Development and Optimization of Terpene-Enriched Vesicles (Terpesomes) for Effective Ocular Delivery of Fenticonazole Nitrate: In vitro Characterization and in vivo Assessment

Rofida Albash,1 Abdulaziz Mohsen Al-mahallawi,2 Mariam Hassan,3 Ahmed Adel Alaa-Eldin4 1Department of Pharmaceutics, College of Pharmaceutical Sciences and Drug Manufacturing, Misr University for Science and Technology, Giza, Egypt; 2Department of Pharmaceutics and Industrial Pharmacy, Faculty of Ph...

Descripción completa

Guardado en:

Detalles Bibliográficos
Autores principales:	Albash R, Al-mahallawi AM, Hassan M, Alaa-Eldin AA
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2021
Materias:	fenticonazole nitrate histopathological study ocular drug delivery microbiological study terpesomes. Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/29740d00fb084e13965d0948ef2751a7
Etiquetas:	Agregar Etiqueta Sin Etiquetas, Sea el primero en etiquetar este registro!

id	oai:doaj.org-article:29740d00fb084e13965d0948ef2751a7
record_format	dspace
spelling	oai:doaj.org-article:29740d00fb084e13965d0948ef2751a72021-12-02T14:23:40ZDevelopment and Optimization of Terpene-Enriched Vesicles (Terpesomes) for Effective Ocular Delivery of Fenticonazole Nitrate: In vitro Characterization and in vivo Assessment1178-2013https://doaj.org/article/29740d00fb084e13965d0948ef2751a72021-01-01T00:00:00Zhttps://www.dovepress.com/development-and-optimization-of-terpene-enriched-vesicles-terpesomes-f-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Rofida Albash,1 Abdulaziz Mohsen Al-mahallawi,2 Mariam Hassan,3 Ahmed Adel Alaa-Eldin4 1Department of Pharmaceutics, College of Pharmaceutical Sciences and Drug Manufacturing, Misr University for Science and Technology, Giza, Egypt; 2Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt; 3Department of Microbiology and Immunology, Faculty of Pharmacy, Cairo University, Cairo, Egypt; 4Department of Pharmaceutics, Faculty of Pharmacy, Fayoum University, Elfayoum, EgyptCorrespondence: Abdulaziz Mohsen Al-mahallawiFaculty of Pharmacy, Cairo University, 11562, EgyptTel +201008226524Email Abdulaziz.mohsen@pharma.cu.edu.egObjective: The aim of the current study was to load fenticonazole nitrate, a slightly water-soluble antifungal agent, into terpene-enriched phospholipid vesicles (terpesomes) as a potential delivery system for the management of ocular fungal infection.Methods: Thin film hydration method was used to prepare terpesomes according to a 32 full factorial design to inspect the effect of several variables on vesicles’ features. The investigated factors were terpenes type (X1) and terpenes amount (X2) while the dependent responses were encapsulation efficiency percent (Y1), particle size (Y2) and polydispersity index (Y3). Design Expert® program was used to chose the best achieved formula. The selected terpesomes were further optimized via incorporation of a positive charge inducer (stearylamine) to enhance adhesion to the negatively charged mucus covering the eye surface. The in vivo performance of the optimized fenticonazole nitrate-loaded terpesomes relative to drug suspension was evaluated by measuring the antifungal activity (against Candida albicans) retained in the tear’s fluid at different time intervals after ocular application in albino rabbits.Results: The optimized terpesomes showed spherical vesicles with entrapment efficiency of 79.02± 2.35%, particle size of 287.25± 9.55 nm, polydispersity index of 0.46± 0.01 and zeta potential of 36.15± 1.06 mV. The in vivo study demonstrated significantly higher ocular retention of the optimized fenticonazole nitrate-loaded terpesomes relative to the drug suspension. Moreover, the histopathological studies proved the safety and biocompatibility of the prepared terpesomes.Conclusion: The obtained results verified the potential of the terpesomes for safe and effective ocular delivery of fenticonazole nitrate.Keywords: fenticonazole nitrate, histopathological study, ocular drug delivery, microbiological study, terpesomesAlbash RAl-mahallawi AMHassan MAlaa-Eldin AADove Medical Pressarticlefenticonazole nitratehistopathological studyocular drug deliverymicrobiological studyterpesomes.Medicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 16, Pp 609-621 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	fenticonazole nitrate histopathological study ocular drug delivery microbiological study terpesomes. Medicine (General) R5-920
spellingShingle	fenticonazole nitrate histopathological study ocular drug delivery microbiological study terpesomes. Medicine (General) R5-920 Albash R Al-mahallawi AM Hassan M Alaa-Eldin AA Development and Optimization of Terpene-Enriched Vesicles (Terpesomes) for Effective Ocular Delivery of Fenticonazole Nitrate: In vitro Characterization and in vivo Assessment
