Biochemistry Department, Faculty of Science, Ege University, Izmir, Turkey.
J Drug Target. 2012 Jul;20(6):509-14. doi: 10.3109/1061186X.2012.686038.
Despite the progress in the diagnosis and management of early stage disease, the management of advanced prostate cancer remains an important problem. Prostate tissue expresses folate receptor (FR) which binds both folic acid and folate-linked drugs or imaging agents. Doxorubicin is the best known and most widely used member of the anthracycline antibiotic group of anticancer agents. The aim of this work is to develop a multifunctional nanoconjugate, (99m)Tc-folate-PEG-doxorubicin, in order to investigate its radiopharmaceutical potential as a prostate cancer imaging and real-time drug location imaging agent. Through this aim, biodistribution studies of (99m)Tc-folate-PEG-doxorubicin and control groups ((99m)Tc-doxorubicin and (99m)Tc-PEG-doxorubicin) in male rats were carried out. Obtained data showed that uptake of (99m)Tc-folate-PEG-doxorubicin in prostate was significantly higher than that of the control groups due to the affinity of folate ligand to folate receptor. As a consequence, it was indicated that (99m)Tc-FOL-PEG-DOX radiolabeled conjugate which has a great target/non-target organ ratio, is specific for target organ and has a high radiopharmaceutical potential as a prostate cancer and real-time drug location imaging agent.
尽管在早期疾病的诊断和治疗方面取得了进展,但晚期前列腺癌的治疗仍然是一个重要问题。前列腺组织表达叶酸受体(FR),它可以结合叶酸和叶酸连接的药物或成像剂。多柔比星是最著名和最广泛使用的蒽环类抗生素抗癌药物之一。本工作的目的是开发一种多功能纳米缀合物,即(99m)Tc-叶酸-PEG-多柔比星,以研究其作为前列腺癌成像和实时药物定位成像剂的放射药物潜力。通过这一目标,对(99m)Tc-叶酸-PEG-多柔比星和对照组((99m)Tc-多柔比星和(99m)Tc-PEG-多柔比星)在雄性大鼠中的生物分布进行了研究。获得的数据表明,由于叶酸配体对叶酸受体的亲和力,(99m)Tc-叶酸-PEG-多柔比星在前列腺中的摄取明显高于对照组。因此,表明(99m)Tc-FOL-PEG-DOX 标记的缀合物具有很大的靶/非靶器官比,对靶器官具有特异性,并且具有作为前列腺癌和实时药物定位成像剂的高放射药物潜力。