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Eluxadoline Loaded Solid Lipid Nanoparticles for Improved Colon Targeting in Rat Model of Ulcerative Colitis
The aim of the current study was to evaluate the therapeutics potential of eluxadoline (ELX) loaded solid lipid nanoparticles (SLNs) in ulcerative colitis. ELX loaded SLNs were prepared using three different lipids according to the solvent emulsification technique. The optimization of prepared SLNs...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2020
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7559404/ https://www.ncbi.nlm.nih.gov/pubmed/32961713 http://dx.doi.org/10.3390/ph13090255 |
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author | Anwer, Md. Khalid Ahmed, Mohammed Muqtader Aldawsari, Mohammed F. Alshahrani, Saad Fatima, Farhat Ansari, Mohd Nazam Rehman, Najeeb Ur Al-Shdefat, Ramadan I. |
author_facet | Anwer, Md. Khalid Ahmed, Mohammed Muqtader Aldawsari, Mohammed F. Alshahrani, Saad Fatima, Farhat Ansari, Mohd Nazam Rehman, Najeeb Ur Al-Shdefat, Ramadan I. |
author_sort | Anwer, Md. Khalid |
collection | PubMed |
description | The aim of the current study was to evaluate the therapeutics potential of eluxadoline (ELX) loaded solid lipid nanoparticles (SLNs) in ulcerative colitis. ELX loaded SLNs were prepared using three different lipids according to the solvent emulsification technique. The optimization of prepared SLNs (F1-F3) were carried out based on size, PDI, zeta potential, percent drug entrapment (%EE), and loading (%DL). The lipid (stearic acid) based SLNs (F2) was optimized with particle size (266.0 ± 6.4 nm), PDI (0.217 ± 0.04), zeta potential (31.2 ± 5.19 mV), EE (65.0 ± 4.8%), and DL (4.60 ± 0.8%). The optimized SLNs (F2) was further evaluated by DSC, FTIR, SEM, in vitro release, and stability studies, which confirmed the successful encapsulation of ELX in SLNs. The efficacy of optimized SLNs (F2) in comparison to the pure ELX drug was assessed in acetic acid induced colitis rat models. It was observed that the delivery of ELX by SLNs alleviated the induced acetic acid colitis significantly. Thus, ELX loaded SLNs delivery to the colon has a significant potential to be developed for the treatment of ulcerative colitis. |
format | Online Article Text |
id | pubmed-7559404 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-75594042020-10-26 Eluxadoline Loaded Solid Lipid Nanoparticles for Improved Colon Targeting in Rat Model of Ulcerative Colitis Anwer, Md. Khalid Ahmed, Mohammed Muqtader Aldawsari, Mohammed F. Alshahrani, Saad Fatima, Farhat Ansari, Mohd Nazam Rehman, Najeeb Ur Al-Shdefat, Ramadan I. Pharmaceuticals (Basel) Article The aim of the current study was to evaluate the therapeutics potential of eluxadoline (ELX) loaded solid lipid nanoparticles (SLNs) in ulcerative colitis. ELX loaded SLNs were prepared using three different lipids according to the solvent emulsification technique. The optimization of prepared SLNs (F1-F3) were carried out based on size, PDI, zeta potential, percent drug entrapment (%EE), and loading (%DL). The lipid (stearic acid) based SLNs (F2) was optimized with particle size (266.0 ± 6.4 nm), PDI (0.217 ± 0.04), zeta potential (31.2 ± 5.19 mV), EE (65.0 ± 4.8%), and DL (4.60 ± 0.8%). The optimized SLNs (F2) was further evaluated by DSC, FTIR, SEM, in vitro release, and stability studies, which confirmed the successful encapsulation of ELX in SLNs. The efficacy of optimized SLNs (F2) in comparison to the pure ELX drug was assessed in acetic acid induced colitis rat models. It was observed that the delivery of ELX by SLNs alleviated the induced acetic acid colitis significantly. Thus, ELX loaded SLNs delivery to the colon has a significant potential to be developed for the treatment of ulcerative colitis. MDPI 2020-09-19 /pmc/articles/PMC7559404/ /pubmed/32961713 http://dx.doi.org/10.3390/ph13090255 Text en © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Anwer, Md. Khalid Ahmed, Mohammed Muqtader Aldawsari, Mohammed F. Alshahrani, Saad Fatima, Farhat Ansari, Mohd Nazam Rehman, Najeeb Ur Al-Shdefat, Ramadan I. Eluxadoline Loaded Solid Lipid Nanoparticles for Improved Colon Targeting in Rat Model of Ulcerative Colitis |
title | Eluxadoline Loaded Solid Lipid Nanoparticles for Improved Colon Targeting in Rat Model of Ulcerative Colitis |
title_full | Eluxadoline Loaded Solid Lipid Nanoparticles for Improved Colon Targeting in Rat Model of Ulcerative Colitis |
title_fullStr | Eluxadoline Loaded Solid Lipid Nanoparticles for Improved Colon Targeting in Rat Model of Ulcerative Colitis |
title_full_unstemmed | Eluxadoline Loaded Solid Lipid Nanoparticles for Improved Colon Targeting in Rat Model of Ulcerative Colitis |
title_short | Eluxadoline Loaded Solid Lipid Nanoparticles for Improved Colon Targeting in Rat Model of Ulcerative Colitis |
title_sort | eluxadoline loaded solid lipid nanoparticles for improved colon targeting in rat model of ulcerative colitis |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7559404/ https://www.ncbi.nlm.nih.gov/pubmed/32961713 http://dx.doi.org/10.3390/ph13090255 |
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