Evaluation of the Theranostic Potential of Perfluorohexane-Based Acoustic Nanodroplets

Biol Pharm Bull. 2019 Dec 1;42(12):2038-2044. doi: 10.1248/bpb.b19-00525. Epub 2019 Sep 25.

Abstract

In this study, we have prepared perfluorohexane (PFH)-based acoustic nanodroplets (PFH-NDs) and evaluated their theranostic characteristics. Nile Red (NR) was incorporated into PFH-NDs as a model of hydrophobic drugs (NR-PFH-NDs). The mean particle diameters of PFH-NDs and NR-PFH-NDs were 205 ± 1.8 nm and 346.3 ± 6 nm, respectively. There was no significant PFH leakage from PFH-NDs during 90 min incubation at 37°C in the presence of 10% rat serum. The in vitro ultrasonography showed that the phase transition of PFH-NDs from liquid droplets to gassed bubbles could be induced by therapeutic low-intensity ultrasound with a frequency of 1 MHz and an intensity of 5 W/cm2. Irradiation of ultrasound in combination with NR-PFH-NDs enhanced uptake of NR in murine adenocarcinoma cells (C26). After intravenous injection of PFH-NDs to mice, PFH gradually disappeared from blood circulation with an elimination half-life of 43.3 min. Intravenous injection of PFH-NDs also resulted in significant contrast enhancement in the mouse carotid artery upon therapeutic low-intensity ultrasound irradiation. These results suggest the potential of PFH-NDs as a novel contrast agent for further theranostic applications.

Keywords: nanodroplet; perfluorohexane; phase-transition; theranostics; ultrasound.

MeSH terms

  • Adenocarcinoma
  • Animals
  • Carotid Arteries / diagnostic imaging
  • Cell Line, Tumor
  • Female
  • Fluorocarbons / blood
  • Fluorocarbons / chemistry*
  • Fluorocarbons / radiation effects*
  • Mice, Inbred ICR
  • Nanoparticles / chemistry*
  • Nanostructures
  • Rats
  • Rats, Wistar
  • Theranostic Nanomedicine
  • Ultrasonography

Substances

  • Fluorocarbons
  • perflexane