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Unravelling the miscibility of poly(2-oxazoline)s : a novel polymer class for the formulation of amorphous solid dispersions

Melissa Everaerts, Ali Tigrine (UGent) , Victor Retamero De La Rosa (UGent) , Richard Hoogenboom (UGent) , Peter Adriaensens, Christian Clasen and Guy Van den Mooter
(2020) MOLECULES. 25(16).
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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.
Keywords
amorphous solid dispersions, poly(2-oxazoline)s, miscibility, modulated differential scanning calorimetry, solid-state nuclear magnetic resonance spectroscopy, GLASS-TRANSITION TEMPERATURE, HOT-MELT EXTRUSION, STABILIZATION, IMMISCIBILITY, BLENDS, FILMS

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MLA
Everaerts, Melissa, et al. “Unravelling the Miscibility of Poly(2-Oxazoline)S : A Novel Polymer Class for the Formulation of Amorphous Solid Dispersions.” MOLECULES, vol. 25, no. 16, 2020, doi:10.3390/molecules25163587.
APA
Everaerts, M., Tigrine, A., Retamero De La Rosa, V., Hoogenboom, R., Adriaensens, P., Clasen, C., & Van den Mooter, G. (2020). Unravelling the miscibility of poly(2-oxazoline)s : a novel polymer class for the formulation of amorphous solid dispersions. MOLECULES, 25(16). https://doi.org/10.3390/molecules25163587
Chicago author-date
Everaerts, Melissa, Ali Tigrine, Victor Retamero De La Rosa, Richard Hoogenboom, Peter Adriaensens, Christian Clasen, and Guy Van den Mooter. 2020. “Unravelling the Miscibility of Poly(2-Oxazoline)S : A Novel Polymer Class for the Formulation of Amorphous Solid Dispersions.” MOLECULES 25 (16). https://doi.org/10.3390/molecules25163587.
Chicago author-date (all authors)
Everaerts, Melissa, Ali Tigrine, Victor Retamero De La Rosa, Richard Hoogenboom, Peter Adriaensens, Christian Clasen, and Guy Van den Mooter. 2020. “Unravelling the Miscibility of Poly(2-Oxazoline)S : A Novel Polymer Class for the Formulation of Amorphous Solid Dispersions.” MOLECULES 25 (16). doi:10.3390/molecules25163587.
Vancouver
1.
Everaerts M, Tigrine A, Retamero De La Rosa V, Hoogenboom R, Adriaensens P, Clasen C, et al. Unravelling the miscibility of poly(2-oxazoline)s : a novel polymer class for the formulation of amorphous solid dispersions. MOLECULES. 2020;25(16).
IEEE
[1]
M. Everaerts et al., “Unravelling the miscibility of poly(2-oxazoline)s : a novel polymer class for the formulation of amorphous solid dispersions,” MOLECULES, vol. 25, no. 16, 2020.
@article{8724457,
  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.}},
  articleno    = {{3587}},
  author       = {{Everaerts, Melissa and Tigrine, Ali and Retamero De La Rosa, Victor and Hoogenboom, Richard and Adriaensens, Peter and Clasen, Christian and Van den Mooter, Guy}},
  issn         = {{1420-3049}},
  journal      = {{MOLECULES}},
  keywords     = {{amorphous solid dispersions,poly(2-oxazoline)s,miscibility,modulated differential scanning calorimetry,solid-state nuclear magnetic resonance spectroscopy,GLASS-TRANSITION TEMPERATURE,HOT-MELT EXTRUSION,STABILIZATION,IMMISCIBILITY,BLENDS,FILMS}},
  language     = {{eng}},
  number       = {{16}},
  pages        = {{21}},
  title        = {{Unravelling the miscibility of poly(2-oxazoline)s : a novel polymer class for the formulation of amorphous solid dispersions}},
  url          = {{http://doi.org/10.3390/molecules25163587}},
  volume       = {{25}},
  year         = {{2020}},
}
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