Impact of porous microsponges in minimizing myotoxic side effects of simvastatin

Simvastatin (SV) is a poorly soluble drug; its oral administration is associated with a significant problem: Myopathy. The present study aims to formulate SV microsponges that have the potential to minimize the myotoxicity accompanying the oral administration of the drug. SV microsponges were prepar...

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Autores principales: Ali, Ahmed U., Abd-Elkareem, Mahmoud, Kamel, Amira A., Abou Khalil, Nasser S., Hamad, D., Nasr, Nasr Eldin Hussein, Hassan, Maha A., El Faham, Tahani H.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group UK 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10082807/
https://www.ncbi.nlm.nih.gov/pubmed/37031209
http://dx.doi.org/10.1038/s41598-023-32545-0
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author Ali, Ahmed U.
Abd-Elkareem, Mahmoud
Kamel, Amira A.
Abou Khalil, Nasser S.
Hamad, D.
Nasr, Nasr Eldin Hussein
Hassan, Maha A.
El Faham, Tahani H.
author_facet Ali, Ahmed U.
Abd-Elkareem, Mahmoud
Kamel, Amira A.
Abou Khalil, Nasser S.
Hamad, D.
Nasr, Nasr Eldin Hussein
Hassan, Maha A.
El Faham, Tahani H.
author_sort Ali, Ahmed U.
collection PubMed
description Simvastatin (SV) is a poorly soluble drug; its oral administration is associated with a significant problem: Myopathy. The present study aims to formulate SV microsponges that have the potential to minimize the myotoxicity accompanying the oral administration of the drug. SV microsponges were prepared by exploiting the emulsion solvent evaporation technique. The % entrapment efficiency (%EE) of the drug approached 82.54 ± 1.27%, the mean particle size of SV microsponges ranged from 53.80 ± 6.35 to 86.03 ± 4.79 µm in diameter, and the % cumulative drug release (%CDR) of SV from microsponges was significantly higher than that from free drug dispersion much more, the specific surface area of the optimized microsponges formulation was found to be 16.6 m(2)/g revealed the porosity of prepared microsponges. Histological and glycogen histochemical studies in the skeletal muscles of male albino rats revealed that microsponges were safer than free SV in minimizing myotoxicity. These findings were proven by Gene expression of Mitochondrial fusion and fission (Mfn1) & (Fis1) and (Peroxisome proliferator-activated receptor gamma co-activator 1α) PGC-1α. Finally, our study ascertained that SV microsponges significantly decreased the myotoxicity of SV.
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spelling pubmed-100828072023-04-10 Impact of porous microsponges in minimizing myotoxic side effects of simvastatin Ali, Ahmed U. Abd-Elkareem, Mahmoud Kamel, Amira A. Abou Khalil, Nasser S. Hamad, D. Nasr, Nasr Eldin Hussein Hassan, Maha A. El Faham, Tahani H. Sci Rep Article Simvastatin (SV) is a poorly soluble drug; its oral administration is associated with a significant problem: Myopathy. The present study aims to formulate SV microsponges that have the potential to minimize the myotoxicity accompanying the oral administration of the drug. SV microsponges were prepared by exploiting the emulsion solvent evaporation technique. The % entrapment efficiency (%EE) of the drug approached 82.54 ± 1.27%, the mean particle size of SV microsponges ranged from 53.80 ± 6.35 to 86.03 ± 4.79 µm in diameter, and the % cumulative drug release (%CDR) of SV from microsponges was significantly higher than that from free drug dispersion much more, the specific surface area of the optimized microsponges formulation was found to be 16.6 m(2)/g revealed the porosity of prepared microsponges. Histological and glycogen histochemical studies in the skeletal muscles of male albino rats revealed that microsponges were safer than free SV in minimizing myotoxicity. These findings were proven by Gene expression of Mitochondrial fusion and fission (Mfn1) & (Fis1) and (Peroxisome proliferator-activated receptor gamma co-activator 1α) PGC-1α. Finally, our study ascertained that SV microsponges significantly decreased the myotoxicity of SV. Nature Publishing Group UK 2023-04-08 /pmc/articles/PMC10082807/ /pubmed/37031209 http://dx.doi.org/10.1038/s41598-023-32545-0 Text en © The Author(s) 2023 https://creativecommons.org/licenses/by/4.0/Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons licence, and indicate if changes were made. The images or other third party material in this article are included in the article's Creative Commons licence, unless indicated otherwise in a credit line to the material. If material is not included in the article's Creative Commons licence and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this licence, visit http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) .
spellingShingle Article
Ali, Ahmed U.
Abd-Elkareem, Mahmoud
Kamel, Amira A.
Abou Khalil, Nasser S.
Hamad, D.
Nasr, Nasr Eldin Hussein
Hassan, Maha A.
El Faham, Tahani H.
Impact of porous microsponges in minimizing myotoxic side effects of simvastatin
title Impact of porous microsponges in minimizing myotoxic side effects of simvastatin
title_full Impact of porous microsponges in minimizing myotoxic side effects of simvastatin
title_fullStr Impact of porous microsponges in minimizing myotoxic side effects of simvastatin
title_full_unstemmed Impact of porous microsponges in minimizing myotoxic side effects of simvastatin
title_short Impact of porous microsponges in minimizing myotoxic side effects of simvastatin
title_sort impact of porous microsponges in minimizing myotoxic side effects of simvastatin
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10082807/
https://www.ncbi.nlm.nih.gov/pubmed/37031209
http://dx.doi.org/10.1038/s41598-023-32545-0
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