Preparation and Characterization of Electrospun Colon-Specific Delivery System for Quercetin and Its Antiproliferative Effect on Cancer Cells
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.
Medienart: |
E-Artikel |
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Erscheinungsjahr: |
2018 |
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Erschienen: |
2018 |
Enthalten in: |
Zur Gesamtaufnahme - volume:66 |
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Enthalten in: |
Journal of agricultural and food chemistry - 66(2018), 44 vom: 07. Nov., Seite 11550-11559 |
Sprache: |
Englisch |
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Beteiligte Personen: |
Wen, Peng [VerfasserIn] |
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Links: |
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Themen: |
9012-76-4 |
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Anmerkungen: |
Date Completed 15.11.2018 Date Revised 15.11.2018 published: Print-Electronic Citation Status MEDLINE |
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doi: |
10.1021/acs.jafc.8b02614 |
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funding: |
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Förderinstitution / Projekttitel: |
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PPN (Katalog-ID): |
NLM287870197 |
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520 | |a 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 | ||
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