Facile preparation of 177Lu-microspheres for hepatocellular carcinoma radioisotope therapy

• Published in: Chinese chemical letters 2022-07, Vol.33 (7), p.3492-3496
• Main Authors: Wu, Manran, Shi, Kexin, Huang, Ruizhe, Liu, Chunyi, Yin, Lingling, Yong, Weipeng, Sun, Jing, Wang, Guanglin, Zhong, Zhiyuan, Gao, Mingyuan
• Format: Article
• Language: English
• Subjects: Hepatocellular carcinoma; Radioactive microspheres; Radioembolization therapy; Radioisotope; SPECT/CT
• ISSN: 1001-8417; 1878-5964
• DOI: 10.1016/j.cclet.2022.01.007

As one of the most common cancers in the world, hepatocellular carcinoma (HCC) has become a major threat to human health. Radioembolization is a first-line option for the treatment of HCC, especially when other conventional treatments fail or there exist some relative contraindications. Herein, we developed a facile and efficient method for preparing 177Lu-microspheres potentially useful for precise radioembolization therapy of HCC. The radiolabeling efficiency of 177Lu-microspheres was as high as 96.8% ± 0.5%, and the radiolabeling process did not alter the morphology of the mother microspheres. The SPECT/CT studies enabled by the unique emissions of 177Lu suggested that almost no 177Lu ion loaded by the microspheres was released over more than 32 d in vivo, which led to remarkable inhibition effect on the growth of HepG2 tumors subcutaneously transplanted in mice. The current approach may thus offer promising 177Lu-microspheres for clinical radioembolization of HCC. [Display omitted] A facile and efficient method was developed for preparing 177Lu-microspheres, which may be useful for precise radioembolization therapy of hepatocellular carcinoma.