Refining the Performance of Abiraterone Acetate through Industry-friendly Techniques for Improving Functionality
DOI:
https://doi.org/10.30827/ars.v66i4.33508Keywords:
Abiraterone; functionality improvement; Neusilin; spray drying; GelucireAbstract
Introduction: Main objective of this study was to enhance solubility and permeability of Abiraterone Acetate (AA) by industry-feasible techniques.
Method: Solid dispersion (SD) of Abiraterone with Gelucire 44/14 (GC44/14), Dexolve, and Eudragit EPO were prepared using various functionality-improving techniques. These properties were characterized by phase solubility, dissolution, permeability, flow properties, differential scanning calorimetry, Fourier transform Infrared Spectroscopy, and X-ray diffraction. Among various techniques and polymers, spray drying with Gelucire was selected based on its ability to enhance solubility. A 32 full factorial design was applied to optimize SD, focusing on dissolution, solubility, and flow property (angle of repose), with material attributes being Abiraterone: Gelucire ratio and Neusilin (NS) amount. Optimal region was selected from overlay plot.
Results: Spray-dried SD exhibited highest solubility, which increased with Gelucire at a 1:2 ratio, resulting in a 405.94-fold increase in solubility. DSC, FTIR, and XRD showed Abiraterone transformation from crystalline to amorphous. Nine batches showed a drug release ranging from 30.85% to 90.33 % at 30 minutes, with solubility between 141.049 μg/mL and 286.307 μg/mL. Angle of repose ranged from fair to excellent. Optimized batch exhibited 85.51% drug release at 30 min, a solubility of 282.296 μg/mL, and good flow. Ex vivo permeability studies revealed 9.32 ± 0.147 % for Abiraterone and 51.72 ± 0.286 % for optimal batch at 90 min.
Conclusion: Solubility, permeability, and dissolution increased significantly when a SD of Abiraterone was prepared with Abiraterone and Neusilin by spray drying method. Systematic, industry-friendly techniques will benefit patients.
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