Physical PEGylation Enhances The Cytotoxicity Of 5-Fluorouracil-Loaded PLGA And PCL Nanoparticles

Abdelkader E Ashour,1,2 Mohammad Badran,3 Ashok Kumar,4 Tajamul Hussain,5 Ibrahim A Alsarra,3 Alaa Eldeen B Yassin3,6,7 1Department of Pharmacology and Toxicology, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia; 2Department of Basic Medical Sciences, Kulliyyah of Medicine, Internati...

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Autores principales:	Ashour AE, Badran M, Kumar A, Hussain T, Alsarra IA, Yassin AEB
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2019
Materias:	hepatocellular carcinoma hepg2 emulsification-solvent evaporation technique colorectal carcinoma ht-29 mtt assay apoptosis. Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/7516dedb80cb4fb7bfbe00af02e9bbc4
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spelling	oai:doaj.org-article:7516dedb80cb4fb7bfbe00af02e9bbc42021-12-02T04:40:31ZPhysical PEGylation Enhances The Cytotoxicity Of 5-Fluorouracil-Loaded PLGA And PCL Nanoparticles1178-2013https://doaj.org/article/7516dedb80cb4fb7bfbe00af02e9bbc42019-11-01T00:00:00Zhttps://www.dovepress.com/physical-pegylation-enhances-the-cytotoxicity-of-5-fluorouracil-loaded-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Abdelkader E Ashour,1,2 Mohammad Badran,3 Ashok Kumar,4 Tajamul Hussain,5 Ibrahim A Alsarra,3 Alaa Eldeen B Yassin3,6,7 1Department of Pharmacology and Toxicology, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia; 2Department of Basic Medical Sciences, Kulliyyah of Medicine, International Islamic University Malaysia, Kuantan 25200, Pahang Darul Makmur, Malaysia; 3Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia; 4Vitiligo Research Chair, College of Medicine, King Saud University, Riyadh, Saudi Arabia; 5Center of Excellence in Biotechnology Research, King Saud University, Riyadh, KSA; 6Pharmaceutical Sciences Department, College of Pharmacy-3163, King Saud Bin Abdulaziz University for Health Sciences, Riyadh, Saudi Arabia; 7King Abdullah International Medical Research Center, Ministry of National Guard, Health Affairs, Riyadh, Saudi ArabiaCorrespondence: Alaa Eldeen B YassinCollege of Pharmacy-3163 King Saud bin Abdulaziz University for Health Sciences PO Box: 3660, Riyadh 11481, Saudi ArabiaTel +966509426323Fax +966114295058Email yassina@ksau-hs.edu.saPurpose: The main goal of this study is to evaluate the impact of physical incorporation of polyethylene glycol (PEG) into 5-fluorouracil (5-FU)-loaded polymeric nanoparticles (NPs).Methods: The 5-FU-loaded NPs were prepared utilizing a simple double emulsion method using polycaprolactone (PCL) and polylactic-co-glycolic acid (PLGA) with or without PEG 6000. The surface charge, particle size, and shape of NPs were evaluated by standard procedures. Both Fourier Transform Infrared Spectroscopy and X-ray diffraction spectra of the 5-FU loaded NPs were compared against the pure 5-FU. The in vitro release profile of 5-FU from the NPs was monitored by the dialysis tubing method. Cell death and apoptosis induction in response to 5-FU NP exposure were measured by MTT and Annexin–V/7-amino-actinomycin D (7-AAD) assays, respectively, in Daoy, HepG2, and HT-29 cancer cell lines.Results: The 5-FU loaded NPs were found to be spherical in shape with size ranging between 176±6.7 and 253.9±8.6 nm. The zeta potential varied between −7.13± 0.13 and −27.06±3.18 mV, and the entrapment efficiency was between 31.96% and 74.09%. The in vitro release of the drug followed a two-phase mode characterized by rapid release in the first 8 hrs followed by a period of slow release up to 72 hrs with composition-based variable extents. Cells exposed to NPs demonstrated a significant cell death which correlated with the ratio of PEG in the formulations in Daoy and HepG2 cells but not in HT-29 cells. Formulations (F1–F3) significantly induced early apoptosis in HT-29 cell lines.Conclusion: The physical PEGylation significantly enhanced the entrapment and loading efficiencies of 5-FU into NPs formulated with PLGA and PCL. It also fostered the in vitro cytotoxicity of 5-FU-loaded NPs in both Daoy and HepG2 cells. Induction of early apoptosis was confirmed for some of the formulations.Keywords: hepatocellular carcinoma HepG2, emulsification-solvent evaporation technique, colorectal carcinoma HT-29, MTT assay, apoptosisAshour AEBadran MKumar AHussain TAlsarra IAYassin AEBDove Medical Pressarticlehepatocellular carcinoma hepg2emulsification-solvent evaporation techniquecolorectal carcinoma ht-29mtt assayapoptosis.Medicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 14, Pp 9259-9273 (2019)
institution	DOAJ
collection	DOAJ
language	EN
