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Superiority of Mesoporous Silica-Based Amorphous Formulations over Spray-Dried Solid Dispersions
The aim of this study was to compare the performance of two amorphous formulation strategies: mesoporous silica via solvent impregnation, and solid dispersions by spray drying. Poorly soluble fenofibrate was chosen as the model drug compound. A total of 30% Fenofibrate-loaded mesoporous silica and s...
Autores principales: | , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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MDPI
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8878785/ https://www.ncbi.nlm.nih.gov/pubmed/35214159 http://dx.doi.org/10.3390/pharmaceutics14020428 |
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author | Zhang, Hongwei Li, Minglu Li, Jianmin Agrawal, Anjali Hui, Ho-Wah Liu, Demin |
author_facet | Zhang, Hongwei Li, Minglu Li, Jianmin Agrawal, Anjali Hui, Ho-Wah Liu, Demin |
author_sort | Zhang, Hongwei |
collection | PubMed |
description | The aim of this study was to compare the performance of two amorphous formulation strategies: mesoporous silica via solvent impregnation, and solid dispersions by spray drying. Poorly soluble fenofibrate was chosen as the model drug compound. A total of 30% Fenofibrate-loaded mesoporous silica and spray-dried solid dispersions (SDD) were prepared for head-to-head comparisons, including accelerated stability, manufacturability, and in vitro biorelevant dissolution. In the accelerated stability study under 40 °C/75% RH in open dish, mesoporous silica was able to maintain amorphous fenofibrate for up to 3 months based on solid-state characterizations by PXRD and DSC. This result was superior compared to SDD, as recrystallization was observed within 2 weeks. Under the same drug load, fenofibrate-loaded mesoporous silica showed much better flowability than fenofibrate-loaded SDD, which is beneficial for powder handling of the intermediate product during the downstream process. The in vitro 2-stage dissolution results indicated a well-controlled release of fenofibrate from mesoporous silica in the biorelevant media, rather than a burst release followed by fast precipitation due to the recrystallization in the early simulated gastric phase for SDD. The present study demonstrates that mesoporous silica is a promising formulation platform alternative to prevailing spray-dried solid dispersions for oral drug product development. |
format | Online Article Text |
id | pubmed-8878785 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-88787852022-02-26 Superiority of Mesoporous Silica-Based Amorphous Formulations over Spray-Dried Solid Dispersions Zhang, Hongwei Li, Minglu Li, Jianmin Agrawal, Anjali Hui, Ho-Wah Liu, Demin Pharmaceutics Article The aim of this study was to compare the performance of two amorphous formulation strategies: mesoporous silica via solvent impregnation, and solid dispersions by spray drying. Poorly soluble fenofibrate was chosen as the model drug compound. A total of 30% Fenofibrate-loaded mesoporous silica and spray-dried solid dispersions (SDD) were prepared for head-to-head comparisons, including accelerated stability, manufacturability, and in vitro biorelevant dissolution. In the accelerated stability study under 40 °C/75% RH in open dish, mesoporous silica was able to maintain amorphous fenofibrate for up to 3 months based on solid-state characterizations by PXRD and DSC. This result was superior compared to SDD, as recrystallization was observed within 2 weeks. Under the same drug load, fenofibrate-loaded mesoporous silica showed much better flowability than fenofibrate-loaded SDD, which is beneficial for powder handling of the intermediate product during the downstream process. The in vitro 2-stage dissolution results indicated a well-controlled release of fenofibrate from mesoporous silica in the biorelevant media, rather than a burst release followed by fast precipitation due to the recrystallization in the early simulated gastric phase for SDD. The present study demonstrates that mesoporous silica is a promising formulation platform alternative to prevailing spray-dried solid dispersions for oral drug product development. MDPI 2022-02-16 /pmc/articles/PMC8878785/ /pubmed/35214159 http://dx.doi.org/10.3390/pharmaceutics14020428 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 Zhang, Hongwei Li, Minglu Li, Jianmin Agrawal, Anjali Hui, Ho-Wah Liu, Demin Superiority of Mesoporous Silica-Based Amorphous Formulations over Spray-Dried Solid Dispersions |
title | Superiority of Mesoporous Silica-Based Amorphous Formulations over Spray-Dried Solid Dispersions |
title_full | Superiority of Mesoporous Silica-Based Amorphous Formulations over Spray-Dried Solid Dispersions |
title_fullStr | Superiority of Mesoporous Silica-Based Amorphous Formulations over Spray-Dried Solid Dispersions |
title_full_unstemmed | Superiority of Mesoporous Silica-Based Amorphous Formulations over Spray-Dried Solid Dispersions |
title_short | Superiority of Mesoporous Silica-Based Amorphous Formulations over Spray-Dried Solid Dispersions |
title_sort | superiority of mesoporous silica-based amorphous formulations over spray-dried solid dispersions |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8878785/ https://www.ncbi.nlm.nih.gov/pubmed/35214159 http://dx.doi.org/10.3390/pharmaceutics14020428 |
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