Formulation Development and Evaluation of Atorvastatin Soy Lecithin Solid Dispersion A Promising Approach for Solubility Enhancement

Abstract

Background: Hyperlipidaemia remains a significant contributor to cardiovascular disorders, with statins being the primary therapeutic agents for its management. However, the clinical efficacy of these drugs, particularly atorvastatin, a statin with an extended plasma half-life of 18-24 hr is hindered by poor aqueous solubility, which limits bioavailability. This study aimed to address this limitation by enhancing the solubility and dissolution profile of atorvastatin through advanced formulation strategies.Materials and Methods: A solid dispersion approach utilizing phospholipids as a matrix-forming agent was employed to improve drug solubility. The dispersion was synthesized via solvent evaporation, with methanol-ethanol (1:1) selected as the optimal solvent system based on preliminary solubility assessments. Adsorbents and disintegrants were integrated to optimize flowability and dissolution kinetics. The impact of varying phospholipid-to-drug ratios on performance was systematically evaluated.Results: The formulation with a 2:3 drug-to-phospholipid ratio demonstrated superior outcomes, achieving a solubility of 614±24 μg/mL and 91.2±2.27% dissolution within 90 min. Advanced analytical techniques, including Differential Scanning Calorimetry (DSC) and powder X-ray Diffraction (XRD), confirmed the amorphous dispersion of atorvastatin within the phospholipid matrix. Subsequently, an orodispersible tablet was developed using the optimized dispersion, exhibiting favorable pharmaceutical attributes.Conclusion: The integration of phospholipids in solid dispersion systems presents a viable strategy to overcome solubility challenges associated with atorvastatin, offering a scalable and effective solution for enhancing its therapeutic potential.

Keywords: Solid dispersion; Atorvastatin; Soy Lecithin; Solubility Enhancement; Orodispersible Tablets