Resveratrol-Encapsulated Mitochondria-Targeting Liposome Enhances Mitochondrial Respiratory Capacity in Myocardial Cells

The development of drug delivery systems for use in the treatment of cardiovascular diseases is an area of great interest. We report herein on an evaluation of the therapeutic potential of a myocardial mitochondria-targeting liposome, a multifunctional envelope-type nano device for targeting pancreatic beta cells (beta-MEND) that was previously developed in our laboratory. Resveratrol (RES), a natural polyphenol compound that has a cardioprotective effect, was encapsulated in the beta-MEND (beta-MEND (RES)), and its efficacy was evaluated using rat myocardioblasts (H9c2 cells). The beta-MEND (RES) was readily taken up by H9c2 cells, as verified by fluorescence-activated cell sorter data, and was observed to be colocalized with intracellular mitochondria by confocal laser scanning microscopy. Myocardial mitochondrial function was evaluated by a Seahorse XF Analyzer and the results showed that the beta-MEND (RES) significantly activated cellular maximal respiratory capacity. In addition, the beta-MEND (RES) showed no cellular toxicity for H9c2 cells as evidenced by Premix WST-1 assays. This is the first report of the use of a myocardial mitochondria-targeting liposome encapsulating RES for activating mitochondrial function, which was clearly confirmed based on analyses using a Seahorse XF Analyzer.

Automated summary

The therapeutic potential of a myocardial mitochondria-targeting liposome encapsulating the cardioprotective compound resveratrol was evaluated in this study. The liposome was readily taken up by myocardial cells and localized to intracellular mitochondria. It significantly activated cellular mitochondrial function without causing cellular toxicity.