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New Biopolymer Nanoparticles Improve the Solubility of Lipophilic Megestrol Acetate

As many substances are poorly soluble in water and thus possess decreased bioavailability, creating orally administered forms of these substances is a challenge. The objective of this study was to determine whether the solubility of megestrol acetate, a Biopharmaceutical Classification System (BCS)...

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Autores principales: Lachowicz, Malwina, Kołodziejczyk, Michał, Lukosek, Marek, Kosno, Jacek, Olszewska, Paulina, Szymański, Paweł
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6273346/
https://www.ncbi.nlm.nih.gov/pubmed/26861275
http://dx.doi.org/10.3390/molecules21020197
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author Lachowicz, Malwina
Kołodziejczyk, Michał
Lukosek, Marek
Kosno, Jacek
Olszewska, Paulina
Szymański, Paweł
author_facet Lachowicz, Malwina
Kołodziejczyk, Michał
Lukosek, Marek
Kosno, Jacek
Olszewska, Paulina
Szymański, Paweł
author_sort Lachowicz, Malwina
collection PubMed
description As many substances are poorly soluble in water and thus possess decreased bioavailability, creating orally administered forms of these substances is a challenge. The objective of this study was to determine whether the solubility of megestrol acetate, a Biopharmaceutical Classification System (BCS) class II drug, can be improved by using a newly-synthesized surfactant (Rofam 70: a rapeseed methyl ester ethoxylate) and compare it with two references surfactants (Tween 80, Pluronic F68) at three different pH values. Spectrophotometry was used to compare the solubility profiles in the presence of three tested surfactants at pH 5.0, 7.4 and 9.0. Rapeseed methyl ester ethoxylate was found to improve the solubility of the BCS Class II drug and increase its bioavailability; It increased drug solubility more effectively than Pluronic F68. Its cytotoxicity results indicate its possible value as a surfactant in Medicine and Pharmacy.
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spelling pubmed-62733462018-12-28 New Biopolymer Nanoparticles Improve the Solubility of Lipophilic Megestrol Acetate Lachowicz, Malwina Kołodziejczyk, Michał Lukosek, Marek Kosno, Jacek Olszewska, Paulina Szymański, Paweł Molecules Article As many substances are poorly soluble in water and thus possess decreased bioavailability, creating orally administered forms of these substances is a challenge. The objective of this study was to determine whether the solubility of megestrol acetate, a Biopharmaceutical Classification System (BCS) class II drug, can be improved by using a newly-synthesized surfactant (Rofam 70: a rapeseed methyl ester ethoxylate) and compare it with two references surfactants (Tween 80, Pluronic F68) at three different pH values. Spectrophotometry was used to compare the solubility profiles in the presence of three tested surfactants at pH 5.0, 7.4 and 9.0. Rapeseed methyl ester ethoxylate was found to improve the solubility of the BCS Class II drug and increase its bioavailability; It increased drug solubility more effectively than Pluronic F68. Its cytotoxicity results indicate its possible value as a surfactant in Medicine and Pharmacy. MDPI 2016-02-06 /pmc/articles/PMC6273346/ /pubmed/26861275 http://dx.doi.org/10.3390/molecules21020197 Text en © 2016 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons by Attribution (CC-BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Lachowicz, Malwina
Kołodziejczyk, Michał
Lukosek, Marek
Kosno, Jacek
Olszewska, Paulina
Szymański, Paweł
New Biopolymer Nanoparticles Improve the Solubility of Lipophilic Megestrol Acetate
title New Biopolymer Nanoparticles Improve the Solubility of Lipophilic Megestrol Acetate
title_full New Biopolymer Nanoparticles Improve the Solubility of Lipophilic Megestrol Acetate
title_fullStr New Biopolymer Nanoparticles Improve the Solubility of Lipophilic Megestrol Acetate
title_full_unstemmed New Biopolymer Nanoparticles Improve the Solubility of Lipophilic Megestrol Acetate
title_short New Biopolymer Nanoparticles Improve the Solubility of Lipophilic Megestrol Acetate
title_sort new biopolymer nanoparticles improve the solubility of lipophilic megestrol acetate
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6273346/
https://www.ncbi.nlm.nih.gov/pubmed/26861275
http://dx.doi.org/10.3390/molecules21020197
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