Ulcerative colitis is a multifactorial disease of the
gastrointestinal
tract which is caused due to chronic inflammation in the colon; it
usually starts from the lower end of the colon and may spread to other
portions of the large intestine, if left unmanaged. Budesonide (BUD)
is a synthetically available second-generation corticosteroidal drug
with potent local anti-inflammatory activity. The pharmacokinetic
properties, such as extensive first-pass metabolism and quite limited
bioavailability, reduce its therapeutic efficacy. To overcome the
limitations, nanosized micelles were developed in this study by conjugating
stearic acid with caffeic acid to make an amphiphilic compound. The
aim of the present study was to evaluate the pharmacological potential
of BUD-loaded micelles in a mouse model of dextran sulfate sodium-induced
colitis. Micelles were formulated by the solvent evaporation method,
and their physicochemical characterizations show their spherical shape
under microscopic techniques like atomic force microscopy, transmission
electron microscopy, and scanning electron microscopy. The in vitro
release experiment shows sustained release behavior in physiological
media. These micelles show cytocompatible behavior against hTERT-BJ
cells up to 500 μg/mL dose, evidenced by more than 85% viable
cells. BUD-loaded micelles successfully normalized the disease activity
index and physical observation of colon length. The treatment with
BUD-loaded micelles alleviates the colitis severity as analyzed in
histopathology and efficiently, overcoming the disease severity via
downregulation of various related cytokines (MPO, NO, and TNF-α)
and inflammatory enzymes such as COX-2 and iNOS. Results of the study
suggest that BUD-loaded nano-sized micelles effectively attenuate
the disease conditions in colitis.