A preclinical and first-in-human study of superstable homogeneous radiolipiodol for revolutionizing interventional diagnosis and treatment of hepatocellular carcinoma.
10.1016/j.apsb.2025.02.021
- Author:
Hu CHEN
1
;
Yongfu XIONG
2
;
Minglei TENG
1
;
Yesen LI
3
;
Deliang ZHANG
4
;
Yongjun REN
2
;
Zheng LI
2
;
Hui LIU
1
;
Xiaofei WEN
3
;
Zhenjie LI
1
;
Yang ZHANG
1
;
Syed Faheem ASKARI RIZVI
1
;
Rongqiang ZHUANG
1
;
Jinxiong HUANG
3
;
Suping LI
2
;
Jingsong MAO
5
;
Hongwei CHENG
1
;
Gang LIU
1
Author Information
1. State Key Laboratory of Infectious Disease Vaccine Development, Xiang An Biomedicine Laboratory, National Innovation Platform for Industry-Education Integration in Vaccine Research, Fujian Engineering Research Center of Molecular Theranostic Technology, Center for Molecular Imaging and Translational Medicine, School of Public Health, Xiamen University, Xiamen 361102, China.
2. Department of Hepatobiliary Surgery, Department of Nuclear Medicine, Academician (Expert) Workstation, Sichuan Digestive System Disease Clinical Medical Research Center, Affiliated Hospital of North Sichuan Medical College, Nanchong 637000, China.
3. Department of Nuclear Medicine, Department of Vascular & Tumor Interventional Radiology, the First Affiliated Hospital of Xiamen University, School of Medicine, Xiamen University, Xiamen 361003, China.
4. Department of Nuclear Medicine, the Xiang'an Affiliated Hospital of Xiamen University, Xiamen 361102, China.
5. Department of Interventional Vascular Surgery, the Sixth School of Clinical Medicine, the Affiliated Qingyuan Hospital (Qingyuan People's Hospital), Guangzhou Medical University, Qingyuan 511518, China.
- Publication Type:Journal Article
- Keywords:
Hepatocellular carcinoma;
Intravascular intervention;
Lipiodol;
Nuclear medicine imaging;
Radionuclide;
Superstable homogeneous iodinated formulation technology;
Theranostics;
Transarterial radioembolization
- From:
Acta Pharmaceutica Sinica B
2025;15(10):5022-5035
- CountryChina
- Language:English
-
Abstract:
Transarterial radioembolization (TARE) is a widely utilized therapeutic approach for hepatocellular carcinoma (HCC), however, the clinical implementation is constrained by the stringent preparation conditions of radioembolization agents. Herein, we incorporated the superstable homogeneous iodinated formulation technology (SHIFT), simultaneously utilizing an enhanced solvent form in a carbon dioxide supercritical fluid environment, to encapsulate radionuclides (such as 131I,177Lu, or 18F) with lipiodol for the preparation of radiolipiodol. The resulting radiolipiodol exhibited exceptional stability and ultra-high labeling efficiency (≥99%) and displayed notable intratumoral radionuclide retention and in vivo stability more than 2 weeks following locoregional injection in subcutaneous tumors in mice and orthotopic liver tumors in rats and rabbits. Given these encouraging findings, 18F was authorized as a radiotracer in radiolipiodol for clinical trials in HCC patients, and showed a favorable tumor accumulation, with a tumor-to-liver uptake ratio of ≥50 and minimal radionuclide leakage, confirming the feasibility of SHIFT for TARE applications. In the context of transforming from preclinical to clinical screening, the preparation of radiolipiodol by SHIFT represents an innovative physical strategy for radionuclide encapsulation. Hence, this work offers a reliable and efficient approach for TARE in HCC, showing considerable promise for clinical application (ChiCTR2400087731).
