Comparison of electrospun and extruded soluplus®-based solid dosage forms of improved dissolution

Zsombor K. Nagy, Attila Balogh, Balázs Vajna, Attila Farkas, Gergo Patyi, Áron Kramarics, György Marosi

Research output: Contribution to journalArticle

149 Citations (Scopus)

Abstract

Electrospinning (ES) and extrusion of a poorly water-soluble active pharmaceutical ingredient were used to improve its dissolution, which is a major challenge in the field of pharmaceutical technology. Spironolactone was applied as model drug and recently developed polyvinyl caprolactame-polyvinyl acetate-polyethylene glycol graft copolymer (Soluplus®) was used as carrier matrix and solubilizer. ES of the polymer matrix from ethanol solution was optimized at first without spironolactone and then the cosolution of the drug and the carrier was used for forming electrospun fibers. It resulted in real solid solution due to its very efficient amorphization effect. On the contrary, a low amount of crystalline spironolactone appeared in the extrudates according to Raman microscopy, X-ray diffraction (XRD), scanning electron microscopy (SEM) and energy-dispersive spectrometry (EDS). Raman microspectrometry had the lowest detection limit of spironolactone crystals compared with XRD and differential scanning calorimetry. Both ES and extrusion techniques resulted in significantly improved dissolution. Electrospun ultrafine fibers increased the dissolution more effectively, owing to the formed solid solution and huge surface. The developed continuous technologies demonstrate great potential to tackle the challenge of inadequate dissolution of poorly water-soluble drugs in several cases.

Original languageEnglish
Pages (from-to)322-332
Number of pages11
JournalJournal of pharmaceutical sciences
Volume101
Issue number1
DOIs
Publication statusPublished - Jan 2012

Keywords

  • Electrospinning
  • Extrusion
  • Improved dissolution rate
  • Nanofibers
  • Nanotechnology
  • Oral drug delivery
  • Polymeric drug delivery
  • Raman microscopy
  • Solid dispersion
  • Solid solution

ASJC Scopus subject areas

  • Pharmaceutical Science

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