ArticleDrug design, development and therapy2026
Development of Amorphous Solid Dispersion to Improve the Dissolution and Antiproliferative Activity of Brazilin.
Article in Drug design, development and therapy, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
Introduction: Brazilin (BRZ), a major bioactive constituent of Methods: ASDs of BRZ with PVP were prepared using the solvent evaporation method with drug-to-polymer weight ratios of 1:1, 1:3, and 1:5. The formulations were characterized using powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), and Fourier-transform infrared (FT-IR) spectroscopy. Solubility, in vitro dissolution, and antiproliferative activity against DU145 prostate cancer cells were evaluated. Physical stability was evaluated over 30 days under dry (25 °C/0% RH) and humid (25 °C/90% RH) storage conditions using PXRD to detect any possible recrystallization. Results: PXRD and DSC analyses confirmed the complete amorphization of BRZ within the ASD matrix, as evidenced by the disappearance of crystalline diffraction peaks and characteristic melting endotherms. FT-IR spectroscopy, supported by in silico studies, revealed hydrogen bond formation between the hydroxyl group of BRZ and the carbonyl group of PVP. The BRZ:PVP (1:5) formulation achieved a 5.7-fold increase in solubility compared to crystalline BRZ. Dissolution testing showed a characteristic spring-and-parachute profile, with ASDs maintaining supersaturation for a prolonged period. Moreover, enhanced antiproliferative activity against DU145 cells was observed for BRZ ASDs, with the lowest IC Conclusion: BRZ ASDs using PVP effectively improved solubility, dissolution profile, and antiproliferative activity. The formulations demonstrated good stability under dry storage conditions but were sensitive to high humidity. These findings suggest that ASDs represent a promising strategy for enhancing the therapeutic potential of poorly soluble natural anticancer compounds.
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