{Reference Type}: Journal Article
{Title}: Preparation and Biological Study of (68)Ga-DOTA-alendronate.
{Author}: Fakhari A;Jalilian AR;Johari-Daha F;Shafiee-Ardestani M;Khalaj A;
{Journal}: Asia Ocean J Nucl Med Biol
{Volume}: 4
{Issue}: 2
{Year}: 2016
暂无{DOI}: 10.7508/aojnmb.2016.02.006
{Abstract}: <B>OBJECTIVE: </B>In line with previous research on the development of conjugated bisphosphonate ligands as new bone-avid agents, in this study, DOTA-conjugated alendronate (DOTA-ALN) was synthesized and evaluated after labeling with gallium-68 ((68)Ga).<BR><B>METHODS: </B>DOTA-ALN was synthesized and characterized, followed by (68)Ga-DOTA-ALN preparation, using DOTA-ALN and (68)GaCl3 (pH: 4-5) at 92-95° C for 10 min. Stability tests, hydroxyapatite assay, partition coefficient calculation, biodistribution studies, and imaging were performed on the developed agent in normal rats.<BR><B>RESULTS: </B>The complex was prepared with high radiochemical purity (>99% as depicted by radio thin-layer chromatography; specific activity: 310-320 GBq/mmol) after solid phase purification and was stabilized for up to 90 min with a log P value of -2.91. Maximum ligand binding (65%) was observed in the presence of 50 mg of hydroxyapatite; a major portion of the activity was excreted through the kidneys. With the exception of excretory organs, gastrointestinal tract organs, including the liver, intestine, and colon, showed significant uptake; however, the bone uptake was low (<1%) at 30 min after the injection. The data were also confirmed by sequential imaging at 30-90 min following the intravenous injection.<BR><B>CONCLUSIONS: </B>The high solubility and anionic properties of the complex led to major renal excretion and low hydroxyapatite uptake; therefore, the complex failed to demonstrate bone imaging behaviors.