Development of a diagnostic and drug evaluation system for acute inflammation using a novel [89Zr]DTPA-sorbitol probe†

Non-invasive imaging techniques employing biomarkers with high selectivity for inflammation are essential not only for the early diagnosis and prevention of chronic inflammatory diseases but also for guiding appropriate drug therapy and enabling real-time evaluation of anti-inflammatory drug efficacy. In this study, we conjugated radioactive zirconium to sorbitol, a compound that can selectively target inflammation, and evaluated its inflammation-specific uptake and potential for assessing anti-inflammatory treatment efficacy in a mouse inflammation model. Pharmacokinetic analysis demonstrated that radiolabeled sorbitol achieved maximal uptake in inflamed tissues within 1 h. Positron emission tomography imaging further confirmed its utility in monitoring therapeutic effects during anti-inflammatory drug treatment. Our findings suggest that [⁸⁹Zr]DTPA-sorbitol is a promising radioprobe for targeting rapid systemic inflammation, particularly in tissues demonstrating minimal non-specific uptake, such as the brain, heart, and lung tissues. Additionally, it holds significant potential for the in vivo evaluation of anti-inflammatory drug efficacy.