Increased bioaffinity and anti-inflammatory activity of florfenicol nanocrystals by wet grinding method
Context: The main objective of the current study is to improve the water solubility of florfenicol (FF) and evaluate changes in its pharmacokinetics and anti-inflammatory activity.Materials and methods: Florfenicol nanocrystals (FF-NC) were prepared by wet grinding combined with spray drying. The characterisations, pharmacokinetics, and anti-inflammatory activity of FF-NC were evaluated.Results: The particle size, polydispersity index (PDI), and zeta potential of FF-NC were 276.4 ± 19.4 nm, 0.166 ± 0.011, and -18.66 ± 5.25 mV, respectively. Compared with FF, FF-NC showed a better dissolution rate in media at different pH. Pharmacokinetic experiments showed the area under the curve (AUC0-t), maximum concentration (Cmax), and mean residence time (MRT) of FF-NC were about 4.62-fold, 2.86-fold, and 1.68-fold higher compared with FF, respectively. In vitro anti-inflammatory experiments showed that FF inhibited the secretion of tumour necrosis factor-α (TNF-α), interleukin-6 (IL-6), and synthesis of NO in a dose-dependent manner, while FF-NC showed a stronger anti-inflammatory effect than FF under the same dose.Conclusion: FF-NC are an effective way to improve the bioaffinity and anti-inflammatory effects of FF.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2020 |
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| Erschienen: |
2020 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:37 |
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| Enthalten in: |
Journal of microencapsulation - 37(2020), 2 vom: 16. März, Seite 109-120 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Fang, Yuqi [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 08.10.2020 Date Revised 08.10.2020 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1080/02652048.2019.1701115 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM304160393 |
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| 100 | 1 | |a Fang, Yuqi |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Increased bioaffinity and anti-inflammatory activity of florfenicol nanocrystals by wet grinding method |
| 264 | 1 | |c 2020 | |
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| 500 | |a Date Completed 08.10.2020 | ||
| 500 | |a Date Revised 08.10.2020 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Context: The main objective of the current study is to improve the water solubility of florfenicol (FF) and evaluate changes in its pharmacokinetics and anti-inflammatory activity.Materials and methods: Florfenicol nanocrystals (FF-NC) were prepared by wet grinding combined with spray drying. The characterisations, pharmacokinetics, and anti-inflammatory activity of FF-NC were evaluated.Results: The particle size, polydispersity index (PDI), and zeta potential of FF-NC were 276.4 ± 19.4 nm, 0.166 ± 0.011, and -18.66 ± 5.25 mV, respectively. Compared with FF, FF-NC showed a better dissolution rate in media at different pH. Pharmacokinetic experiments showed the area under the curve (AUC0-t), maximum concentration (Cmax), and mean residence time (MRT) of FF-NC were about 4.62-fold, 2.86-fold, and 1.68-fold higher compared with FF, respectively. In vitro anti-inflammatory experiments showed that FF inhibited the secretion of tumour necrosis factor-α (TNF-α), interleukin-6 (IL-6), and synthesis of NO in a dose-dependent manner, while FF-NC showed a stronger anti-inflammatory effect than FF under the same dose.Conclusion: FF-NC are an effective way to improve the bioaffinity and anti-inflammatory effects of FF | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Video-Audio Media | |
| 650 | 4 | |a Wet grinding | |
| 650 | 4 | |a anti-inflammatory | |
| 650 | 4 | |a florfenicol nanocrystals | |
| 650 | 4 | |a pharmacokinetics | |
| 650 | 4 | |a solubility | |
| 650 | 7 | |a Anti-Inflammatory Agents |2 NLM | |
| 650 | 7 | |a Il6 protein, rat |2 NLM | |
| 650 | 7 | |a Interleukin-6 |2 NLM | |
| 650 | 7 | |a Tumor Necrosis Factor-alpha |2 NLM | |
| 650 | 7 | |a Nitric Oxide |2 NLM | |
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| 650 | 7 | |a florfenicol |2 NLM | |
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| 650 | 7 | |a Thiamphenicol |2 NLM | |
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| 700 | 1 | |a Li, Shuqi |e verfasserin |4 aut | |
| 700 | 1 | |a Ye, Lijuan |e verfasserin |4 aut | |
| 700 | 1 | |a Yi, Jun |e verfasserin |4 aut | |
| 700 | 1 | |a Li, Xiaofang |e verfasserin |4 aut | |
| 700 | 1 | |a Gao, Chongkai |e verfasserin |4 aut | |
| 700 | 1 | |a Wu, Fang |e verfasserin |4 aut | |
| 700 | 1 | |a Guo, Bohong |e verfasserin |4 aut | |
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