Detailed stability investigation of amorphous solid dispersions prepared by single-needle and high speed electrospinning

B. Démuth, A. Farkas, H. Pataki, A. Balogh, B. Szabó, E. Borbás, P. L. Sóti, T. Vigh, Kiserdei, B. Farkas, J. Mensch, G. Verreck, I. Van Assche, G. Marosi, Z. K. Nagy

Research output: Contribution to journalArticle

28 Citations (Scopus)

Abstract

In this research the long-term stability (one year) of amorphous solid dispersions (ASDs) prepared by high speed electrospinning was investigated at 25 °C/60% relative humidity (RH) (closed conditions) and 40 °C/75% RH (open conditions). Single needle electrospinning and film casting were applied as reference technologies. Itraconazole (ITR) was used as the model API in 40% concentration and the ASDs consisted of either one of the following polymers as a comparison: polyvinylpyrrolidone-vinyl acetate 6:4 copolymer (no hydrogen bonds between API and polymer) and hydroxypropyl methylcellulose (possible hydrogen bonds between oxo or tertiary nitrogen function of API and hydroxyl moiety of polymer). DSC, XRPD and dissolution characteristics of samples at 0, 3 and 12 months were investigated. In addition, Raman maps of certain electrospun ASDs were assessed to investigate crystallinity. A new chemometric method, based on Multivariate Curve Resolution-Alternating Least Squares algorithm, was developed to calculate the spectrum of amorphous ITR in the matrices and to determine the crystalline/amorphous ratio of aged samples. As it was expected ITR in single needle electrospun SDs was totally amorphous at the beginning, in addition hydroxypropyl methylcellulose could keep ITR in this form at 40 °C/75% RH up to one year due to the hydrogen bonds and high glass transition temperature of the SD. In polyvinylpyrrolidone-vinyl acetate matrix ITR remained amorphous at 25 °C/60% RH throughout one year. Materials prepared by scaled-up, high throughput version of electrospinning, which is compatible with pharmaceutical industry, also gained the same quality. Therefore these ASDs are industrially applicable and with an appropriate downstream process it would be possible to bring them to the market.

Original languageEnglish
Pages (from-to)234-244
Number of pages11
JournalInternational Journal of Pharmaceutics
Volume498
Issue number1-2
DOIs
Publication statusPublished - Feb 10 2016

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Itraconazole
Needles
Humidity
Hydrogen
Povidone
Polymers
Transition Temperature
Drug Industry
Least-Squares Analysis
Hydroxyl Radical
Glass
Nitrogen
Technology
Research

Keywords

  • Amorphous solid dispersion
  • High speed electrospinning
  • Long-term stability
  • Oral drug delivery
  • Raman mapping

ASJC Scopus subject areas

  • Pharmaceutical Science

Cite this

Detailed stability investigation of amorphous solid dispersions prepared by single-needle and high speed electrospinning. / Démuth, B.; Farkas, A.; Pataki, H.; Balogh, A.; Szabó, B.; Borbás, E.; Sóti, P. L.; Vigh, T.; Kiserdei; Farkas, B.; Mensch, J.; Verreck, G.; Van Assche, I.; Marosi, G.; Nagy, Z. K.

In: International Journal of Pharmaceutics, Vol. 498, No. 1-2, 10.02.2016, p. 234-244.

Research output: Contribution to journalArticle

Démuth, B, Farkas, A, Pataki, H, Balogh, A, Szabó, B, Borbás, E, Sóti, PL, Vigh, T, Kiserdei, Farkas, B, Mensch, J, Verreck, G, Van Assche, I, Marosi, G & Nagy, ZK 2016, 'Detailed stability investigation of amorphous solid dispersions prepared by single-needle and high speed electrospinning', International Journal of Pharmaceutics, vol. 498, no. 1-2, pp. 234-244. https://doi.org/10.1016/j.ijpharm.2015.12.029
Démuth, B. ; Farkas, A. ; Pataki, H. ; Balogh, A. ; Szabó, B. ; Borbás, E. ; Sóti, P. L. ; Vigh, T. ; Kiserdei ; Farkas, B. ; Mensch, J. ; Verreck, G. ; Van Assche, I. ; Marosi, G. ; Nagy, Z. K. / Detailed stability investigation of amorphous solid dispersions prepared by single-needle and high speed electrospinning. In: International Journal of Pharmaceutics. 2016 ; Vol. 498, No. 1-2. pp. 234-244.
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