Formulation, Development and Evaluation of Budesonide Oral Nano-sponges Using DOE Approach: In-vivo Evidences

Purpose: The prevalent types of idiopathic inflammatory bowel disease are ulcerative colitis (UC) and Crohn’s disease, which affects a large number of populations. Budesonide (BUD) is a glucocorticoid with potent anti-inflammatory activity but low systemic efficacy because of high receptor affinity and rapid diversion. To overcome low efficacy and availability, a novel BUD nano-sponges was formulated using quasi- solvent diffusion and Eudragit S-100 as polymer. It was then investigated for the effect of process variables using Box-Behnken design.

Methods: The BUD Nano sponges were evaluated for particle size, particle size, polydispersity, percent drug entrapment, drug release pattern. The formulation was evaluated by an in vivo study using male Wistar rats and parameters such as clinical activity score, colon/body weight ratio (C/B ratio), macroscopic ulceration (damage score) activity were performed. Finally, histopathological examination was performed on colon tissue samples.

Results: The formulation showed better efficacy and availability as compared with the available formulations of BUD, which indicates the good efficacy of the formulated nanosponges. The clinical activity score was attenuated by the formulated nanosponges in the Wistar rats. The colon to body weight ratio was significantly reduced as compared with the control formulation. The histopathology of colon treated with nanosponges showed normal structure and architecture of the colon.

Conclusion: The results of the present work confirmed the utility of BUD nano-sponges as novel carriers in management IBD.