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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...

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Autores principales: Le Khanh, Ha Pham, Haimhoffer, Ádám, Nemes, Dániel, Józsa, Liza, Vasvári, Gábor, Budai, István, Bényei, Attila, Ujhelyi, Zoltán, Fehér, Pálma, Bácskay, Ildikó
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
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.
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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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