Bilosomes as Promising Nanovesicular Carriers for Improved Transdermal Delivery: Construction, in vitro Optimization, ex vivo Permeation and in vivo Evaluation

Sadek Ahmed, Mohamed Aly Kassem,&dagger; Sinar Sayed Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt&dagger;Mohamed Kassem, passed away on August 21, 2020Correspondence: Sinar SayedFaculty of Pharmacy, Cairo University, Kasr El-Aini, C...

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Autores principales:	Ahmed S, Kassem MA, Sayed S
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2020
Materias:	lornoxicam permeation enhancer factorial design confocal laser scanning microscopy antinociceptive. Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/85f968c445b84aaf9485b503f6537185
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spelling	oai:doaj.org-article:85f968c445b84aaf9485b503f65371852021-12-02T10:34:07ZBilosomes as Promising Nanovesicular Carriers for Improved Transdermal Delivery: Construction, in vitro Optimization, ex vivo Permeation and in vivo Evaluation1178-2013https://doaj.org/article/85f968c445b84aaf9485b503f65371852020-12-01T00:00:00Zhttps://www.dovepress.com/bilosomes-as-promising-nanovesicular-carriers-for-improved-transdermal-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Sadek Ahmed, Mohamed Aly Kassem,&dagger; Sinar Sayed Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt&dagger;Mohamed Kassem, passed away on August 21, 2020Correspondence: Sinar SayedFaculty of Pharmacy, Cairo University, Kasr El-Aini, Cairo 11562, EgyptTel +2 0 1010421543Email sinar.fouad@pharma.cu.edu.egPurpose: The goal of this research was to enhance the transdermal delivery of lornoxicam (LX), using nanovesicular carriers composed of the bile salt sodium deoxycholate (SDC), soybean phosphatidyl choline (SPC) and a permeation enhancer limonene.Methods: Thin-film hydration was the technique employed for the fabrication using a Box–Behnken design with three central points. The investigated factors were SPC molar concentration, SDC amount in mg and limonene percentage (%). The studied responses were percent entrapment efficiency (%EE), particle size (PS), polydispersity index (PDI), zeta potential (ZP), and in vitro drug release (after 2, 10 h). In order to obtain the optimum formula, numerical optimization by Design-Expert® software was used. Electing the optimized bilosomal formula was based on boosting %EE, ZP (as absolute value) and in vitro drug release, taking in consideration diminishing PS and PDI. Further assessment of the selected formula was achieved by transmission electron microscopy (TEM), differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), stability testing, ex vivo skin permeation and deposition. The in vivo pharmacodynamics activities of the optimized formula were examined on male rats and mice and compared to that of the oral market product.Results: The optimized bilosomal formula demonstrated to be nonirritant, with noticeably enhanced anti-inflammatory and antinociceptive activities. Superior in vivo permeation was proved by confocal laser scanning microscopy (CLSM).Conclusion: The outcomes demonstrated that bilosomes could improve transdermal delivery of lornoxicam.Keywords: lornoxicam, permeation enhancer, factorial design, confocal laser scanning microscopy, antinociceptiveAhmed SKassem MASayed SDove Medical Pressarticlelornoxicampermeation enhancerfactorial designconfocal laser scanning microscopyantinociceptive.Medicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 15, Pp 9783-9798 (2020)
institution	DOAJ
collection	DOAJ
language	EN
topic	lornoxicam permeation enhancer factorial design confocal laser scanning microscopy antinociceptive. Medicine (General) R5-920
spellingShingle	lornoxicam permeation enhancer factorial design confocal laser scanning microscopy antinociceptive. Medicine (General) R5-920 Ahmed S Kassem MA Sayed S Bilosomes as Promising Nanovesicular Carriers for Improved Transdermal Delivery: Construction, in vitro Optimization, ex vivo Permeation and in vivo Evaluation
description	Sadek Ahmed, Mohamed Aly Kassem,&dagger; Sinar Sayed Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt&dagger;Mohamed Kassem, passed away on August 21, 2020Correspondence: Sinar SayedFaculty of Pharmacy, Cairo University, Kasr El-Aini, Cairo 11562, EgyptTel +2 0 1010421543Email sinar.fouad@pharma.cu.edu.egPurpose: The goal of this research was to enhance the transdermal delivery of lornoxicam (LX), using nanovesicular carriers composed of the bile salt sodium deoxycholate (SDC), soybean phosphatidyl choline (SPC) and a permeation enhancer limonene.Methods: Thin-film hydration was the technique employed for the fabrication using a Box–Behnken design with three central points. The investigated factors were SPC molar concentration, SDC amount in mg and limonene percentage (%). The studied responses were percent entrapment efficiency (%EE), particle size (PS), polydispersity index (PDI), zeta potential (ZP), and in vitro drug release (after 2, 10 h). In order to obtain the optimum formula, numerical optimization by Design-Expert® software was used. Electing the optimized bilosomal formula was based on boosting %EE, ZP (as absolute value) and in vitro drug release, taking in consideration diminishing PS and PDI. Further assessment of the selected formula was achieved by transmission electron microscopy (TEM), differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), stability testing, ex vivo skin permeation and deposition. The in vivo pharmacodynamics activities of the optimized formula were examined on male rats and mice and compared to that of the oral market product.Results: The optimized bilosomal formula demonstrated to be nonirritant, with noticeably enhanced anti-inflammatory and antinociceptive activities. Superior in vivo permeation was proved by confocal laser scanning microscopy (CLSM).Conclusion: The outcomes demonstrated that bilosomes could improve transdermal delivery of lornoxicam.Keywords: lornoxicam, permeation enhancer, factorial design, confocal laser scanning microscopy, antinociceptive
format	article
author	Ahmed S Kassem MA Sayed S
author_facet	Ahmed S Kassem MA Sayed S
author_sort	Ahmed S
title	Bilosomes as Promising Nanovesicular Carriers for Improved Transdermal Delivery: Construction, in vitro Optimization, ex vivo Permeation and in vivo Evaluation
title_short	Bilosomes as Promising Nanovesicular Carriers for Improved Transdermal Delivery: Construction, in vitro Optimization, ex vivo Permeation and in vivo Evaluation
title_full	Bilosomes as Promising Nanovesicular Carriers for Improved Transdermal Delivery: Construction, in vitro Optimization, ex vivo Permeation and in vivo Evaluation
title_fullStr	Bilosomes as Promising Nanovesicular Carriers for Improved Transdermal Delivery: Construction, in vitro Optimization, ex vivo Permeation and in vivo Evaluation
title_full_unstemmed	Bilosomes as Promising Nanovesicular Carriers for Improved Transdermal Delivery: Construction, in vitro Optimization, ex vivo Permeation and in vivo Evaluation
title_sort	bilosomes as promising nanovesicular carriers for improved transdermal delivery: construction, in vitro optimization, ex vivo permeation and in vivo evaluation
publisher	Dove Medical Press
publishDate	2020
url	https://doaj.org/article/85f968c445b84aaf9485b503f6537185
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Bilosomes as Promising Nanovesicular Carriers for Improved Transdermal Delivery: Construction, in vitro Optimization, ex vivo Permeation and in vivo Evaluation

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