Solubility Enhancement of Atazanavir Sulfate by Inclusion Complexation with β-cyclodextrin using Solid Dispersion Technique

Similar to other antiretroviral medications, atazanavir, is a protease inhibitor (PI) that is used to treat human immunodeficiency virus (HIV) infection. This work aimed to adopt a solid dispersion approach with βcyclodextrin as the carrier to increase the atazanavir sulfate’s water solubility. Different batches of atazanavir sulfate solid dispersions and physical mixes were produced, and the effects of carrier type and concentration on the solubility and dissolution of atazanavir sulfate were systematically examined. Various analytical techniques such as Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), X-ray diffraction (XRD), and Scanning Electron Microscopy (SEM), were utilized to study the compatibility between the carrier and drug, and the degree of crystallinity and surface morphology of the solid dispersion to assess the increase in the solubility and dissolution rate. Studies on compatibility using FTIR and DSC revealed that there was no interaction between drug with carrier. The batch formulated employing a 1:5 ratio of drug to polymer by kneading method showed good in vitro dissolution properties over the other batches and pure drug. The drug release from the formulation was found to obey first-order kinetics and diffusion as their main mechanism of release.