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Enhancing the Dissolution of Flutamide Through Supersaturation Using Beta-Cyclodextrin: a Promising Approach for Improved Solubility of Poorly Water-Soluble Drugs.

Authors :
Hoseini Aghdam, Shaghayegh
Allahyari, Saeideh
Source :
Journal of Pharmaceutical Innovation; Dec2023, Vol. 18 Issue 4, p2294-2304, 11p
Publication Year :
2023

Abstract

Purpose: The study aims to explore the potential of amorphous solid dispersion (ASD) technology in improving the solubility and bioavailability of flutamide (FLT), a poorly water-soluble drug. The introduction of beta-cyclodextrin (β-CD) is investigated as a strategy to overcome FLT's solubility limitations. Methods: The study employed various methods, including a validated UV spectrophotometric technique to assess FLT solubility and the creation of supersaturation through different β-CD and FLT combinations. Two formulation approaches, physical mixtures (PMs) and solid dispersions (SDs), were developed using freeze-drying and solvent evaporation methods. Analysis involved differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR), along with loading and release tests, including statistical analysis of dissolution profiles. Results: The FTIR analysis indicated that molecular interactions and chemical bonds remained largely unchanged. DSC results demonstrated the transformation of FLT from a crystalline to an amorphous state in the SDs. In the supersaturation test, it was evident that the solution with 30% β-CD and 70% FLT achieved a remarkable 5.69-fold increase in FLT concentration compared to the pure drug. Solid dispersion formulations exhibited varying drug release profiles, with the 30% β-CD and 70% FLT combination showing the most rapid release, reaching approximately 50% within 240 min. Conclusion: The study underscores the effectiveness of β-CD in the 30:70 β-CD to FLT combination to enhance FLT solubility and bioavailability. However, higher proportions of β-CD led to reduced drug release, potentially due to cyclodextrin aggregation, which could hinder drug interactions. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
18725120
Volume :
18
Issue :
4
Database :
Complementary Index
Journal :
Journal of Pharmaceutical Innovation
Publication Type :
Academic Journal
Accession number :
174658184
Full Text :
https://doi.org/10.1007/s12247-023-09793-8