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Effect of Molecular Weight on the Dissolution Profiles of PEG Solid Dispersions Containing Ketoprofen
Solid dispersions are typically binary systems with a hydrophilic matrix polymer and a lipophilic active substance. During formulation, the drug undergoes a crystalline to amorphous phase transition, which leads to a supersaturated solution providing enhanced bioavailability. The interaction of the...
Autores principales: | , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2023
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10096880/ https://www.ncbi.nlm.nih.gov/pubmed/37050371 http://dx.doi.org/10.3390/polym15071758 |
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author | Le Khanh, Ha Pham Haimhoffer, Ádám Nemes, Dániel Józsa, Liza Vasvári, Gábor Budai, István Bényei, Attila Ujhelyi, Zoltán Fehér, Pálma Bácskay, Ildikó |
author_facet | Le Khanh, Ha Pham Haimhoffer, Ádám Nemes, Dániel Józsa, Liza Vasvári, Gábor Budai, István Bényei, Attila Ujhelyi, Zoltán Fehér, Pálma Bácskay, Ildikó |
author_sort | Le Khanh, Ha Pham |
collection | PubMed |
description | Solid dispersions are typically binary systems with a hydrophilic matrix polymer and a lipophilic active substance. During formulation, the drug undergoes a crystalline to amorphous phase transition, which leads to a supersaturated solution providing enhanced bioavailability. The interaction of the active substance and the polymer is unique and influences the level of supersaturation. We aimed to investigate the relationship between low molecular weight polyethylene glycol derivates PEG 1000, 1500, and 2000 and ketoprofen regarding the effect of molecular weight. The physicochemical properties of solid dispersions prepared with hot melt homogenization and their respective physical mixtures were investigated with Fourier transform infrared spectroscopy, powder X-ray diffraction and scanning electron microscopy techniques. A phase solubility study was carried out in hydrochloric acid media which showed no difference between the three polymers, but the dissolution curves differed considerably. PEG 1000 had higher percentage of released drug than PEG 1500 and 2000, which had similar results. These results indicate that when multiple low molecular weight PEGs are suitable as matrix polymers of solid dispersions, the molecular weight has only limited impact on physicochemical characteristics and interactions and further investigation is needed to select the most applicable candidate. |
format | Online Article Text |
id | pubmed-10096880 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-100968802023-04-13 Effect of Molecular Weight on the Dissolution Profiles of PEG Solid Dispersions Containing Ketoprofen Le Khanh, Ha Pham Haimhoffer, Ádám Nemes, Dániel Józsa, Liza Vasvári, Gábor Budai, István Bényei, Attila Ujhelyi, Zoltán Fehér, Pálma Bácskay, Ildikó Polymers (Basel) Article Solid dispersions are typically binary systems with a hydrophilic matrix polymer and a lipophilic active substance. During formulation, the drug undergoes a crystalline to amorphous phase transition, which leads to a supersaturated solution providing enhanced bioavailability. The interaction of the active substance and the polymer is unique and influences the level of supersaturation. We aimed to investigate the relationship between low molecular weight polyethylene glycol derivates PEG 1000, 1500, and 2000 and ketoprofen regarding the effect of molecular weight. The physicochemical properties of solid dispersions prepared with hot melt homogenization and their respective physical mixtures were investigated with Fourier transform infrared spectroscopy, powder X-ray diffraction and scanning electron microscopy techniques. A phase solubility study was carried out in hydrochloric acid media which showed no difference between the three polymers, but the dissolution curves differed considerably. PEG 1000 had higher percentage of released drug than PEG 1500 and 2000, which had similar results. These results indicate that when multiple low molecular weight PEGs are suitable as matrix polymers of solid dispersions, the molecular weight has only limited impact on physicochemical characteristics and interactions and further investigation is needed to select the most applicable candidate. MDPI 2023-03-31 /pmc/articles/PMC10096880/ /pubmed/37050371 http://dx.doi.org/10.3390/polym15071758 Text en © 2023 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 Le Khanh, Ha Pham Haimhoffer, Ádám Nemes, Dániel Józsa, Liza Vasvári, Gábor Budai, István Bényei, Attila Ujhelyi, Zoltán Fehér, Pálma Bácskay, Ildikó Effect of Molecular Weight on the Dissolution Profiles of PEG Solid Dispersions Containing Ketoprofen |
title | Effect of Molecular Weight on the Dissolution Profiles of PEG Solid Dispersions Containing Ketoprofen |
title_full | Effect of Molecular Weight on the Dissolution Profiles of PEG Solid Dispersions Containing Ketoprofen |
title_fullStr | Effect of Molecular Weight on the Dissolution Profiles of PEG Solid Dispersions Containing Ketoprofen |
title_full_unstemmed | Effect of Molecular Weight on the Dissolution Profiles of PEG Solid Dispersions Containing Ketoprofen |
title_short | Effect of Molecular Weight on the Dissolution Profiles of PEG Solid Dispersions Containing Ketoprofen |
title_sort | effect of molecular weight on the dissolution profiles of peg solid dispersions containing ketoprofen |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10096880/ https://www.ncbi.nlm.nih.gov/pubmed/37050371 http://dx.doi.org/10.3390/polym15071758 |
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