COLON SPECIFIC DELIVERY OF EUDRAGIT E-100 AND EUDRAGIT-FS30D COATED TABLETS OF LEFLUNOMIDE USING CHITOSAN-CHONDROITIN SULPHATE INTERPOLYMER COMPLEX
Objectives: In the present study, site specific colonic drug delivery system was developed on the principles of the combination of pH and microbially triggered controlled system.
Methods: The basic design consists of chitosan-chondroitin sulphate inter-polymer complex containing leflunomide. The core tablet was enteric coated with Eudragit E-100 so that colon specific drug release can be achieved.Â TheÂ leflunomide, chitosan (CH), chondroitin sulphate (ChS), chitosan-chondroitin sulphate inter-polymer complex (CH-ChS IPC) were characterized byÂ Fourier Transform Infrared Spectroscopy (FT-IR). In vitro drug release study was conducted using sequential dissolution technique at 0.1 N HCl buffer (simulated gastric fluid), phosphate buffer pH 7.4 (simulated intestinal fluid) and finally in phosphate buffer pH 6.8 (simulated colonic fluid) with or without rat caecal content.
Results: FTIRÂ studiesÂ confirmedÂ thatÂ thereÂ wasÂ noÂ interactionÂ betweenÂ drugÂ andÂ polymer.Â Tablets coated with Eudragit E-100 with different coat weights showed less than 10% of drug release in the stomach whereas same tablets showed 13.42%, 9.5%, 12.37% and 12.83% release of drug in phosphate buffer pH 7.4 and95.43%, 90.31%, 98.44% and 96.64% release of drug in phosphate buffer pH 6.8. Histopathology of rat colon after administration of Eudragit E-100 coated tablets containing chitosan-chondroitin sulphate inter-polymer complex revealed the marked reduction in acetic acid induced colitis in the test group.
Conclusion: The present study confirmed that coating with Eudragit E-100 delivered the leflunomide to colon in highest efficacy with the least toxic effects of an anti-inflammatory therapy.
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