Chitosan coated yeast microcapsules for efficient delivery of cefadroxil for the treatment of inflammatory bowel disease.

Abstract

Inflammatory bowel disease (IBD) is a chronic inflammatory disorder of the gastrointestinal tract (GIT). Cefadroxil, a semisynthetic anti-bacterial cephalosporin, was investigated for repurposing in IBD therapy. Yeast microcapsules (YM) have attracted a lot of attention due to their ability to target the inflamed colonic region. However, premature drug release has hindered its applicability in oral drug delivery. Chitosan has been frequently used for stabilizing the premature release of a drug from a carrier system through surface coating. Hence, the aim of the current study is to evaluate the in vivo efficacy of cefadroxil in IBD treatment and to formulate and characterise cefadroxil-loaded YM coated with chitosan. An in vivo efficacy study in a mouse model demonstrates good therapeutic activity by improving disease pathology, exhibiting strong antioxidant activity, and reducing the expression of inflammatory biomarkers and cell infiltration. YM showed an irregular, porous structure with a size of 2.833 ± 0.72 μm. The % entrapment was 92.54 % and drug loading was 79.14 %. The 0.5, 1, and 1.5 % of chitosan-coated YM showed a regular spheroidal shape with a size of 2.78 ± 0.06 μm, 3.03 ± 0.16 μm, and 3.33 ± 0.15 μm, respectively. Moreover, drug-excipient interaction studies indicate no possible interaction, with a release of 60 % in intestinal pH within 24 h. Cefadroxil-loaded YM coated with chitosan showed significant therapeutic activity in the IBD animal model and also achieved colon targeting. Therefore, this cefadroxil-loaded YM coated with chitosan could be used as a targeted oral drug delivery system for the treatment of IBD.