Improved antimicrobial activity and oral bioavailability of delafloxacin by self-nanoemulsifying drug delivery system (SNEDDS)

In the current study, a novel self-nanoemulsifying drug delivery system (SNEDDS) was developed in order to improve the oral bioavailability of delafloxacin (DLF). Various oils, surfactants and co-surfactants were screened by solubility studies. Based on solubilization, potential of DLF in various vehicles, LauroglycolTM-90 (oil), Tween (R) 80 (surfactant) and Transcutol (R)-HP (co-surfactant) were selected for the development of DLF loaded SNEDDS (DLF-SNEDDS). Four formulae of DLF loaded SNEDDS (DLF1-DLF4) were prepared and evaluated for their droplet size, polydispersity index (PDI), zeta potential (ZP), refractive index (RI), percent transmittance (% T), thermodynamic stability, emulsifying efficiency and in vitro release studies. Among developed DLF loaded SNEDDS (DLF1-DLF4), DLFI was found optimum with a droplet size (73.3 +/- 6.5 nm) PDI (0.298) ZP (-22.3) RI (1.334 +/- 0.05) and %T (99.2 +/- 0.09). Optimized DLF loaded SNEDDS (DLF1) demonstrated a superior antimicrobial activity against tested gram positive and gram negative strains with no resistance. The pharmacokinetic studies showed that oral bioavailability of DLF was significantly improved (3- fold) by optimized DLF loaded SNEDDS (DLF1) in comparison to pure DLF suspension. Hence, the results of this work suggest that the developed SNEDDS could be a potential carrier in enhancing bioavailability and therapeutic efficacy of DLF.