Formulation, optimization, and nephrotoxicity evaluation of an antifungal in situ nasal gel loaded with voriconazole‒clove oil transferosomal nanoparticles

Fungal infections of the paranasal cavity are among the most widely spread illnesses nowadays. The aim of the current study was to estimate the effectiveness of an in situ gel loaded with voriconazole‒clove oil nano-transferosomes (VRC-CO-NT) in enhancing the activity of voriconazole against Aspergi...

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Autores principales:	Ahmed K. Kammoun, Alaa Khedr, Maha A. Hegazy, Ahmad J. Almalki, Khaled M. Hosny, Walaa A. Abualsunun, Samar S. A. Murshid, Rana B. Bakhaidar
Formato:	article
Lenguaje:	EN
Publicado:	Taylor & Francis Group 2021
Materias:	antifungal clove oil box‒behnken design voriconazole transferosomes rhinosinusitis Therapeutics. Pharmacology RM1-950
Acceso en línea:	https://doaj.org/article/e6724045d1cd410b83387b329e31c42c
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spelling	oai:doaj.org-article:e6724045d1cd410b83387b329e31c42c2021-11-11T14:23:41ZFormulation, optimization, and nephrotoxicity evaluation of an antifungal in situ nasal gel loaded with voriconazole‒clove oil transferosomal nanoparticles1071-75441521-046410.1080/10717544.2021.1992040https://doaj.org/article/e6724045d1cd410b83387b329e31c42c2021-01-01T00:00:00Zhttp://dx.doi.org/10.1080/10717544.2021.1992040https://doaj.org/toc/1071-7544https://doaj.org/toc/1521-0464Fungal infections of the paranasal cavity are among the most widely spread illnesses nowadays. The aim of the current study was to estimate the effectiveness of an in situ gel loaded with voriconazole‒clove oil nano-transferosomes (VRC-CO-NT) in enhancing the activity of voriconazole against Aspergillus flavus, which causes rhinosinusitis. The nephrotoxic side effects of voriconazole may be reduced through the incorporation of the clove oil, which has antioxidant activity that protects tissue. The Box‒Behnken design was applied to formulate the VRC-CO-NT. The particle size, entrapment efficiency, antifungal inhibition zone, and serum creatinine concentration were considered dependent variables, and the soybean lecithin, VRC, and CO concentrations were considered independent ones. The final optimized formulation was loaded into a deacetylated gellan gum base and evaluated for its gelation, rheological properties, drug release profile, permeation capabilities, and in vivo nephrotoxicity. The optimum formulation was determined to be composed of 50 mg/mL lecithin, 18 mg/mL VRC, and 75 mg/mL CO, with a minimum particle size of 102.96 nm, an entrapment efficiency of 71.70%, an inhibition zone of 21.76 mm, and a serum creatinine level of 0.119 mmol/L. The optimized loaded in situ gel released 82.5% VRC after 12 hours and resulted in a 5.4-fold increase in drug permeation. The in vivo results obtained using rabbits resulted in a nonsignificant differentiation among the renal function parameters compared with the negative control group. In conclusion, nasal in situ gel loaded with VRC-CO-NT is considered an efficient novel carrier with enhanced antifungal properties with no signs of nephrotoxicity.Ahmed K. KammounAlaa KhedrMaha A. HegazyAhmad J. AlmalkiKhaled M. HosnyWalaa A. AbualsununSamar S. A. MurshidRana B. BakhaidarTaylor & Francis Grouparticleantifungalclove oilbox‒behnken designvoriconazoletransferosomesrhinosinusitisTherapeutics. PharmacologyRM1-950ENDrug Delivery, Vol 28, Iss 1, Pp 2229-2240 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	antifungal clove oil box‒behnken design voriconazole transferosomes rhinosinusitis Therapeutics. Pharmacology RM1-950
