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, G. Marosi

Research output: Contribution to journalArticle

135 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

Fingerprint

Spironolactone
Dosage Forms
X-Ray Diffraction
Pharmaceutical Technology
Pharmaceutical Preparations
Polyvinyls
Drug Carriers
Water
Differential Scanning Calorimetry
Electron Scanning Microscopy
Limit of Detection
Microscopy
Spectrum Analysis
Polymers
Ethanol
Technology
Transplants
polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer

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

Cite this

Comparison of electrospun and extruded soluplus®-based solid dosage forms of improved dissolution. / Nagy, Zsombor K.; Balogh, Attila; Vajna, Balázs; Farkas, Attila; Patyi, Gergo; Kramarics, Áron; Marosi, G.

In: Journal of Pharmaceutical Sciences, Vol. 101, No. 1, 01.2012, p. 322-332.

Research output: Contribution to journalArticle

Nagy, Zsombor K. ; Balogh, Attila ; Vajna, Balázs ; Farkas, Attila ; Patyi, Gergo ; Kramarics, Áron ; Marosi, G. / Comparison of electrospun and extruded soluplus®-based solid dosage forms of improved dissolution. In: Journal of Pharmaceutical Sciences. 2012 ; Vol. 101, No. 1. pp. 322-332.
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