Solvent-free melt electrospinning for preparation of fast dissolving drug delivery system and comparison with solvent-based electrospun and melt extruded systems

Zsombor Kristóf Nagy, Attlia Balogh, Gábor Drávavölgyi, James Ferguson, Hajnalka Pataki, Balázs Vajna, G. Marosi

Research output: Contribution to journalArticle

82 Citations (Scopus)

Abstract

The solvent-free melt electrospinning (MES) method was developed to prepare a drug delivery system with fast release of carvedilol (CAR), a drug with poor water solubility. To the authors knowledge, this is the first report for preparing drug-loaded melt electrospun fibers. Cationic methacrylate copolymer of Eudragit® E type was used as a fiber forming polymer matrix. For comparison, ethanol-based electrospinning and melt extrusion (EX) methods were used to produce samples that had the same composition as the melt electrospun system. According to the results of scanning electron microscopy, X-ray diffraction, differential scanning calorimetry, and Fourier transformed infrared spectrometry investigations, amorphous solid nanodispersions/solutions of CAR in Eudragit® E matrix were obtained in all cases with 20 m/m% drug content. In vitro drug release in acidic media from the extrudates was significantly faster (5 min) than that from crystalline CAR. Moreover, ultrafast drug release was achieved from the solvent-free melt and ethanol-based electrospun samples because of their huge surface area and the soluble polymer matrix in the acidic media. These results demonstrate that solvent-free MES is a promising, novel technique for the production of drug delivery systems with enhanced dissolution because it can combine the advantages of EX (e.g., solvent-free, continuous process, and effective amorphization) and solvent-based electrospinning (huge product surface area).

Original languageEnglish
Pages (from-to)508-517
Number of pages10
JournalJournal of Pharmaceutical Sciences
Volume102
Issue number2
DOIs
Publication statusPublished - Feb 2013

Fingerprint

Drug Delivery Systems
Polymers
Ethanol
Pharmaceutical Preparations
Methacrylates
Differential Scanning Calorimetry
X-Ray Diffraction
Electron Scanning Microscopy
Solubility
Spectrum Analysis
Water
carvedilol
Drug Liberation
Eudragit-E

Keywords

  • Amorphous
  • Continuous pharmaceutical manufacturing
  • Electrospun nanofibers
  • Enhanced dissolution rate
  • Extrusion
  • Melt electrospinning
  • Oral drug delivery
  • Solid dispersion
  • Solid solution

ASJC Scopus subject areas

  • Pharmaceutical Science

Cite this

Solvent-free melt electrospinning for preparation of fast dissolving drug delivery system and comparison with solvent-based electrospun and melt extruded systems. / Nagy, Zsombor Kristóf; Balogh, Attlia; Drávavölgyi, Gábor; Ferguson, James; Pataki, Hajnalka; Vajna, Balázs; Marosi, G.

In: Journal of Pharmaceutical Sciences, Vol. 102, No. 2, 02.2013, p. 508-517.

Research output: Contribution to journalArticle

Nagy, Zsombor Kristóf ; Balogh, Attlia ; Drávavölgyi, Gábor ; Ferguson, James ; Pataki, Hajnalka ; Vajna, Balázs ; Marosi, G. / Solvent-free melt electrospinning for preparation of fast dissolving drug delivery system and comparison with solvent-based electrospun and melt extruded systems. In: Journal of Pharmaceutical Sciences. 2013 ; Vol. 102, No. 2. pp. 508-517.
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