افزایش محلولیت فلوتامید با کمک بتاسیکلودکسترین از طریق روش فوق اشباعیت: یک راه قابل اعتماد جهت افزایش محلولیت داروهای کم محلول در آب

عنوان انگليسی

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

خلاصه انگلیسی

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.

Document Downloads