%0 Journal Article
%A Rodríguez‐Nogales, Carlos
%A Desmaële, Didier
%A Sebastián, Víctor
%A Couvreur, Patrick
%A Blanco‐Prieto, María J.
%T Decoration of Squalenoyl‐Gemcitabine Nanoparticles with Squalenyl‐Hydroxybisphosphonate for the Treatment of Bone Tumors
%D 2021
%@ 1860-7179
%@ 1860-7187
%U https://hdl.handle.net/20.500.14352/132893
%X Therapeutic perspectives of bone tumors such as osteosarcoma remain restricted due to the inefficacy of current treatments. We propose here the construction of a novel anticancer squalene-based nanomedicine with bone affinity and retention capacity. A squalenyl-hydroxybisphosphonate molecule was synthetized by chemical conjugation of a 1-hydroxyl-1,1-bisphosphonate moiety to the squalene chain. This amphiphilic compound was inserted onto squalenoyl-gemcitabine nanoparticles using the nanoprecipitation method. The co-assembly led to nanoconstructs of 75 nm, with different morphology and colloidal properties. The presence of squalenyl-hydroxybi-sphosphonate enhanced the nanoparticles binding affinity for hydroxyapatite, a mineral present in the bone. Moreover, the in vitro anticancer activity was preserved when tested in commercial and patient-treated derived pediatric osteosarcoma cells. Further in vivo studies will shed light on the potential of these nanomedicines for the treatment of bone sarcomas.
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