Formulation Development and Evaluation of Colon Targeting Nanosponges of Deflazacort Using Box Behnken Design

Abstract

Deflazacort is a glucocorticoid that is often used as an anti-inflammatory and immunosuppressant for patients suffering from Inflammatory Bowel Disease such as ulcerative colitis (UC) and Crohn's disease (CD). IBD is difficult to manage, and the most difficult issue for doctors is the recurrence. There are several regulated and colon focused medication delivery devices available for therapy, however they have a low success rate. The goal of this work was to create nanosponges loaded with deflazacort using the quasi-emulsion solvent diffusion technique using Eudragit S-100 and to investigate the influence of process factors on response using the Box-Behnken design. The effect of three independent parameters, Eudragit S100, PMMA, and PVA, on two dependent responses, particle size and percent drug entrapment, was investigated. Using the Box-behnken design, seventeen nanosponge formulations were created using the quasi-emulsion solvent diffusion technique and Eudragit S-100 (0.2 percent to 0.5 percent w/v), PMMA (0.2 percent to 0.5 percent w/v), and PVA (0.5 percent -1.5 percent w/v). Particle size, percent drug entrapment, shape and surface morphology, drug content determination, and in vitro drug release behaviour were all evaluated in the nanosponge formulations. The generated nanosponge was virtually spherical in form and spongy in character, with particle size 170.45 nm and a drug entrapment percentage of 73.42 percent. Over a 24-hour period, in vitro drug release of optimised formulations was shown to have a maximum drug release of 90.33.3 percent in colonic fluid with 4 percent w/v caecal content. The observed values of several assessment parameters were found to be in close agreement with the projected values using the Design expert programme. The nanosponge formulation obtained using Eudragit S-100 in low concentration, optimum concentration ratio of eudragit: PVA along with low stirring speed showed desired features. The mathematical models were further designed to develop nanosponge with required characteristics.