Development of trans-Chalcone loaded pectin/casein biodegradable microcapsules : Efficacy improvement in the management of experimental colitis
Copyright © 2023 Elsevier B.V. All rights reserved..
Improved therapies for inflammatory bowel diseases are sorely needed. Novel therapeutic agents and the development of controlled release systems for targeted tissue delivery are interesting approaches to overcome these barriers. We investigated the activity of trans-chalcone (T) in acetic acid-induced colitis in mice and developed, characterized, and determined the therapeutic effect of pectin/casein polymer microcapsules containing T (MT) in a colitis mouse model. In vitro, compound release was achieved in simulated intestinal fluid but not in the simulated gastric fluid. In vivo, since T at the dose of 3 mg/kg but not 0.3 mg/kg ameliorated colitis, we next tested the effects of MT at 0.3 mg/kg (non-effective dose). MT, but not free T at 0.3 mg/kg, significantly improved colitis outcomes such as neutrophil recruitment, antioxidant capacity, cytokine production, and NF-kB activation. This translated into reduced macro and microscopic damage in the colon. T release from the microcapsules is mediated by a pH-dependent and pectinase-regulated mechanism that provide controlled and prolonged release of T. Moreover, MT lowered the required dose for T therapeutic effect, indicating that could be a suitable pharmaceutical approach to colitis treatment. This is the first demonstration that T or MT is effective at reducing the signs of colitis.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2023 |
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| Erschienen: |
2023 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:642 |
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| Enthalten in: |
International journal of pharmaceutics - 642(2023) vom: 25. Juli, Seite 123206 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Guazelli, Carla F S [VerfasserIn] |
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| Links: |
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| Themen: |
5S5A2Q39HX |
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| Anmerkungen: |
Date Completed 23.10.2023 Date Revised 23.10.2023 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.ijpharm.2023.123206 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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NLM359204929 |
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| 100 | 1 | |a Guazelli, Carla F S |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Development of trans-Chalcone loaded pectin/casein biodegradable microcapsules |b Efficacy improvement in the management of experimental colitis |
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| 520 | |a Copyright © 2023 Elsevier B.V. All rights reserved. | ||
| 520 | |a Improved therapies for inflammatory bowel diseases are sorely needed. Novel therapeutic agents and the development of controlled release systems for targeted tissue delivery are interesting approaches to overcome these barriers. We investigated the activity of trans-chalcone (T) in acetic acid-induced colitis in mice and developed, characterized, and determined the therapeutic effect of pectin/casein polymer microcapsules containing T (MT) in a colitis mouse model. In vitro, compound release was achieved in simulated intestinal fluid but not in the simulated gastric fluid. In vivo, since T at the dose of 3 mg/kg but not 0.3 mg/kg ameliorated colitis, we next tested the effects of MT at 0.3 mg/kg (non-effective dose). MT, but not free T at 0.3 mg/kg, significantly improved colitis outcomes such as neutrophil recruitment, antioxidant capacity, cytokine production, and NF-kB activation. This translated into reduced macro and microscopic damage in the colon. T release from the microcapsules is mediated by a pH-dependent and pectinase-regulated mechanism that provide controlled and prolonged release of T. Moreover, MT lowered the required dose for T therapeutic effect, indicating that could be a suitable pharmaceutical approach to colitis treatment. This is the first demonstration that T or MT is effective at reducing the signs of colitis | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Flavonoids | |
| 650 | 4 | |a Inflammatory bowel disease | |
| 650 | 4 | |a Microencapsulated delivery system | |
| 650 | 4 | |a Nuclear factor-κB | |
| 650 | 4 | |a Oxidative stress | |
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| 700 | 1 | |a Fattori, Victor |e verfasserin |4 aut | |
| 700 | 1 | |a Colombo, Barbara B |e verfasserin |4 aut | |
| 700 | 1 | |a Ludwig, Isabela S |e verfasserin |4 aut | |
| 700 | 1 | |a Vicente, Laisa G |e verfasserin |4 aut | |
| 700 | 1 | |a Martinez, Renata M |e verfasserin |4 aut | |
| 700 | 1 | |a Georgetti, Sandra R |e verfasserin |4 aut | |
| 700 | 1 | |a Urbano, Alexandre |e verfasserin |4 aut | |
| 700 | 1 | |a Casagrande, Rubia |e verfasserin |4 aut | |
| 700 | 1 | |a Baracat, Marcela M |e verfasserin |4 aut | |
| 700 | 1 | |a Verri, Waldiceu A |c Jr |e verfasserin |4 aut | |
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