¹⁸F-Labeled perfluorocarbon droplets for positron emission tomography imaging

Area of Science:

• Radiochemistry
• Nanotechnology
• Biomedical Imaging

Background:

• Perfluorocarbon (PFC) nanodroplets are used for imaging and drug delivery.
• Characterizing PFC droplet formulations in vivo is challenging due to limited quantitative assessment methods.

Purpose of the Study:

• Develop a general method for radiolabeling the core of nanoscale PFC droplets with fluorine-18.
• Enable quantitative biodistribution and pharmacokinetic studies of PFC nanodroplets using PET imaging.

Main Methods:

• Synthesized a novel fluorine-18 labeled compound, [18F]CF3(CF2)7(CH2)3F.
• Integrated the radiolabel into perfluorohexane (PFH) and perfluorooctylbromide (PFOB) nanodroplets.
• Evaluated in vivo distribution and pharmacokinetics in mice using PET imaging and tissue biodistribution assays.

Main Results:

• The [18F]radiolabel was successfully incorporated into PFH and PFOB nanodroplets without altering their physical properties.
• No radiolabel leakage was observed in vitro.
• PET imaging and biodistribution data revealed distinct in vivo behaviors for the PFH and PFOB nanodroplets.

Conclusions:

• A convenient method for producing 18F-labeled PFC droplets was established.
• This radiolabeling strategy facilitates pre-clinical evaluation of diverse PFC droplet formulations.
• The technique allows for direct core labeling and assessment of PFC nanodroplets in vivo.