99mTc-D-penicillamine-glucuronide: Synthesis, radiolabeling, in vitro and in vivo evaluation

PubMed ID: 21950558The current study was aimed at synthesizing a glucuronide derivative of D-penicillamine (D-PA) to be used for imaging purposes. First of all, D-PA-glucuronide (D-PA-Glu) was synthesized by experimental treatments starting with uridine 5'-diphospho-glucuronosyltransferase enzyme rich microsome preparate. Then, the synthesized compound was labeled with technetium ( 99mTc) by using a reduction method with stannous chloride. Quality controls were performed by using high-performance liquid chromatography and thin-layer radio chromatography (TLRC). Radiolabeling yield of 99mTc-D-PA-Glu was more than 98% according to TLRC results. In vitro evaluations of radiolabeled complexes were investigated on PC-3 human prostate cancer cells. 99mTc-D-PA-Glu exhibited more accumulation on PC-3 cells versus 99mTc-D-PA at 240 minutes. In order to determine its radiopharmaceutical potential, biodistribution studies were carried out in male Albino Wistar rats. The biodistribution results of 99mTc-D-PA-Glu, showed the highest uptake in prostate at 120 minutes postinjection with the main excretion route being through kidneys and bladder. 99mTc-D-PA-Glu and 99mTc-D-PA have exhibited different biodistribution results. © 2011, Mary Ann Liebert, Inc