Formulation, Optimization and Evaluation of Ticagrelor Liquisolid Tablets for Enhanced Solubility

Abstract

Purpose The study aims to use liquisolid compacts technology as a novel carrier to enhance Ticagrelor's solubility and release profile. Method: Formulation of liquisolid tablets was developed using the Design of Experiment (DOE) approach where the drug Ticagrelor was dispersed in PEG-600 and incorporated into carrier material (Neusilin US2) in the mortar, the liquid drug was permitted to absorb in the second stage. Aerosil-200 was used as a coating material, and Magnesium stearate and Sodium starch Glycolate were used as Lubricant and Disintegrating Agent respectively. The formulations were optimized and the carrier-to-coating ratio and mixing Aerosil-200 with Neusilin US2 effect on drug release from the formulation was investigated. The prepared liquisolid compacts were subjected to micrometric characterization, post-compression parameters, Fourier Transform Infrared Spectroscopy (FTIR), and Differential Scanning Calorimetry (DSC). Result: The cumulative drug release of all formulations in dissolution media varies from 82% to 96% and Formulation F9 showed a maximum cumulative drug release of about 96%. The drug contents of all formulations ranged from 91.06% to 99.01%. Disintegration time for all 1-9 formulations, clearly, all compositions disintegrate in less than 10 minutes. The cumulative drug release of all formulations varies from 82% to 96% Formulation F9 showed a maximum cumulative drug release of about 96% and the conventional tablet showed a cumulative drug release of about 80 %. The optimized liquisolid formulation F8 outperformed the other batches in terms of flow and compressibility across all formulations. Conclusion: Therefore, as per the results, it can be inferred that Ticagrelor, when formulated by a liquisolid approach, produce ameliorated dissolution and stability profile.