Synthesize and characterization of a radio-MOF as a novel potential agent for pain palliationof metastatic bone

The bone seeking ligand 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraaminomethylenephosphonate (DOTMP), 159Gd and Cu are used to assemble a radio-labeled metal−organic framework (MOF) as a potential thernostic agent in treatment of metastatic bone. Gadolinium-159 [T1/2 = 18.479 h, Eβ(max) = 970.60 keV, Eγ = 363.55 (11.4%)] has radionuclidic properties suitable to be used in palliative therapy and also diagnosis of bone metastases.159Gd can be produced by a relatively easy route involving thermal neutron bombardment on natural gadolinium oxide in medium flux research reactors. The requirement for an enriched target does not arise and radionuclidic impurities are not formed by radiative capture during neutron activation. In this study 159Gd was produced using Gd2O3, prepared by one week neutron activation (3–4 × 1013) of a natural sample. It was then used in synthesize of bone seeking radio-MOF in a molecular ratio of (DOTMP/Gd/Cu: 1/2/1) that is of a great advantage over former bone seeking radiopharmaceuticals in which a higher amount of bone seeking chelating agents are normally used. The product stability was checked for one week andit was found to retain its stability at room temperature. The prepared formula is going to be fully bio-evaluated in the next studies.

Keywords:

MOF , 159Gd , DOTMP , bone-metastases , Theranostics