Long-circulating liposomes radiolabeled with [18F]fluorodipalmitin ([18F]FDP)

Jan Marik, Michaelann S. Tartis, Hua Zhang, Jennifer Y. Fung, Azadeh Kheirolomoom, Julie Sutcliffe, Katherine W. Ferrara

Research output: Contribution to journalArticle

83 Scopus citations

Abstract

Synthesis of a radiolabeled diglyceride, 3-[18F]fluoro-1,2-dipalmitoylglycerol [[18F]fluorodipalmitin ([18F]FDP)], and its potential as a reagent for radiolabeling long-circulating liposomes were investigated. The incorporation of 18F into the lipid molecule was accomplished by nucleophilic substitution of the p-toluenesulfonyl moiety with a decay-corrected yield of 43±10% (n=12). Radiolabeled, long-circulating polyethylene-glycol-coated liposomes were prepared using a mixture of 1,2-dipalmitoyl-sn-glycero-3-phosphocholine, cholesterol, 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethyleneglycol)-2000] ammonium salt (61:30:9) and [18F]FDP with a decay-corrected yield of 70±8% (n=4). PET imaging and biodistribution studies were performed with free [18F]FDP and liposome-incorporated [18F]FDP. Freely injected [18F]FDP had the highest uptake in the liver, spleen and lungs. Liposomal [18F]FDP remained in blood circulation at near-constant levels for at least 90 min, with a peak concentration near 2.5%ID/cc. Since [18F]FDP was incorporated into the phospholipid bilayer, it could potentially be used for radiolabeling a variety of lipid-based drug carriers.

Original languageEnglish (US)
Pages (from-to)165-171
Number of pages7
JournalNuclear Medicine and Biology
Volume34
Issue number2
DOIs
StatePublished - Feb 2007

Keywords

  • [F]FDP
  • [F]fluorodipalmitin
  • Fluorine-18
  • Liposome
  • Positron emission tomography

ASJC Scopus subject areas

  • Cancer Research
  • Molecular Medicine
  • Radiology Nuclear Medicine and imaging

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    Marik, J., Tartis, M. S., Zhang, H., Fung, J. Y., Kheirolomoom, A., Sutcliffe, J., & Ferrara, K. W. (2007). Long-circulating liposomes radiolabeled with [18F]fluorodipalmitin ([18F]FDP). Nuclear Medicine and Biology, 34(2), 165-171. https://doi.org/10.1016/j.nucmedbio.2006.12.004