Chitosan–xanthan gum microparticle-based oral tablet for colon-targeted and sustained delivery of quercetin. (November 2014)

• Record Type: Journal Article
• Authors: Caddeo, Carla; Nácher, Amparo; Díez-Sales, Octavio; Merino-Sanjuán, Matilde; Fadda, Anna Maria; Manconi, Maria
• Is Part Of: Journal of microencapsulation. Volume 31:Number 7(2014:Nov.)
• Page Start: 694
• Page End: 699
• Publication Date: 2014-11
• Subjects: Microencapsulation -- Periodicals; Controlled release technology -- Periodicals; 615.19
• DOI: 10.3109/02652048.2014.913726
• Languages: English
• ISSNs: 0265-2048

Abstract

<abstract> <title>Abstract</title> <p> <italic>Context</italic>: Quercetin (QUE) is a flavonoid with antioxidant/anti-inflammatory properties, poorly absorbed when orally administered. <italic>Objectives</italic>: To prepare chitosan/xanthan gum microparticles to increase QUE oral bioavailability and optimize its release in the colon. <italic>Materials and methods</italic>: Chitosan/xanthan gum hydrogel embedding QUE was spray-dried to obtain microparticles characterized by size, scanning electron microscopy, differential scanning calorimetry and X-ray diffraction. Microparticles were compressed into tablets, coated with Eudragit® to further prevent degradation in acidic pH. The swelling degree and QUE release in simulated gastric and intestinal pH were investigated. <italic>Results</italic>: Microparticles were smooth and spherical, around 5 µm, with successful QUE loading. Microparticle tablets provided resistance to acidic conditions, allowing complete drug release in alkaline pH, mimicking colonic environment. The release was controlled by non-Fickian diffusion of the dissolved drug out of the swollen polymeric tablet. <italic>Discussion and conclusion</italic>: Microparticle tablets represent a promising dosage form for QUE delivery to the colon in the oral therapy of inflammatory-based disorders.</p> </abstract>