Inherently fluorescent and porous zirconia colloids : preparation, characterization and drug adsorption studies

Naszályi Nagy, Lívia and Mihály, Judith and Polyák, András and Debreczeni, Balázs and Császár, Barbara and Szigyártó, Imola Csilla and Wacha, András and Czégény, Zsuzsanna and Jakab, Emma and Klébert, Szilvia and Drotár, Eszter and Dabasi, Gabriella and Bóta, Attila and Balogh, Lajos and Kiss, Éva (2015) Inherently fluorescent and porous zirconia colloids : preparation, characterization and drug adsorption studies. JOURNAL OF MATERIALS CHEMISTRY B, 3. pp. 7529-7537. ISSN 2050-750X

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Abstract

Porous, fluorescent zirconia particles of nearly 380 nm diameter were prepared without template molecules or labeling dyes. The porous structure is the result of aggregation-induced particle formation. The inherent fluorescence is assigned to coordinatively unsaturated Zr4+ ions at the sol–gel derived ZrO2 surface. After physico-chemical characterization of the native zirconia particles carboxyl and/or amine bearing drug molecules (D,L-a-difluoromethylornithine – DFMO, ursolic acid – UA and doxorubicin – DOX) were adsorbed onto their surface, and the products were analyzed with Fourier-transform infrared spectroscopy (FTIR), thermogravimetry (TG), small-angle X-ray scattering (SAXS), fluorimetry and zeta potential vs. pH measurements. We have found that DOX complexes coordinatively unsaturated Zr4+ ions without dislocating them, while carboxyl-bearing drugs interact with basic surface Zr–OH sites eliminating some of the carbonate species. The adsorption of UA at the zirconia surface shifts considerably the isoelectric point of the surface and thus provides kinetic stability to the particles at physiological pH. An in vivo biodistribution study in two healthy dogs performed by SPECT/CT detection after 99mTc labeling of the nanocarriers has shown the possibility of drug delivery application.

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