Pomegranate extract-loaded solid lipid nanoparticles: design, optimization, and in vitro cytotoxicity study

Noha M Badawi,1 Mahmoud H Teaima,2 Khalid M El-Say,3 Dalia A Attia,1 Mohamed A El-Nabarawi,2 Mohey M Elmazar4 1Department of Pharmaceutics, Faculty of Pharmacy, The British University in Egypt, Cairo, Egypt; 2Department of Pharmaceutics and Industrial Pharmacy, Cairo University, Cairo, Egy...

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Autores principales: Badawi NM, Teaima MH, El-Say KM, Attia DA, El-Nabarawi MA, Elmazar MM
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Publicado: Dove Medical Press 2018
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spelling oai:doaj.org-article:7c155d184abc457db8b1bf771731f7322021-12-02T02:42:32ZPomegranate extract-loaded solid lipid nanoparticles: design, optimization, and in vitro cytotoxicity study1178-2013https://doaj.org/article/7c155d184abc457db8b1bf771731f7322018-03-01T00:00:00Zhttps://www.dovepress.com/pomegranate-extract-loaded-solid-lipid-nanoparticles-design-optimizati-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Noha M Badawi,1 Mahmoud H Teaima,2 Khalid M El-Say,3 Dalia A Attia,1 Mohamed A El-Nabarawi,2 Mohey M Elmazar4 1Department of Pharmaceutics, Faculty of Pharmacy, The British University in Egypt, Cairo, Egypt; 2Department of Pharmaceutics and Industrial Pharmacy, Cairo University, Cairo, Egypt; 3Department of Pharmaceutics, King Abdulaziz University, Jeddah, Saudi Arabia; 4Department of Pharmacology, Faculty of Pharmacy, The British University in Egypt, Cairo, Egypt Background: Pomegranate extract (PE) is a natural product with potent antioxidant and anticancer activity because of its polyphenols content. The main purpose of this study was to maximize the PE chemotherapeutic efficacy by loading it in an optimized solid lipid nanoparticles (SLNs) formula.Materials and methods: The influence of independent variables, which were lipid concentration (X1), surfactant concentration (X2) and cosurfactant concentration (X3), on dependent ones, which were particle size (Y1), polydispersity index (Y2), zeta potential (Y3), entrapment efficiency (Y4) and cumulative % drug release (Y5), were studied and optimized using the Box–Behnken design. Fifteen formulations of PE-SLNs were prepared using hot homogenization followed by ultra-sonication technique. Response surface plots, Pareto charts and mathematical equations were produced to study the impact of independent variables on the dependent quality parameters. The anti-proliferative activity of the optimized formula was then evaluated in three different cancer cell lines, namely, MCF-7, PC-3 and HepG-2, in addition to one normal cell line, HFB-4.Results: The results demonstrated that the particle sizes ranged from 407.5 to 651.9 nm and the entrapment efficiencies ranged from 56.02 to 65.23%. Interestingly, the 50% inhibitory concentration of the optimized formula had more than a 40-fold improved effect on the cell growth inhibition in comparison with its free counterpart. Furthermore, it was more selective against cancer cells than normal cells particularly in MCF-7 breast cancer cells.Conclusion: These data proved that nanoencapsulation of PE enhanced its anticancer efficacy. Therefore, our results suggested that a PE-loaded SLNs optimized-formula could be a promising chemo­therapeutic agent. Keywords: pomegranate extract, solid lipid nanoparticles, Box–Behnken design, optimization, cancer cell linesBadawi NMTeaima MHEl-Say KMAttia DAEl-Nabarawi MAElmazar MMDove Medical PressarticlePomegranate extractSolid lipid nanoparticlesBox–Behnken designoptimizationcancer cell linesMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 13, Pp 1313-1326 (2018)
institution DOAJ
collection DOAJ
language EN
topic Pomegranate extract
Solid lipid nanoparticles
