Treatment of ulcerative colitis by sustained release curcumin pellets coated with ethyl ascorbic acid; in-vitro, in-vivo, and in-silico analysis
Abstract
The present work aimed to protect the rapid reduction of Curcumin (Cur) in alkaline pH by newly synthesized ethyl ascorbic acid (EAA) in dual-coated Cur pellets (CCur-P4d) used for the treatment of inflammatory bowel disease (IBD). Physicochemical and morphological analysis was performed by FTIR, DSC, XRD, and SEM-EDS and in vitro release study. 92.87 ± 6.26 % release of Cur from uncoated Cur pellets (UCur-P4) in 0.1 M HCl at pH 1.2 was controlled to 5 % by coating with Eudragit L-100 (EL-100) which interns increased to 97.99 ± 7.35 % in 100 mM phosphate buffer of pH 7.4. The scavenging activity of 2,2-Diphenyl-1-picrylhydrazyl (DPPH) and hydrogen peroxides (H2O2) was 95.88 ± 1.22 % and 85.35 ± 1.43 %, respectively. Acute toxicity study and anti-ulcerative effect of CCur-P4d in ulcerative colitis (UC) induced albino rats were evaluated by microscopic and macroscopic analysis. In protein-ligand binding interaction, Cur showed a potent inhibitory effect on inflammatory markers C-reactive protein, IL-6, and TNF-α. Conclusively, CCur-P4d is considered an alternative to locally acting therapeutics agents used in IBD.
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