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Conjugation of squalene to gemcitabine as unique approach exploiting endogenous lipoproteins for drug delivery

Author

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  • Dunja Sobot

    (Institut Galien Paris-Sud, UMR 8612, CNRS, Univ Paris-Sud, Université Paris-Saclay, Faculté de Pharmacie)

  • Simona Mura

    (Institut Galien Paris-Sud, UMR 8612, CNRS, Univ Paris-Sud, Université Paris-Saclay, Faculté de Pharmacie)

  • Semen O. Yesylevskyy

    (Institute of Physics of the National Academy of Sciences of Ukraine)

  • Laura Dalbin

    (Institut Galien Paris-Sud, UMR 8612, CNRS, Univ Paris-Sud, Université Paris-Saclay, Faculté de Pharmacie)

  • Fanny Cayre

    (Institut Galien Paris-Sud, UMR 8612, CNRS, Univ Paris-Sud, Université Paris-Saclay, Faculté de Pharmacie)

  • Guillaume Bort

    (Institut Galien Paris-Sud, UMR 8612, CNRS, Univ Paris-Sud, Université Paris-Saclay, Faculté de Pharmacie)

  • Julie Mougin

    (Institut Galien Paris-Sud, UMR 8612, CNRS, Univ Paris-Sud, Université Paris-Saclay, Faculté de Pharmacie)

  • Didier Desmaële

    (Institut Galien Paris-Sud, UMR 8612, CNRS, Univ Paris-Sud, Université Paris-Saclay, Faculté de Pharmacie)

  • Sinda Lepetre-Mouelhi

    (Institut Galien Paris-Sud, UMR 8612, CNRS, Univ Paris-Sud, Université Paris-Saclay, Faculté de Pharmacie)

  • Grégory Pieters

    (CEA Saclay, iBiTecS-S/SCBM, Labex LERMIT)

  • Bohdan Andreiuk

    (Laboratoire de Biophotonique et Pharmacologie, UMR CNRS 7213, University of Strasbourg
    Chemistry Faculty, Taras Shevchenko National University of Kyiv)

  • Andrey S. Klymchenko

    (Laboratoire de Biophotonique et Pharmacologie, UMR CNRS 7213, University of Strasbourg)

  • Jean-Louis Paul

    (AP-HP, Hôpital Européen Georges Pompidou, Service de Biochimie
    Lip(Sys)2, Athérosclérose: homéostasie et trafic du cholestérol des macrophages, Univ Paris-Sud, Université Paris-Saclay)

  • Christophe Ramseyer

    (Laboratoire Chrono Environnement UMR CNRS 6249, Université de Bourgogne Franche-Comté)

  • Patrick Couvreur

    (Institut Galien Paris-Sud, UMR 8612, CNRS, Univ Paris-Sud, Université Paris-Saclay, Faculté de Pharmacie)

Abstract

Once introduced in the organism, the interaction of nanoparticles with various biomolecules strongly impacts their fate. Here we show that nanoparticles made of the squalene derivative of gemcitabine (SQGem) interact with lipoproteins (LPs), indirectly enabling the targeting of cancer cells with high LP receptors expression. In vitro and in vivo experiments reveal preeminent affinity of the squalene-gemcitabine bioconjugates towards LP particles with the highest cholesterol content and in silico simulations further display their incorporation into the hydrophobic core of LPs. To the best of our knowledge, the use of squalene to induce drug insertion into LPs for indirect cancer cell targeting is a novel concept in drug delivery. Interestingly, not only SQGem but also other squalene derivatives interact similarly with lipoproteins while such interaction is not observed with liposomes. The conjugation to squalene represents a versatile platform that would enable efficient drug delivery by simply exploiting endogenous lipoproteins.

Suggested Citation

  • Dunja Sobot & Simona Mura & Semen O. Yesylevskyy & Laura Dalbin & Fanny Cayre & Guillaume Bort & Julie Mougin & Didier Desmaële & Sinda Lepetre-Mouelhi & Grégory Pieters & Bohdan Andreiuk & Andrey S. , 2017. "Conjugation of squalene to gemcitabine as unique approach exploiting endogenous lipoproteins for drug delivery," Nature Communications, Nature, vol. 8(1), pages 1-9, August.
    • Handle: RePEc:nat:natcom:v:8:y:2017:i:1:d:10.1038_ncomms15678
    DOI: 10.1038/ncomms15678
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