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Enhancing the Antitumor Activity of Berberine Hydrochloride by Solid Lipid Nanoparticle Encapsulation

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An Erratum to this article was published on 29 May 2014

Abstract

Berberine hydrochloride (BH) is an isoquinolin alkaloid with promising anticancer efficacies. Nevertheless, further development and application of this compound had been hampered by its poor aqueous solubility, low gastrointestinal absorption, and rapid metabolism in the body. In this study, a solid lipid nanoparticle (SLN)-based system was developed for efficient incorporation and persistent release of BH. The drug-loading SLNs (BH-loaded SLNs) were stable, with a mean particle size of 81.42 ± 8.48 nm and zeta potential of −28.67 ± 0.71 mV. BH-loaded SLNs showed desirable drug entrapment efficiency and drug-loaded, and the release of BH from SLNs was significantly slower than free BH. Importantly, our in vitro study indicated that BH-loaded SLNs more significantly inhibited cell proliferation on MCF-7, HepG 2, and A549 cancer cells. Meanwhile, clone formation, cellular uptake, cell cycle arrest, and cell apoptosis studies also demonstrated that BH-loaded SLNs enhanced the antitumor efficacies of BH on MCF-7 cancer cells. Taken together, our results suggest that this SLN formulation may serve as a novel, simple, and efficient system for the delivery of BH.

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Acknowledgments

This study was supported by the Macao Science and Technology Development Fund (102/2012/A3) and the Research Fund of the University of Macau (SRG025-ICMS13-CMW).

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Authors and Affiliations

  1. State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Av. Padre Tomas Pereira S.J., Taipa, 999078, Macau, China

    Lu Wang, Shengpeng Wang, Chunming Wang, Yitao Wang & Meiwan Chen

  2. State Key Laboratory of Respiratory Diseases, First Affiliated Hospital of Guangzhou Medical College, 510120, Guangzhou, China

    Hongtao Li & Rong Liu

  3. Beijing University of Chinese Medicine, 100102, Beijing, China

    Zhisheng Wu

Authors
  1. Lu Wang
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  2. Hongtao Li
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  3. Shengpeng Wang
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  4. Rong Liu
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  6. Chunming Wang
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Corresponding authors

Correspondence to Chunming Wang or Meiwan Chen.

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Lu Wang and Hongtao Li contributed equally to this work.

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Wang, L., Li, H., Wang, S. et al. Enhancing the Antitumor Activity of Berberine Hydrochloride by Solid Lipid Nanoparticle Encapsulation. AAPS PharmSciTech 15, 834–844 (2014). https://doi.org/10.1208/s12249-014-0112-0

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  • DOI: https://doi.org/10.1208/s12249-014-0112-0

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