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• W2110672054 abstract "<b>1537</b> <h3><b>Objectives</b></h3> Several liposome formulations in the size range of 90-100 nm are clinically approved as compositions for chemotherapeutic drug delivery, while PET imaging can provide an effective method of noninvasively tracking and quantifying liposomal biodistribution. Although a number of methods for radiolabeling liposomes with various radionuclides have been developed, the most useful radionuclide for PET imaging is F-18, although it represents a radiolabeling challenge and can be inefficient. Herein, we report a new and efficient approach to F-18 radiolabeling of a preformed liposome using ‘click’ chemistry. <h3><b>Methods</b></h3> We synthesized an F-18 labeled liposome by ‘click’ chemistry using a [18F]23-azido-1-fluoro-3, 6, 9, 12, 15, 18, 21-heptaoxatricosane hapten and a dibenzyl cyclooctyne (DBCO)-appended liposome. The DBCO-liposome was first prepared within a limited size range of 80-90nm, and then coupled with the [18F]azide ligand followed by radiolabeled liposome purification using a size-exclusion PD10 column. <h3><b>Results</b></h3> The [18F]azide ligand was synthesized in a 24% (n=12) uncorrected radiochemical yield in 50 minutes. The [18F]azide ligand and the DBCO-liposome were combined at 37°C for 45 min. The uncorrected radiochemical yield was 47% (37%-63%, n=3). The overall uncorrected radiochemical yield was 11% in a 95min synthesis time starting from [18F]fluoride. <h3><b>Conclusions</b></h3> The approach represents a new method for radiolabeling a preformed liposome with F-18. <h3><b>Research Support</b></h3> This work was funded by the intramural program of the National Institutes of Health" @default.
• W2110672054 created "2016-06-24" @default.
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• W2110672054 date "2012-07-21" @default.
• W2110672054 modified "2023-10-16" @default.
• W2110672054 title "Temporal trends in the incidence and recurrence of hospitalised atherothrombotic disease in an Australian population, 2000–07: data linkage study" @default.
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• W2110672054 doi "https://doi.org/10.1136/heartjnl-2012-302181" @default.
• W2110672054 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/22821274" @default.
• W2110672054 hasPublicationYear "2012" @default.
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