Preparation, Characterization, and In Vitro/In Vivo Evaluation of 3-O-β-D-Galactosylated Resveratrol-Loaded Polydopamine Nanoparticles
| Autor: | Beilei Wang, Xiaoxiao Shan, Liqiong Zha, Weidong Chen, Caiyun Zhang, Qiannian Dong, Shujie Lv |
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| Rok vydání: | 2021 |
| Předmět: |
Indoles
Polymers Dispersity Pharmaceutical Science Aquatic Science Resveratrol chemistry.chemical_compound Pharmacokinetics Drug Discovery Zeta potential Tissue Distribution Particle Size Ecology Evolution Behavior and Systematics Drug Carriers Ecology Chemistry technology industry and agriculture Area under the curve General Medicine Bioavailability Drug delivery Nanoparticles Drug carrier Agronomy and Crop Science Nuclear chemistry |
| Zdroj: | AAPS PharmSciTech. 22 |
| ISSN: | 1530-9932 |
| DOI: | 10.1208/s12249-021-02079-7 |
| Popis: | 3-O-β-D-galactosylated resveratrol (Gal-Res) was synthesized from resveratrol (Res) and 3-O-β-D-galactose (Gal) in our previous study. In order to improve the pH sensitivity and bioavailability of Gal-Res, Gal-Res nanoparticles (Gal-Res NPs) were prepared using polydopamine (PDA) as a drug carrier. The drug loading (DL %) and entrapment efficiency (EE %) of Gal-Res NPs were 46.80% and 88.06%. The average particle size, polydispersity index (PDI), and Zeta potential of Gal-Res NPs were 179.38 ± 2.83 nm, 0.129 ± 0.013, and - 28.05 ± 0.36 mV, respectively. The transmission electron microscope (TEM) showed that Gal-Res NPs had uniform spherical morphology. Compared with the fast release of raw Gal-Res, the in vitro release of Gal-Res NPs was slow and pH-sensitive. The results of the blood vessel irritation and hemolysis test demonstrated that Gal-Res NPs had good hemocompatibility. The pharmacokinetics study in rats showed that area under the curve of plasma drug concentration time (AUC0→600) and half-life (t1/2) of Gal-Res NPs were enhanced 1.82-fold and 2.19-fold higher than those of raw Gal-Res. The in vivo biodistribution results showed that Gal-Res NPs were more distributed in liver tissue than Gal-Res. Gal-Res NPs with high bioavailability and liver accumulation were hopeful drug delivery systems (DDS) to treat liver diseases. |
| Databáze: | OpenAIRE |
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