Formulation Development and Evaluation of Bicalutamide Nano Suspension with Enhanced Solubility

Abstract

Background: Bicalutamide, a non-steroidal anti-androgen, is commonly prescribed for the treatment of prostate cancer. A drug categorized under BCS Class II due to its low solubility and higher permeability. The inherent poor aqueous solubility of the drug leads to delays in its onset of action. Therefore, the primary objective of this research is to leverage nanosuspension technology to formulate a solution that enhances the dissolution rate of the drug, consequently improving its bioavailability. Materials and Methods: Nanosuspensions were synthesized using the solvent diffusion method, incorporating selected stabilizers at varying concentrations. Results: The nanosuspensions underwent characterization for Polydispersity Index, mean particle size, zeta potential, entrapment efficiency and in vitro drug release. In vitro dissolution testing validated that the drug's dissolution rate was notably higher compared to the pure drug. the % drug release was found to be 95.4% which is the highest drug release as compared to other batches in 6 hr. A 23 factorial design was employed to examine the effects of independent variables, specifically, Stabilizer Concentration [X1], Surfactant concentration [X2] and sonication time [X3], on the dependent variables: mean particle size (Y1) and in vitro release study (Y2). The obtained data underwent statistical analysis and were further analyzed using three-dimensional response surface methodology to discern the impact of variables on responses. Subsequently the optimized batch underwent evaluation of in vitro parameters including particle size and in vitro drug release. Conclusion: The nanosuspension formulation presents a promising solution for enhancing the bioavailability of poorly water-soluble drugs when administered orally, offering improved efficacy and cost-effectiveness compared to traditional methods. The investigation of Bicalutamide-loaded nanosuspension serves as a novel delivery platform aimed at enhancing the oral bioavailability of the drug.