Evaluation of Different Formulations and Routes for the Delivery of the Ionizing Radiation Mitigator GS-Nitroxide (JP4-039)

In Vivo. 2018 Sep-Oct;32(5):1009-1023. doi: 10.21873/invivo.11341.

Abstract

Background/aim: The mitochondrial targeted GS-nitroxide, JP4-039, is an effective total body irradiation (TBI) mitigator when delivered intravenously (IV) up to 72 h after exposure. Effective systemic and localized administration to oral cavity/oropharynx and esophagus has been demonstrated. The objective of the study was to establish alternatives to IV administration suitable for JP4-039 delivery to mass casualties.

Materials and methods: JP4-039 was administered to C57BL/6 mice by topically applied carboxy-methyl-cellulose microneedle arrays (MNAs) or by intramuscular (IM) injection. Three different formulations that have passed Food and Drug Administration review, namely Captisol, 2-hydroxypropyl-β-cyclodextrin (cyclodextrin), and Miglyol-812-N, were used for drug delivery. Intraoral (IO) administration with each formulation was also evaluated.

Results: All tested formulations and MNAs successfully delivered JP4-039. However, IM delivery of the Miglyol-812-N displayed very efficient and highly reproducible radiation mitigation.

Conclusion: Effective IM delivery of JP4-039 in animal models after TBI or partial-body irradiation suggested the use of the Miglyol-812-N formulation in both medical indications and radiation countermeasures.

Keywords: Ionizing irradiation; JP4-039; radiation mitigation.

MeSH terms

  • Administration, Intravenous
  • Administration, Oral
  • Animals
  • Apoptosis / drug effects
  • DNA Damage / radiation effects
  • DNA Repair / drug effects
  • Drug Administration Routes*
  • Drug Compounding*
  • Drug Stability
  • Female
  • Injections, Intramuscular
  • Mice
  • Mice, Knockout
  • Mitochondria / drug effects
  • Mitochondria / genetics
  • Mitochondria / metabolism
  • Molecular Structure
  • Nitrogen Oxides / administration & dosage*
  • Nitrogen Oxides / chemistry*
  • Nitrogen Oxides / pharmacokinetics
  • Radiation Injuries, Experimental
  • Radiation, Ionizing
  • Radiation-Protective Agents / administration & dosage*
  • Radiation-Protective Agents / chemistry*
  • Radiation-Protective Agents / pharmacokinetics
  • Reproducibility of Results
  • Survival Rate
  • Whole-Body Irradiation

Substances

  • JP4-039
  • Nitrogen Oxides
  • Radiation-Protective Agents