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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...

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Autores principales: Anwer, Md. Khalid, Ahmed, Mohammed Muqtader, Aldawsari, Mohammed F., Alshahrani, Saad, Fatima, Farhat, Ansari, Mohd Nazam, Rehman, Najeeb Ur, Al-Shdefat, Ramadan I.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
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.
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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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