Formulation, optimization and evaluation of ticagrelor liquisolid tablets for enhanced solubility

The study aims to use liquisolid compacts technology as a novel carrier to enhance Ticagrelor's solubility and release profile.

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).

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.

Therefore, as per the results, it can be inferred that Ticagrelor, when formulated by a liquisolid approach, produce ameliorated dissolution and stability profile.