Regression of melanoma following intravenous injection of plumbagin entrapped in transferrin-conjugated, lipid–polymer hybrid nanoparticles

Sakpakdeejaroen, Intouch and Somani, Sukrut and Laskar, Partha and Mullin, Margaret and Dufès, Christine (2021) Regression of melanoma following intravenous injection of plumbagin entrapped in transferrin-conjugated, lipid–polymer hybrid nanoparticles. International Journal of Nanomedicine, 16. pp. 2615-2631. ISSN 1176-9114

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    Abstract

    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.

    ORCID iDs

    Sakpakdeejaroen, Intouch ORCID logoORCID: https://orcid.org/0000-0002-5045-7581, Somani, Sukrut ORCID logoORCID: https://orcid.org/0000-0002-0697-1110, Laskar, Partha, Mullin, Margaret and Dufès, Christine ORCID logoORCID: https://orcid.org/0000-0002-7963-6364;