Physical pegylation enhances the cytotoxicity of 5-fluorouracil-loaded PLGA And PCL nanoparticles.

Purpose : 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...

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Main Authors: Ashour, Abdelkader Elbadawy Abbas, Badran, Mohamed M., Kumar, Ashok, Hussain, Tajamul, A Alsarra, Ibrahim, Yassin, Alaa Eldeen Bakry
Format: Article
Language:English
English
English
Published: Dove Medical Press 2019
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Online Access:http://irep.iium.edu.my/78959/
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http://irep.iium.edu.my/78959/1/Physical%20PEGylation%20Enhances%20The%20Cytotoxicity%20Of%205-Fluorouracil-Loaded%20PLGA%20And%20PCL%20Nanoparticles.pdf
http://irep.iium.edu.my/78959/7/78959_Physical%20pegylation%20enhances%20the%20cytotoxicity_scopus.pdf
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spelling iium-789592020-02-27T04:36:48Z http://irep.iium.edu.my/78959/ Physical pegylation enhances the cytotoxicity of 5-fluorouracil-loaded PLGA And PCL nanoparticles. Ashour, Abdelkader Elbadawy Abbas Badran, Mohamed M. Kumar, Ashok Hussain, Tajamul A Alsarra, Ibrahim Yassin, Alaa Eldeen Bakry RM300 Drugs and their action Purpose : 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. Dove Medical Press 2019 Article PeerReviewed application/pdf en http://irep.iium.edu.my/78959/1/Physical%20PEGylation%20Enhances%20The%20Cytotoxicity%20Of%205-Fluorouracil-Loaded%20PLGA%20And%20PCL%20Nanoparticles.pdf application/pdf en http://irep.iium.edu.my/78959/7/78959_Physical%20pegylation%20enhances%20the%20cytotoxicity_scopus.pdf application/pdf en http://irep.iium.edu.my/78959/8/78959_Physical%20pegylation%20enhances%20the%20cytotoxicity_wos.pdf Ashour, Abdelkader Elbadawy Abbas and Badran, Mohamed M. and Kumar, Ashok and Hussain, Tajamul and A Alsarra, Ibrahim and Yassin, Alaa Eldeen Bakry (2019) Physical pegylation enhances the cytotoxicity of 5-fluorouracil-loaded PLGA And PCL nanoparticles. International Journal of Nanomedicine, 14. pp. 9259-9273. ISSN 1176-9114 E-ISSN 1178-2013 https://www.dovepress.com/physical-pegylation-enhances-the-cytotoxicity-of-5-fluorouracil-loaded-peer-reviewed-article-IJN 10.2147/IJN.S223368
repository_type Digital Repository
institution_category Local University
institution International Islamic University Malaysia
building IIUM Repository
collection Online Access
language English
English
English
topic RM300 Drugs and their action
spellingShingle RM300 Drugs and their action
Ashour, Abdelkader Elbadawy Abbas
Badran, Mohamed M.
Kumar, Ashok
Hussain, Tajamul
A Alsarra, Ibrahim
Yassin, Alaa Eldeen Bakry
Physical pegylation enhances the cytotoxicity of 5-fluorouracil-loaded PLGA And PCL nanoparticles.
description Purpose : 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.
format Article
author Ashour, Abdelkader Elbadawy Abbas
Badran, Mohamed M.
Kumar, Ashok
Hussain, Tajamul
A Alsarra, Ibrahim
Yassin, Alaa Eldeen Bakry
author_facet Ashour, Abdelkader Elbadawy Abbas
Badran, Mohamed M.
Kumar, Ashok
Hussain, Tajamul
A Alsarra, Ibrahim
Yassin, Alaa Eldeen Bakry
author_sort Ashour, Abdelkader Elbadawy Abbas
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 http://irep.iium.edu.my/78959/
http://irep.iium.edu.my/78959/
http://irep.iium.edu.my/78959/
http://irep.iium.edu.my/78959/1/Physical%20PEGylation%20Enhances%20The%20Cytotoxicity%20Of%205-Fluorouracil-Loaded%20PLGA%20And%20PCL%20Nanoparticles.pdf
http://irep.iium.edu.my/78959/7/78959_Physical%20pegylation%20enhances%20the%20cytotoxicity_scopus.pdf
http://irep.iium.edu.my/78959/8/78959_Physical%20pegylation%20enhances%20the%20cytotoxicity_wos.pdf
first_indexed 2023-09-18T21:51:07Z
last_indexed 2023-09-18T21:51:07Z
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