Colon-targeted quercetin delivery using natural polymer to enhance its bioavailability

Abstract

The aim of the present study is to develop a polymer (Guar Gum)-based matrix tablet (using quercetin as a model drug) with sufficient mechanical strength, and promising in vitro mouth-to-colon release profile. By definition, an oral colonic delivery system should retard drug release in the stomach and small intestine, and allow complete release in the colon. By drug delivery to the colon would therefore ensure direct treatment at the disease site, lower dosing, and fewer systemic side effects. Quercetin is antioxidant in nature and used to treat colon cancer, but they have poor absorption in the upper part of the gastrointestinal tract (GIT). As a site for drug delivery, the colon offers a near neutral pH, reduced digestive enzymatic activity, a long transit time, and an increased responsiveness to absorption enhancers. By achieving a colon-targeted drug delivery system, the absorption of quercetin may be increased, which leads to better bioactivity in fewer doses.

Role of the Encapsulation in Bioavailability of Phenolic Compounds

“…The goal of quercetin encapsulation is to preserve it as it passes through the stomach and small intestine and to allow its release in the large intestine [ 215 ]. Singhal et al [ 216 ] conducted an in vitro study where guar gum was shown to be a desirable material for encapsulation of quercetin due to its ability to preserve the active compound during its passage through the upper part of the GIT. Guar gum is profoundly branched galactomannans and due to that structure, it holds out against enzymatic breakdown in GIT [ 216 ].…”

“…Singhal et al [ 216 ] conducted an in vitro study where guar gum was shown to be a desirable material for encapsulation of quercetin due to its ability to preserve the active compound during its passage through the upper part of the GIT. Guar gum is profoundly branched galactomannans and due to that structure, it holds out against enzymatic breakdown in GIT [ 216 ]. The combination of chitosan and xanthan gum can be promising for the controlled release of quercetin.…”

A novel dissolution method for evaluation of polysaccharide based colon specific delivery systems: A suitable alternative to animal sacrifice

“…The methods that have been reported for evaluation of colon targeted delivery systems include triggering by enzymes (Philip et al, 2008;Fetzner et al, 2004;Macfarlane et al, 1989;Maculotti et al, 2009;Maestrelli et al, 2008;Liu et al, 2012;Semde et al, 2000a,b Omar et al, 2007Jain et al, 2007a,b et al, 2010), rat caecal contents (Rubinstein et al, 1993;Jain et al, 2007a,b;Watanabe et al, 1998;Takemura et al, 2000;Tiwari et al, 2011;Shukla et al, 2012Shukla et al, , 2011Krishnaiah et al, 2001;Shyale et al, 2005;Ravi et al, 2008;Varshosaz et al, 2010;Singhal et al, 2011;Wei et al, 2007;Seal and Mathers, 2001), human faecal slurries (Salunkhe and Kulkarni, 2008;Siew et al, 2000Siew et al, , 2004McConnel et al, 2007;Karrout et al, 2009;Krenzlin et al, 2011), and multi stage compound culture system (Yang, 2008;Kotla et al, 2014;Schacht et al, 1996). Despite a large number of research reports on microbially triggered delivery systems for colon delivery, no such product is commercially available.…”

Chitosan–xanthan gum microparticle-based oral tablet for colon-targeted and sustained delivery of quercetin

“…In particular, quercetin (QUE; 3,3 0 ,4 0 ,5,7-pentahydroxyflavone) has been demonstrated to exert strong antioxidant and anti-inflammatory activities against osteoporosis, certain forms of cancer, pulmonary and cardiovascular diseases and aging (Boots et al, 2008). Furthermore, these properties may be crucial in the treatment of colon disorders, such as inflammatory bowel diseases (ulcerative colitis and Crohn's disease), irritable bowel syndrome and cancer (Chessa et al, 2011;Singhal et al, 2011). It was demonstrated that QUE reduced cell proliferation and tumour incidence in vitro on colonic cancer cell lines and in vivo in mice (Shan et al, 2009).…”