Supersaturable Self-Emulsifying Drug Delivery System of Krill Oil with Improved Oral Absorption and Hypotriglyceridemic Function.

Abstract

This study aimed to develop a supersaturable self-emulsifying drug delivery system (S-SEDDS) of krill oil (KO), a rich source of docosahexaenoic acid and eicosapentaenoic acid (EPA), to improve its hypotriglyceridemic function. S-SEDDS of KO (KO/S-SEDDS) was prepared by the addition of lysolecithin, glycerin, and hydroxypropyl methylcellulose (HPMC). Self-emulsifying drug delivery system of KO (KO/SEDDS) and KO with HPMC (KO/HPMC) were also prepared for comparison purposes. The physicochemical and pharmacokinetic properties of KO samples were characterized, and the hypotriglyceridemic function of KO/S-SEDDS was evaluated. Micronized droplets in KO/SEDDS and KO/S-SEDDS with a mean diameter of ca. 270 nm could be observed in comparison to KO and KO/HPMC. Both KO/HPMC and KO/S-SEDDS tended to enhance the dissolution behavior of KO, and the S-SEDDS formulation improved the dissolution behavior of KO as a result of micronized droplets and the addition of HPMC. KO/S-SEDDS (60 mg of EPA/kg) improved the oral absorption of KO based on the pharmacokinetic profiling of EPA, and repeated oral administration of KO/S-SEDDS (250 mg of KO kg-1 day-1) for 7 days had a potent hypotriglyceridemic effect on rats with corn-oil-induced hypertriglyceridemia compared to orally administered KO. On the basis of these findings, the S-SEDDS approach might be an efficacious dosage option to enhance the nutraceutical properties of KO.

• Authors: Yoshiki Seto, Chikara Morizane, Kodai Ueno, Hideyuki Sato, Satomi Onoue
• Journal: Journal of agricultural and food chemistry (J Agric Food Chem) Vol. 66 Issue 21 Pg. 5352-5358 (May 30 2018) ISSN: 1520-5118 [Electronic] United States
• PMID: 29754485 (Publication Type: Journal Article)

Chemical References

• Emulsifying Agents
• Emulsions
• Fatty Acids, Omega-3
• Oils
• Triglycerides

Topics

• Administration, Oral
• Animals
• Biological Availability
• Drug Delivery Systems
• Emulsifying Agents
• Emulsions
• Euphausiacea (chemistry)
• Fatty Acids, Omega-3 (administration & dosage, blood)
• Male
• Oils (administration & dosage, chemistry, pharmacokinetics)
• Rats
• Rats, Sprague-Dawley
• Solubility
• Triglycerides (blood)