Ultrastable PLGA-Coated 177 Lu-Microspheres for Radioembolization Therapy of Hepatocellular Carcinoma.

Transarterial radioembolization (TARE) is a highly effective localized radionuclide therapy that has been successfully used to treat hepatocellular carcinoma (HCC). Extensive research has been conducted on the use of radioactive microspheres (MSs) in TARE, and the development of ideal radioactive MSs is crucial for clinical trials and patient treatment. This study presents the development of a radioactive MS for TARE of HCC. These MSs, referred to as 177 Lu-MS@PLGA, consist of poly(lactic- co -glycolic acid) (PLGA) copolymer and radioactive silica MSs, labeled with 177 Lu and then coated with PLGA. It has an extremely high level of radiostability. Cellular experiments have shown that it can cause DNA double-strand breaks, leading to cell death. In vivo radiostability of 177 Lu-MS@PLGA is demonstrated by microSPECT/CT imaging. In addition, the antitumor study has shown that TARE of 177 Lu-MS@PLGA can effectively restrain tumor growth without harmful side effects. Thus, 177 Lu-MS@PLGA exhibits significant potential as a radioactive MS for the treatment of HCC.