Tailoring of PEGylated bilosomes for promoting the transdermal delivery of olmesartan medoxomil: in-vitro characterization, ex-vivo permeation and in-vivo assessment

Rofida Albash,1 Mohamed A El-Nabarawi,2 Hanan Refai,1 Aly A Abdelbary2,31Department of Pharmaceutics, Faculty of Pharmaceutical Sciences and Drug Manufacturing, Misr University for Science and Technology, Giza, Egypt; 2Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo U...

Descripción completa

Guardado en:

Detalles Bibliográficos
Autores principales:	Albash R, El-Nabarawi MA, Refai H, Abdelbary AA
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2019
Materias:	Bilosomes confocal laser scanning microscopy ex-vivo permeation olmesartan medoxomil pharmacodynamic study pharmacokinetic study Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/dfd2c64b92cd413fb223383da359cfb7
Etiquetas:	Agregar Etiqueta Sin Etiquetas, Sea el primero en etiquetar este registro!

id	oai:doaj.org-article:dfd2c64b92cd413fb223383da359cfb7
record_format	dspace
spelling	oai:doaj.org-article:dfd2c64b92cd413fb223383da359cfb72021-12-02T08:18:07ZTailoring of PEGylated bilosomes for promoting the transdermal delivery of olmesartan medoxomil: in-vitro characterization, ex-vivo permeation and in-vivo assessment1178-2013https://doaj.org/article/dfd2c64b92cd413fb223383da359cfb72019-08-01T00:00:00Zhttps://www.dovepress.com/tailoring-of-pegylated-bilosomes-for-promoting-the-transdermal-deliver-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Rofida Albash,1 Mohamed A El-Nabarawi,2 Hanan Refai,1 Aly A Abdelbary2,31Department of Pharmaceutics, Faculty 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 Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, October 6 University, Giza, EgyptIntroduction: The intention of this work was to load olmesartan medoxomil (OLM), a sparsely water soluble antihypertensive bioactive with low oral bioavailability (26%), into PEGylated bilosomes (PBs) for augmenting its transdermal delivery. PBs contain PEGylated single chain edge activator besides the components of traditional bilosomes (Span 60, cholesterol and bile salts). The PEG gives further resilience to vesicle membrane and is speculated to augment both permeability and bioavailability of OLM.Methods: A 24 factorial experiment was constructed to inspect the impact of diverse variables on vesicles’ features and sort out the optimal formula adopting Design Expert® software utilizing thin film hydration technique. Vesicles’ evaluation was done by finding out entrapment efficiency percent (EE%), particle size (PS), polydispersity index (PDI), zeta potential (ZP) and amount of drug released after 6 hrs (Q6h). The optimal formula was selected and characterized for further investigations.Results: The optimal formula (PB15) showed spherical vesicles with EE% of 72.49±0.38%, PS of 559.30±10.70 nm, PDI of 0.57±0.15, ZP of −38.35±0.65 mV and Q6h of 59.60±0.24%. PB15 showed higher deformability index (28.39±5.71 g) compared to traditional bilosomes (5.88±0.90 g) and transethosomes (14.94±0.63 g). Further, PB15 showed superior skin permeation from rat’s skin relative to the drug suspension. Moreover, confocal laser scanning microscopy examination revealed efficient penetration of the fluoro-labeled PB15 through skin. Histopathological study ensured the safety of PB15. In addition, in-vivo skin deposition studies showed higher OLM deposition in rat’s skin from PB15 compared to transethosomes and OLM suspension. Furthermore, pharmacodynamic and pharmacokinetic studies performed using male Wistar rats and male Albino rabbits, respectively, showed the superiority of PB15 over oral tablets. PB15 was found to have significantly higher AUC0–48 and AUC0–∞ relative to the oral tablets. As well, the relative bioavailability of PB15 was found to be 235.04%.Conclusion: Overall, the obtained results confirmed the creditable effect of PB15 for transdermal delivery.Keywords: bilosomes, confocal laser scanning microscopy, ex-vivo permeation, olmesartan medoxomil, pharmacodynamic study, pharmacokinetic studyAlbash REl-Nabarawi MARefai HAbdelbary AADove Medical PressarticleBilosomesconfocal laser scanning microscopyex-vivo permeationolmesartan medoxomilpharmacodynamic studypharmacokinetic studyMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 14, Pp 6555-6574 (2019)
institution	DOAJ
collection	DOAJ
language	EN
topic	Bilosomes confocal laser scanning microscopy ex-vivo permeation olmesartan medoxomil pharmacodynamic study pharmacokinetic study Medicine (General) R5-920
spellingShingle	Bilosomes confocal laser scanning microscopy ex-vivo permeation olmesartan medoxomil pharmacodynamic study pharmacokinetic study Medicine (General) R5-920 Albash R El-Nabarawi MA Refai H Abdelbary AA Tailoring of PEGylated bilosomes for promoting the transdermal delivery of olmesartan medoxomil: in-vitro characterization, ex-vivo permeation and in-vivo assessment
