbiology, Faculty of Pharmacy, Mansoura University, Mansoura 35516, EgyptCorrespondence: Germeen NS GirgisDepartment of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura 35516, EgyptTel +2 01200960016Fax +20 (50) 239733Email g.girgis2012@yahoo.comBackground: Voriconazole (VRC) is a triazole broad spectrum antifungal drug, used in the management of versatile fungal infections, particularly fungal keratitis. The obligatory use of niosomal delivery of VRC may reduce the frequency of dosing intervals resulting from its short biological half time and consequently improve patient compliance.Methods: VRC loaded proniosomes (VRC-PNs) were set by the coacervation technique and completely characterized. The developed formula was comprehensively assessed concerning in- vitro release behavior, kinetic investigation, and its conflict against refrigerated and room temperature conditions. A selected noisomal formula was incorporated into ocusert (VRC-PNs Ocu) formulated by 1% w/w hydroxypropyl methyl cellulose HPMC and 0.1% w/w carbopol 940. Eventually, in vitro antifungal activity against Candida albicans and Aspergillus nidulans was assessed by the cup diffusion method.Results: The optimized VRC-PNs (Pluronic F127: cholesterol weight ratio 1:1 w/w) exhibited the highest entrapment efficiency (87.4± 2.55%) with a spherical shape, proper size in nano range and a suitable Zeta potential of 209.7± 8.13 nm and − 33.5± 1.85 mV, respectively. Assurance of drug encapsulation in nanovesicles was accomplished by several means such as attenuated total reflection Fourier-transform infrared spectroscopy, differential scanning calorimetry in addition to powder X-ray diffraction investigations. It displayed a biphasic in vitro release pattern and after 6 months of storage at a refrigerated temperature, the optimized formula preserved its stability. VRC-PNs Ocu proved a very highly significant antifungal activity matched with the free drug or nanosuspension which was extra assured by comparing its mean inhibition zone with that of 5% natamycin market eye drops.Conclusion: In conclusion, VRC-PNs Ocu could be considered as a promising stable sustained release topical ocular nanoparticulate system for the management of fungal infections.Keywords: voriconazole, proniosomes, coacervation, ocusert, antifungal activity
format	article
author	El-Emam GA Girgis GNS El-Sokkary MMA El-Azeem Soliman OA Abd El Gawad AEGH
author_facet	El-Emam GA Girgis GNS El-Sokkary MMA El-Azeem Soliman OA Abd El Gawad AEGH
author_sort	El-Emam GA
title	Ocular Inserts of Voriconazole-Loaded Proniosomal Gels: Formulation, Evaluation and Microbiological Studies
title_short	Ocular Inserts of Voriconazole-Loaded Proniosomal Gels: Formulation, Evaluation and Microbiological Studies
title_full	Ocular Inserts of Voriconazole-Loaded Proniosomal Gels: Formulation, Evaluation and Microbiological Studies
title_fullStr	Ocular Inserts of Voriconazole-Loaded Proniosomal Gels: Formulation, Evaluation and Microbiological Studies
title_full_unstemmed	Ocular Inserts of Voriconazole-Loaded Proniosomal Gels: Formulation, Evaluation and Microbiological Studies
title_sort	ocular inserts of voriconazole-loaded proniosomal gels: formulation, evaluation and microbiological studies
publisher	Dove Medical Press
publishDate	2020
url	https://doaj.org/article/699c807c72c84970beac81f2188071c3
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Ocular Inserts of Voriconazole-Loaded Proniosomal Gels: Formulation, Evaluation and Microbiological Studies

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