Electrospun amorphous solid dispersions of meloxicam: Influence of polymer type and downstream processing to orodispersible dosage forms

Tibor Casian, Enikő Borbás, Kinga Ilyés, Balázs Démuth, Attila Farkas, Zsolt Rapi, Cătălina Bogdan, Sonia Iurian, Valentin Toma, Rares Știufiuc, Balázs Farkas, Attila Balogh, G. Marosi, Ioan Tomuță, Zsombor Kristóf Nagy

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Abstract

The objectives of this work were to develop meloxicam based amorphous solid dispersion through electrospinning technique and evaluate the effect of the polymeric matrix on the physicochemical properties of the fibers and the downstream processing ability to orodispersible dosage forms. Drug – polymer interactions formed between Eudragit E and meloxicam, confirmed through Raman and 1HNMR spectra, enabled the development of fibers from ethanol, thus allowing an increased production rate compared to PVPk30 where a DMF:THF solvent system was suitable. Microflux dissolution-permeation studies showed a significantly higher diffusion from amorphous solid dispersions compared to crystalline meloxicam. The flux through the membrane was influenced by the polymers only under basic conditions, where the precipitation of Eudragit E limited the complete resolubilization of the active ingredient. This phenomenon was not observed during large volume conventional dissolution testing. The effect of formulation on long term stability could not be highlighted as all products were stable up to 15 months, stored in closed holders at 25 °C ± 2 °C and 50%RH ± 10%. The increased surface area of fibers enabled tablet preparation with low pressures due to favorable bonding between particles during compression. PVPk30 formulation presented higher tabletability and compactability, as higher tensile strength compacts could be prepared. Eudragit E formulation had lower detachment and ejection stress, suggesting a lower sticking tendency during tableting. The presence of HPßCD in PVPk30 formulation offered improved morphological features of the fibers, however no significant effect was observed on dissolution, permeation or mechanical properties. Downstream processing was guided by polymer mechanical properties and solubility, thus PVPk30 fibers could be delivered in the form of orodispersible webs and conventional tablets, whereas Eudragit E fibers as orodispersible tablets.

Original languageEnglish
Article number118593
JournalInternational Journal of Pharmaceutics
Volume569
DOIs
Publication statusPublished - Oct 5 2019

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Keywords

  • Amorphous solid dispersion
  • Compaction analysis
  • Dissolution-permeation
  • Electrospinning
  • Orodispersible forms
  • Polymer
  • Stability

ASJC Scopus subject areas

  • Pharmaceutical Science

Cite this

Casian, T., Borbás, E., Ilyés, K., Démuth, B., Farkas, A., Rapi, Z., Bogdan, C., Iurian, S., Toma, V., Știufiuc, R., Farkas, B., Balogh, A., Marosi, G., Tomuță, I., & Nagy, Z. K. (2019). Electrospun amorphous solid dispersions of meloxicam: Influence of polymer type and downstream processing to orodispersible dosage forms. International Journal of Pharmaceutics, 569, [118593]. https://doi.org/10.1016/j.ijpharm.2019.118593