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High-Contrast and Fast Photorheological Switching of a Twist-Bend Nematic Liquid Crystal

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Compression-Induced Phase Transitions of Bicalutamide.

Joanna Szafraniec-Szczęsny^1,2, Agata Antosik-Rogóż¹, Justyna Knapik-Kowalczuk³

¹Department of Pharmaceutical Technology and Biopharmaceutics, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Krakow, Poland.

|May 14, 2020

Summary

This study explores amorphous solid dispersions of bicalutamide with PVP/VA, revealing that high polymer content enhances stability against recrystallization. These dispersions significantly improve drug dissolution and wettability compared to crystalline forms.

Keywords:

Kollidon®VA64 amorphous solid dispersions bicalutamide compression dissolution physical stability

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Published on: February 18, 2014

Area of Science:

Pharmaceutical Sciences
Materials Science

Background:

Amorphous solid dispersions enhance oral absorption of poorly soluble drugs.
Recrystallization of amorphous drugs is a major formulation challenge.

Purpose of the Study:

To investigate the amorphization and recrystallization behavior of bicalutamide in amorphous solid dispersions (ASDs) with poly(vinylpyrrolidone-co-vinyl acetate) (PVP/VA).
To understand the factors influencing the stability of bicalutamide ASDs.

Main Methods:

Amorphous solid dispersions prepared by ball milling and spray drying.
Characterization using X-ray diffraction (XRD), differential scanning calorimetry (DSC), and infrared spectroscopy (IR).
Assessment of drug-polymer miscibility using non-isothermal dielectric measurements and evaluation of mechanical stability under compression.

Main Results:

Both ball milling and spray drying successfully produced amorphous bicalutamide.
Compression of physical blends induced amorphization or polymorphic transition.
High drug-polymer miscibility and hydrogen bond formation contributed to ASD stability.
ASDs showed 2.5- to 11-fold enhanced dissolution compared to crystalline bicalutamide.
Bicalutamide remained amorphous upon compression at PVP/VA content >20% (spray-dried) or >33% (milled).

Conclusions:

Amorphous solid dispersions of bicalutamide with PVP/VA offer improved dissolution and wettability.
The stability of ASDs against recrystallization is dependent on polymer content and preparation method.
Understanding amorphization-recrystallization pathways is crucial for developing stable amorphous drug formulations.