Fabrication and In Vitro/Vivo Evaluation of Drug Nanocrystals Self-Stabilized Pickering Emulsion for Oral Delivery of Quercetin
The aim of this study was to develop a new drug nanocrystals self-stabilized Pickering emulsion (NSSPE) for improving oral bioavailability of quercetin (QT). Quercetin nanocrystal (QT–NC) was fabricated by high pressure homogenization method, and QT–NSSPE was then prepared by ultrasound method with...
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| Format: | Article |
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MDPI AG
2022-04-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/14/5/897 |
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| author | Zhe Wang Bo Dai Xiaohan Tang Zhihui Che Fei Hu Chengying Shen Wei Wu Baode Shen Hailong Yuan |
| author_facet | Zhe Wang Bo Dai Xiaohan Tang Zhihui Che Fei Hu Chengying Shen Wei Wu Baode Shen Hailong Yuan |
| author_sort | Zhe Wang |
| collection | DOAJ |
| description | The aim of this study was to develop a new drug nanocrystals self-stabilized Pickering emulsion (NSSPE) for improving oral bioavailability of quercetin (QT). Quercetin nanocrystal (QT–NC) was fabricated by high pressure homogenization method, and QT–NSSPE was then prepared by ultrasound method with QT–NC as solid particle stabilizer and optimized by Box-Behnken design. The optimized QT–NSSPE was characterized by fluorescence microscope (FM), scanning electron micrograph (SEM), X-ray diffraction (XRD), and differential scanning calorimetry (DSC). The stability, in vitro release, and in vivo oral bioavailability of QT–NSSPE were also investigated. Results showed that the droplets of QT–NSSPE with the size of 10.29 ± 0.44 μm exhibited a core-shell structure consisting of a core of oil and a shell of QT–NC. QT–NSSPE has shown a great stability in droplets shape, size, creaming index, zeta potential, and QT content during 30 days storage at 4, 25, and 40 °C. In vitro release studies showed that QT–NSSPE performed a better dissolution behavior (65.88% within 24 h) as compared to QT–NC (50.71%) and QT coarse powder (20.15%). After oral administration, the AUC<sub>0–t</sub> of QT–NSSPE was increased by 2.76-times and 1.38 times compared with QT coarse powder and QT–NC. It could be concluded that NSSPE is a promising oral delivery system for improving the oral bioavailability of QT. |
| first_indexed | 2024-03-10T03:08:51Z |
| format | Article |
| id | doaj.art-b68524cc5a434aba83ca84e900d0c6cb |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-10T03:08:51Z |
| publishDate | 2022-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-b68524cc5a434aba83ca84e900d0c6cb2023-11-23T12:36:07ZengMDPI AGPharmaceutics1999-49232022-04-0114589710.3390/pharmaceutics14050897Fabrication and In Vitro/Vivo Evaluation of Drug Nanocrystals Self-Stabilized Pickering Emulsion for Oral Delivery of QuercetinZhe Wang0Bo Dai1Xiaohan Tang2Zhihui Che3Fei Hu4Chengying Shen5Wei Wu6Baode Shen7Hailong Yuan8Department of Pharmacy, Air Force Medical Center, PLA, Beijing 100142, ChinaDepartment of Pharmacy, Air Force Medical Center, PLA, Beijing 100142, ChinaSchool of Pharmacy, Anhui Medical University, Hefei 230032, ChinaDepartment of Pharmacy, Air Force Medical Center, PLA, Beijing 100142, ChinaDepartment of Pharmacy, Air Force Medical Center, PLA, Beijing 100142, ChinaDepartment of Pharmacy, Jiangxi Provincial People’s Hospital, Nanchang 330004, ChinaKey Laboratory of Smart Drug Delivery of Ministry of Education, School of Pharmacy, Fudan University, Shanghai 201203, ChinaDepartment of Pharmacy, Air Force Medical Center, PLA, Beijing 100142, ChinaDepartment of Pharmacy, Air Force Medical Center, PLA, Beijing 100142, ChinaThe aim of this study was to develop a new drug nanocrystals self-stabilized Pickering emulsion (NSSPE) for improving oral bioavailability of quercetin (QT). Quercetin nanocrystal (QT–NC) was fabricated by high pressure homogenization method, and QT–NSSPE was then prepared by ultrasound method with QT–NC as solid particle stabilizer and optimized by Box-Behnken design. The optimized QT–NSSPE was characterized by fluorescence microscope (FM), scanning electron micrograph (SEM), X-ray diffraction (XRD), and differential scanning calorimetry (DSC). The stability, in vitro release, and in vivo oral bioavailability of QT–NSSPE were also investigated. Results showed that the droplets of QT–NSSPE with the size of 10.29 ± 0.44 μm exhibited a core-shell structure consisting of a core of oil and a shell of QT–NC. QT–NSSPE has shown a great stability in droplets shape, size, creaming index, zeta potential, and QT content during 30 days storage at 4, 25, and 40 °C. In vitro release studies showed that QT–NSSPE performed a better dissolution behavior (65.88% within 24 h) as compared to QT–NC (50.71%) and QT coarse powder (20.15%). After oral administration, the AUC<sub>0–t</sub> of QT–NSSPE was increased by 2.76-times and 1.38 times compared with QT coarse powder and QT–NC. It could be concluded that NSSPE is a promising oral delivery system for improving the oral bioavailability of QT.https://www.mdpi.com/1999-4923/14/5/897pickering emulsionself-stabilizingpoorly soluble drugquercetinnanocrystalsoral bioavailability |
| spellingShingle | Zhe Wang Bo Dai Xiaohan Tang Zhihui Che Fei Hu Chengying Shen Wei Wu Baode Shen Hailong Yuan Fabrication and In Vitro/Vivo Evaluation of Drug Nanocrystals Self-Stabilized Pickering Emulsion for Oral Delivery of Quercetin Pharmaceutics pickering emulsion self-stabilizing poorly soluble drug quercetin nanocrystals oral bioavailability |
| title | Fabrication and In Vitro/Vivo Evaluation of Drug Nanocrystals Self-Stabilized Pickering Emulsion for Oral Delivery of Quercetin |
| title_full | Fabrication and In Vitro/Vivo Evaluation of Drug Nanocrystals Self-Stabilized Pickering Emulsion for Oral Delivery of Quercetin |
| title_fullStr | Fabrication and In Vitro/Vivo Evaluation of Drug Nanocrystals Self-Stabilized Pickering Emulsion for Oral Delivery of Quercetin |
| title_full_unstemmed | Fabrication and In Vitro/Vivo Evaluation of Drug Nanocrystals Self-Stabilized Pickering Emulsion for Oral Delivery of Quercetin |
| title_short | Fabrication and In Vitro/Vivo Evaluation of Drug Nanocrystals Self-Stabilized Pickering Emulsion for Oral Delivery of Quercetin |
| title_sort | fabrication and in vitro vivo evaluation of drug nanocrystals self stabilized pickering emulsion for oral delivery of quercetin |
| topic | pickering emulsion self-stabilizing poorly soluble drug quercetin nanocrystals oral bioavailability |
| url | https://www.mdpi.com/1999-4923/14/5/897 |
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