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Open AccessArticle

Molecular Disorder of Bicalutamide—Amorphous Solid Dispersions Obtained by Solvent Methods

Department of Pharmaceutical Technology and Biopharmaceutics, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Krakow, Poland
Department of Physical Chemistry and Electrochemistry, Faculty of Chemistry, Jagiellonian University, Gronostajowa 2, 30-387 Krakow, Poland
Division of Biophysics and Molecular Physics, Institute of Physics, University of Silesia, Uniwersytecka 4, 40-007 Katowice, Poland
Silesian Center for Education and Interdisciplinary Research, 75 Pulku Piechoty 1a, 41-500 Chorzow, Poland
Author to whom correspondence should be addressed.
Pharmaceutics 2018, 10(4), 194;
Received: 14 September 2018 / Revised: 12 October 2018 / Accepted: 16 October 2018 / Published: 18 October 2018
(This article belongs to the Special Issue New Approaches to Enhance Drug Solubility and Bioavailability)
The effect of solvent removal techniques on phase transition, physical stability and dissolution of bicalutamide from solid dispersions containing polyvinylpyrrolidone (PVP) as a carrier was investigated. A spray dryer and a rotavapor were applied to obtain binary systems containing either 50% or 66% of the drug. Applied techniques led to the formation of amorphous solid dispersions as confirmed by X-ray powder diffractometry and differential scanning calorimetry. Moreover, solid–solid transition from polymorphic form I to form II was observed for bicalutamide spray dried without a carrier. The presence of intermolecular interactions between the drug and polymer molecules, which provides the stabilization of molecularly disordered bicalutamide, was analyzed using infrared spectroscopy. Spectral changes within the region characteristic for amide vibrations suggested that the amide form of crystalline bicalutamide was replaced by a less stable imidic one, characteristic of an amorphous drug. Applied processes also resulted in changes of particle geometry and size as confirmed by scanning electron microscopy and laser diffraction measurements, however they did not affect the dissolution significantly as confirmed by intrinsic dissolution study. The enhancement of apparent solubility and dissolution were assigned mostly to the loss of molecular arrangement by drug molecules. Performed statistical analysis indicated that the presence of PVP reduces the mean dissolution time and improve the dissolution efficiency. Although the dissolution was equally affected by both applied methods of solid dispersion manufacturing, spray drying provides better control of particle size and morphology as well as a lower tendency for recrystallization of amorphous solid dispersions. View Full-Text
Keywords: bicalutamide; PVP; solid dispersion; spray drying; evaporation; dissolution; amorphization bicalutamide; PVP; solid dispersion; spray drying; evaporation; dissolution; amorphization
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Szafraniec, J.; Antosik, A.; Knapik-Kowalczuk, J.; Gawlak, K.; Kurek, M.; Szlęk, J.; Jamróz, W.; Paluch, M.; Jachowicz, R. Molecular Disorder of Bicalutamide—Amorphous Solid Dispersions Obtained by Solvent Methods. Pharmaceutics 2018, 10, 194.

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