Discovery of a long-acting nanocrystal formulation of INND-2201, a new co-drug of pregabalin and palmitoylethanolamide with synergistic analgesic effects
Laboratory studyOther animalsWith INND-2201 (a co-drug combining pregabalin and PEA, tested as a single conjugate molecule)
This study tested palmitoylethanolamide together with INND-2201 (a co-drug combining pregabalin and PEA, tested as a single conjugate molecule). Its results cannot be assigned to palmitoylethanolamide alone. More combination studies.
- Design
- Laboratory study
- Subjects
- Mice (inflammatory and neuropathic pain models); microsomal stability test in vitro
- Dose used in the study
- Oral INND-2201 (ED50 4.43 mg/kg inflammatory pain, 5.54 mg/kg neuropathic pain); intramuscular INND-2201 nanocrystals, particle size 107.1±2.7 nm
- Duration
- Pain relief from intramuscular nanocrystals lasted up to 5 days
- What was measured
- Metabolic stability of INND-2201 into pregabalin and PEA; antinociceptive effects in inflammatory and neuropathic pain models; nanocrystal particle size; acute toxicity, muscular irritation, rotarod and open field safety tests.
What the authors reported
INND-2201 was slowly metabolised into pregabalin and PEA and produced synergistic antinociceptive effects orally, with ED50 values of 4.43 mg/kg (inflammatory pain) and 5.54 mg/kg (neuropathic pain). Intramuscular nanocrystals gave pain relief lasting up to 5 days in a chronic inflammatory pain model in mice, with a good safety profile on toxicity and motor tests.
Limits of this study
A mouse study of a novel synthetic co-drug, not PEA alone; it cannot show effect in people. The authors declare no competing interests.
Source
PubMed 41550657 · doi:10.1016/j.pscia.2025.100099
Entry checked against the abstract on PubMed on 2026-09-22. The dose shown is the dose the researchers used. It is not a recommendation. How to read this page.