Please use this identifier to cite or link to this item:
http://hdl.handle.net/1942/32840
Title: | Unravelling the Miscibility of Poly(2-oxazoline)s: A Novel Polymer Class for the Formulation of Amorphous Solid Dispersions | Authors: | Everaerts, Melissa Tigrine, Ali de la Rosa, Victor R. Hoogenboom, Richard ADRIAENSENS, Peter Clasen, Christian Van den Mooter, Guy |
Issue Date: | 2020 | Publisher: | MDPI | Source: | Molecules (Basel. Online), 25 (16) (Art N° 3587) | Abstract: | Water-soluble polymers are still the most popular carrier for the preparation of amorphous solid dispersions (ASDs). The advantage of this type of carrier is the fast drug release upon dissolution of the water-soluble polymer and thus the initial high degree of supersaturation of the poorly soluble drug. Nevertheless, the risk for precipitation due to fast drug release is a phenomenon that is frequently observed. In this work, we present an alternative carrier system for ASDs where a water-soluble and water-insoluble carrier are combined to delay the drug release and thus prevent this onset of precipitation. Poly(2-alkyl-2-oxazoline)s were selected as a polymer platform since the solution properties of this polymer class depend on the length of the alkyl sidechain. Poly(2-ethyl-2-oxazoline) (PEtOx) behaves as a water-soluble polymer at body temperature, while poly(2-n-propyl-2-oxazoline) (PPrOx) and poly(2-sec-butyl-2-oxazoline) (PsecBuOx) are insoluble at body temperature. Since little was known about the polymer's miscibility behaviour and especially on how the presence of a poorly-water soluble drug impacted their miscibility, a preformulation study was performed. Formulations were investigated with X-ray powder diffraction, differential scanning calorimetry (DSC) and solid-state nuclear magnetic resonance spectroscopy. PEtOx/PPrOx appeared to form an immiscible blend based on DSC and this was even more pronounced after heating. The six drugs that were tested in this work did not show any preference for one of the two phases. PEtOx/PsecBuOx on the other hand appeared to be miscible forming a homogeneous blend between the two polymers and the drugs. | Notes: | Van den Mooter, G (corresponding author), Katholieke Univ Leuven, Drug Delivery & Disposit, Dept Pharmaceut & Pharmacol Sci, B-3000 Leuven, Belgium. melissa.everaerts@kuleuven.be; ali.tigrine@ugent.be; victor.retamerodelarosa@ugent.be; richard.hoogenboom@ugent.be; peter.adriaensens@uhasselt.be; christian.clasen@kuleuven.be; guy.vandenmooter@kuleuven.be |
Other: | Van den Mooter, G (corresponding author), Katholieke Univ Leuven, Drug Delivery & Disposit, Dept Pharmaceut & Pharmacol Sci, B-3000 Leuven, Belgium. melissa.everaerts@kuleuven.be; ali.tigrine@ugent.be; victor.retamerodelarosa@ugent.be; richard.hoogenboom@ugent.be; peter.adriaensens@uhasselt.be; christian.clasen@kuleuven.be; guy.vandenmooter@kuleuven.be | Keywords: | amorphous solid dispersions;poly(2-oxazoline)s;miscibility;modulated differential scanning calorimetry;solid-state nuclear magnetic resonance spectroscopy | Document URI: | http://hdl.handle.net/1942/32840 | e-ISSN: | 1420-3049 | DOI: | 10.3390/molecules25163587 | ISI #: | WOS:000578911500001 | Rights: | © 2020 by the authors. 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 (http://creativecommons.org/licenses/by/4.0/). | Category: | A1 | Type: | Journal Contribution | Validations: | ecoom 2021 |
Appears in Collections: | Research publications |
Files in This Item:
File | Description | Size | Format | |
---|---|---|---|---|
molecules-25-03587-v2.pdf | Published version | 3 MB | Adobe PDF | View/Open |
WEB OF SCIENCETM
Citations
8
checked on Oct 13, 2024
Page view(s)
30
checked on Sep 6, 2022
Download(s)
20
checked on Sep 6, 2022
Google ScholarTM
Check
Altmetric
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.