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Solvent electrospinning amorphous solid dispersions with high itraconazole, celecoxib, mebendazole and fenofibrate drug loading and release potential

Jana Becelaere, Olmo Frateur (UGent) , Ella Schoolaert (UGent) , Valérie Vanhoorne (UGent) , Dagmar D'hooge (UGent) , Chris Vervaet (UGent) , Richard Hoogenboom (UGent) and Karen De Clerck (UGent)
(2023) JOURNAL OF CONTROLLED RELEASE. 362. p.268-277
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Abstract
In this work, the feasibility of ultra-high drug loaded amorphous solid dispersions (ASDs) for the poorly soluble itraconazole, mebendazole and celecoxib via solvent electrospinning in combination with poly(2-ethyl-2-oxazoline) and fenofibrate in combination with polyvinylpyrrolidone is demonstrated. By lowering the polymer concentration in the electrospinning solution below its individual spinnable limit, ASDs with a drug content of up to 80 wt% are obtained. This is attributed to drug-polymer interactions not being limited by default to hydrogen bonds, as also Van der Waals interactions can result in high drug loadings. The theoretically predicted miscibility by the Flory-Huggins theory is corroborated by the experimental findings based on (modulated) differential scanning calorimetry and x-ray diffraction. Globally, the maximally obtained amorphous drug loadings are higher compared to the loadings found in literature. Additionally, non-sink dissolution tests demonstrate an increase in solubility of up to 50 times compared to their crystalline counterparts. Moreover, due to the lack of precipitation biocompatible PEtOx succeeds in stabilizing the dissolved drug and inhibiting its instant precipitation. The current work thus demonstrates the broader applicability of the electrospinning technique for the production of physically stable ASDs with ultra-high drug loadings, a result which has been validated for several Biopharmaceutics Classification System class II drugs.
Keywords
Amorphous solid dispersions (ASDs), Poly(2-ethyl-2-oxazoline) (PEtOx), Solvent electrospinning, Solubility enhancement, Poorly soluble drugs, Flory-Huggins

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Citation

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MLA
Becelaere, Jana, et al. “Solvent Electrospinning Amorphous Solid Dispersions with High Itraconazole, Celecoxib, Mebendazole and Fenofibrate Drug Loading and Release Potential.” JOURNAL OF CONTROLLED RELEASE, vol. 362, 2023, pp. 268–77, doi:10.1016/j.jconrel.2023.08.054.
APA
Becelaere, J., Frateur, O., Schoolaert, E., Vanhoorne, V., D’hooge, D., Vervaet, C., … De Clerck, K. (2023). Solvent electrospinning amorphous solid dispersions with high itraconazole, celecoxib, mebendazole and fenofibrate drug loading and release potential. JOURNAL OF CONTROLLED RELEASE, 362, 268–277. https://doi.org/10.1016/j.jconrel.2023.08.054
Chicago author-date
Becelaere, Jana, Olmo Frateur, Ella Schoolaert, Valérie Vanhoorne, Dagmar D’hooge, Chris Vervaet, Richard Hoogenboom, and Karen De Clerck. 2023. “Solvent Electrospinning Amorphous Solid Dispersions with High Itraconazole, Celecoxib, Mebendazole and Fenofibrate Drug Loading and Release Potential.” JOURNAL OF CONTROLLED RELEASE 362: 268–77. https://doi.org/10.1016/j.jconrel.2023.08.054.
Chicago author-date (all authors)
Becelaere, Jana, Olmo Frateur, Ella Schoolaert, Valérie Vanhoorne, Dagmar D’hooge, Chris Vervaet, Richard Hoogenboom, and Karen De Clerck. 2023. “Solvent Electrospinning Amorphous Solid Dispersions with High Itraconazole, Celecoxib, Mebendazole and Fenofibrate Drug Loading and Release Potential.” JOURNAL OF CONTROLLED RELEASE 362: 268–277. doi:10.1016/j.jconrel.2023.08.054.
Vancouver
1.
Becelaere J, Frateur O, Schoolaert E, Vanhoorne V, D’hooge D, Vervaet C, et al. Solvent electrospinning amorphous solid dispersions with high itraconazole, celecoxib, mebendazole and fenofibrate drug loading and release potential. JOURNAL OF CONTROLLED RELEASE. 2023;362:268–77.
IEEE
[1]
J. Becelaere et al., “Solvent electrospinning amorphous solid dispersions with high itraconazole, celecoxib, mebendazole and fenofibrate drug loading and release potential,” JOURNAL OF CONTROLLED RELEASE, vol. 362, pp. 268–277, 2023.
@article{01HA25M3577S3JXMWKYCTN1GGJ,
  abstract     = {{In this work, the feasibility of ultra-high drug loaded amorphous solid dispersions (ASDs) for the poorly soluble itraconazole, mebendazole and celecoxib via solvent electrospinning in combination with poly(2-ethyl-2-oxazoline) and fenofibrate in combination with polyvinylpyrrolidone is demonstrated. By lowering the polymer concentration in the electrospinning solution below its individual spinnable limit, ASDs with a drug content of up to 80 wt% are obtained. This is attributed to drug-polymer interactions not being limited by default to hydrogen bonds, as also Van der Waals interactions can result in high drug loadings. The theoretically predicted miscibility by the Flory-Huggins theory is corroborated by the experimental findings based on (modulated) differential scanning calorimetry and x-ray diffraction. Globally, the maximally obtained amorphous drug loadings are higher compared to the loadings found in literature. Additionally, non-sink dissolution tests demonstrate an increase in solubility of up to 50 times compared to their crystalline counterparts. Moreover, due to the lack of precipitation biocompatible PEtOx succeeds in stabilizing the dissolved drug and inhibiting its instant precipitation. The current work thus demonstrates the broader applicability of the electrospinning technique for the production of physically stable ASDs with ultra-high drug loadings, a result which has been validated for several Biopharmaceutics Classification System class II drugs.}},
  author       = {{Becelaere, Jana and Frateur, Olmo and Schoolaert, Ella and Vanhoorne, Valérie and D'hooge, Dagmar and Vervaet, Chris and Hoogenboom, Richard and De Clerck, Karen}},
  issn         = {{0168-3659}},
  journal      = {{JOURNAL OF CONTROLLED RELEASE}},
  keywords     = {{Amorphous solid dispersions (ASDs),Poly(2-ethyl-2-oxazoline) (PEtOx),Solvent electrospinning,Solubility enhancement,Poorly soluble drugs,Flory-Huggins}},
  language     = {{eng}},
  pages        = {{268--277}},
  title        = {{Solvent electrospinning amorphous solid dispersions with high itraconazole, celecoxib, mebendazole and fenofibrate drug loading and release potential}},
  url          = {{http://doi.org/10.1016/j.jconrel.2023.08.054}},
  volume       = {{362}},
  year         = {{2023}},
}
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