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Volume 14
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10.3390/pharmaceutics14050897
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Article

Fabrication and In Vitro/Vivo Evaluation of Drug Nanocrystals Self-Stabilized Pickering Emulsion for Oral Delivery of Quercetin

by
Zhe Wang
1,2,
Bo Dai
1,
Xiaohan Tang
3,
Zhihui Che
1,
Fei Hu
1,4,
Chengying Shen
5,
Wei Wu
6,
Baode Shen
1,4,* and
Hailong Yuan
1,*
1
Department of Pharmacy, Air Force Medical Center, PLA, Beijing 100142, China
2
College of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China
3
School of Pharmacy, Anhui Medical University, Hefei 230032, China
4
Key Lab of Modern Preparation of Traditional Chinese Medicine, Ministry of Education, Jiangxi University of Chinese Medicine, Nanchang 330004, China
5
Department of Pharmacy, Jiangxi Provincial People’s Hospital, Nanchang 330004, China
6
Key Laboratory of Smart Drug Delivery of Ministry of Education, School of Pharmacy, Fudan University, Shanghai 201203, China
*
Authors to whom correspondence should be addressed.
Pharmaceutics 2022, 14(5), 897; https://doi.org/10.3390/pharmaceutics14050897
Submission received: 18 February 2022 / Revised: 24 March 2022 / Accepted: 30 March 2022 / Published: 20 April 2022
(This article belongs to the Topic Advances in Natural Products from Plants and Associated Microbes)
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Abstract

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 AUC0–t 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.
Keywords: pickering emulsion; self-stabilizing; poorly soluble drug; quercetin; nanocrystals; oral bioavailability pickering emulsion; self-stabilizing; poorly soluble drug; quercetin; nanocrystals; oral bioavailability
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MDPI and ACS Style

Wang, Z.; Dai, B.; Tang, X.; Che, Z.; Hu, F.; Shen, C.; Wu, W.; Shen, B.; Yuan, H. Fabrication and In Vitro/Vivo Evaluation of Drug Nanocrystals Self-Stabilized Pickering Emulsion for Oral Delivery of Quercetin. Pharmaceutics 2022, 14, 897. https://doi.org/10.3390/pharmaceutics14050897

AMA Style

Wang Z, Dai B, Tang X, Che Z, Hu F, Shen C, Wu W, Shen B, Yuan H. Fabrication and In Vitro/Vivo Evaluation of Drug Nanocrystals Self-Stabilized Pickering Emulsion for Oral Delivery of Quercetin. Pharmaceutics. 2022; 14(5):897. https://doi.org/10.3390/pharmaceutics14050897

Chicago/Turabian Style

Wang, Zhe, Bo Dai, Xiaohan Tang, Zhihui Che, Fei Hu, Chengying Shen, Wei Wu, Baode Shen, and Hailong Yuan. 2022. "Fabrication and In Vitro/Vivo Evaluation of Drug Nanocrystals Self-Stabilized Pickering Emulsion for Oral Delivery of Quercetin" Pharmaceutics 14, no. 5: 897. https://doi.org/10.3390/pharmaceutics14050897

APA Style

Wang, Z., Dai, B., Tang, X., Che, Z., Hu, F., Shen, C., Wu, W., Shen, B., & Yuan, H. (2022). Fabrication and In Vitro/Vivo Evaluation of Drug Nanocrystals Self-Stabilized Pickering Emulsion for Oral Delivery of Quercetin. Pharmaceutics, 14(5), 897. https://doi.org/10.3390/pharmaceutics14050897

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