Stealth, biocompatible monoolein-based lyotropic liquid crystalline nanoparticles for enhanced aloe-emodin delivery to breast cancer cells: in vitro and in vivo studies

May S Freag,1 Yosra SR Elnaggar,1,2 Doaa A Abdelmonsif,3 Ossama Y Abdallah1 1Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, 2Department of Pharmaceutics, Faculty of Pharmacy and Drug Manufacturing, Pharos University in Alexandria, 3Department of Medical Biochemistry, Facul...

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Autores principales:	Freag MS, Elnaggar YSR, Abdelmonsif DA, Abdallah OY
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2016
Materias:	Aloe-emodin Anticancer Breast cancer cell line Liquid crystalline nanoparticles Monoolein Pharmacokinetics Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/bfd70363c4d040febcf8fe716c29610d
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spelling	oai:doaj.org-article:bfd70363c4d040febcf8fe716c29610d2021-12-02T07:28:29ZStealth, biocompatible monoolein-based lyotropic liquid crystalline nanoparticles for enhanced aloe-emodin delivery to breast cancer cells: in vitro and in vivo studies1178-2013https://doaj.org/article/bfd70363c4d040febcf8fe716c29610d2016-09-01T00:00:00Zhttps://www.dovepress.com/stealth-biocompatible-monoolein-based-lyotropic-liquid-crystalline-nan-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013May S Freag,1 Yosra SR Elnaggar,1,2 Doaa A Abdelmonsif,3 Ossama Y Abdallah1 1Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, 2Department of Pharmaceutics, Faculty of Pharmacy and Drug Manufacturing, Pharos University in Alexandria, 3Department of Medical Biochemistry, Faculty of Medicine, Alexandria University, Alexandria, Egypt Abstract: Recently, research has progressively highlighted on clues from conventional use of herbal medicines to introduce new anticancer drugs. Aloe-emodin (AE) is a herbal drug with promising anticancer activity. Nevertheless, its clinical utility is handicapped by its low solubility. For the first time, this study aims to the fabrication of surface-functionalized polyethylene glycol liquid crystalline nanoparticles (PEG-LCNPs) of AE to enhance its water solubility and enable its anticancer use. Developed AE-PEG-LCNPs were optimized via particle size and zeta potential measurements. Phase behavior, solid state characteristics, hemocompatibility, and serum stability of LCNPs were assessed. Sterile formulations were developed using various sterilization technologies. Furthermore, the potential of the formulations was investigated using cell culture, pharmacokinetics, biodistribution, and toxicity studies. AE-PEG-LCNPs showed particle size of 190 nm and zeta potential of -49.9, and PEGylation approach reduced the monoolein hemolytic tendency to 3% and increased the serum stability of the nanoparticles. Sterilization of liquid and lyophilized AE-PEG-LCNPs via autoclaving and γ-radiations, respectively, insignificantly affected the physicochemical properties of the nanoparticles. Half maximal inhibitory concentration of AE-PEG-LCNPs was 3.6-fold lower than free AE after 48 hours and their cellular uptake was threefold higher than free AE after 24-hour incubation. AE-PEG-LCNPs presented 5.4-fold increase in t1/2 compared with free AE. Biodistribution and toxicity studies showed reduced AE-PEG-LCNP uptake by reticuloendothelial system organs and good safety profile. PEGylated LCNPs could serve as a promising nanocarrier for efficient delivery of AE to cancerous cells. Keywords: aloe-emodin, anticancer, breast cancer cell line, liquid crystalline nanoparticles, monoolein, pharmacokineticsFreag MSElnaggar YSRAbdelmonsif DAAbdallah OYDove Medical PressarticleAloe-emodinAnticancerBreast cancer cell lineLiquid crystalline nanoparticlesMonooleinPharmacokineticsMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 11, Pp 4799-4818 (2016)
institution	DOAJ
collection	DOAJ
language	EN
topic	Aloe-emodin Anticancer Breast cancer cell line Liquid crystalline nanoparticles Monoolein Pharmacokinetics Medicine (General) R5-920
