Development and Evaluation of Bioresponsive Tablets of a Selective COX-2 Inhibitor for Colonic Delivery

Abstract

Background: We report the effectiveness of a targeted delivery system containing Meloxicam using polysaccharides for the treatment of colorectal cancer. We also propose a novel biorelevant dissolution method to overcome drawbacks of existing dissolution methodologies of polysaccharidebased systems. The proposed method includes a mixture of probiotics cultured under anaerobic conditions in the presence of prebiotic in the in vitro dissolution study to surrogate colonic conditions. Polysaccharide- based system can be simple, safe and effective drug delivery system to target drugs to colon. Methods: Press-coated tablets of Meloxicam were prepared by direct compression using various polysaccharides, such as xanthan gum, guar gum and pectin as coating polysaccharides. Developed tablets were evaluated for physical parameters, lag phase and in vitro drug release. Developed probioticsbased dissolution method was validated and explored for versatility using other polysaccharides. Results: Press-coated tablets of Meloxicam were successfully developed exhibiting targeted delivery to the colon using guar gum as coat and releasing more than 80% of drug in simulated colonic fluid. The developed probiotics based dissolution method may prove to be useful as a bio-relevant and discriminatory method. Conclusion: Developed Meloxicam tablets press-coated with guar gum can be taken orally for treatment or as an adjuvant therapy in colon cancer. Polymers used in this formulation are abundant, nontoxic, biodegradable and inexpensive which make this a a very promising approach for the treatment of different colonic diseases. The proposed biorelevant, animal sparing, probiotics based dissolution medium was found to be versatile to study drug release from other polysaccharide based formulations for colonic delivery.