ABSTRACT
The aim of this work was to evaluate the tumoral fibrosis effect on the radiation absorbed dose of the radiopharmaceuticals (177)Lu-Tyr(3)-octreotate (monomeric) and (177)Lu-Tyr(3)-octreotate-gold nanoparticles (multimeric) using an experimental HeLa cells tumoral model and the Monte Carlo PENELOPE code. Experimental and computer micro-environment models with or without fibrosis were constructed. Results showed that fibrosis increases up to 33% the tumor radiation absorbed dose, although the major effect on the dose was produced by the type of radiopharmaceutical (112Gy-multimeric vs. 43Gy-monomeric).
Subject(s)
Lutetium/administration & dosage , Neoplasms/pathology , Neoplasms/radiotherapy , Octreotide/analogs & derivatives , Radioisotopes/administration & dosage , Radiopharmaceuticals/administration & dosage , Fibrosis , Gold , HeLa Cells , Humans , Lutetium/chemistry , Lutetium/pharmacokinetics , Metal Nanoparticles/administration & dosage , Metal Nanoparticles/chemistry , Models, Biological , Monte Carlo Method , Neoplasms/metabolism , Octreotide/administration & dosage , Octreotide/chemistry , Octreotide/pharmacokinetics , Radioisotopes/chemistry , Radioisotopes/pharmacokinetics , Radiopharmaceuticals/chemistry , Radiopharmaceuticals/pharmacokinetics , Radiotherapy Dosage , Theranostic NanomedicineABSTRACT
Nanoparticles can be near infrared (NIR)-fluorescent (e.g., gold nanoparticles, quantum dots or carbon nanotubes) or can have magnetic properties (e.g., iron oxide nanoparticles). These optical or magnetic properties can be exploited for use in thermal therapy and molecular imaging. Radiolabeled nanoparticles have proven to be promising tools in the diagnosis and therapy of malignant processes due to their multivalency and as multi-modal imaging agents. Furthermore, these radiopharmaceuticals may function simultaneously as both radiotherapy systems and thermal-ablation systems. This review examines the application of radiolabeled nanoparticles in the development of multifunctional nanosystems for targeted therapy.
Subject(s)
Molecular Targeted Therapy/methods , Nanoparticles/therapeutic use , Animals , Humans , Isotope Labeling , Nanoparticles/chemistryABSTRACT
(99m)Tc-HYNIC labeled Lys(3)-bombesin has shown specific binding to gastrin-releasing peptide receptors (GRP-r) over-expressed in cancer cells. Click chemistry offers an innovative functionalization strategy for biomolecules such as bombesin. The aim of this research was to apply a click chemistry approach for [(99m)Tc(CO)(3)] labeling of Lys(3)-bombesin and to compare the in vitro MCF7 breast cancer cell uptake and biodistribution profile in mice with that of (99m)Tc-EDDA/HYNIC-Lys(3)-bombesin. The results suggest a higher lipophilicity for (99m)Tc(CO)(3)-triazole-Lys(3)-bombesin which explains its higher in vivo hepatobiliary elimination. Pancreas-to-blood ratio for (99m)Tc(CO)(3)-triazole-Lys(3)-bombesin was 4.46 at 3 h and both bombesin radiopharmaceuticals showed specific recognition for GRP receptors in MCF7 cancer cells. Click chemistry is a reliable approach for [(99m)Tc(CO)(3)] labeling of Lys(3)-bombesin.
