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Piperine-Loaded Glycyrrhizic Acid- and PLGA-Based Nanoparticles Modified with Transferrin for Antitumor

Piperine-Loaded Glycyrrhizic Acid- and PLGA-Based Nanoparticles

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A Correction to this article was published on 15 November 2021

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Abstract

The purpose of this study was to enhance the antitumor effect of piperine by constructing the nanoparticles modified with transferrin (Tf-PIP-NPs) and evaluating their efficacy in vitro and in vivo. The Tf-PIP-NPs were prepared by the solvent evaporation method, and their properties were characterized. The effects of Tf-PIP-NPs on cytotoxicity, cell uptake, apoptosis, and mitochondrial membrane potential were evaluated in HepG2 cells, MDA-MB-231 cells, and 4T1 cells. In a 4T1 tumor-bearing mouse model, the antitumor efficacy of Tf-PIP-NPs was assessed in terms of tumor volumes, changes in body weight, HE staining, and immunohistochemical analysis. With a mean particle size of 112.2 ± 1.27 nm, the zeta potential of (− 28.0 ± 1.6 mV) Tf-PIP-NPs were rapidly internalized by tumor cells after 1 h through the transferrin receptor (TfR)-mediated endocytosis pathway, significantly inducing cellular apoptosis and mitochondrial membrane potential loss. Although Tf-PIP-NPs had no significant difference with PIP-NPs in tumor volume inhibition due to the presence of tumor microenvironment, it could significantly upregulate the expression of related pro-apoptotic proteins and induce tumor necrosis. We used the self-assembly properties of glycyrrhizic acid (GL) and polymer-PLGA to encapsulate piperine and modified with the transferrin, which provided a promising approach to improve the antitumor efficacy for anticarcinogen.

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Funding

The work was supported by the Natural Science Foundation of Ningxia Province (no. 2020AAC03140), the Key Research and Development Program of Ningxia Province (no. 2017BY084), and the Key Research Funding of Ningxia Province (2018BFH02001).

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Authors and Affiliations

  1. Department of Pharmaceutics, School of Pharmacy, Ningxia Medical University, No. 1160 Shengli South Street, Yinchuan, 750004, China

    Shuang Li, Jueshuo Guo, Zonghua Tian, Li Li & Jianhong Yang

  2. Department of Preparation Center, General Hospital of Ningxia Medical University, Yinchuan, China

    Jing Chen

  3. Department of Medical Chemistry, School of Basic Medicine, Ningxia Medical University, Yinchuan, China

    Guojing Gou

  4. Key Laboratoryratory of NingXia Ethnomedicine Modernization, Ministry of Education, Ningxia Medical University, Yinchuan, China

    Yang Niu

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  1. Shuang Li
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  2. Jueshuo Guo
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  3. Zonghua Tian
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  4. Jing Chen
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  5. Guojing Gou
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  7. Li Li
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Contributions

Conceptualization, Jianhong Yang; investigation, Shuang Li; methodology, Shuang Li, Jueshuo Guo, and Zonghua Tian; project administration, Jianhong Yang, Li Li, and Yang Niu; data curation, Shuang Li, Li Li, and Yang Niu; writing—original draft, Shuang Li, Jueshuo Guo, and Zonghua Tian; writing—review and editing, Shuang Li and Jueshuo Guo. All authors have read and agreed to the published version of the manuscript.

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Correspondence to Li Li or Jianhong Yang.

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Shuang Li and Jueshuo Guo contributed equally to this work

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Li, S., Guo, J., Tian, Z. et al. Piperine-Loaded Glycyrrhizic Acid- and PLGA-Based Nanoparticles Modified with Transferrin for Antitumor. AAPS PharmSciTech 22, 239 (2021). https://doi.org/10.1208/s12249-021-02123-6

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