Development, optimization and evaluation of losartan potassium loaded Self Emulsifying Drug Delivery System

Abstract

In the current research work, losartan potassium (LP) loaded Self Emulsifying Drug Delivery System (SEDDS) was formulated using various ratios of lipids, surfactants and co-surfactants to prevent its first pass metabolism. A pseudo-ternary phase diagram was plotted to establish the emulsification region. Total of eight batches (F1 to F8) were prepared and subjected to different characterizations (thermodynamic study, phase separation, zeta potential and particle size) studies to obtain the optimized formulation. The optimized SEDDS (F8) with 40% oil, 60% surfactant and co-surfactant mixture (Smix) (6:1 ratio) was found to be a thermodynamically stable emulsion, with droplet size at around 204.7 ± 5.0 nm, surface charge −13.38 ± 1.5 mV and polydispersity index 0.221 ± 0.03. The SEM study confirmed the spherical shape and even surface of the droplets. The In-vitro drug release profile of optimized formulation exhibited a similar rate and extent of dissolution as compared to the marketed formulation. Further, the optimized formulation had shown equivalent therapeutic efficacy (anti-hypertensive) with respect to the marketed tablet at half of the dose of the drug in SEDDS formulation.