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Erbium-169 [ 1/2 = 9.4 d, (max) = 342 keV (45%) and 351 keV (55%), = 110.5 KeV (0.0014%)] is the most preferred radionuclide for radiation synovectomy (RSV) of digital joints. Radiolabeled particulates of appropriate size, wherein the radionuclide is irreversibly attached to the preformed particles, offer distinct advantages as the radiopharmaceuticals for use in RSV over other radiotherapeutic agents in terms of minimal leakage of radioactivity from the joint cavity. Hyroxyapatite (HA) particles, regarded as one of the most suitable carrier moiety for radiosynoviortheses applications, have been envisaged for labeling with 169 Er with an aim to developing an agent for RSV of digital joints. Erbium-169 was produced with a specific activity of 415 ± 23 MBq/mg and radionuclidic purity of 99.22 ± 0.17% (both at the end of bombardment) by thermal neutron irradiation of enriched (98.2% in 168 Er) erbium target at a flux of ∼ 8 × 10 13 n/cm 2 s for 21 d. HA particles (1-10 m size), synthesized in-house, were labeled with 169 Er in high yield and radiochemical purity (> 99%) using 5 mg of HA particulates at pH 7.5. The radiolabeled particulates showed excellent in vitro stability in normal saline and human serum. Biodistribution and imaging studies (using 171 Er-HA) carried out in normal Wistar rats following intra-articular injection of 169 Er-HA particulates in the knee joint showed near-complete retention of injected radioactivity within the synovial cavity with almost no activity leaching out to the other organs/tissue.

Lutetium-177 is an assured therapeutic radionuclide with favorable half-life and suitable β(-) energy. Radiolabeled (177)Lu-EDTMP (Ethylenediamine tetramethylene phosphonic acid) is by and large used for bone pain palliation in cancer patients. In vitro cell studies are carried out in osteosarcoma cells MG-63 to evaluate the combined effect of anticancer drug camptothecin (CPT) and (177)Lu-EDTMP. Two concentrations of (177)Lu-EDTMP (3.7 and 37 MBq) were incubated with MG63 cell line for 48 hours with and without pretreatment of CPT (10 nM) for 1 hour. After completion of incubation, the cells were harvested and cellular toxicity was estimated by LDH, MTT, and trypan blue dye. Apoptotic DNA fragmentation was estimated by ELISA kit. The expression of proteins such as bcl2, PARP, and MAPK (mitogen-activated protein kinase) that were related to apoptotic signaling pathways was assessed by western blotting. The results indicated that cellular toxicity and apoptosis were relatively higher in MG63 cells that were treated with CPT prior to treating with (177)Lu-EDTMP in comparison with the corresponding individual controls.

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