ISSN: 2161-0495
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Inserm U 1195 Diseases and Hormones of the Nervous System, Inserm and University Paris-Saclay, 94276 Le Kremlin-Bicêtre, France
Research Article
Optimizing Structure and Activity of the Squalenoyl-siRNA Nanoparticles
Author(s): Suzan Boutary*, Guy Khalaf, Marie Caillaud, Didier Desmaële, Semen Yesylevskyy, Christophe Ramseyer and Liliane Massaad-Massade
siRNA is a promising tool for targeted therapy. Previously we conjugated the siRNA to Squalene (SQ) by copper-
free click chemistry, which has been proven to successfully deliver siRNA to tumors with fusion oncogenes and Schwann cells. To go further for future human application, this study aims to optimize the synthesis and the nanoprecipitation of siRNA-SQ conjugates while conserving their physicochemical characteristics and efficiency. We succeeded in increasing the yield of the siRNA-SQ conjugation reaction making it scalable up to 50-times. The size, the polydispersity index and the ζ-potential of the nanoparticles obtained are strongly dependent on the solvent used. Moreover, the molecular dynamics simulations reveal the physical mechanisms of nanoparticle formation at the early stage of their growth. However, these parameters do not influence the activity of the nanopart.. View More»
DOI:
10.35248/2161-0495.23.13.530