Decoration of squalenoyl-gemcitabine nanoparticles with squalenyl-hydroxybisphosphonate for the treatment of bone tumors
Keywords: 
Osteosarcome
Antitumor agents
Nanoparticles
Hydroxyapatite
Issue Date: 
14-Dec-2021
Publisher: 
Wiley
ISSN: 
1860-7179
Note: 
This is an open access article under the terms of the Creative Commons Attribution Non-Commercial No Derivs License
Citation: 
Rodriguez-Nogales, C. (Carlos); Sebastian, V. (Víctor); Blanco-Prieto, M.J. (María José); et al. "Decoration of squalenoyl-gemcitabine nanoparticles with squalenyl-hydroxybisphosphonate for the treatment of bone tumors". ChemMedChem. 16 (24), 2021-12-14, 3730 - 3738
Abstract
Therapeutic perspectives of bone tumors such as osteosarcom are main restricted due to the inefficacy of current treatments. We propose here the construction of a novel anticancers qualene-based nanomedicine with bone affinity and retention capacity. A squalenyl-hydroxybisphosphonate molecule was synthetized by chemical conjugation of a 1-hydroxyl-1,1-bi-sphosphonatemoiety to the squalenechain. This amphiphilic compound was inserted onto squalenoyl-gemcitabinenano-particles using the nanoprecipitation method. The co-assemblyled to nanoconstructsof 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 pedia tricoste osarcomacells. Furtherin vivo studies will shed lighton the potential of these nano medicines for the treatment of bones arcomas.

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