Preparation and preliminary biological evaluation of 177Lu-labelled hydroxyapatite as a promising agent for radiation synovectomy of small joints

Abstract

Studies with (177)Lu-hydroxyapatite indicate its potential for use as an agent for radiation synovectomy of digital joints, as a viable alternative to (169)Er-based agents. The results also demonstrate the possibility of preparing a large number of patient doses of (177)Lu-hydroxyapatite from indigenously produced (177)Lu using a natural target.

Radiosynovectomy using yttrium-90, phosphorus-32 or rhenium-188 radiocolloids versus corticoid instillation for rheumatoid arthritis of the knee

“…Several candidates have been proposed to replace commercially available radiocolloid formulations of yttrium-90, rhenium-186 and erbium-169. These formulations include phosphorus-32 colloid [9,10], rhenium-186 sulphide [11], samarium-153 conjugated to particulate hydroxyapatite [12,13], dysprosium-165 ferric hydroxide [14,15], holmium-166 boromacroaggregates [16,17], ytterbium-175 and lutetium-177 hydroxyapatite [18,19]. In this study, the therapeutic efficacy of yttrium-90 citrate was compared to that of phosphorus-32 and rhenium-188 colloids.…”

Production of 177Lu for Targeted Radionuclide Therapy: Available Options

“…The in vivo applications of key 177 Lu radiopharmaceuticals for a variety of therapeutic procedures include peptide receptor radionuclide therapy [11][12][13][14][15][16][17][18][19][20][21][22][23][24][25][26], bone pain palliation [27][28][29][30][31][32][33], radiation synovectomy [34][35][36][37][38][39] and radioimmonutherapy [40][41][42][43][44][45][46]. There is a steadily expanding list of 177 Lu-labeled radiopharmaceuticals that is currently being evaluated at the preclinical research or at product development stages; these may potentially be used in vivo in humans for evaluation for radionuclide therapy [1][2][3].…”

Hydroxyapatite labelled with yttrium-90 or lutetium 177 for radiation synovectomy

“…Therefore, an ideal agent for RSV would be one in which the radionuclide is irreversibly attached to preformed particles of appropriate size. The size of such particles is reported to be 2-10 µm, the ideal size to be phagocytosed and not be leaked out of the cavity (Chakraborty et al, 2006), which can result in a high-dose delivery to nontarget organs. In addition, the particles should be biodegradable and the biological half-life of such particles should be longer than the physical half-life of the radionuclide tagged with them (Chakraborty et al, 2006).…”

“…The size of such particles is reported to be 2-10 µm, the ideal size to be phagocytosed and not be leaked out of the cavity (Chakraborty et al, 2006), which can result in a high-dose delivery to nontarget organs. In addition, the particles should be biodegradable and the biological half-life of such particles should be longer than the physical half-life of the radionuclide tagged with them (Chakraborty et al, 2006). After an injection of a beta-emitting radiopharmaceutical into the joint space, some of the injected radioactivity is absorbed by phagocytic lining cells along the synovial surface.…”

“…It decays to a stable daughter, 90 Zr (Heuf-Dorenbosch, 2000). Lutetium-177 is considered to be a promising radionuclide for use in RSV of small-sized joints owing to its favourable decay characteristics (t ½ = 6.73 days, E βmáx = 0.49 MeV, E β = 113 keV (6,4%), 208 keV (11%)) (Chakraborty et al, 2006).…”