topic	hepatocellular carcinoma hepg2 emulsification-solvent evaporation technique colorectal carcinoma ht-29 mtt assay apoptosis. Medicine (General) R5-920
spellingShingle	hepatocellular carcinoma hepg2 emulsification-solvent evaporation technique colorectal carcinoma ht-29 mtt assay apoptosis. Medicine (General) R5-920 Ashour AE Badran M Kumar A Hussain T Alsarra IA Yassin AEB Physical PEGylation Enhances The Cytotoxicity Of 5-Fluorouracil-Loaded PLGA And PCL Nanoparticles
description	Abdelkader E Ashour,1,2 Mohammad Badran,3 Ashok Kumar,4 Tajamul Hussain,5 Ibrahim A Alsarra,3 Alaa Eldeen B Yassin3,6,7 1Department of Pharmacology and Toxicology, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia; 2Department of Basic Medical Sciences, Kulliyyah of Medicine, International Islamic University Malaysia, Kuantan 25200, Pahang Darul Makmur, Malaysia; 3Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia; 4Vitiligo Research Chair, College of Medicine, King Saud University, Riyadh, Saudi Arabia; 5Center of Excellence in Biotechnology Research, King Saud University, Riyadh, KSA; 6Pharmaceutical Sciences Department, College of Pharmacy-3163, King Saud Bin Abdulaziz University for Health Sciences, Riyadh, Saudi Arabia; 7King Abdullah International Medical Research Center, Ministry of National Guard, Health Affairs, Riyadh, Saudi ArabiaCorrespondence: Alaa Eldeen B YassinCollege of Pharmacy-3163 King Saud bin Abdulaziz University for Health Sciences PO Box: 3660, Riyadh 11481, Saudi ArabiaTel +966509426323Fax +966114295058Email yassina@ksau-hs.edu.saPurpose: The main goal of this study is to evaluate the impact of physical incorporation of polyethylene glycol (PEG) into 5-fluorouracil (5-FU)-loaded polymeric nanoparticles (NPs).Methods: The 5-FU-loaded NPs were prepared utilizing a simple double emulsion method using polycaprolactone (PCL) and polylactic-co-glycolic acid (PLGA) with or without PEG 6000. The surface charge, particle size, and shape of NPs were evaluated by standard procedures. Both Fourier Transform Infrared Spectroscopy and X-ray diffraction spectra of the 5-FU loaded NPs were compared against the pure 5-FU. The in vitro release profile of 5-FU from the NPs was monitored by the dialysis tubing method. Cell death and apoptosis induction in response to 5-FU NP exposure were measured by MTT and Annexin–V/7-amino-actinomycin D (7-AAD) assays, respectively, in Daoy, HepG2, and HT-29 cancer cell lines.Results: The 5-FU loaded NPs were found to be spherical in shape with size ranging between 176±6.7 and 253.9±8.6 nm. The zeta potential varied between −7.13± 0.13 and −27.06±3.18 mV, and the entrapment efficiency was between 31.96% and 74.09%. The in vitro release of the drug followed a two-phase mode characterized by rapid release in the first 8 hrs followed by a period of slow release up to 72 hrs with composition-based variable extents. Cells exposed to NPs demonstrated a significant cell death which correlated with the ratio of PEG in the formulations in Daoy and HepG2 cells but not in HT-29 cells. Formulations (F1–F3) significantly induced early apoptosis in HT-29 cell lines.Conclusion: The physical PEGylation significantly enhanced the entrapment and loading efficiencies of 5-FU into NPs formulated with PLGA and PCL. It also fostered the in vitro cytotoxicity of 5-FU-loaded NPs in both Daoy and HepG2 cells. Induction of early apoptosis was confirmed for some of the formulations.Keywords: hepatocellular carcinoma HepG2, emulsification-solvent evaporation technique, colorectal carcinoma HT-29, MTT assay, apoptosis
format	article
author	Ashour AE Badran M Kumar A Hussain T Alsarra IA Yassin AEB
author_facet	Ashour AE Badran M Kumar A Hussain T Alsarra IA Yassin AEB
author_sort	Ashour AE
title	Physical PEGylation Enhances The Cytotoxicity Of 5-Fluorouracil-Loaded PLGA And PCL Nanoparticles
title_short	Physical PEGylation Enhances The Cytotoxicity Of 5-Fluorouracil-Loaded PLGA And PCL Nanoparticles
title_full	Physical PEGylation Enhances The Cytotoxicity Of 5-Fluorouracil-Loaded PLGA And PCL Nanoparticles
title_fullStr	Physical PEGylation Enhances The Cytotoxicity Of 5-Fluorouracil-Loaded PLGA And PCL Nanoparticles
title_full_unstemmed	Physical PEGylation Enhances The Cytotoxicity Of 5-Fluorouracil-Loaded PLGA And PCL Nanoparticles
title_sort	physical pegylation enhances the cytotoxicity of 5-fluorouracil-loaded plga and pcl nanoparticles
publisher	Dove Medical Press
publishDate	2019
url	https://doaj.org/article/7516dedb80cb4fb7bfbe00af02e9bbc4
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Physical PEGylation Enhances The Cytotoxicity Of 5-Fluorouracil-Loaded PLGA And PCL Nanoparticles

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