研究目的
To radioiodinate 4-IBA without destroying the molecular structure and evaluate its potential application for SPECT imaging with long blood half-life and excellent in vivo stability, aiming to develop a versatile agent for blood pool, tumor, and lymph node imaging.
研究成果
The radioiodinated IBA agent demonstrates high efficiency in synthesis, excellent stability, and strong albumin-binding affinity, enabling clear SPECT imaging of blood pool, tumors, and lymph nodes with high target-to-background ratios. It holds promise as a versatile theranostic agent for improving pharmacokinetics and diagnostic imaging, with potential for clinical translation and further development in targeted radioligands.
研究不足
The study is limited to preclinical mouse models, and further validation in larger animals or humans is needed. The stability and efficacy in clinical settings may vary, and the method's applicability to other radionuclides or conditions requires additional investigation.
1：Experimental Design and Method Selection:
The study involved synthesizing [131I]IBA using copper-mediated cross-coupling of aryl boronic acids, evaluating its albumin-binding capability through in vitro, ex vivo, and in vivo tests, and assessing its pharmacokinetic properties and imaging potential in various mouse models.
2：Sample Selection and Data Sources:
Samples included human serum albumin (HSA), bovine serum albumin (BSA), hemoglobin, immunoglobulin, and mouse models (normal, 4T1 tumor-bearing, orthotopic U87MG glioblastoma, and inflamed lymph node models). Data were acquired from laboratory experiments and imaging studies.
3：List of Experimental Equipment and Materials:
Equipment included Mini-Scan radio-TLC Scanner (BioScan, USA), Dionex Ulti-Mate 3000 HPLC (Thermo Scientific, USA), γ-counter (WIZARD 2480, Perkin-Elmer, USA), CRC-25R Dose Calibrator (CAPINTEC, USA), nanoScan SPECT/CT scanner (Mediso, HUNGARY), and others. Materials included Na131I, polyacetamide film, silica gel plates, complete Freund adjuvant, 4T1 and U87MG cells, and various chemicals.
4：Experimental Procedures and Operational Workflow:
Procedures included radioiodination of 4-IBA, dialysis and ultrafiltration experiments for protein binding, biodistribution studies in mice, SPECT/CT imaging at various time points, and MTT assays for toxicity.
5：Data Analysis Methods:
Data were analyzed using γ-counter for radioactivity measurement, HPLC and TLC for purity, GraphPad Prism for nonlinear regression, and OLINDA/EXM software for dosimetry estimation.
独家科研数据包，助您复现前沿成果，加速创新突破
获取完整内容
