Title:Site Targeted Press Coated Delivery of Methylprednisolone Using Eudragit RS 100 and Chitosan for Treatment of Colitis
Volume: 11
Issue: 1
Author(s): Swati Jagdale and Apoorva Chandekar
Affiliation:
Keywords:
Chitosan, coated, colitis, colon, eudragit, methylprednisolone.
Abstract: Background: Inflammatory bowel disease (IBD) is one of the five most prevalent
gastrointestinal disease burdens which commonly require lifetime care. Worldwide incidence
rate of ulcerative colitis and Crohn’s disease is about 16.8% and 13.4% respectively.
Colitis is an inflammation of the colon. Colon targeted drug delivery will direct the
drug to the colon. The drug will reach at the site of action and hence its side effects as well
as dose can be reduced. Recent patent describes treatment of ulcerative colitis using anti
CD3 antibodies, with nicotine and anti-depressant drugs, budesonide foam etc.
Objective: Present study deals with optimization of site targeted methylprednisolone delivery for treatment of
colitis.
Method: Chitosan and Eudragit RS 100 were used as coating polymers. Tablets were prepared by press coated
technology. The core tablets contain drug, avicel as binder, croscarmellose sodium as super disintegrant and
dicalcium phosphate as diluent. Drug excipient compatibility was carried out using FTIR, UV and DSC. Design
of experiment was used to optimize the formulation. Tablets were evaluated for thickness, weight variation,
hardness, swelling index, in-vitro drug release and release of drug in simulated media.
Results: Optimized batch (B2) contained chitosan 40% and eudragit RS 100 17.5%. B2 showed in-vitro drug
release 85.65 ± 7.6% in 6.8 pH phosphate buffer and 96.7 ±9.1% in simulated media after 7.5 hours.
Conclusion: In-vivo x-ray placebo study for formulation B2 had shown that the tablet reached to the ascending
colon after 5 hours. This indicated a potential site targeted delivery of optimized batch B2.
