This research aimed to compare two
solvent-based methods for the
preparation of amorphous solid dispersions (ASDs) made up of poorly
soluble spironolactone and poly(vinylpyrrolidone-co-vinyl acetate). The same apparatus was used to produce, in continuous
mode, drug-loaded electrospun (ES) and spray-dried (SD) materials
from dichloromethane and ethanol-containing solutions. The main differences
between the two preparation methods were the concentration of the
solution and application of high voltage. During electrospinning,
a solution with a higher concentration and high voltage was used to
form a fibrous product. In contrast, a dilute solution and no electrostatic
force were applied during spray drying. Both ASD products showed an
amorphous structure according to differential scanning calorimetry
and X-ray powder diffraction results. However, the dissolution of
the SD sample was not complete, while the ES sample exhibited close
to 100% dissolution. The polarized microscopy images and Raman microscopy
mapping of the samples highlighted that the SD particles contained
crystalline traces, which can initiate precipitation during dissolution.
Investigation of the dissolution media with a borescope made the precipitated
particles visible while Raman spectroscopy measurements confirmed
the appearance of the crystalline active pharmaceutical ingredient.
To explain the micro-morphological differences, the shape and size
of the prepared samples, the evaporation rate of residual solvents,
and the influence of the electrostatic field during the preparation
of ASDs had to be considered. This study demonstrated that the investigated
factors have a great influence on the dissolution of the ASDs. Consequently,
it is worth focusing on the selection of the appropriate ASD preparation
method to avoid the deterioration of dissolution properties due to
the presence of crystalline traces.
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