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.
Highlights
Anti-Inflammatory Effect ofAt present, polyunsaturated fatty acids (PUFAs), including an ω-3 series, are mainly used as dietary supplements
The results showed that eicosapentaenoic acid (EPA)-liposomes dramatically decreased the production of nitric oxides (NO), reactive oxygen species (ROS), and cytokines compared to EPA alone, and the molecular mechanism is associated with biosynthesis of resolving E1 (RvE1) from
When observed under a transmission microscope, transformation when the dry gridsshowed for transmission microscopy (TEM) imaging the structure of the EPA-liposomes a sphericalelectron shape, with a bit of transformation were prepared, as observed in could be released gradually when the dry grids for transmission electron microscopy (TEM) imaging were prepared, over time from
Summary
At present, polyunsaturated fatty acids (PUFAs), including an ω-3 series, are mainly used as dietary supplements. It was found that these dietary PUFAs affect a wide variety of physiological processes, such as antiatherogenic [1], antiaggregatory [2], and anti-inflammatory [3] effects. Lipid-based nanocarriers can be efficiently internalized by phagocytic cells and are an attractive system to deliver PUFAs to immune cells. Macrophages and neutrophils are known to be the most efficient uptake of nanoparticles and may act as a reservoir for nanotherapeutics. The characteristics of these immune cells may facilitate the conversion of omega 3 polyunsaturated fatty acids to the cascade metabolites like resolving D1. The application of PUFAs is limited to diet due to their low transformation in vivo
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