Preparation and evaluation in vitro and in vivo of pristinamycin enteric-coated granules based on albumin nanoparticles
CONTEXT: The purpose of this study was to prepare enteric-coated particles based on albumin nanoparticles (NPs) using a mixture of PIA albumin NPs freeze-dried powder (PA-PIA) and PIIA albumin NPs freeze-dried powder (PA-PIIA) to improve the bioavailability effect of pristinamycin.
OBJECTIVE: This is the first study on the preparation of pristinamycin into enteric-coated granules based on albumin NPs, and our study has effectively improved the bioavailability of pristinamycin and ensured its safety.
METHODS: Pristinamycin albumin enteric-coated granules (PAEGs) were prepared by hybrid wet granulation. The characterizations of albumin NPs were performed by in vitro and in vivo studies of PAEGs. The assays were analyzed using zeta-sizer, transmission electron microscopy, high-performance liquid chromatography, and a fully automated biochemical index analyzer.
RESULTS: The morphology of NPs was close to spherical. PIA-NPs and PIIA-NPs respectively had a zeta potential of (-24.33 ± 0.75) mV and (+7.30 ± 0.27) mV and mean size of (251.91 ± 19.64) nm and (232.83 ± 22.61) nm. The release of PIA and PIIA from PAEGs in the artificial gastrointestinal fluid was as high as 58.46% and 87.79%. In the experimental group of oral PAEGs, PIA and PIIA were AUC(0-t) (3.68 ± 0.58) mg·L-1·h-1 and (2.81 ± 1.06) mg·L-1·h-1. The results of aspartate aminotransferase and alanine aminotransferase biochemical indices showed that there was no significant difference between the experimental and normal groups of oral PAEGs.
CONCLUSION: The PAEGs significantly increased the release of PIA and PIIA in simulated intestinal fluid and improved the bioavailability. The oral administration of PAEGs may not damage the liver of rats. We hope that our study will promote its industrial development or clinical application.
Medienart: |
E-Artikel |
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Erscheinungsjahr: |
2023 |
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Erschienen: |
2023 |
Enthalten in: |
Zur Gesamtaufnahme - volume:49 |
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Enthalten in: |
Drug development and industrial pharmacy - 49(2023), 1 vom: 20. Jan., Seite 84-91 |
Sprache: |
Englisch |
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Beteiligte Personen: |
Shan, Wanxin [VerfasserIn] |
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Links: |
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Themen: |
Albumin nanoparticles |
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Anmerkungen: |
Date Completed 22.03.2023 Date Revised 22.03.2023 published: Print-Electronic Citation Status MEDLINE |
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doi: |
10.1080/03639045.2023.2182602 |
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funding: |
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Förderinstitution / Projekttitel: |
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PPN (Katalog-ID): |
NLM353099139 |
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500 | |a published: Print-Electronic | ||
500 | |a Citation Status MEDLINE | ||
520 | |a CONTEXT: The purpose of this study was to prepare enteric-coated particles based on albumin nanoparticles (NPs) using a mixture of PIA albumin NPs freeze-dried powder (PA-PIA) and PIIA albumin NPs freeze-dried powder (PA-PIIA) to improve the bioavailability effect of pristinamycin | ||
520 | |a OBJECTIVE: This is the first study on the preparation of pristinamycin into enteric-coated granules based on albumin NPs, and our study has effectively improved the bioavailability of pristinamycin and ensured its safety | ||
520 | |a METHODS: Pristinamycin albumin enteric-coated granules (PAEGs) were prepared by hybrid wet granulation. The characterizations of albumin NPs were performed by in vitro and in vivo studies of PAEGs. The assays were analyzed using zeta-sizer, transmission electron microscopy, high-performance liquid chromatography, and a fully automated biochemical index analyzer | ||
520 | |a RESULTS: The morphology of NPs was close to spherical. PIA-NPs and PIIA-NPs respectively had a zeta potential of (-24.33 ± 0.75) mV and (+7.30 ± 0.27) mV and mean size of (251.91 ± 19.64) nm and (232.83 ± 22.61) nm. The release of PIA and PIIA from PAEGs in the artificial gastrointestinal fluid was as high as 58.46% and 87.79%. In the experimental group of oral PAEGs, PIA and PIIA were AUC(0-t) (3.68 ± 0.58) mg·L-1·h-1 and (2.81 ± 1.06) mg·L-1·h-1. The results of aspartate aminotransferase and alanine aminotransferase biochemical indices showed that there was no significant difference between the experimental and normal groups of oral PAEGs | ||
520 | |a CONCLUSION: The PAEGs significantly increased the release of PIA and PIIA in simulated intestinal fluid and improved the bioavailability. The oral administration of PAEGs may not damage the liver of rats. We hope that our study will promote its industrial development or clinical application | ||
650 | 4 | |a Journal Article | |
650 | 4 | |a Pristinamycin | |
650 | 4 | |a albumin nanoparticles | |
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700 | 1 | |a Shen, Qi |e verfasserin |4 aut | |
700 | 1 | |a Zhang, Jun |e verfasserin |4 aut | |
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