Comparison of spray drying, electroblowing and electrospinning for preparation of Eudragit E and itraconazole solid dispersions

Abstract

Three solvent based methods: spray drying (SD), electrospinning (ES) and air-assisted electrospinning (electroblowing; EB) were used to prepare solid dispersions of itraconazole and Eudragit E. Samples with the same API/polymer ratios were prepared in order to make the three technologies comparable. The structure and morphology of solid dispersions were identified by scanning electron microscopy and solid phase analytical methods such as, X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC) and Raman chemical mapping. Moreover, the residual organic solvents of the solid products were determined by static headspace-gas chromatography/mass spectroscopy measurements and the wettability of samples was characterized by contact angle measurement. The pharmaceutical performance of the three dispersion type, evaluated by dissolution tests, proved to be very similar. According to XRPD and DSC analyses, made after the production, all the solid dispersions were free of any API crystal clusters but about 10 wt% drug crystallinity was observed after three months of storage in the case of the SD samples in contrast to the samples produced by ES and EB in which the polymer matrix preserved the API in amorphous state.

Characterization and Bioavailability of Wogonin by Different Administration Routes in Beagles

“…In PM with a mount of the polymer (1:5 ratio), no diffraction peaks were discovered due to the polymer dilution effect [ 32 , 33 ]. The disappearance of characteristic peaks in all SDs suggested a significant decrease in wogonin crystallinity, demonstrating a drug amorphization or its solvation in the amorphous carriers [ 5 , 33 , 34 ]. DSC analysis enables the quantitative detection of all processes in which energy is required or produced.…”

Scale‐up of electrospinning technology: Applications in the pharmaceutical industry

“…However, no notable increase in productivity has been reported using multiple needles, and presumably it is the reason why these methods did not spread in practical usage. Much higher production rates can be achieved with electroblowing (Figure e) when an additional air flow facilitates the solvent evaporation (Armantrout, Bryner, & Spiers, ; Balogh et al, ; Kakoria & Sinha‐Ray, ; Medeiros, Glenn, Klamczynski, Orts, & Mattoso, ; Pokorny, Rassushin, Wolfova, & Velebny, ; Sóti et al, ). Although the feeding rate is increased during the electroblowing process, beads or droplets can also appear among the fibers more frequently due to the effects of the air flow.…”

“…In this work, the air‐assisted method was successfully applied for preparing fibrous diclofenac sodium‐cyclodextrin complex‐based reconstitution injection. Even higher feeding rate was reached with electroblowing in the case of itraconazole‐loaded samples (Sóti et al, ). In this work, the authors compared electroblowing to spray drying and they not only showed that increased productivity (50 g/hr) is achievable using the air‐assisted technology, but they also demonstrated that the prepared amorphous solid dispersion showed better stability than the spray‐dried samples.…”

Electrospinning for healthcare: recent advancements

“…There exist a range of other routes to preparing SDs and ASDs, with the most commonly applied being hot melt extrusion (HME), spray drying and freeze drying. [10][11][12][13] All these technologies have great utility in the pharmaceutical industry, and there are marketed products fabricated using all three. However, all have fundamental disadvantages associated with them.…”