Bioaccessibility, Pharmacokinetics and Bioavailability of an Eicosapentaenoic acid (EPA) rich triglyceride emulsion

Martinez-Ferez, A.1, Martin-Garcia, A.2, Romero-Aguilar, A.3, Jimenez-Morales A.4
1 Department of Chemical Engineering, Faculty of Sciences, University of Granada, Spain
2 Clinical Trials Unit, University Hospital Complex of Granada, Spain
3 Haematology Department, University Hospital Virgen de las Nieves, Granada, Spain
Hospital Pharmacy, University Hospital Virgen de las Nieves, Granada, Spain


Eicosapentaenoic acid (EPA) is an important component of the cell membranes with key roles in RNA
and cell-cell signaling. For years, nutritionists and government agencies have agreed that routine
consumption of EPA is a pillar in a healthy diet. In addition, a low Omega-3 Index in erythrocytes is
associated with cardiac, cerebral, and other health issues. However, bioavailability of EPA varies with
a number of factors, like specific emulsification, inter-individual differences, concomitant food intake
vs fasted state) or chemical form [1]. Moreover, the safety, tolerability and palatability of any new
food supplement need to be documented. To this end, the bioaccessibility (fraction of the total amount
of a substance that is potentially available for absorption) of an EPA rich triglyceride emulsion has
been tested in a dynamic simulated gastrointestinal model. Fed
vs fasted conditions were simulated
through the presence/absence of the carboxylester lipase and a different biliary salt concentration. We
found that the EPA rich triglyceride emulsion showed higher total bioaccesibility in both, fed and
fasted conditions - 95.1±4.7% and 87.6.1±4.9% respectively, values significantly (p<0.05) higher than
for EPA as ethyl ester emulsion - 49.4±4.2% and 16.1±2.2% - or as triglyceride oil - 18.8±3.0% and
10.6±1.6%. In addition, we determined the pharmacokinetics and bioavailability (extent to which a
nutrient can be absorbed and transported into systemic circulation or site of physiological activity) of
the EPA rich triglyceride emulsion (an oral single dose of a strawberry flavor emulsion containing 3
grams of EPA) in 8 healthy subjects (inclusion criteria: age 18-50; BMI 20-29 Kg/m
2). Blood samples
for pharmacokinetic measurements were collected before and after dosing during 24 hours. The main
findings were: Total average bioavailable EPA fraction: 46,1% (±18%), Average T
max (time to
maximum EPA concentration): 5,214 h (±17%), Average C
max (maximum EPA concentration): 0,146
nmol/µL plasma (±29%), Average First positive time of EPA in plasma: 2,714 h (±17%), Average
concentration of EPA in plasma after 24h: 0,059 nmol/µL plasma (±28%) and Elimination Half-life,
: 5,73 h. With regard to safety and tolerability, we found total acceptability and tolerance of the
testing product and absence of adverse drug effects during the study. In light of these results, the tested
Eicosapentaenoic acid (EPA) rich triglyceride emulsion represents a highly bioaccessible and
bioavailable formulation of EPA.

[1] Schuchardt J.P., Hahn A. Bioavailability of long-chain omega-3 fatty acids. Prostaglandins Leukot. Essent. Fatty Acids.

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