Liver Targeting of Daclatasvir via Tailoring Sterically Stabilized Bilosomes: Fabrication, Comparative In Vitro/In Vivo Appraisal and Biodistribution Studies

Mohamed El-Nabarawi,1 Mohamed Nafady,2 Shahira Elmenshawe,3 Marwa Elkarmalawy,4 Mahmoud Teaima1 1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt; 2Department of Pharmaceutics and Clinical Pharmacy, Faculty of Pharmacy, Nahda University, Beni-S...

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Autores principales:	El-Nabarawi M, Nafady M, Elmenshawe S, Elkarmalawy M, Teaima M
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2021
Materias:	antiviral drug – nano drug delivery system- bile based nano-vesicles- box-behnken approach -liver targeting parameters – pharmacokinetic- bioavailability Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/a2aa5588f39c45a9b0ba265c8c74606d
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spelling	oai:doaj.org-article:a2aa5588f39c45a9b0ba265c8c74606d2021-12-02T19:14:25ZLiver Targeting of Daclatasvir via Tailoring Sterically Stabilized Bilosomes: Fabrication, Comparative In Vitro/In Vivo Appraisal and Biodistribution Studies1178-2013https://doaj.org/article/a2aa5588f39c45a9b0ba265c8c74606d2021-09-01T00:00:00Zhttps://www.dovepress.com/liver-targeting-of-daclatasvir-via-tailoring-sterically-stabilized-bil-peer-reviewed-fulltext-article-IJNhttps://doaj.org/toc/1178-2013Mohamed El-Nabarawi,1 Mohamed Nafady,2 Shahira Elmenshawe,3 Marwa Elkarmalawy,4 Mahmoud Teaima1 1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt; 2Department of Pharmaceutics and Clinical Pharmacy, Faculty of Pharmacy, Nahda University, Beni-Suef, Egypt; 3Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, Egypt; 4Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Modern University of Technology and Information, Cairo, EgyptCorrespondence: Shahira Elmenshawe Email Shahira.elmenshawe@yahoo.comIntroduction: Hepatitis C virus (HCV) is a significant public health concern that threatens millions of individuals worldwide. Daclatasvir (DAC) is a promising direct-acting antiviral approved for treating HCV infection around the world. The goal of this study was to encapsulate DAC into novel polyethylene glycol (PEG) decorated bilosomes (PEG-BILS) to achieve enhanced drug delivery to the liver.Methods: DAC-loaded BILS were primed by a thin film hydrating technique. The study of the impact of various formulation variables on the properties of BILS and selection of the optimal formulation was generated using Design-Expert® software. The optimum preparation was then pegylated via the incorporation of PEG-6-stearate (5% w/w, with respect to the lipid phase).Results: The optimum PEG-BILS formulation, containing PL:SDC ratio (5:1), 5 mg cholesterol, and 30 min sonication, yielded spherical vesicles in the nanoscale (200± 15.2 nm), elevated percent of entrapment efficiency (95.5± 7.77%), and a sustained release profile of DAC with 35.11± 2.3% release. In vivo and drug distribution studies revealed an enhanced hepatocellular delivery of DAC-loaded PEG-BILS compared to DAC-unPEG-BILS and DAC suspension, where DAC-PEG-BILS achieved 1.19- and 1.54 times the AUC0– 24 of DAC-unPEG-BILS and DAC suspension, respectively. Compared with DAC-unPEG-BILS and DAC suspension, DAC-PEG-BILS delivered about 2 and 3 times higher DAC into the liver, respectively.Conclusion: The innovative encapsulation of DAC-PEG-BILS has a great potential for liver targeting.Keywords: antiviral drug, nanodrug delivery system, bile-based nanovesicles, Box–Behnken approach, liver targeting parameters, pharmacokinetic, bioavailabilityEl-Nabarawi MNafady MElmenshawe SElkarmalawy MTeaima MDove Medical Pressarticleantiviral drug – nano drug delivery system- bile based nano-vesicles- box-behnken approach -liver targeting parameters – pharmacokinetic- bioavailabilityMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 16, Pp 6413-6426 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	antiviral drug – nano drug delivery system- bile based nano-vesicles- box-behnken approach -liver targeting parameters – pharmacokinetic- bioavailability Medicine (General) R5-920
