Design and optimization of rifaximin macroparticles for colon targeting

Year 2024, Volume: 28 Issue: 5, 1609 - 1618, 28.06.2025

Ashwani K Chaturvedi Uvs Sara Ram Dayal Gupta

Abstract

This study is focused to design a colon specific pellet formulation of rifaximin based on the combination of time-dependent and pH sensitive delivery system using Quality-by-Design (QbD) approach for better and promising treatment of inflammatory bowel disease (IBD). An extrusion/spheronization process was utilized for the preparation of core macroparticles using ethyl cellulose (EC) as matrix former and microcrystalline cellulose (MCC) as a spheronizing aid. Two critical process parameters (CPPs) i.e., spheronization time and spheronizer speed were taken as independent factors while aspect ratio, sphericity, carr's index, and particle size were taken as dependent responses to optimize the composition of the core macroparticles. To regulate the drug release, core macroparticles were coated with Eudragit NE40D and Eudragit FS30D to impart time-dependent and pH sensitive release of drug. The optimized coated macroparticles were characterized for drug content and in vitrodrug release in different pH media of stomach and intestine. The coating levels of the inner and outer polymers were further optimized for the time required for 10 %, 50 % and 90 % drug release. The result showed that the 90% of drug of P3 and P4 formulation were found to be released in 10.87 and 13.19hrs respectively. When exposed to Scanning Electron Microscopy the images of coated macroparticles suggested a uniform and smooth coat of polymers over the surface of macroparticles. This formulation reduces the dose and the side effects due to its specific targeting at the site of inflammation makes it a better choice over the tablets. The result indicates that the developed formulation may possibly reduce the dosing frequency and side effects associated with the conventional tablet formulation for the site-specific targeting at inflammation site.

Keywords

Macroparticles , colon targeted , rifaximin , Eudragit , MCC , Optimization

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