Amino Acid Derivatives as Palmitoylethanolamide Prodrugs: Synthesis, In Vitro Metabolism and In Vivo Plasma Profile in Rats
Laboratory studyOther animalsWith L-Val-PEA and D-Val-PEA (amino-acid ester prodrugs of PEA, tested alone)
This study tested palmitoylethanolamide together with L-Val-PEA and D-Val-PEA (amino-acid ester prodrugs of PEA, tested alone). Its results cannot be assigned to palmitoylethanolamide alone. More combination studies.
- Design
- Laboratory study
- Subjects
- Rats given oral doses of the amino-acid ester prodrugs, alongside in vitro plasma and liver-homogenate stability tests
- Dose used in the study
- L-Val-PEA and D-Val-PEA given orally at doses equimolar to PEA
- Duration
- Plasma measured at several time points after dosing
- What was measured
- Chemical stability of carbonate, ester and carbamate PEA derivatives; plasma and liver stability; plasma levels of prodrug and released PEA after oral dosing in rats.
What the authors reported
The study of amino acid ester prodrugs found:
- Ester prodrugs made by joining PEA to amino acids allowed control over how fast PEA was released in plasma and how stable they were in the liver.
- L-Val-PEA released PEA readily in plasma, and D-Val-PEA resisted liver breakdown.
- Both released PEA after oral dosing in rats, but gave lower plasma PEA levels than an equal dose of PEA itself.
Limits of this study
A chemistry and rat pharmacokinetic study, not a treatment trial; it does not show clinical effect in people or animals treated in practice. The authors declare no competing interests.
Source
PubMed 26053855 · doi:10.1371/journal.pone.0128699
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.