Box–Behnken design
optimization
cancer cell lines
Medicine (General)
R5-920
spellingShingle Pomegranate extract
Solid lipid nanoparticles
Box–Behnken design
optimization
cancer cell lines
Medicine (General)
R5-920
Badawi NM
Teaima MH
El-Say KM
Attia DA
El-Nabarawi MA
Elmazar MM
Pomegranate extract-loaded solid lipid nanoparticles: design, optimization, and in vitro cytotoxicity study
description Noha M Badawi,1 Mahmoud H Teaima,2 Khalid M El-Say,3 Dalia A Attia,1 Mohamed A El-Nabarawi,2 Mohey M Elmazar4 1Department of Pharmaceutics, Faculty of Pharmacy, The British University in Egypt, Cairo, Egypt; 2Department of Pharmaceutics and Industrial Pharmacy, Cairo University, Cairo, Egypt; 3Department of Pharmaceutics, King Abdulaziz University, Jeddah, Saudi Arabia; 4Department of Pharmacology, Faculty of Pharmacy, The British University in Egypt, Cairo, Egypt Background: Pomegranate extract (PE) is a natural product with potent antioxidant and anticancer activity because of its polyphenols content. The main purpose of this study was to maximize the PE chemotherapeutic efficacy by loading it in an optimized solid lipid nanoparticles (SLNs) formula.Materials and methods: The influence of independent variables, which were lipid concentration (X1), surfactant concentration (X2) and cosurfactant concentration (X3), on dependent ones, which were particle size (Y1), polydispersity index (Y2), zeta potential (Y3), entrapment efficiency (Y4) and cumulative % drug release (Y5), were studied and optimized using the Box–Behnken design. Fifteen formulations of PE-SLNs were prepared using hot homogenization followed by ultra-sonication technique. Response surface plots, Pareto charts and mathematical equations were produced to study the impact of independent variables on the dependent quality parameters. The anti-proliferative activity of the optimized formula was then evaluated in three different cancer cell lines, namely, MCF-7, PC-3 and HepG-2, in addition to one normal cell line, HFB-4.Results: The results demonstrated that the particle sizes ranged from 407.5 to 651.9 nm and the entrapment efficiencies ranged from 56.02 to 65.23%. Interestingly, the 50% inhibitory concentration of the optimized formula had more than a 40-fold improved effect on the cell growth inhibition in comparison with its free counterpart. Furthermore, it was more selective against cancer cells than normal cells particularly in MCF-7 breast cancer cells.Conclusion: These data proved that nanoencapsulation of PE enhanced its anticancer efficacy. Therefore, our results suggested that a PE-loaded SLNs optimized-formula could be a promising chemo­therapeutic agent. Keywords: pomegranate extract, solid lipid nanoparticles, Box–Behnken design, optimization, cancer cell lines
format article
author Badawi NM
Teaima MH
El-Say KM
Attia DA
El-Nabarawi MA
Elmazar MM
author_facet Badawi NM
Teaima MH
El-Say KM
Attia DA
El-Nabarawi MA
Elmazar MM
author_sort Badawi NM
title Pomegranate extract-loaded solid lipid nanoparticles: design, optimization, and in vitro cytotoxicity study
title_short Pomegranate extract-loaded solid lipid nanoparticles: design, optimization, and in vitro cytotoxicity study
title_full Pomegranate extract-loaded solid lipid nanoparticles: design, optimization, and in vitro cytotoxicity study
title_fullStr Pomegranate extract-loaded solid lipid nanoparticles: design, optimization, and in vitro cytotoxicity study
title_full_unstemmed Pomegranate extract-loaded solid lipid nanoparticles: design, optimization, and in vitro cytotoxicity study
title_sort pomegranate extract-loaded solid lipid nanoparticles: design, optimization, and in vitro cytotoxicity study
publisher Dove Medical Press
publishDate 2018
url https://doaj.org/article/7c155d184abc457db8b1bf771731f732
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