spellingShingle	Aloe-emodin Anticancer Breast cancer cell line Liquid crystalline nanoparticles Monoolein Pharmacokinetics Medicine (General) R5-920 Freag MS Elnaggar YSR Abdelmonsif DA Abdallah OY Stealth, biocompatible monoolein-based lyotropic liquid crystalline nanoparticles for enhanced aloe-emodin delivery to breast cancer cells: in vitro and in vivo studies
description	May S Freag,1 Yosra SR Elnaggar,1,2 Doaa A Abdelmonsif,3 Ossama Y Abdallah1 1Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, 2Department of Pharmaceutics, Faculty of Pharmacy and Drug Manufacturing, Pharos University in Alexandria, 3Department of Medical Biochemistry, Faculty of Medicine, Alexandria University, Alexandria, Egypt Abstract: Recently, research has progressively highlighted on clues from conventional use of herbal medicines to introduce new anticancer drugs. Aloe-emodin (AE) is a herbal drug with promising anticancer activity. Nevertheless, its clinical utility is handicapped by its low solubility. For the first time, this study aims to the fabrication of surface-functionalized polyethylene glycol liquid crystalline nanoparticles (PEG-LCNPs) of AE to enhance its water solubility and enable its anticancer use. Developed AE-PEG-LCNPs were optimized via particle size and zeta potential measurements. Phase behavior, solid state characteristics, hemocompatibility, and serum stability of LCNPs were assessed. Sterile formulations were developed using various sterilization technologies. Furthermore, the potential of the formulations was investigated using cell culture, pharmacokinetics, biodistribution, and toxicity studies. AE-PEG-LCNPs showed particle size of 190 nm and zeta potential of -49.9, and PEGylation approach reduced the monoolein hemolytic tendency to 3% and increased the serum stability of the nanoparticles. Sterilization of liquid and lyophilized AE-PEG-LCNPs via autoclaving and γ-radiations, respectively, insignificantly affected the physicochemical properties of the nanoparticles. Half maximal inhibitory concentration of AE-PEG-LCNPs was 3.6-fold lower than free AE after 48 hours and their cellular uptake was threefold higher than free AE after 24-hour incubation. AE-PEG-LCNPs presented 5.4-fold increase in t1/2 compared with free AE. Biodistribution and toxicity studies showed reduced AE-PEG-LCNP uptake by reticuloendothelial system organs and good safety profile. PEGylated LCNPs could serve as a promising nanocarrier for efficient delivery of AE to cancerous cells. Keywords: aloe-emodin, anticancer, breast cancer cell line, liquid crystalline nanoparticles, monoolein, pharmacokinetics
format	article
author	Freag MS Elnaggar YSR Abdelmonsif DA Abdallah OY
author_facet	Freag MS Elnaggar YSR Abdelmonsif DA Abdallah OY
author_sort	Freag MS
title	Stealth, biocompatible monoolein-based lyotropic liquid crystalline nanoparticles for enhanced aloe-emodin delivery to breast cancer cells: in vitro and in vivo studies
title_short	Stealth, biocompatible monoolein-based lyotropic liquid crystalline nanoparticles for enhanced aloe-emodin delivery to breast cancer cells: in vitro and in vivo studies
title_full	Stealth, biocompatible monoolein-based lyotropic liquid crystalline nanoparticles for enhanced aloe-emodin delivery to breast cancer cells: in vitro and in vivo studies
title_fullStr	Stealth, biocompatible monoolein-based lyotropic liquid crystalline nanoparticles for enhanced aloe-emodin delivery to breast cancer cells: in vitro and in vivo studies
title_full_unstemmed	Stealth, biocompatible monoolein-based lyotropic liquid crystalline nanoparticles for enhanced aloe-emodin delivery to breast cancer cells: in vitro and in vivo studies
title_sort	stealth, biocompatible monoolein-based lyotropic liquid crystalline nanoparticles for enhanced aloe-emodin delivery to breast cancer cells: in vitro and in vivo studies
publisher	Dove Medical Press
publishDate	2016
url	https://doaj.org/article/bfd70363c4d040febcf8fe716c29610d
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Stealth, biocompatible monoolein-based lyotropic liquid crystalline nanoparticles for enhanced aloe-emodin delivery to breast cancer cells: in vitro and in vivo studies

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