Paliperidone-Loaded Self-Emulsifying Drug Delivery Systems (SEDDS) for Improved Oral Delivery

The present research is aimed to improve the oral delivery of paliperidone by loading into self-emulsifying drug delivery systems (SEDDS). Oleic acid, Tween 80, and capmul MCM L8 were selected as oil, surfactant, and co-surfactant, respectively and phase diagram was constructed and the region was identified for the formation of SEDDS. The stable formulations were analyzed for globule size, robustness to dilution and in vitro drug release. The globule size of all the formulations was found to be in the range of 205 to 310 nm with good size uniformity and seems to be dependent on the proportion of oil in SEEDS formulation. The optimized formulation (F3) has been adsorbed onto neusilin and characterized. The DSC and XRD spectra unravel the presence of molecular state of paliperidone in solid SEDDS. The in vitro dissolution study indicates improved dissolution characteristics with higher dissolution efficiency for solid SEDDS (SEDDS-N) compared to pure drug. Further ex vivo permeation studies carried out using rat intestine suggest a 2- to 3-fold improvement in permeation for SEDDS compared to pure drug. In conclusion, SEDDS prove to be potential carriers for improved oral delivery of paliperidone.