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Fabrication, In Vitro and In Vivo Evaluation of Non-Ordered Mesoporous Silica-Based Ternary Solid Dispersions for Enhanced Solubility of Flurbiprofen

The aim of this study was to improve the solubility and prevent the ulcerogenic effect of flurbiprofen. Initially, binary and ternary solid dispersions (BSDs and TSDs) of flurbiprofen were prepared by using non-ordered mesoporous silica and gelucire. After preformulation testing (solubility, flow pr...

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Autores principales: Munir, Muhammad Usman, Ikraam, Mahnoor, Nadeem, Muhammad, Khalid, Syed Haroon, Asghar, Sajid, Khalid, Ikrima, Irfan, Muhammad, Islam, Nayyer, Ajaz, Nyla, Khan, Ikram Ullah
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9324605/
https://www.ncbi.nlm.nih.gov/pubmed/35890153
http://dx.doi.org/10.3390/ph15070856
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author Munir, Muhammad Usman
Ikraam, Mahnoor
Nadeem, Muhammad
Khalid, Syed Haroon
Asghar, Sajid
Khalid, Ikrima
Irfan, Muhammad
Islam, Nayyer
Ajaz, Nyla
Khan, Ikram Ullah
author_facet Munir, Muhammad Usman
Ikraam, Mahnoor
Nadeem, Muhammad
Khalid, Syed Haroon
Asghar, Sajid
Khalid, Ikrima
Irfan, Muhammad
Islam, Nayyer
Ajaz, Nyla
Khan, Ikram Ullah
author_sort Munir, Muhammad Usman
collection PubMed
description The aim of this study was to improve the solubility and prevent the ulcerogenic effect of flurbiprofen. Initially, binary and ternary solid dispersions (BSDs and TSDs) of flurbiprofen were prepared by using non-ordered mesoporous silica and gelucire. After preformulation testing (solubility, flow properties, % yield, and entrapment efficiency), four formulations were selected for further detailed studies. Solid-state characterization of optimized formulations (S1, S6, S7, and S12) showed successful drug incorporation in the solid dispersion at the molecular state without any noticeable interactions. The in vitro solubility and release study showed an increase in solubility and 98–100% of drug release in 30–45 min. The in vivo gastro-protective effect of the optimized formulations containing flurbiprofen and silica (1:1) with 25% w/w gelucire (S6 and S12) showed a reduction in the gastric lesion index (GLI) after four days of treatment. Moreover, histological images of the stomach lining (S6 and S12) illustrated normal epithelial cells and a partially protected mucosal membrane. Thus, TSD exhibited a significant increase in solubility and the dissolution rate and reduced the gastric ulceration. Therefore, TSDs are dubbed as efficacious carriers to enhance the bioavailability of flurbiprofen while simultaneously reducing its side effects.
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spelling pubmed-93246052022-07-27 Fabrication, In Vitro and In Vivo Evaluation of Non-Ordered Mesoporous Silica-Based Ternary Solid Dispersions for Enhanced Solubility of Flurbiprofen Munir, Muhammad Usman Ikraam, Mahnoor Nadeem, Muhammad Khalid, Syed Haroon Asghar, Sajid Khalid, Ikrima Irfan, Muhammad Islam, Nayyer Ajaz, Nyla Khan, Ikram Ullah Pharmaceuticals (Basel) Article The aim of this study was to improve the solubility and prevent the ulcerogenic effect of flurbiprofen. Initially, binary and ternary solid dispersions (BSDs and TSDs) of flurbiprofen were prepared by using non-ordered mesoporous silica and gelucire. After preformulation testing (solubility, flow properties, % yield, and entrapment efficiency), four formulations were selected for further detailed studies. Solid-state characterization of optimized formulations (S1, S6, S7, and S12) showed successful drug incorporation in the solid dispersion at the molecular state without any noticeable interactions. The in vitro solubility and release study showed an increase in solubility and 98–100% of drug release in 30–45 min. The in vivo gastro-protective effect of the optimized formulations containing flurbiprofen and silica (1:1) with 25% w/w gelucire (S6 and S12) showed a reduction in the gastric lesion index (GLI) after four days of treatment. Moreover, histological images of the stomach lining (S6 and S12) illustrated normal epithelial cells and a partially protected mucosal membrane. Thus, TSD exhibited a significant increase in solubility and the dissolution rate and reduced the gastric ulceration. Therefore, TSDs are dubbed as efficacious carriers to enhance the bioavailability of flurbiprofen while simultaneously reducing its side effects. MDPI 2022-07-12 /pmc/articles/PMC9324605/ /pubmed/35890153 http://dx.doi.org/10.3390/ph15070856 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/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 (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Munir, Muhammad Usman
Ikraam, Mahnoor
Nadeem, Muhammad
Khalid, Syed Haroon
Asghar, Sajid
Khalid, Ikrima
Irfan, Muhammad
Islam, Nayyer
Ajaz, Nyla
Khan, Ikram Ullah
Fabrication, In Vitro and In Vivo Evaluation of Non-Ordered Mesoporous Silica-Based Ternary Solid Dispersions for Enhanced Solubility of Flurbiprofen
title Fabrication, In Vitro and In Vivo Evaluation of Non-Ordered Mesoporous Silica-Based Ternary Solid Dispersions for Enhanced Solubility of Flurbiprofen
title_full Fabrication, In Vitro and In Vivo Evaluation of Non-Ordered Mesoporous Silica-Based Ternary Solid Dispersions for Enhanced Solubility of Flurbiprofen
title_fullStr Fabrication, In Vitro and In Vivo Evaluation of Non-Ordered Mesoporous Silica-Based Ternary Solid Dispersions for Enhanced Solubility of Flurbiprofen
title_full_unstemmed Fabrication, In Vitro and In Vivo Evaluation of Non-Ordered Mesoporous Silica-Based Ternary Solid Dispersions for Enhanced Solubility of Flurbiprofen
title_short Fabrication, In Vitro and In Vivo Evaluation of Non-Ordered Mesoporous Silica-Based Ternary Solid Dispersions for Enhanced Solubility of Flurbiprofen
title_sort fabrication, in vitro and in vivo evaluation of non-ordered mesoporous silica-based ternary solid dispersions for enhanced solubility of flurbiprofen
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9324605/
https://www.ncbi.nlm.nih.gov/pubmed/35890153
http://dx.doi.org/10.3390/ph15070856
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