spellingShingle	antiviral drug – nano drug delivery system- bile based nano-vesicles- box-behnken approach -liver targeting parameters – pharmacokinetic- bioavailability Medicine (General) R5-920 El-Nabarawi M Nafady M Elmenshawe S Elkarmalawy M Teaima M Liver Targeting of Daclatasvir via Tailoring Sterically Stabilized Bilosomes: Fabrication, Comparative In Vitro/In Vivo Appraisal and Biodistribution Studies
description	Mohamed El-Nabarawi,1 Mohamed Nafady,2 Shahira Elmenshawe,3 Marwa Elkarmalawy,4 Mahmoud Teaima1 1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt; 2Department of Pharmaceutics and Clinical Pharmacy, Faculty of Pharmacy, Nahda University, Beni-Suef, Egypt; 3Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, Egypt; 4Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Modern University of Technology and Information, Cairo, EgyptCorrespondence: Shahira Elmenshawe Email Shahira.elmenshawe@yahoo.comIntroduction: Hepatitis C virus (HCV) is a significant public health concern that threatens millions of individuals worldwide. Daclatasvir (DAC) is a promising direct-acting antiviral approved for treating HCV infection around the world. The goal of this study was to encapsulate DAC into novel polyethylene glycol (PEG) decorated bilosomes (PEG-BILS) to achieve enhanced drug delivery to the liver.Methods: DAC-loaded BILS were primed by a thin film hydrating technique. The study of the impact of various formulation variables on the properties of BILS and selection of the optimal formulation was generated using Design-Expert® software. The optimum preparation was then pegylated via the incorporation of PEG-6-stearate (5% w/w, with respect to the lipid phase).Results: The optimum PEG-BILS formulation, containing PL:SDC ratio (5:1), 5 mg cholesterol, and 30 min sonication, yielded spherical vesicles in the nanoscale (200± 15.2 nm), elevated percent of entrapment efficiency (95.5± 7.77%), and a sustained release profile of DAC with 35.11± 2.3% release. In vivo and drug distribution studies revealed an enhanced hepatocellular delivery of DAC-loaded PEG-BILS compared to DAC-unPEG-BILS and DAC suspension, where DAC-PEG-BILS achieved 1.19- and 1.54 times the AUC0– 24 of DAC-unPEG-BILS and DAC suspension, respectively. Compared with DAC-unPEG-BILS and DAC suspension, DAC-PEG-BILS delivered about 2 and 3 times higher DAC into the liver, respectively.Conclusion: The innovative encapsulation of DAC-PEG-BILS has a great potential for liver targeting.Keywords: antiviral drug, nanodrug delivery system, bile-based nanovesicles, Box–Behnken approach, liver targeting parameters, pharmacokinetic, bioavailability
format	article
author	El-Nabarawi M Nafady M Elmenshawe S Elkarmalawy M Teaima M
author_facet	El-Nabarawi M Nafady M Elmenshawe S Elkarmalawy M Teaima M
author_sort	El-Nabarawi M
title	Liver Targeting of Daclatasvir via Tailoring Sterically Stabilized Bilosomes: Fabrication, Comparative In Vitro/In Vivo Appraisal and Biodistribution Studies
title_short	Liver Targeting of Daclatasvir via Tailoring Sterically Stabilized Bilosomes: Fabrication, Comparative In Vitro/In Vivo Appraisal and Biodistribution Studies
title_full	Liver Targeting of Daclatasvir via Tailoring Sterically Stabilized Bilosomes: Fabrication, Comparative In Vitro/In Vivo Appraisal and Biodistribution Studies
title_fullStr	Liver Targeting of Daclatasvir via Tailoring Sterically Stabilized Bilosomes: Fabrication, Comparative In Vitro/In Vivo Appraisal and Biodistribution Studies
title_full_unstemmed	Liver Targeting of Daclatasvir via Tailoring Sterically Stabilized Bilosomes: Fabrication, Comparative In Vitro/In Vivo Appraisal and Biodistribution Studies
title_sort	liver targeting of daclatasvir via tailoring sterically stabilized bilosomes: fabrication, comparative in vitro/in vivo appraisal and biodistribution studies
publisher	Dove Medical Press
publishDate	2021
url	https://doaj.org/article/a2aa5588f39c45a9b0ba265c8c74606d
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Liver Targeting of Daclatasvir via Tailoring Sterically Stabilized Bilosomes: Fabrication, Comparative In Vitro/In Vivo Appraisal and Biodistribution Studies

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