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In Vitro Cytotoxicity and Bioavailability of Ginsenoside-Modified Nanostructured Lipid Carrier Containing Curcumin

  • Research Article
  • Theme: Lipid-Based Drug Delivery Strategies for Oral Drug Delivery
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Abstract

Our aim was to investigate the cellular uptake, in vitro cytotoxicity and bioavailability of ginsenoside-modified nanostructured lipid carrier loaded with curcumin (G-NLC). The formulation was prepared by melt emulsification technique, in which water was added to the melted lipids and homogenized to give a uniform suspension of NLC (without ginsenoside) and G-NLC. Cellular uptake of curcumin in two colon cancer cell lines (HCT116 and HT29) was increased when administered using both NLC and G-NLC compared to control (curcumin dissolved into DMSO) as measured by fluorescence microscopy. Ginsenoside modification resulted in 2.0-fold and 1.4-fold increases in fluorescence intensity in HCT116 and HT29 cell lines, respectively, compared to plain NLC. In vitro cytotoxicity (assessed by MTT assay) had a dose-dependent relationship with curcumin concentration for both NLC and G-NLC. Although G-NLC was taken up more readily in HCT116 cells, ginsenoside modification did not produce a significant increase in cytotoxic effect; a significant increase was observed in HT29 cells. Oral administration of G-NLC in ten colon cancer patients produced an appreciable plasma level of unbound curcumin (2.9 ng/mL). In conclusion, introduction of ginsenoside into NLC enhanced the cellular uptake and cytotoxicity of curcumin as well as its oral bioavailability, and this strategy can be used to improve clinical outcomes in the treatment of colon cancer with similar genotype to HT29.

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Acknowledgements

We thank Dr. Sung Won Park for his assistance with clinical study.

Funding

This study was supported by the Research Center Hospital Project of Gachon University Gil Medical Center (FRD2014-06-02).

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Authors and Affiliations

  1. College of Pharmacy, Gachon University, 191 Hambakmoero, Yeonsu-gu, Incheon, 21936, South Korea

    Ajay Vijayakumar, Pasupathi Sundaramoorthy & Bong Kyu Yoo

  2. Department of New Drug Development, College of Medicine, Inha University, 100 Inharo, Michuhol-gu, Incheon, 22212, South Korea

    Rengarajan Baskaran

  3. Division of Colon and Rectal Surgery, Department of Surgery, Gil Medical Center, Gachon University College of Medicine, 21 Namdong-daero, 774 Beon-gil, Namdong-gu, Incheon, 21545, South Korea

    Jeong-Heum Baek

Authors
  1. Ajay Vijayakumar
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  2. Rengarajan Baskaran
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  3. Jeong-Heum Baek
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  4. Pasupathi Sundaramoorthy
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  5. Bong Kyu Yoo
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Corresponding authors

Correspondence to Jeong-Heum Baek or Bong Kyu Yoo.

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The study protocol was approved by the Institutional Review Board of Gachon University Gil Medical Center (GAIRB2015-87), and written informed consent was obtained from patients before their entry into the study.

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The authors declare that they have no conflict of interest.

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Guest Editor: Sanyog Jain

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Vijayakumar, A., Baskaran, R., Baek, JH. et al. In Vitro Cytotoxicity and Bioavailability of Ginsenoside-Modified Nanostructured Lipid Carrier Containing Curcumin. AAPS PharmSciTech 20, 88 (2019). https://doi.org/10.1208/s12249-019-1295-1

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  • DOI: https://doi.org/10.1208/s12249-019-1295-1

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