Oral colon delivery platform based on a novel combination approach: Design concept and preliminary evaluation

An oral colon delivery platform based on a novel combination strategy, leveraging multiple physiological characteristics of the intestine, is proposed. The system comprises drug core, water-swellable/soluble inner layer hydrophilic cellulose derivative and an enteric outer (Eudragit® S) containing microbially-degradable polysaccharide (high-amylose starch, Amylo N460), acting synergistically to prevent early release in small intestine one hand, failure other. Eudragit® S:Amylo N460 solid weight ratio external coating was 7:3; triethyl citrate glyceryl monostearate were used as plasticizer anti-tacking agent, respectively. S/Amylo applied fluid bed using hydro-alcoholic or aqueous formulations. Two types “inner” systems studied: (i) Drug-loaded tablets coated with low-viscosity hydroxypropyl methylcellulose (by spray-coating), (ii) capsules prepared by injection-molding (filled paracetamol analytical tracer). obtained dosage forms thoroughly characterized, including vitro measurements various media. In all cases, pulsatile profiles after medium change from 0.1 N HCl phosphate buffer pH 7.4, lag phases depending type preparation technique polymer layer. role microbiota performance explored simulated colonic (SCF), consisting culture inoculated fecal samples inflammatory bowel disease patients. Clear differences observed SCF versus free feces, indicating effect microbial degradation.