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J Agric Food Chem. 2018 Nov 7;66(44):11550-11559. doi: 10.1021/acs.jafc.8b02614. Epub 2018 Sep 7.

Preparation and Characterization of Electrospun Colon-Specific Delivery System for Quercetin and Its Antiproliferative Effect on Cancer Cells.

Author information

1
School of Food Science and Engineering , South China University of Technology , Guangzhou 510640 , China.
2
School of Chemical Engineering and Energy Technology , Dongguan University of Technology , Dongguan 523808 , China.
3
Guangdong Province Key Laboratory for Green Processing of Natural Products and Product Safety , Guangzhou 510640 , China.

Abstract

To improve the oral bioavailability of quercetin (Q) and achieve colon-specific release, a core-sheath electrospun fiber mat containing Q-loaded chitosan nanoparticle (Q-loaded EFM) was developed in this study. The nanoparticle was first fabricated, and its antioxidant activity was as effective as free Q. Then the uniform Q-loaded EFM was obtained using response surface methodology optimization, and its core-sheath structure was characterized by confocal laser scanning microscopy. In vitro release kinetics confirmed the colon targeting profile, and the release rate of Q varied inversely with fiber diameter. The data of Cell Counting Kit-8 suggested Q-loaded EFM inhibited the proliferation of Caco-2 cells in a dose- and time-dependent manner with an IC50 of 4.36, 2.81, and 2.01 mg/mL after 24, 48, and 72 h, respectively, and it was caused by arresting cell cycle on G0/G1 phase and triggering apoptotic cell death. This study suggests that the Q-loaded EFM represents a promising form in the oral therapy of colon disorders.

KEYWORDS:

bioactivity; coaxial electrospinning; colon-specific delivery; core−sheath nanostructure; quercetin

PMID:
30148954
DOI:
10.1021/acs.jafc.8b02614
[Indexed for MEDLINE]

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