Liposomal Formulations Enhance the Anti-Inflammatory Effect of Eicosapentaenoic Acid in HL60 Cells

Abstract

Dietary omega 3 polyunsaturated fatty acids (PUFAs), including docosahexaenoic acid (DHA) and eicosapentaenoic acid (EPA), have been reported to be beneficial for cardiovascular diseases and cancer. Such diseases share a common pathophysiological feature of inflammation responses, such as unbalanced oxidative stress and increased cytokine release. PUFAs show anti-inflammatory effects, and thus, they are potential therapeutics to treat inflammatory disorders. Here, we proposed a novel liposomal formulation of EPA (EPA-liposomes), and the liposome was PEGylated to increase their stability. In the study, we measured the physicochemical characteristics of EPA-liposomes and their anti-inflammatory effects in neutrophil-like cells (HL 60 cells). The results showed that EPA-liposomes dramatically decreased the production of NO, ROS, and cytokines compared to EPA alone, and the molecular mechanism is associated with biosynthesis of RvE1 from EPA, and RvE1 binds to GPCRs to mediate the anti-inflammatory effects.