Effect of particle size on the oral absorption of isoliquiritigenin nanocrystals
Abstract As one of the most promising formulations for poorly water-soluble drugs, nanocrystals have been attracting increasing attention in recent years. Isoliquiritigenin (ISL) is a flavonoid with a chalcone structure, and possesses many biological activities. However, its clinical application is...
| Main Authors: | , , , , , |
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| Format: | Article |
| Language: | English |
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Universidade de São Paulo
2023-01-01
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| Series: | Brazilian Journal of Pharmaceutical Sciences |
| Subjects: | |
| Online Access: | http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502022000100405&tlng=en |
| _version_ | 1797951321538560000 |
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| author | Yanni Ma Xiaoying Yang Guoting Chen Yuxin Zhang Hao Zhang Wenping Zhang |
| author_facet | Yanni Ma Xiaoying Yang Guoting Chen Yuxin Zhang Hao Zhang Wenping Zhang |
| author_sort | Yanni Ma |
| collection | DOAJ |
| description | Abstract As one of the most promising formulations for poorly water-soluble drugs, nanocrystals have been attracting increasing attention in recent years. Isoliquiritigenin (ISL) is a flavonoid with a chalcone structure, and possesses many biological activities. However, its clinical application is significantly limited mainly due to its low oral bioavailability caused by poor hydrophilicity. To address this, ISL nanocrystals were developed in this study to improve its oral bioavailability. Three types of nanocrystals with differing particle size; R1, R2, and R3, were prepared by anti- solvent precipitation or anti-solvent precipitation combined with sonication, which was optimized by single-factor experiments. These nanocrystals were characterized based on their physical properties, in vitro release, and in vivo absorption performance. The mean particle size of R1, R2, and R3 was 555.7, 271.0, and 46.2, respectively. The dissolution ratio of ISL in the nanocrystals was significantly improved, with the quickest rate recorded in R2. Peak concentration and area under the concentration-time curve of R2 after oral administration in rats was 5.83- and 2.72-fold higher than that of the ISL solution, respectively. These findings indicate that the dissolution and absorption of ISL can be significantly enhanced by nanocrystals, and the dissolution behavior and pharmacokinetic properties of nanocrystals is significantly influenced by particle size. |
| first_indexed | 2024-04-10T22:28:43Z |
| format | Article |
| id | doaj.art-8a738c6c53d14aa8a9c07ab49a0b911c |
| institution | Directory Open Access Journal |
| issn | 2175-9790 |
| language | English |
| last_indexed | 2024-04-10T22:28:43Z |
| publishDate | 2023-01-01 |
| publisher | Universidade de São Paulo |
| record_format | Article |
| series | Brazilian Journal of Pharmaceutical Sciences |
| spelling | doaj.art-8a738c6c53d14aa8a9c07ab49a0b911c2023-01-17T07:34:25ZengUniversidade de São PauloBrazilian Journal of Pharmaceutical Sciences2175-97902023-01-015810.1590/s2175-97902022e201186Effect of particle size on the oral absorption of isoliquiritigenin nanocrystalsYanni MaXiaoying YangGuoting ChenYuxin ZhangHao ZhangWenping Zhanghttps://orcid.org/0000-0002-3905-3332Abstract As one of the most promising formulations for poorly water-soluble drugs, nanocrystals have been attracting increasing attention in recent years. Isoliquiritigenin (ISL) is a flavonoid with a chalcone structure, and possesses many biological activities. However, its clinical application is significantly limited mainly due to its low oral bioavailability caused by poor hydrophilicity. To address this, ISL nanocrystals were developed in this study to improve its oral bioavailability. Three types of nanocrystals with differing particle size; R1, R2, and R3, were prepared by anti- solvent precipitation or anti-solvent precipitation combined with sonication, which was optimized by single-factor experiments. These nanocrystals were characterized based on their physical properties, in vitro release, and in vivo absorption performance. The mean particle size of R1, R2, and R3 was 555.7, 271.0, and 46.2, respectively. The dissolution ratio of ISL in the nanocrystals was significantly improved, with the quickest rate recorded in R2. Peak concentration and area under the concentration-time curve of R2 after oral administration in rats was 5.83- and 2.72-fold higher than that of the ISL solution, respectively. These findings indicate that the dissolution and absorption of ISL can be significantly enhanced by nanocrystals, and the dissolution behavior and pharmacokinetic properties of nanocrystals is significantly influenced by particle size.http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502022000100405&tlng=enIsoliquiritigeninNanocrystalsParticle sizeOral bioavailabilityHPLC-MS/MS |
| spellingShingle | Yanni Ma Xiaoying Yang Guoting Chen Yuxin Zhang Hao Zhang Wenping Zhang Effect of particle size on the oral absorption of isoliquiritigenin nanocrystals Brazilian Journal of Pharmaceutical Sciences Isoliquiritigenin Nanocrystals Particle size Oral bioavailability HPLC-MS/MS |
| title | Effect of particle size on the oral absorption of isoliquiritigenin nanocrystals |
| title_full | Effect of particle size on the oral absorption of isoliquiritigenin nanocrystals |
| title_fullStr | Effect of particle size on the oral absorption of isoliquiritigenin nanocrystals |
| title_full_unstemmed | Effect of particle size on the oral absorption of isoliquiritigenin nanocrystals |
| title_short | Effect of particle size on the oral absorption of isoliquiritigenin nanocrystals |
| title_sort | effect of particle size on the oral absorption of isoliquiritigenin nanocrystals |
| topic | Isoliquiritigenin Nanocrystals Particle size Oral bioavailability HPLC-MS/MS |
| url | http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502022000100405&tlng=en |
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