Preparation and 68 Ga-radiolabeling of porous zirconia nanoparticle platform for PET/CT-imaging guided drug delivery

• Published in: Journal of pharmaceutical and biomedical analysis Vol. 137; p. 146
• Main Authors: Polyak, Andras, Naszalyi Nagy, Lívia, Mihaly, Judith, Görres, Sebastian, Wittneben, Alexander, Leiter, Ina, Bankstahl, Jens P, Sajti, Laszlo, Kellermayer, Miklós, Zrínyi, Miklós, Ross, Tobias L
• Format: Journal Article
• Language: English
• Published: England 15.04.2017
• Subjects: Chelating Agents - chemistry; Chelating Agents - metabolism; Drug Delivery Systems - methods; Gallium Radioisotopes - chemistry; Gallium Radioisotopes - metabolism; Nanoparticles - chemistry; Nanoparticles - metabolism; Positron Emission Tomography Computed Tomography - methods; Positron-Emission Tomography - methods; Radiopharmaceuticals - chemistry; Radiopharmaceuticals - metabolism; Tissue Distribution - drug effects; Zirconium - chemistry; Zirconium - metabolism; Nanoparticles; Imaging guided therapy; 68Ga; DOTA; Theranostics; PET
• ISSN: 1873-264X

This paper describes the preparation of gallium-68 ( Ga) isotope labeled porous zirconia (ZrO ) nanoparticle (NP) platform of nearly 100nm diameter and its first pharmacokinetic and biodistribution evaluation accomplished with a microPET/CT (μPet/CT) imaging system. Objectives of the investigations were to provide a nanoparticle platform which can be suitable for specific delivery of various therapeutic drugs using surface attached specific molecules as triggering agents, and at the same time, suitable for positron emission tomography (PET) tracing of the prospective drug delivery process. Radiolabeling was accomplished using DOTA bifunctional chelator. DOTA was successfully adsorbed onto the surface of nanoparticles, while the Ga-radiolabeling method proved to be simple and effective. In the course of biodistribution studies, the Ga-labeled DOTA-ZrNPs showed proper radiolabeling stability in their original suspension and in blood serum. μPet/CT imaging studies confirmed a RES-biodistribution profile indicating stable nano-sized labeled particles in vivo. Results proved that the new method offers the opportunity to examine further specifically targeted and drug payload carrier variants of zirconia NP systems using PET/CT imaging.