2016 Volume 5 Issue 2 Pages 180-187
Recently, we reported the antidiabetic activity of ω-3 polyunsaturated fatty acids (n-3 PUFAs), such as α-linolenic acid (αLA) and docosahexaenoic acid (DHA), by using mouse colon segments. In that study, however, it was difficult to further enhance the therapeutic potential of n-3 PUFAs because of their poor solubility in aqueous media. The present study, therefore, was designed to establish a method to increase the dose of n-3 PUFA, particularly αLA; the lipidic drug delivery carrier, liposome was used. The prepared liposomes contained high content of αLA and were characterized as uniformly sized particles (approximately 100nm) with relative stability for more than 11 weeks. An animal study showed that intracolonic administration of αLA-loaded liposome reduced the blood glucose levels of mice with hyperglycemia. In addition, quantitative analysis of the plasma concentrations of insulin and glucagon-like peptide-1 (GLP-1) suggested enhanced secretion of insulin and GLP-1 via stimulation of colonic fatty acid receptor by αLA-loaded liposome-mediated hypoglycemic action. Thus, we found that liposomes can be a feasible carrier for increasing the dose of n-3 PUFA, and n-3 PUFA-loaded liposomes may become a new class of effective antidiabetic candidates without hypoglycemic risks.
