Zein/Phospholipid Composite Nanoparticles for Successful Delivery of Gallic Acid into aHSCs: Influence of Size, Surface Charge, and Vitamin A Coupling

Shaimaa Ali Ali Radwan,1 Walaa H El-Maadawy,2 Carol Yousry,1 Aliaa Nabil ElMeshad,1 Raguia Aly Shoukri1 1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt; 2Department of Pharmacology, Theodor Bilharz Research Institute, Giza 12411, EgyptCorresp...

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Autores principales:	Radwan SAA, El-Maadawy WH, Yousry C, ElMeshad AN, Shoukri RA
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2020
Materias:	zein phospholipids gallic acid hepatic fibrosis hepatic stellate cells vitamin a Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/3f8680134c604911b758ae9a0b2d67ee
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spelling	oai:doaj.org-article:3f8680134c604911b758ae9a0b2d67ee2021-12-02T11:16:07ZZein/Phospholipid Composite Nanoparticles for Successful Delivery of Gallic Acid into aHSCs: Influence of Size, Surface Charge, and Vitamin A Coupling1178-2013https://doaj.org/article/3f8680134c604911b758ae9a0b2d67ee2020-10-01T00:00:00Zhttps://test.dovepress.com/zeinphospholipid-composite-nanoparticles-for-successful-delivery-of-ga-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Shaimaa Ali Ali Radwan,1 Walaa H El-Maadawy,2 Carol Yousry,1 Aliaa Nabil ElMeshad,1 Raguia Aly Shoukri1 1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt; 2Department of Pharmacology, Theodor Bilharz Research Institute, Giza 12411, EgyptCorrespondence: Aliaa Nabil ElMeshadDepartment of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr Al Aini Street, Cairo 11562, EgyptTel +201000101551Email aliaa.elmeshad@pharma.cu.edu.egPurpose: Zein/phospholipid composite nanoparticles (CNPs) were developed as a delivery platform for gallic acid (GA), a polyphenolic compound with reported preclinical antifibrotic activities. However, the therapeutic applicability of GA is hampered owing to its low bioavailability and rapid clearance. Accordingly, we developed GA-loaded CNPs. The effect of their size, surface charge and targeting strategies was investigated and optimized, with the aim of enhancing their ability to deliver GA to the activated hepatic stellate cells (aHSCs) in order to suppress hepatic fibrosis progression.Methods: Different CNP systems were prepared and characterized with regard to their particle size, zeta potential, and GA entrapment efficiency (EE%). Also, they were statistically optimized via response surface methodology. The optimized systems were investigated with regard to their in vitro GA release, in vitro efficacy on aHSCs, and in vivo biodistribution in healthy rats.Results: The GA-loaded cationic CNPs coupled with vitamin A (GA-CACNP/VA; 192 nm) showed high GA EE% (60% w/w), highest cellular internalization via active targeting, and more selective hepatic distribution, relative to free GA solution, GA-loaded anionic, and GA-loaded cationic systems. Furthermore, GA-CACNP/VA markedly triggered the apoptosis of aHSCs, repressed collagen deposition, and inhibited HSCs’ activation to a lesser extent.Conclusion: The GA-CACNP/VA was shown to be a promising candidate for specific and controlled delivery of GA to aHSCs, which may provide an effective antifibrotic therapeutic approach.Keywords: zein, phospholipids, gallic acid, hepatic fibrosis, hepatic stellate cells, vitamin ARadwan SAAEl-Maadawy WHYousry CElMeshad ANShoukri RADove Medical Pressarticlezeinphospholipidsgallic acidhepatic fibrosishepatic stellate cellsvitamin aMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 15, Pp 7995-8018 (2020)
institution	DOAJ
collection	DOAJ
language	EN
topic	zein phospholipids gallic acid hepatic fibrosis hepatic stellate cells vitamin a Medicine (General) R5-920
