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 oralbioavailability of lipophilic drugs. The aim of this study was the preparation and characterization of aSNEDDS for the oral delivery of budesonide as a poorly soluble drug.Methods: To prepare SNEDDS, budesonide (۲۰ mg) was dissolved in the mixture of liquid paraffin,Tween ۸۰, and propylene glycol, followed by using the Box-Behnken response surface methodology forstatistical 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 morphologicallyevaluated using transmission electron microscopy (TEM). Finally, the in vitro release profile of budesonidefrom nano-droplets was determined in the SIF.Results: Based on the results, the size, polydispersity index, zeta potential, and entrapment efficiencyof statistically optimized SNEEDS were reported as ۱۴۶±۳۷ nm, ۰.۲۱۱±۰.۰۶, +۳.۶±۰.۸۴ mV, and۹۴.۳±۶.۵۸%, respectively. In addition, TEM images revealed spherical nano-droplets. Further, the releaseprofile of budesonide from nano-droplets exhibited ۳۳.۸۱±۱.۶۷% of drug release in SIF during ۳۶۰minutes of incubation at ۳۷°C, indicating sustained drug release.Conclusion: The obtained data demonstrated that SNEDDS could be regarded as a good candidate fororal delivery of budesonide as a poorly water-soluble drug representing a high first-pass metabolism.

کلیدواژه ها:

Budesonide ، Poorly water-soluble drugs ، Self-nanoemulsifying drug delivery system ، Oraldelivery ، Lymphatic absorption ، Statistical optimization