spellingShingle	antifungal clove oil box‒behnken design voriconazole transferosomes rhinosinusitis Therapeutics. Pharmacology RM1-950 Ahmed K. Kammoun Alaa Khedr Maha A. Hegazy Ahmad J. Almalki Khaled M. Hosny Walaa A. Abualsunun Samar S. A. Murshid Rana B. Bakhaidar Formulation, optimization, and nephrotoxicity evaluation of an antifungal in situ nasal gel loaded with voriconazole‒clove oil transferosomal nanoparticles
description	Fungal infections of the paranasal cavity are among the most widely spread illnesses nowadays. The aim of the current study was to estimate the effectiveness of an in situ gel loaded with voriconazole‒clove oil nano-transferosomes (VRC-CO-NT) in enhancing the activity of voriconazole against Aspergillus flavus, which causes rhinosinusitis. The nephrotoxic side effects of voriconazole may be reduced through the incorporation of the clove oil, which has antioxidant activity that protects tissue. The Box‒Behnken design was applied to formulate the VRC-CO-NT. The particle size, entrapment efficiency, antifungal inhibition zone, and serum creatinine concentration were considered dependent variables, and the soybean lecithin, VRC, and CO concentrations were considered independent ones. The final optimized formulation was loaded into a deacetylated gellan gum base and evaluated for its gelation, rheological properties, drug release profile, permeation capabilities, and in vivo nephrotoxicity. The optimum formulation was determined to be composed of 50 mg/mL lecithin, 18 mg/mL VRC, and 75 mg/mL CO, with a minimum particle size of 102.96 nm, an entrapment efficiency of 71.70%, an inhibition zone of 21.76 mm, and a serum creatinine level of 0.119 mmol/L. The optimized loaded in situ gel released 82.5% VRC after 12 hours and resulted in a 5.4-fold increase in drug permeation. The in vivo results obtained using rabbits resulted in a nonsignificant differentiation among the renal function parameters compared with the negative control group. In conclusion, nasal in situ gel loaded with VRC-CO-NT is considered an efficient novel carrier with enhanced antifungal properties with no signs of nephrotoxicity.
format	article
author	Ahmed K. Kammoun Alaa Khedr Maha A. Hegazy Ahmad J. Almalki Khaled M. Hosny Walaa A. Abualsunun Samar S. A. Murshid Rana B. Bakhaidar
author_facet	Ahmed K. Kammoun Alaa Khedr Maha A. Hegazy Ahmad J. Almalki Khaled M. Hosny Walaa A. Abualsunun Samar S. A. Murshid Rana B. Bakhaidar
author_sort	Ahmed K. Kammoun
title	Formulation, optimization, and nephrotoxicity evaluation of an antifungal in situ nasal gel loaded with voriconazole‒clove oil transferosomal nanoparticles
title_short	Formulation, optimization, and nephrotoxicity evaluation of an antifungal in situ nasal gel loaded with voriconazole‒clove oil transferosomal nanoparticles
title_full	Formulation, optimization, and nephrotoxicity evaluation of an antifungal in situ nasal gel loaded with voriconazole‒clove oil transferosomal nanoparticles
title_fullStr	Formulation, optimization, and nephrotoxicity evaluation of an antifungal in situ nasal gel loaded with voriconazole‒clove oil transferosomal nanoparticles
title_full_unstemmed	Formulation, optimization, and nephrotoxicity evaluation of an antifungal in situ nasal gel loaded with voriconazole‒clove oil transferosomal nanoparticles
title_sort	formulation, optimization, and nephrotoxicity evaluation of an antifungal in situ nasal gel loaded with voriconazole‒clove oil transferosomal nanoparticles
publisher	Taylor & Francis Group
publishDate	2021
url	https://doaj.org/article/e6724045d1cd410b83387b329e31c42c
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Formulation, optimization, and nephrotoxicity evaluation of an antifungal in situ nasal gel loaded with voriconazole‒clove oil transferosomal nanoparticles

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