Silica@zirconia@poly(malic acid) nanoparticles: Promising nanocarriers for theranostic applications

TitleSilica@zirconia@poly(malic acid) nanoparticles: Promising nanocarriers for theranostic applications
Publication TypeJournal Article
Year of Publication2016
AuthorsNagy, LNaszályi, Polyak, A, Mihály, J, Szécsényi, Á, Szigyártó, ICs., Czégény, Z, Jakab, E, Németh, P, Magda, B, Szabó, P, Veres, Z, Jemnitz, K, Bertóti, I, Jóba, RP, Trencsényi, G, Balogh, L, Bóta, A
JournalJournal of Materials Chemistry B
KeywordsBeta-cyclodextrin, Concentration-dependent, Core shell structure, Diagnosis, Lyophilized powders, Nanoparticles, Phosphate buffers, Proof of concept, Stable suspensions, Suspensions (fluids), Targeted delivery, Zirconia

Silicaatzirconiaatpoly(malic acid) nanocarriers of 110 nm mean diameter were designed, synthesized and characterized for the targeted delivery of diagnostic and therapeutic 99mTc to folate-overexpressing tumors. An important achievement was that a multifunctional l-(-)-malic-acid-based copolymer was formed in situ at the surface of the inorganic cores in a single synthetic step incorporating l-(-)-malic acid, β-cyclodextrin rings, folic acid moieties, and polyethylene glycol chains. Morphological and in-depth structural analysis of the particles proved their core@shell structure. Stability experiments in aqueous media evidenced that stable suspensions can be obtained from the lyophilized powder in 10 mM phosphate buffer at pH 7.4. During 14-day degradation experiments, the nanoparticles were found to be slowly dissolving (including inorganic core) in saline and also in total cell medium. An in vitro toxicity assay on hepatocytes showed a concentration-dependent decrease of cell viability down to 63 ± 1% at the highest applied concentration (0.5 mg ml-1). Proof of concept experiments of technetium-99m radiolabelling and in vivo labelling stability are presented. © The Royal Society of Chemistry 2016.