Novel injectable fluorinated contrast agents with enhanced radiopacity

Area of Science:

• Radiology and Medical Imaging
• Materials Science
• Biomedical Engineering

Background:

• Development of advanced contrast agents is crucial for improved diagnostic imaging.
• Existing contrast agents may have limitations in terms of persistence and efficacy.
• Novel iodinated fluorinated radiopaque (IFR) molecules offer potential for enhanced properties.

Purpose of the Study:

• To prepare and evaluate novel emulsions of IFR molecules as injectable contrast agents.
• To assess the radiopacity, stability, and in vivo tolerance of these new emulsions.
• To compare the efficacy of IFR-based agents with existing contrast agents.

Main Methods:

• Preparation of stable IFR/egg yolk phospholipid emulsions.
• Heat sterilization and evaluation of shelf-stability over 3 months at 40°C.
• In vivo studies in rabbits, rats, and mice to assess radiopacity, pharmacokinetics, and tolerance.

Main Results:

• Stable emulsions with no significant particle size change over 3 months.
• High contrast in liver and spleen observed after intravenous injection in rabbits.
• Achieved equivalent liver radiopacity with 7x less IFR compared to perfluorooctyl bromide.
• Demonstrated normal liver function and blood parameters post-injection.
• High doses of IFR (neat and emulsified) showed good in vivo tolerance.

Conclusions:

• IFR emulsions are stable and exhibit excellent radiopacity.
• These novel agents demonstrate prolonged intravascular persistence and good in vivo tolerance.
• IFR molecules show promise for developing new, effective diagnostic contrast agents.