Background: Plumbagin, a naphthoquinone extracted from the officinal leadwort presenting promising anti-cancer properties, has its therapeutic potential limited by its inability to reach tumors in a specific way at a therapeutic concentration following systemic injection. The purpose of this study is to assess whether a novel tumor-targeted, lipid–polymer hybrid nanoparticle formulation of plumbagin would suppress the growth of B16-F10 melanoma in vitro and in vivo.
Methods: Novel lipid–polymer hybrid nanoparticles entrapping plumbagin and conjugated with transferrin, whose receptors are present in abundance on many cancer cells, have been developed. Their cellular uptake, anti-proliferative and apoptosis efficacy were assessed on various cancer cell lines in vitro. Their therapeutic efficacy was evaluated in vivo after tail vein injection to mice bearing B16-F10 melanoma tumors.
Results: The transferrin-bearing lipid–polymer hybrid nanoparticles loaded with plumbagin resulted in the disappearance of 40% of B16-F10 tumors and regression of 10% of the tumors following intravenous administration. They were well tolerated by the mice.
Conclusion: These therapeutic effects, therefore, make transferrin-bearing lipid–polymer hybrid nanoparticles entrapping plumbagin a highly promising anti-cancer nanomedicine.
Sakpakdeejaroen I, Somani S, Laskar P, Mullin M, Dufès C. Regression of Melanoma Following Intravenous Injection of Plumbagin Entrapped in Transferrin-Conjugated, Lipid–Polymer Hybrid Nanoparticles. Int J Nanomedicine. 2021;16:2615-2631 https://doi.org/10.2147/IJN.S293480
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International Journal of Nanomedicine
Immunology and Microbiology