spellingShingle	zein phospholipids gallic acid hepatic fibrosis hepatic stellate cells vitamin a Medicine (General) R5-920 Radwan SAA El-Maadawy WH Yousry C ElMeshad AN Shoukri RA Zein/Phospholipid Composite Nanoparticles for Successful Delivery of Gallic Acid into aHSCs: Influence of Size, Surface Charge, and Vitamin A Coupling
description	Shaimaa Ali Ali Radwan,1 Walaa H El-Maadawy,2 Carol Yousry,1 Aliaa Nabil ElMeshad,1 Raguia Aly Shoukri1 1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt; 2Department of Pharmacology, Theodor Bilharz Research Institute, Giza 12411, EgyptCorrespondence: Aliaa Nabil ElMeshadDepartment of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr Al Aini Street, Cairo 11562, EgyptTel +201000101551Email aliaa.elmeshad@pharma.cu.edu.egPurpose: Zein/phospholipid composite nanoparticles (CNPs) were developed as a delivery platform for gallic acid (GA), a polyphenolic compound with reported preclinical antifibrotic activities. However, the therapeutic applicability of GA is hampered owing to its low bioavailability and rapid clearance. Accordingly, we developed GA-loaded CNPs. The effect of their size, surface charge and targeting strategies was investigated and optimized, with the aim of enhancing their ability to deliver GA to the activated hepatic stellate cells (aHSCs) in order to suppress hepatic fibrosis progression.Methods: Different CNP systems were prepared and characterized with regard to their particle size, zeta potential, and GA entrapment efficiency (EE%). Also, they were statistically optimized via response surface methodology. The optimized systems were investigated with regard to their in vitro GA release, in vitro efficacy on aHSCs, and in vivo biodistribution in healthy rats.Results: The GA-loaded cationic CNPs coupled with vitamin A (GA-CACNP/VA; 192 nm) showed high GA EE% (60% w/w), highest cellular internalization via active targeting, and more selective hepatic distribution, relative to free GA solution, GA-loaded anionic, and GA-loaded cationic systems. Furthermore, GA-CACNP/VA markedly triggered the apoptosis of aHSCs, repressed collagen deposition, and inhibited HSCs’ activation to a lesser extent.Conclusion: The GA-CACNP/VA was shown to be a promising candidate for specific and controlled delivery of GA to aHSCs, which may provide an effective antifibrotic therapeutic approach.Keywords: zein, phospholipids, gallic acid, hepatic fibrosis, hepatic stellate cells, vitamin A
format	article
author	Radwan SAA El-Maadawy WH Yousry C ElMeshad AN Shoukri RA
author_facet	Radwan SAA El-Maadawy WH Yousry C ElMeshad AN Shoukri RA
author_sort	Radwan SAA
title	Zein/Phospholipid Composite Nanoparticles for Successful Delivery of Gallic Acid into aHSCs: Influence of Size, Surface Charge, and Vitamin A Coupling
title_short	Zein/Phospholipid Composite Nanoparticles for Successful Delivery of Gallic Acid into aHSCs: Influence of Size, Surface Charge, and Vitamin A Coupling
title_full	Zein/Phospholipid Composite Nanoparticles for Successful Delivery of Gallic Acid into aHSCs: Influence of Size, Surface Charge, and Vitamin A Coupling
title_fullStr	Zein/Phospholipid Composite Nanoparticles for Successful Delivery of Gallic Acid into aHSCs: Influence of Size, Surface Charge, and Vitamin A Coupling
title_full_unstemmed	Zein/Phospholipid Composite Nanoparticles for Successful Delivery of Gallic Acid into aHSCs: Influence of Size, Surface Charge, and Vitamin A Coupling
title_sort	zein/phospholipid composite nanoparticles for successful delivery of gallic acid into ahscs: influence of size, surface charge, and vitamin a coupling
publisher	Dove Medical Press
publishDate	2020
url	https://doaj.org/article/3f8680134c604911b758ae9a0b2d67ee
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Zein/Phospholipid Composite Nanoparticles for Successful Delivery of Gallic Acid into aHSCs: Influence of Size, Surface Charge, and Vitamin A Coupling

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