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593
Radiometal-Labeled Chitosan Microspheres as Transarterial Radioembolization Agents against Hepatocellular Carcinoma
Hui-Wen Chan1, Yi-Hsuan Lo1, Deng-Yuan Chang1
1Department of Biomedical Imaging and Radiological Sciences, National Yang Ming Chiao Tung University, Taipei Branch, Taipei 112, Taiwan.
Gels (Basel, Switzerland)
|March 24, 2022
Summary
New radiometal-labeled chitosan microspheres show promise for treating liver cancer. This targeted therapy effectively reduced tumor size in preclinical models, offering a potential new option for hepatocellular carcinoma (HCC) patients.
Area of Science:
- Nuclear medicine
- Radiopharmaceutical chemistry
- Oncology
Background:
- Transarterial radioembolization (TARE) is an emerging treatment for unresectable hepatocellular carcinoma (HCC).
- Development of effective targeted radiotherapeutics is crucial for improving HCC patient outcomes.
Purpose of the Study:
- To develop and evaluate novel radiometal-labeled chitosan microspheres (111In/177Lu-DTPA-CMS) for TARE in treating hepatocellular carcinoma.
- To assess the efficacy and biodistribution of these microspheres in a preclinical HCC model.
Main Methods:
- Synthesis of 111In/177Lu-DTPA-CMS with controlled particle size (36.5 ± 5.3 μm).
- Evaluation of radiochemical yield and purity (>90% yield, >98% purity).
- Assessment of microsphere retention in tumor and liver post-intraarterial administration in a rat model.
- Evaluation of biodistribution and radioactivity in normal organs up to 72 hours post-injection.
- Assessment of tumor size reduction following 177Lu-DTPA-CMS treatment.
Main Results:
- High radiochemical yields (>90%) and purity (>98%) were achieved for 111In/177Lu-DTPA-CMS.
- Microspheres demonstrated good retention in the hepatoma and liver within 1 hour of administration.
- Minimal radioactivity (<1% IA) was observed in normal organs at 72 hours post-injection.
- Significant reduction in hepatoma size (approx. 81%) was observed 10 days after 177Lu-DTPA-CMS treatment.
- Control group tumors continued to grow, highlighting treatment efficacy.
Conclusions:
- 177Lu-DTPA-CMS are effective in reducing hepatoma size in a preclinical model.
- 111In/177Lu-DTPA-CMS exhibit favorable biodistribution and retention characteristics for TARE.
- These microspheres show potential as a superior theranostic agent for clinical hepatoma treatment.

