Enhanced anticancer activity and oral bioavailability of ellagic acid through encapsulation in biodegradable polymeric nanoparticles

Fatma M Mady,1,2 Mohamed A Shaker1,3 1Pharmaceutics and Pharmaceutical Technology Department, College of Pharmacy, Taibah University, Al Madina Al Munawara, Saudi Arabia; 2Pharmaceutics Department, Faculty of Pharmacy, Minia University, Minia, 3Pharmaceutics Department, Faculty of Pharmacy, Helwan...

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Autores principales:	Mady FM, Shaker MA
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2017
Materias:	Nanoparticles Ellagic acid Poly ε-caprolactone Bioavailability Cytotoxicity Oral administration. Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/23fbd974770743f0a52f7661a1c441fb
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spelling	oai:doaj.org-article:23fbd974770743f0a52f7661a1c441fb2021-12-02T00:43:21ZEnhanced anticancer activity and oral bioavailability of ellagic acid through encapsulation in biodegradable polymeric nanoparticles1178-2013https://doaj.org/article/23fbd974770743f0a52f7661a1c441fb2017-10-01T00:00:00Zhttps://www.dovepress.com/enhanced-anticancer-activity-and-oral-bioavailability-of-ellagic-acid--peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Fatma M Mady,1,2 Mohamed A Shaker1,3 1Pharmaceutics and Pharmaceutical Technology Department, College of Pharmacy, Taibah University, Al Madina Al Munawara, Saudi Arabia; 2Pharmaceutics Department, Faculty of Pharmacy, Minia University, Minia, 3Pharmaceutics Department, Faculty of Pharmacy, Helwan University, Cairo, Egypt Abstract: Despite the fact that various studies have investigated the clinical relevance of ellagic acid (EA) as a naturally existing bioactive substance in cancer therapy, little has been reported regarding the efficient strategy for improving its oral bioavailability. In this study, we report the formulation of EA-loaded nanoparticles (EA-NPs) to find a way to enhance its bioactivity as well as bioavailability after oral administration. Poly(ε-caprolactone) (PCL) was selected as the biodegradable polymer for the formulation of EA-NPs through the emulsion–diffusion–evaporation technique. The obtained NPs have been characterized by measuring particle size, zeta potential, Fourier transform infrared, differential scanning calorimetry, and X-ray diffraction. The entrapment efficiency and the release profile of EA was also determined. In vitro cellular uptake and cytotoxicity of the obtained NPs were evaluated using Caco-2 and HCT-116 cell lines, respectively. Moreover, in vivo study has been performed to measure the oral bioavailability of EA-NPs compared to free EA, using New Zealand white rabbits. NPs with distinct shape were obtained with high entrapment and loading efficiencies. Diffusion-driven release profile of EA from the prepared NPs was determined. EA-NP-treated HCT-116 cells showed relatively lower cell viability compared to free EA-treated cells. Fluorometric imaging revealed the cellular uptake and efficient localization of EA-NPs in the nuclear region of Caco-2 cells. In vivo testing revealed that the oral administration of EA-NPs produced a 3.6 times increase in the area under the curve compared to that of EA. From these results, it can be concluded that incorporation of EA into PCL as NPs enhances its oral bioavailability and activity. Keywords: nanoparticles, ellagic acid, poly(ε-caprolactone), bioavailability, cytotoxicity, oral administrationMady FMShaker MADove Medical PressarticleNanoparticlesEllagic acidPoly ε-caprolactoneBioavailabilityCytotoxicityOral administration.Medicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 12, Pp 7405-7417 (2017)
institution	DOAJ
collection	DOAJ
language	EN
topic	Nanoparticles Ellagic acid Poly ε-caprolactone Bioavailability Cytotoxicity Oral administration. Medicine (General) R5-920
spellingShingle	Nanoparticles Ellagic acid Poly ε-caprolactone Bioavailability Cytotoxicity Oral administration. Medicine (General) R5-920 Mady FM Shaker MA Enhanced anticancer activity and oral bioavailability of ellagic acid through encapsulation in biodegradable polymeric nanoparticles
description	Fatma M Mady,1,2 Mohamed A Shaker1,3 1Pharmaceutics and Pharmaceutical Technology Department, College of Pharmacy, Taibah University, Al Madina Al Munawara, Saudi Arabia; 2Pharmaceutics Department, Faculty of Pharmacy, Minia University, Minia, 3Pharmaceutics Department, Faculty of Pharmacy, Helwan University, Cairo, Egypt Abstract: Despite the fact that various studies have investigated the clinical relevance of ellagic acid (EA) as a naturally existing bioactive substance in cancer therapy, little has been reported regarding the efficient strategy for improving its oral bioavailability. In this study, we report the formulation of EA-loaded nanoparticles (EA-NPs) to find a way to enhance its bioactivity as well as bioavailability after oral administration. Poly(ε-caprolactone) (PCL) was selected as the biodegradable polymer for the formulation of EA-NPs through the emulsion–diffusion–evaporation technique. The obtained NPs have been characterized by measuring particle size, zeta potential, Fourier transform infrared, differential scanning calorimetry, and X-ray diffraction. The entrapment efficiency and the release profile of EA was also determined. In vitro cellular uptake and cytotoxicity of the obtained NPs were evaluated using Caco-2 and HCT-116 cell lines, respectively. Moreover, in vivo study has been performed to measure the oral bioavailability of EA-NPs compared to free EA, using New Zealand white rabbits. NPs with distinct shape were obtained with high entrapment and loading efficiencies. Diffusion-driven release profile of EA from the prepared NPs was determined. EA-NP-treated HCT-116 cells showed relatively lower cell viability compared to free EA-treated cells. Fluorometric imaging revealed the cellular uptake and efficient localization of EA-NPs in the nuclear region of Caco-2 cells. In vivo testing revealed that the oral administration of EA-NPs produced a 3.6 times increase in the area under the curve compared to that of EA. From these results, it can be concluded that incorporation of EA into PCL as NPs enhances its oral bioavailability and activity. Keywords: nanoparticles, ellagic acid, poly(ε-caprolactone), bioavailability, cytotoxicity, oral administration
format	article
author	Mady FM Shaker MA
author_facet	Mady FM Shaker MA
author_sort	Mady FM
title	Enhanced anticancer activity and oral bioavailability of ellagic acid through encapsulation in biodegradable polymeric nanoparticles
title_short	Enhanced anticancer activity and oral bioavailability of ellagic acid through encapsulation in biodegradable polymeric nanoparticles
title_full	Enhanced anticancer activity and oral bioavailability of ellagic acid through encapsulation in biodegradable polymeric nanoparticles
title_fullStr	Enhanced anticancer activity and oral bioavailability of ellagic acid through encapsulation in biodegradable polymeric nanoparticles
title_full_unstemmed	Enhanced anticancer activity and oral bioavailability of ellagic acid through encapsulation in biodegradable polymeric nanoparticles
title_sort	enhanced anticancer activity and oral bioavailability of ellagic acid through encapsulation in biodegradable polymeric nanoparticles
publisher	Dove Medical Press
publishDate	2017
url	https://doaj.org/article/23fbd974770743f0a52f7661a1c441fb
work_keys_str_mv	AT madyfm enhancedanticanceractivityandoralbioavailabilityofellagicacidthroughencapsulationinbiodegradablepolymericnanoparticles AT shakerma enhancedanticanceractivityandoralbioavailabilityofellagicacidthroughencapsulationinbiodegradablepolymericnanoparticles
_version_	1718403480906891264

Enhanced anticancer activity and oral bioavailability of ellagic acid through encapsulation in biodegradable polymeric nanoparticles

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