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Towards a clinical application of freeze-dried squalene-based nanomedicines

Marie Rouquette 1 Karine Ser-Le Roux 2 Mélanie Polrot 2 Claudie Bourgaux 1 Jean-Philippe Michel 1 Fabienne Testard 3 Frédéric Gobeaux 3 Sinda Lepetre-Mouelhi 1 
2 PFEP - Plateforme d’évaluation préclinique
AMMICa - Analyse moléculaire, modélisation et imagerie de la maladie cancéreuse
3 LIONS - Laboratoire Interdisciplinaire sur l'Organisation Nanométrique et Supramoléculaire
NIMBE UMR 3685 - Nanosciences et Innovation pour les Matériaux, la Biomédecine et l'Energie (ex SIS2M)
Abstract : Squalene-adenosine (SQAd) nanoparticles (NPs) were found to display promising pharmacological activity similar to many other nanomedicines, but their long-term stability was still limited, and their preparation required specific know-how and material. These drawbacks represented important restrictions for their potential use in the clinic. Freeze-drying nanoparticles is commonly presented as a solution to allow colloidal stability, but this process needs to be adapted to each nanoformulation. Hence, we aimed at developing a specific protocol for freeze-drying SQAd NPs while preserving their structural features. NPs were lyophilised, resuspended and analysed by dynamic light scattering, atomic force microscopy and small-angle scattering. Among four different cryoprotectants, trehalose was found to be the most efficient in preserving NPs physico-chemical characteristics. Interestingly, we identified residual ethanol in NP suspensions as a key parameter which could severely affect the freeze-drying outcome, leading to NPs aggregation. Long-term stability was also assessed. No significant change in size distribution or zeta potential could be detected after three-month storage at 4?°C. Finally, freeze-dried NPs innocuity was checked in vitro on cultured hepatocytes and in vivo on mice. In conclusion, optimisation of freeze-drying conditions resulted in safe lyophilised SQAd NPs that can be easily stored, shipped and simply reconstituted into an injectable form.
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Submitted on : Thursday, March 14, 2019 - 4:37:33 PM
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Marie Rouquette, Karine Ser-Le Roux, Mélanie Polrot, Claudie Bourgaux, Jean-Philippe Michel, et al.. Towards a clinical application of freeze-dried squalene-based nanomedicines. Journal of Drug Targeting, Informa Healthcare, 2019, 27, pp.1-10. ⟨10.1080/1061186X.2019.1566340⟩. ⟨cea-02068204⟩



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