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A colon-specific delivery system for quercetin with enhanced cancer prevention based on co-axial electrospinning

Abstract

The antioxidant quercetin (Q) is a bioactive compound that can inhibit the colon cancer. However, the poor stability in the upper gastro-intestine tract and low bioavailability of Q compromised its benefits. In this study, a biopolymer-based colon-specific delivery system for Q was constructed by co-axial electrospinning. The quercetin-loaded chitosan nanoparticles (QCNP) were firstly prepared and characterized. Then, Q-loaded electrospun fiber mat (Q-loaded EFM) containing prebiotics (galactooligosaccharide, GOS)) were fabricated using sodium alginate as shell layer and the above QCNP and prebiotics as core layer. DPPH assay showed that the antioxidant activity of Q was maintained in the obtained film. Owing to the addition of prebiotics GOS, the obtained fiber mat possessed good prebiotic effects. In vitro release kinetics showed a sustained and targeted colon-specific release of Q from the Q-loaded EFM containing GOS, and the release rate of Q was enhanced by the presence of GOS. The obtained film also exhibited inhibition effects on Caco-2 cells in a dose- and time-dependent manner. Flow cytometry and fluorescence microscopy analysis indicated that Q-loaded EFM containing GOS exerted its activity on colonic cancer cells by arresting cell cycle on G0/G1 phase and triggering apoptotic cell death. This study demonstrates the potential of obtained film as oral delivery system for encapsulation, protection, and release of Q at colon for the oral therapy of colon disorders.

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Supplementary files

Publication details

The article was received on 19 Jun 2018, accepted on 07 Oct 2018 and first published on 08 Oct 2018


Article type: Paper
DOI: 10.1039/C8FO01216D
Citation: Food Funct., 2018, Accepted Manuscript
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    A colon-specific delivery system for quercetin with enhanced cancer prevention based on co-axial electrospinning

    P. Wen, T. Hu, L. Li, M. Zong and H. Wu, Food Funct., 2018, Accepted Manuscript , DOI: 10.1039/C8FO01216D

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