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. 2023 Feb 23;24(5):4454. doi: 10.3390/ijms24054454

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© 2023 by the authors.

Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).

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(A) PLGA (a biodegradable polymer) reduces the burst release of NPs, whose release rate is also prolonged; Eudragit S100 (a pH-sensitive polymer) protects NPs from destruction in the stomach and small intestine, then releases the flavonoid in the colon (pH ≥ 6.8). (B) Disturbed mucosal barrier, loss of epithelial integrity, widening of gaps between enterocytes, and increased recruitment of immune cells are usually present in IBD. The pathological changes disrupt the barrier function of the epithelium with increased translocation of bacteria and loss of fluid and electrolytes. Meanwhile, they facilitate increased accumulation and penetration of NPs across the epithelium and uptake by enterocytes and immune cells such as macrophages. (C) Mechanism of flavonoid release from pH-sensitive NPs: Eudragit S100 (a pH-sensitive polymer) deprotonates when exposed to a threshold pH ≥ 6.8, causing polymer swelling, dissolution, and erosion with subsequent flavonoid release. ( decrease; increase).

Inline graphic — (A) PLGA (a biodegradable polymer) reduces the burst release of NPs, whose release rate is also prolonged; Eudragit S100 (a pH-sensitive polymer) protects NPs from destruction in the stomach and small intestine, then releases the flavonoid in the colon (pH ≥ 6.8). (B) Disturbed mucosal barrier, loss of epithelial integrity, widening of gaps between enterocytes, and increased recruitment of immune cells are usually present in IBD. The pathological changes disrupt the barrier function of the epithelium with increased translocation of bacteria and loss of fluid and electrolytes. Meanwhile, they facilitate increased accumulation and penetration of NPs across the epithelium and uptake by enterocytes and immune cells such as macrophages. (C) Mechanism of flavonoid release from pH-sensitive NPs: Eudragit S100 (a pH-sensitive polymer) deprotonates when exposed to a threshold pH ≥ 6.8, causing polymer swelling, dissolution, and erosion with subsequent flavonoid release. ( decrease; increase).