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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Dove Medical Press
2021-09-01
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| Series: | International Journal of Nanomedicine |
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| Online Access: | https://www.dovepress.com/liver-targeting-of-daclatasvir-via-tailoring-sterically-stabilized-bil-peer-reviewed-fulltext-article-IJN |
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| 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 |
| collection | DOAJ |
| 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 |
| first_indexed | 2024-12-19T02:37:38Z |
| format | Article |
| id | doaj.art-a2aa5588f39c45a9b0ba265c8c74606d |
| institution | Directory Open Access Journal |
| issn | 1178-2013 |
| language | English |
| last_indexed | 2024-12-19T02:37:38Z |
| publishDate | 2021-09-01 |
| publisher | Dove Medical Press |
| record_format | Article |
| series | International Journal of Nanomedicine |
| spelling | doaj.art-a2aa5588f39c45a9b0ba265c8c74606d2022-12-21T20:39:19ZengDove Medical PressInternational Journal of Nanomedicine1178-20132021-09-01Volume 166413642668943Liver Targeting of Daclatasvir via Tailoring Sterically Stabilized Bilosomes: Fabrication, Comparative In Vitro/In Vivo Appraisal and Biodistribution StudiesEl-Nabarawi MNafady MElmenshawe SElkarmalawy MTeaima MMohamed 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, bioavailabilityhttps://www.dovepress.com/liver-targeting-of-daclatasvir-via-tailoring-sterically-stabilized-bil-peer-reviewed-fulltext-article-IJNantiviral drug – nano drug delivery system- bile based nano-vesicles- box-behnken approach -liver targeting parameters – pharmacokinetic- bioavailability |
| spellingShingle | 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 International Journal of Nanomedicine antiviral drug – nano drug delivery system- bile based nano-vesicles- box-behnken approach -liver targeting parameters – pharmacokinetic- bioavailability |
| title | 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_short | 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 |
| topic | antiviral drug – nano drug delivery system- bile based nano-vesicles- box-behnken approach -liver targeting parameters – pharmacokinetic- bioavailability |
| url | https://www.dovepress.com/liver-targeting-of-daclatasvir-via-tailoring-sterically-stabilized-bil-peer-reviewed-fulltext-article-IJN |
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