Development and Characterization of Bosentan Monohydrate-loaded Self-Nano Emulsifying Drug Delivery System

The present investigation aims to develop a solid Self-nano emulsifying Drug Delivery System for enhancing the solubility and in vitro characteristics of poorly soluble anti-hypertensive drug Bosentan Monohydrate. The selection of formulation components on the basis of equilibrium solubility and pseudo-ternary phase titration studies revealed the suitability of Isopropyl myristate, Tween 80 and Polyethylene glycol as the lipidic excipients and their optimized concentration ranges resulted in a stable microemulsion region. The systematic optimization of the liquid SNEDD formulations of Bosentan was performed using in vitro tests and detailed characterization studies. The results revealed that the F4 formulation produces excellent results and satisfactory results in all the CQA of liquid SNEDDS. The optimized liquid SNEDD formulations exhibited globule size of less than 100 nm, high and negative values of zeta potential, quick self-emulsification rate, negligible phase separation, and a high degree of physical stability during thermodynamic evaluation studies. SEM revealed nanostructured particles with negligible aggregation. In vitro dissolution studies of Bosentan in optimized liquid SNEDDS (F4) unveiled a multi-fold enhancement in release profile, as compared to pure API.