Preparation, Box-Behnken Statistical Optimization, and In Vitro Characterization of a Self-nanoemulsifying Drug Delivery System for the Oral Delivery of Budesonide as a Poorly Soluble Drug

Background: Self-nanoemulsifying drug delivery systems (SNEDDS) can be used to improve the oral bioavailability of lipophilic drugs. The aim of this study was the preparation and characterization of a SNEDDS for the oral delivery of budesonide as a poorly soluble drug. Methods: To prepare SNEDDS, budesonide (20 mg) was dissolved in the mixture of liquid paraffin, Tween 80, and propylene glycol, followed by using the Box-Behnken response surface methodology for statistical optimization. The prepared mixtures were then diluted in the simulated intestinal fluid (SIF) and their physico-chemical characteristics were studied as well. Then, SNEDDS were morphologically evaluated using transmission electron microscopy (TEM). Finally, the in vitro release profile of budesonide from nano-droplets was determined in the SIF. Results: Based on the results, the size, polydispersity index, zeta potential, and entrapment efficiency of statistically optimized SNEEDS were reported as 146±37 nm, 0.211±0.06, +3.6±0.84 mV, and 94.3±6.58%, respectively. In addition, TEM images revealed spherical nano-droplets. Further, the release profile of budesonide from nano-droplets exhibited 33.81±1.67% of drug release in SIF during 360 minutes of incubation at 37° C, indicating sustained drug release. Conclusion: The obtained data demonstrated that SNEDDS could be regarded as a good candidate for oral delivery of budesonide as a poorly water-soluble drug representing a high first-pass metabolism.