Lipid-based nanocarrier-mediated targeted delivery of celecoxib attenuate severity of ulcerative colitis

Abstract Ulcerative colitis is a chronic mucosal inflammatory condition that adversely affects colon and rectum. Celecoxib is a selective inhibitor of inducible cyclooxygenase-2 (COX-2) and is prescribed for the management of pain and other inflammatory disorders. The physicochemical properties of celecoxib limit its clinical potency. Here we developed nanostructured lipid carriers (NLCs) using Generally Recognized as Safe and US-FDA approved compounds for encapsulating celecoxib. Present study was aimed to evaluate efficacy of eudragit-S100-coated celecoxib-loaded NLCs against DSS-induced colitis in mice. NLCs were formulated by hot-melt method and possessed the average particle size of 250.90 nm and entrapment efficiency (%) was 59.89%. Furthermore, size, shape and morphology of NLCs were confirmed using TEM, SEM and AFM. The blank NLCs were cytocompatible against hTERT-BJ cells up to a dose of 200 μg/ml. Treatment with celecoxib-loaded NLCs alleviated severity of colitis as demonstrated by disease activity index, colon length, fecal occult blood test, and histopathological analysis. Moreover, treatment with celecoxib-loaded NLCs reduced disintegration of goblets cells and restores sulfomucin in colon. Celecoxib-nanoformulation markedly reduced colonic inflammation as evidenced by decreased immunohistochemical expression of COX-2 and iNOS. The observations of study suggest that lipid-based colon specific delivery of celecoxib may be used for management of colitis.