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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2019
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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 |
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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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