description	Rofida Albash,1 Abdulaziz Mohsen Al-mahallawi,2 Mariam Hassan,3 Ahmed Adel Alaa-Eldin4 1Department of Pharmaceutics, College of Pharmaceutical Sciences and Drug Manufacturing, Misr University for Science and Technology, Giza, Egypt; 2Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt; 3Department of Microbiology and Immunology, Faculty of Pharmacy, Cairo University, Cairo, Egypt; 4Department of Pharmaceutics, Faculty of Pharmacy, Fayoum University, Elfayoum, EgyptCorrespondence: Abdulaziz Mohsen Al-mahallawiFaculty of Pharmacy, Cairo University, 11562, EgyptTel +201008226524Email Abdulaziz.mohsen@pharma.cu.edu.egObjective: The aim of the current study was to load fenticonazole nitrate, a slightly water-soluble antifungal agent, into terpene-enriched phospholipid vesicles (terpesomes) as a potential delivery system for the management of ocular fungal infection.Methods: Thin film hydration method was used to prepare terpesomes according to a 32 full factorial design to inspect the effect of several variables on vesicles’ features. The investigated factors were terpenes type (X1) and terpenes amount (X2) while the dependent responses were encapsulation efficiency percent (Y1), particle size (Y2) and polydispersity index (Y3). Design Expert® program was used to chose the best achieved formula. The selected terpesomes were further optimized via incorporation of a positive charge inducer (stearylamine) to enhance adhesion to the negatively charged mucus covering the eye surface. The in vivo performance of the optimized fenticonazole nitrate-loaded terpesomes relative to drug suspension was evaluated by measuring the antifungal activity (against Candida albicans) retained in the tear’s fluid at different time intervals after ocular application in albino rabbits.Results: The optimized terpesomes showed spherical vesicles with entrapment efficiency of 79.02± 2.35%, particle size of 287.25± 9.55 nm, polydispersity index of 0.46± 0.01 and zeta potential of 36.15± 1.06 mV. The in vivo study demonstrated significantly higher ocular retention of the optimized fenticonazole nitrate-loaded terpesomes relative to the drug suspension. Moreover, the histopathological studies proved the safety and biocompatibility of the prepared terpesomes.Conclusion: The obtained results verified the potential of the terpesomes for safe and effective ocular delivery of fenticonazole nitrate.Keywords: fenticonazole nitrate, histopathological study, ocular drug delivery, microbiological study, terpesomes
format	article
author	Albash R Al-mahallawi AM Hassan M Alaa-Eldin AA
author_facet	Albash R Al-mahallawi AM Hassan M Alaa-Eldin AA
author_sort	Albash R
title	Development and Optimization of Terpene-Enriched Vesicles (Terpesomes) for Effective Ocular Delivery of Fenticonazole Nitrate: In vitro Characterization and in vivo Assessment
title_short	Development and Optimization of Terpene-Enriched Vesicles (Terpesomes) for Effective Ocular Delivery of Fenticonazole Nitrate: In vitro Characterization and in vivo Assessment
title_full	Development and Optimization of Terpene-Enriched Vesicles (Terpesomes) for Effective Ocular Delivery of Fenticonazole Nitrate: In vitro Characterization and in vivo Assessment
title_fullStr	Development and Optimization of Terpene-Enriched Vesicles (Terpesomes) for Effective Ocular Delivery of Fenticonazole Nitrate: In vitro Characterization and in vivo Assessment
title_full_unstemmed	Development and Optimization of Terpene-Enriched Vesicles (Terpesomes) for Effective Ocular Delivery of Fenticonazole Nitrate: In vitro Characterization and in vivo Assessment
title_sort	development and optimization of terpene-enriched vesicles (terpesomes) for effective ocular delivery of fenticonazole nitrate: in vitro characterization and in vivo assessment
publisher	Dove Medical Press
publishDate	2021
url	https://doaj.org/article/29740d00fb084e13965d0948ef2751a7
work_keys_str_mv	AT albashr developmentandoptimizationofterpeneenrichedvesiclesterpesomesforeffectiveoculardeliveryoffenticonazolenitrateinvitrocharacterizationandinvivoassessment AT almahallawiam developmentandoptimizationofterpeneenrichedvesiclesterpesomesforeffectiveoculardeliveryoffenticonazolenitrateinvitrocharacterizationandinvivoassessment AT hassanm developmentandoptimizationofterpeneenrichedvesiclesterpesomesforeffectiveoculardeliveryoffenticonazolenitrateinvitrocharacterizationandinvivoassessment AT alaaeldinaa developmentandoptimizationofterpeneenrichedvesiclesterpesomesforeffectiveoculardeliveryoffenticonazolenitrateinvitrocharacterizationandinvivoassessment
_version_	1718391416787304448

Development and Optimization of Terpene-Enriched Vesicles (Terpesomes) for Effective Ocular Delivery of Fenticonazole Nitrate: In vitro Characterization and in vivo Assessment

Ejemplares similares