Pharmacokinetics of a Single Intake of a Self-Emulsifying Drug Delivery System Containing the Triglyceride Form of DHA: A Randomized, Double-Blinded, Crossover Study

BACKGROUND: The health benefits of n–3 (ω-3) PUFAs are well studied. A self-emulsifying drug delivery system (SEDDS) is expected to improve n–3 PUFA absorption. OBJECTIVES: The present study investigated how a single ingestion of a new SEDDS containing the triglyceride (TG) form of DHA (22:6n–3) (DHA/TG) would affect the plasma DHA concentration in healthy participants. METHODS: Fifteen healthy participants (age: 20–65 y; BMI: 18.5–25 kg/m(2)) were enrolled in this randomized, double-blind, crossover study. Participants in a fasting state consumed a single dose of 920 mg DHA and 80 mg EPA (20:5n–3) in SEDDS soft capsules (SEDDS capsule) or non-emulsifying soft capsules (control capsule). Blood was sampled at 0, 1.5, 3, 5, 7, and 9 h after dosing. The primary outcome was the baseline-adjusted incremental AUC (iAUC) for plasma DHA concentrations (iAUC_DHA). RESULTS: The iAUC_DHA was significantly higher for the SEDDS capsule (147.9 ± 15.8 µg·h/mL) than for the control capsule (106.4 ± 18.1 µg·h/mL) (P = 0.018; SEDDS/control ratio: 1.4:1). However, plasma EPA concentrations and iAUC values did not significantly differ between the SEDDS and control capsules. Cmax was significantly higher with the SEDDS capsule for both DHA (P = 0.019) and EPA (P = 0.012) than with the control capsule. CONCLUSIONS: These results suggest that a SEDDS improves the absorbability of DHA/TG in healthy participants. This indicates that SEDDS capsules would be beneficial for efficient ingestion of DHA. This trial was registered at https://www.umin.ac.jp/ctr/ as UMIN000044188.