Electroblowing and electrospinning of fibrous diclofenac sodium-cyclodextrin complex-based reconstitution injection

Balogh, Attila and Horvathova, T. and Fulop, Z. and Loftsson, T. and Harasztos, Anna Helga and Marosi, György and Nagy, Zsombor Kristóf (2015) Electroblowing and electrospinning of fibrous diclofenac sodium-cyclodextrin complex-based reconstitution injection. JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY, 26. pp. 28-34. ISSN 1773-2247

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Abstract

Electrospinning, electroblowing and freeze-drying were investigated to prepare fast dissolving cyclodextrin-based drug-loaded solid complexes. Combining the huge surface area of fibrous mats with the capabilities of cyclodextrins to prepare a reconstitution injection was tested to overcome the instability of liquid-based products. Diclofenac sodium was used as drug with limited water solubility and 2-hydroxypropyl-β-cyclodextrin (HPβCD) as carrier and solubilizer. The applied composition of the complex was determined based on phase solubility measurements. In order to resolve the frequent unavoidable interruption of the fiber formation during electrospinning from the HPβCD solution, high-speed blowing air was coupled with the electrostatic force (electroblowing) to draw polymer-free HPβCD fibers steadily, moreover, at increased flow rates. According to the scanning electron microscopic images, X-ray diffraction, differential scanning calorimetry no traces of crystallinity of the drug were detectable in the fibers as opposed to the freeze-dried product. Reconstitution tests of the fibers showed fast dissolution obtaining clear solutions equivalent to a marketed liquid-based bolus injection. The results demonstrate the first time the viability of electroblowing for preparing drug delivery systems.

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