Formulation and Evaluation of Dabigatran Solid Self-Nano Emulsifying Drug Delivery System

Abstract

Dabigatran Etexilate (DE), a prodrug of dabigatran, is a strong oral, reversible, and direct thrombin inhibitor with low oral bioavailability because of active efflux via intestinal P-glycoprotein receptors. By creating a self-emulsifying drug delivery system, the current work largely focused on improving the solubility of dabigatran. Dabigatran is a BCS class II medication with high permeability and poor water solubility. UV-spectroscopy was used to determine Dabigatran's saturated solubility in different oils, surfactants, and co-surfactants. Based on their maximum solubility and compatibility with Dabigatran, the excipients were chosen. Different oils, surfactants, and co-surfactant combinations were used to create SEDDS formulations of dabigatran (4:1 and 3:1). Pseudo ternary phase diagrams were created, and the nano emulsification area was assessed using these. Formulations were created utilising different ratios of oil (Capmul MCM NF), surfactant (Labrasol ALF), and co-surfactant (Transcutol HP) based on the pseudo ternary phase diagram. The produced formulations were chosen, and the 4:1 formulation underwent optimization and was subjected to additional tests, including self-emulsification time, phase separation and stability tests, thermodynamic stability studies, droplet size and zeta potential, and in vitro drug release investigations. According to the report's results, Dabigatran SEDDS are a viable system to increase Dabigatran's solubility.