Isoliquiritigenin Containing PH Sensitive Micelles for Enhanced Anti-Colitis Activity
Copyright © 2023 American Pharmacists Association. Published by Elsevier Inc. All rights reserved..
Isoliquiritigenin (ISL) is known to have a variety of pharmacological activities, but its poor water solubility limits its application. In order to improve the bioavailability of ISL and its anti-colitis activity, this study aims to develop an effective drug delivery system loaded with ISL. In this study, ISL pH-sensitive micelles (ISL-M) were prepared by thin film hydration method. The micellar size (PS), polydispersity index (PDI), electrokinetic potential (ζ-potential), drug loading (DL), encapsulation rate (EE) and other physical parameters were characterized. The storage stability of ISL-M was tested, release in vitro and pharmacokinetic studies in rats were performed, and the anti-inflammatory effect of ISL-M on ulcerative colitis induced by dextran sulfate sodium (DSS) was evaluated. The results showed that PS, PDI, ZP, EE% and DL% of ISL-M were 151.15±1.04 nm, 0.092±0.014, -31.32±0.721 mV, 93.97±1.53 % and 8.42±0.34 %, respectively. Compared with unformulated ISL (F-ISL), the cumulative release rate of ISL-M in the three different media was significantly increased and showed a certain pH sensitivity. The area under drug curve (AUC0-t) and peak concentration (Cmax) of ISL-M group were 2.94 and 4.06 times higher than those of ISL group. In addition, ISL-M is expected to develop new methods for increasing the bioavailability and anti-inflammatory activity of ISL.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2024 |
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| Erschienen: |
2024 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:113 |
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| Enthalten in: |
Journal of pharmaceutical sciences - 113(2024), 4 vom: 01. März, Seite 918-929 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Shi, Feng [VerfasserIn] |
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| Links: |
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| Themen: |
Anti-Inflammatory Agents |
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| Anmerkungen: |
Date Completed 19.03.2024 Date Revised 19.03.2024 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.xphs.2023.09.020 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| 520 | |a Isoliquiritigenin (ISL) is known to have a variety of pharmacological activities, but its poor water solubility limits its application. In order to improve the bioavailability of ISL and its anti-colitis activity, this study aims to develop an effective drug delivery system loaded with ISL. In this study, ISL pH-sensitive micelles (ISL-M) were prepared by thin film hydration method. The micellar size (PS), polydispersity index (PDI), electrokinetic potential (ζ-potential), drug loading (DL), encapsulation rate (EE) and other physical parameters were characterized. The storage stability of ISL-M was tested, release in vitro and pharmacokinetic studies in rats were performed, and the anti-inflammatory effect of ISL-M on ulcerative colitis induced by dextran sulfate sodium (DSS) was evaluated. The results showed that PS, PDI, ZP, EE% and DL% of ISL-M were 151.15±1.04 nm, 0.092±0.014, -31.32±0.721 mV, 93.97±1.53 % and 8.42±0.34 %, respectively. Compared with unformulated ISL (F-ISL), the cumulative release rate of ISL-M in the three different media was significantly increased and showed a certain pH sensitivity. The area under drug curve (AUC0-t) and peak concentration (Cmax) of ISL-M group were 2.94 and 4.06 times higher than those of ISL group. In addition, ISL-M is expected to develop new methods for increasing the bioavailability and anti-inflammatory activity of ISL | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Anti-colitis | |
| 650 | 4 | |a ISL | |
| 650 | 4 | |a ISL-M | |
| 650 | 4 | |a pH sensitive micelles | |
| 650 | 7 | |a Micelles |2 NLM | |
| 650 | 7 | |a isoliquiritigenin |2 NLM | |
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| 700 | 1 | |a Du, Mengzhe |e verfasserin |4 aut | |
| 700 | 1 | |a Wang, Qin |e verfasserin |4 aut | |
| 700 | 1 | |a Adu-Frimpong, Michael |e verfasserin |4 aut | |
| 700 | 1 | |a Li, Chenlu |e verfasserin |4 aut | |
| 700 | 1 | |a Zhang, Xinyue |e verfasserin |4 aut | |
| 700 | 1 | |a Ji, Hao |e verfasserin |4 aut | |
| 700 | 1 | |a Toreniyazov, Elmurat |e verfasserin |4 aut | |
| 700 | 1 | |a Cao, Xia |e verfasserin |4 aut | |
| 700 | 1 | |a Wang, Qilong |e verfasserin |4 aut | |
| 700 | 1 | |a Xu, Ximing |e verfasserin |4 aut | |
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