Pharmacokinetics of Omega-3 Monoglycerides

Overview

North American diets have insufficient omega-3 fatty acid (n-3 FA) content. Consequently, they display low plasma concentrations of docosahexaenoic acid (DHA) and eicosapentaenoic acid (EPA), the two main long chain n-3 FA. A quick and easy way to increase the level of dietary n-3 FA is to take supplements. However, people report side effects in using the currently available supplements, such as gastrointestinal discomfort, nausea and gastric reflux; especially those where EPA and DHA are esterified as ethyl esters (EE). Moreover, EE supplements are less absorbed compared to other esterification forms, such as mono-, di- or triglycerides. The objective of this study was to test the pharmacokinetics of a new n-3 FA supplementation formulation rich in FAs esterified as monoacylglyceride (MAG).

The growing presence on the North American as well as European market of food products enriched with fish oil as a source of polyunsaturated fatty acids (PUFA) omega-3 in the diet requires evaluation and comment. Research exploring health influence of the consumption of fish oil started in 1990 years. It was established that long-chain omega-3 PUFA (EPA C20:5 and DHA C22:6) has beneficial effect on human health. Fish oil is the main dietary source of long-chain omega-3 PUFA. Dietary recommendations suggest that the consumption of omega-3 PUFA should increase. The European Academy of Nutritional Sciences (EANS) and the United Kingdom dietary guidelines recommend a daily average intake of 0.2g of EPA plus DHA. In 2000, the Food and Drug Administration stated that the daily intake of EPA and DHA should increase up to 3.0 g per person in the form of fish oil, from food and dietary supplements. According to the World Health Organization recommendations for preventing cardiovascular diseases, one portion of fish should provide an equivalent of 200-500 mg of EPA and DHA. Due to the low fish consumption in developed societies, it seems reasonable to introduce fish oil in capsule supplement dosage forms and several food products enriched with fish oil that can be an additional source of the desirable long-chain omega-3 PUFA in the diet. For this purpose, reaching the recommended daily intake may require taking several capsules of fish oil per day. Several studies have been performed to evaluate the potential health benefits brought by the consumption of food enriched with fish oil. Some studies suggest that different amounts of long-chain omega-3 - DHA and EPA, provided in a supplement form or added to food products, result in the same effect in changes in the blood lipid profile. The development of fish oil enriched food must be based on the scientific knowledge of the target function in the body and show that the effects are relevant for improved health or reduction of disease risk. The physiological effects of the intake of omega-3 fatty acids added to foods may differ depending on the quality of the fish oil used and the type of product. Fish oil benefits range from decreasing risk of the so-called life-style diseases, particularly cardiovascular diseases, to combating depression, bipolar disorder and schizophrenia. Fish oil has also prophylaxis effects and treatment effects on inflammation, arthritis, anti-aging, age-related macular degeneration and mental health. Most of dietary lipids ingested from food consist of triacyglycerols. Prior to passive diffusion into the enterocytes, lipid digestion and emulsification are initiated by the action of different lipases resulting in the release of 2 free fatty acids and one monoglyceride-linked fatty acid. They are incorporated into mixed micelles to facilitate absorption into the bloodstream. The process of manufacturing the fish oil determines the quality which also depends on the type of fish used and the purity standards followed when refining the oil. Emulsified forms of fish oil have led to improved digestion and absorption of EPA and DHA in human healthy volunteers. Flavored emulsified liquid preparations provide a simplified approach to fish oil delivery; emulsion as new approach seems to have advantages in the digestion and absorption of fatty acids which will increase the bioavailability. Using a novel approach of fish oil emulsification, preliminary results have indicated that both the rate and the extent of absorption of the fatty acids, particularly EPA and DHA, may be increased when digested. The present study was designed to establish that fish oil pre-emulsified using a novel approach will lead to increased absorption of EPA and DHA compared with the non-emulsified form of the fish oil.