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SHR Neuro Cancer Cardio Lipid Metab Microb

Helbok, A; Decristoforo, C; Dobrozemsky, G; Rangger, C; Diederen, E; Stark, B; Prassl, R; von Guggenberg, E.
Radiolabeling of lipid-based nanoparticles for diagnostics and therapeutic applications: a comparison using different radiometals
J LIPOSOME RES. 2010; 20(3): 219-227. Doi: 10.3109/08982100903311812
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Co-authors Med Uni Graz: Prassl Ruth
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Abstract:: Radiolabeling of nanoparticles (NPs) has been performed for a variety of reasons, such as for studying pharmacokinetics, for imaging, or for therapy. Here, we describe the in vitro and in vivo evaluation of DTPA-derivatized lipid-based NP (DTPA-NP) radiolabeled with different radiometals, including (111)In and (99m)Tc, for single-photon emission computed tomography (SPECT), (68)Ga for positron emission tomography (PET), and (177)Lu for therapeutic applications. PEGylated DTPA-NP with varying DTPA amounts, different composition, and size were radiolabeled with (111)In, (177)Lu, and (68)Ga, using various buffers. (99m)Tc-labeling was performed directly and by using the carbonyl aquaion, [(99m)Tc(H(2)O)(3)(CO)(3)](+). Stability was tested and biodistribution evaluated. High labeling yields (>90%) were achieved for all radionuclides and different liposomal formulations. Specific activities (SAs) were highest for (111)In (>4 MBq/mug liposome), followed by (68)Ga and (177)Lu; for (99m)Tc, high labeling yields and SA were only achieved by using [(99m)Tc(H(2)O)(3)(CO)(3)](+). Stability toward DTPA/histidine and in serum was high (>80 % RCP, 24 hours postpreparation).). Biodistribution in Lewis rats revealed no significant differences between NP in terms of DTPA loading and particle composition; however, different uptake patterns were found between the radionuclides used. We observed lower retention in blood (<3.3 %ID/g) and lower liver uptake (< 2.7 %ID/g) for (99m)Tc- and (68)Ga, compared to (111)In-NP (blood, <4 %ID/g; liver, <3.6 %ID/g). Imaging potential was shown by both PET magnetic resonance imaging fusion imaging and SPECT imaging. Overall, our study shows that PEGylated DTPA-NP are suitable for radiolabeling studies with a variety of radiometals, thereby achieving high SA suitable for targeting applications.
Find related publications in this database (using NLM MeSH Indexing): Animals -; Gallium Radioisotopes - diagnostic use; Indium Radioisotopes - diagnostic use; Isotope Labeling - methods; Liposomes - chemistry Liposomes - pharmacokinetics; Lutetium - therapeutic use; Magnetic Resonance Imaging -; Nanoparticles - chemistry; Organotechnetium Compounds - diagnostic use; Pentetic Acid - analogs and derivatives Pentetic Acid - pharmacokinetics; Positron-Emission Tomography -; Radioisotopes - therapeutic use; Radiopharmaceuticals - diagnostic use; Rats -; Rats, Inbred Lew -; Tomography, Emission-Computed, Single-Photon -
Find related publications in this database (Keywords): Nanotechnology; long circulatory; targeting