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Preparation, Characterization, and In Vitro/In Vivo Evaluation of 3-O-β-D-Galactosylated Resveratrol-Loaded Polydopamine Nanoparticles

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Abstract

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.

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Funding

The authors acknowledge the financial support from the National Natural Science Foundation of China (81703805, 51303006), the Provincial Natural Science Foundation of Anhui Province (1408085MH196, KJ2018ZD031), and the University excellent top-notch personnel training fund of Anhui Province (gxfx2017050).

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Authors and Affiliations

  1. School of Pharmacy, Anhui University of Traditional Chinese Medicine, Anhui Academy of Chinese Medicine, Hefei, 230012, Anhui, China

    Beilei Wang, Xiaoxiao Shan, Shujie Lv, Liqiong Zha, Caiyun Zhang, Qiannian Dong & Weidong Chen

  2. Hefei Sunrise Aluminum Pigments Co. LTD, Hefei, 231131, Anhui, China

    Qiannian Dong

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  1. Beilei Wang
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Correspondence to Caiyun Zhang, Qiannian Dong or Weidong Chen.

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Beilei Wang and Xiaoxiao Shan contributed to the work equally and should be regarded as co-first authors.

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Wang, B., Shan, X., Lv, S. et al. Preparation, Characterization, and In Vitro/In Vivo Evaluation of 3-O-β-D-Galactosylated Resveratrol-Loaded Polydopamine Nanoparticles. AAPS PharmSciTech 22, 220 (2021). https://doi.org/10.1208/s12249-021-02079-7

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