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Colon-targeted dexamethasone microcrystals with pH-sensitive chitosan/alginate/Eudragit S multilayers for the treatment of inflammatory bowel disease

Oshi, Murtada A., Naeem, Muhammad, Bae, Junhwan, Kim, Jihyun, Lee, Juho, Hasan, Nurhasni, Kim, Wooseong, Im, Eunok, Jung, Yunjin, Yoo, Jin-Wook
Carbohydrate polymers 2018 v.198 pp. 434-442
alginates, animal models, anti-inflammatory activity, chitosan, colitis, dexamethasone, oligosaccharides, pH, particle size, small intestine, stomach, therapeutics
Oral colon-targeted drug delivery has gained popularity as an effective strategy for treatment of inflammatory bowel disease (IBD). In this study, we prepared colon-targeted dexamethasone microcrystals (DXMCs) coated with multilayers of chitosan oligosaccharide (CH), alginate (AG), and finally Eudragit S 100 (ES) (ES1AG4CH5-DXMCs) using a layer-by-layer (LBL) coating technique. Particle size, surface charge, in vitro drug release, and in vivo anti-inflammatory activity of ES1AG4CH5-DXMCs were evaluated. ES1AG4CH5-DXMCs had an average particle size of 2.34 ± 0.19 μm and a negative surface charge of - 48 ± 9 mV. ES1AG4CH5-DXMCs demonstrated pH-dependent dexamethasone release, avoiding initial burst drug release in acidic pH conditions of the stomach and small intestine, and providing subsequent sustained drug release in the colonic pH. Importantly, ES1AG4CH5-DXMCs exhibited a significant therapeutic activity in a mouse model of colitis compared to other DXMCs. Overall, the LBL-coated DXMCs presented here could be a promising colon-targeted therapy for IBD.