FORMULATION DEVELOPMENT AND IN VITRO - IN VIVO EVALUATION OF DARUNAVIR SELF EMULSIFYING DRUG DELIVERY SYSTEM (SEDDS)

The main objective of present work was to prepare a solid SEDDS for enhancement of oral bioavailability of Darunavir, a poorly water soluble drug. The solubility of the drug was determined in various vehicles. A pseudo ternary phase diagram was constructed to identify the self-micro emulsification region. Further, the resultant formulations were investigated for clarity, phase separation, globule size, effect of pH and dilutions and freeze-thaw stability. The optimized SMEDDS (F4) formulation of Darunavir contained Capmul MCM (Oil), Kolliphor HS 15 (Surfactant) and PEG 400 (Co-surfactant). Optimized liquid SEDDS having particle size (71.1nm), zeta potential (-40.6mV), in-vitro dissolution study (96.34%).This optimized formulation was converted in to solid SEDDS by adding required quantity of Neusilin US2 as adsorbing agent used for in vitro dissolution and bioavailability assessment. The oral bioavailability of Darunavir from solid SEDDS was 1.6-fold higher compared to that of Darunavir suspension in rats, suggesting a significant increase (p < 0.05) in oral bioavailability of Darunavir from solid SEDDS. The present exploratory work successfully illustrates the potential utility of S-SMEDDS formulation for the delivery of poor water-soluble drug Darunavir, which may result in improved therapeutic performance.