Colon Targeting of Naringin for Cytoprotection against Ulcerative Colitis: In Vitro-In Vivo Study
Journal Title: IOSR Journal of Pharmacy and Biological Sciences (IOSR-JPBS) - Year 2017, Vol 12, Issue 2
Abstract
Naringin has low oral bioavailability because of its degradation at the upper gut. Therefore, this study involved formulation of compression-coated tablets of naringin using mixtures of Eudragit L100-55 (EUD-L) and hydroxypropyl methylcellulose (HPMC) at two different respective weight ratios of 95:5 (F1) and 90:10 (F2). Evaluation of the tablets regarding drug content, physical characters, swelling and in vitro release has been performed. Kinetic analysis of release data was done. The effects of the selected tablet formulation on indomethacin-induced colitis in rabbits were investigated. The results showed that average values of drug content were 99.66 ± 2.18 and 104.00 ± 1.58 for F1 and F2, respectively. The prepared tablets showed good hardness (7.97-8.85 kg/cm²) and friability (less than 1%) that were within the pharmacopeal range. The increase in HPMC content to 10% of the coating weight (F2) resulted in higher swelling degree of the coated tablets. Therefore, more retarded release and colon targeting were obtained with higher HPMC content (F2) as clarified by percentage drug release of 17.80 ± 2.70 after 5 h. In accordance, this tablet formulation provided effective protection against indomethacin-induced colitis in rabbits as confirmed by normal mucosa of colon, significant (p < 0.05) decrease in levels of serum pANCA and colonic TNF-α.
Authors and Affiliations
Thanaa M. Borg a, Elham A. Mohamed, Eman E. El Naggar a, Ahmed R. El-Sheakh, , Mohammed F. Hamed
Keywords
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- EP ID EP388380
- DOI 10.9790/3008-1202012329
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