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

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. Klymchenko, Jean-Louis Paul, Christophe Ramseyer and Patrick Couvreur ()
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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
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
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

Nature Communications, 2017, vol. 8, issue 1, 1-9

Abstract: 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.

Date: 2017
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Persistent link: https://EconPapers.repec.org/RePEc:nat:natcom:v:8:y:2017:i:1:d:10.1038_ncomms15678

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DOI: 10.1038/ncomms15678

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