Homogenization of amorphous solid dispersions prepared by electrospinning in low-dose tablet formulation

Gergő Fülöp, Attila Balogh, Balazs Farkas, Attila Farkas, Bence Szabó, Balázs Démuth, Enikő Borbás, Zsombor Kristóf Nagy, G. Marosi

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Abstract

Low-dose tablet formulations were produced with excellent homogeneity based on drug-loaded electrospun fibers prepared by single-needle as well as scaled-up electrospinning (SNES and HSES). Carvedilol (CAR), a BCS II class compound, served as the model drug while poly (vinylpyrrolidone-co-vinyl acetate) (PVPVA64) was adopted as the fiber-forming polymer. Scanning electron microscopy (SEM) imaging was used to study the morphology of HSES and SNES samples. Different homogenization techniques were compared to maximize homogeneity: mixing in plastic bags and in a high-shear granulator resulting in low-shear mixing (LSM) and high-shear mixing (HSM). Drug content and homogeneity of the tablets were measured by UV-Vis spectrometry, the results revealed acceptably low-dose fluctuations especially with formulations homogenized with HSM. Sieve analysis was used on the final LSM and HSM powder mixtures in order to elucidate the observed differences between tablet homogeneity. Tablets containing drug-loaded electrospun fibers were also studied by Raman mapping demonstrating evenly distributed CAR within the corpus.

Original languageEnglish
Article number114
JournalPharmaceutics
Volume10
Issue number3
DOIs
Publication statusPublished - Sep 1 2018

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Keywords

  • Carvedilol
  • High-shear mixing
  • High-speed electrospinning
  • Homogenization
  • Poly (vinylpyrrolidone-co-vinyl acetate)
  • Raman mapping
  • Sieve analysis

ASJC Scopus subject areas

  • Pharmaceutical Science

Cite this

Fülöp, G., Balogh, A., Farkas, B., Farkas, A., Szabó, B., Démuth, B., Borbás, E., Nagy, Z. K., & Marosi, G. (2018). Homogenization of amorphous solid dispersions prepared by electrospinning in low-dose tablet formulation. Pharmaceutics, 10(3), [114]. https://doi.org/10.3390/pharmaceutics10030114