Varum, F; Cristina Freire, A; Fadda, HM; Bravo, R; Basit, AW; (2020) A dual pH and microbiota-triggered coating (Phloral™) for fail-safe colonic drug release. International Journal of Pharmaceutics , 583 , Article 119379. 10.1016/j.ijpharm.2020.119379.

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Abstract

Enteric-coated dosage forms are widely used for targeting the ileo-colonic region of the gastrointestinal (GI) tract. However, accurate targeting is challenging due to intra- and inter-individual variability in intestinal paramaters such as fluid pH and transit times, which occasionally lead to enteric coating failure. As such, a unique coating technology (Phloral™), which combines two independent release mechanisms – a pH trigger (Eudragit® S; dissolving at pH 7) and a microbiota-trigger (resistant starch), has been developed, offering a fail-safe approach to colonic targeting. Here, we demonstrate that the inclusion of resistant starch in the coating does not affect the pH mediated drug release mechanism or the robustness of the coating in the upper GI tract. In order to make the resistant starch more digestible by bacterial enzymes, heat treatment of the starch in the presence of butanol was required to allow disruption of the crystalline structure of the starch granules. Under challenging conditions of limited exposure to high pH in the distal small intestine fluid and rapid transit through the colon, often observed in patients with inflammatory bowel disease, particularly in ulcerative colitis, this dual-trigger pH-enzymatic coating offers a revolutionary approach for site specific drug delivery to the large intestine.

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