Synthesis and evaluation of 68Ga labeled palmitic acid for cardiac metabolic imaging. (October 2018)

• Record Type: Journal Article
• Authors: Jain, Akanksha; Mathur, Anupam; Pandey, Usha; Sarma, Haladhar Dev; Dash, Ashutosh
• Is Part Of: Applied radiation and isotopes. Volume 140(2018:Oct.)
• Page Start: 35
• Page End: 40
• Publication Date: 2018-10
• Subjects: 68Ga -- Cardiac metabolic imaging -- NOTA -- Palmitic acid -- 125I-IPPA -- Heart metabolite analysis; Radiology -- Periodicals; Radiation -- Industrial applications -- Periodicals; Nuclear chemistry -- Periodicals; Internet resource; Periodical; 660.298
• DOI: 10.1016/j.apradiso.2018.06.003
• Languages: English
• ISSNs: 0969-8043

Abstract

Abstract: This work evaluates the potential of a 68 Ga labeled long chain 16C fatty acid for cardiac metabolic imaging. For radiolabeling with 68 Ga, hexadecanedioic acid was coupled with the chelator p -NH2 -Bn-NOTA. Under the optimized conditions, NOTA-hexadecanoic acid could be radiolabeled with 68 Ga in ≥95% yields. In biodistribution studies carried out in Swiss mice, 68 Ga-NOTA-hexadecanoic acid showed low myocardial uptake at 2 min p.i. (3.7 ± 1.3%ID/g). While 68 Ga-NOTA-hexadecanoic acid cleared rapidly from non-target organs such as blood, lungs, intestine and kidney, wash out from liver was slow. Radio-HPLC analyses of myocardial extracts of rats injected with 68 Ga-NOTA-hexadecanoic acid confirmed its metabolic transformation in the myocardium. Highlights: NOTA-hexadecanoic acid synthesized and characterized by 1 H NMR and ESI-MS. NOTA-hexadecanoic acid radiolabeled with 68 Ga in >95% yields. Formation of 68 Ga-conjugate confirmed by characterization of its nat Ga surrogate. Myocardial uptake of 68 Ga-conjugate was 3.7 ± 1.34%ID/g at 2 min p.i. Heart metabolite analysis showed metabolic transformation of fatty acid conjugate.