description	Rofida Albash,1 Mohamed A El-Nabarawi,2 Hanan Refai,1 Aly A Abdelbary2,31Department of Pharmaceutics, Faculty 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 Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, October 6 University, Giza, EgyptIntroduction: The intention of this work was to load olmesartan medoxomil (OLM), a sparsely water soluble antihypertensive bioactive with low oral bioavailability (26%), into PEGylated bilosomes (PBs) for augmenting its transdermal delivery. PBs contain PEGylated single chain edge activator besides the components of traditional bilosomes (Span 60, cholesterol and bile salts). The PEG gives further resilience to vesicle membrane and is speculated to augment both permeability and bioavailability of OLM.Methods: A 24 factorial experiment was constructed to inspect the impact of diverse variables on vesicles’ features and sort out the optimal formula adopting Design Expert® software utilizing thin film hydration technique. Vesicles’ evaluation was done by finding out entrapment efficiency percent (EE%), particle size (PS), polydispersity index (PDI), zeta potential (ZP) and amount of drug released after 6 hrs (Q6h). The optimal formula was selected and characterized for further investigations.Results: The optimal formula (PB15) showed spherical vesicles with EE% of 72.49±0.38%, PS of 559.30±10.70 nm, PDI of 0.57±0.15, ZP of −38.35±0.65 mV and Q6h of 59.60±0.24%. PB15 showed higher deformability index (28.39±5.71 g) compared to traditional bilosomes (5.88±0.90 g) and transethosomes (14.94±0.63 g). Further, PB15 showed superior skin permeation from rat’s skin relative to the drug suspension. Moreover, confocal laser scanning microscopy examination revealed efficient penetration of the fluoro-labeled PB15 through skin. Histopathological study ensured the safety of PB15. In addition, in-vivo skin deposition studies showed higher OLM deposition in rat’s skin from PB15 compared to transethosomes and OLM suspension. Furthermore, pharmacodynamic and pharmacokinetic studies performed using male Wistar rats and male Albino rabbits, respectively, showed the superiority of PB15 over oral tablets. PB15 was found to have significantly higher AUC0–48 and AUC0–∞ relative to the oral tablets. As well, the relative bioavailability of PB15 was found to be 235.04%.Conclusion: Overall, the obtained results confirmed the creditable effect of PB15 for transdermal delivery.Keywords: bilosomes, confocal laser scanning microscopy, ex-vivo permeation, olmesartan medoxomil, pharmacodynamic study, pharmacokinetic study
format	article
author	Albash R El-Nabarawi MA Refai H Abdelbary AA
author_facet	Albash R El-Nabarawi MA Refai H Abdelbary AA
author_sort	Albash R
title	Tailoring of PEGylated bilosomes for promoting the transdermal delivery of olmesartan medoxomil: in-vitro characterization, ex-vivo permeation and in-vivo assessment
title_short	Tailoring of PEGylated bilosomes for promoting the transdermal delivery of olmesartan medoxomil: in-vitro characterization, ex-vivo permeation and in-vivo assessment
title_full	Tailoring of PEGylated bilosomes for promoting the transdermal delivery of olmesartan medoxomil: in-vitro characterization, ex-vivo permeation and in-vivo assessment
title_fullStr	Tailoring of PEGylated bilosomes for promoting the transdermal delivery of olmesartan medoxomil: in-vitro characterization, ex-vivo permeation and in-vivo assessment
title_full_unstemmed	Tailoring of PEGylated bilosomes for promoting the transdermal delivery of olmesartan medoxomil: in-vitro characterization, ex-vivo permeation and in-vivo assessment
title_sort	tailoring of pegylated bilosomes for promoting the transdermal delivery of olmesartan medoxomil: in-vitro characterization, ex-vivo permeation and in-vivo assessment
publisher	Dove Medical Press
publishDate	2019
url	https://doaj.org/article/dfd2c64b92cd413fb223383da359cfb7
work_keys_str_mv	AT albashr tailoringofpegylatedbilosomesforpromotingthetransdermaldeliveryofolmesartanmedoxomilinvitrocharacterizationexvivopermeationandinvivoassessment AT elnabarawima tailoringofpegylatedbilosomesforpromotingthetransdermaldeliveryofolmesartanmedoxomilinvitrocharacterizationexvivopermeationandinvivoassessment AT refaih tailoringofpegylatedbilosomesforpromotingthetransdermaldeliveryofolmesartanmedoxomilinvitrocharacterizationexvivopermeationandinvivoassessment AT abdelbaryaa tailoringofpegylatedbilosomesforpromotingthetransdermaldeliveryofolmesartanmedoxomilinvitrocharacterizationexvivopermeationandinvivoassessment
_version_	1718398574189871104

Tailoring of PEGylated bilosomes for promoting the transdermal delivery of olmesartan medoxomil: in-vitro characterization, ex-vivo permeation and in-vivo assessment

Ejemplares similares