Ameliorating vascular endothelial injury for lipolysacharide-induced via mitochondrial targeting function of octaarginine-modified essential oil from Fructus (EOFAZ) lipid microspheres.

OBJECTIVE

To investigate the therapeutic potential of octaarginine (R8)-modified essential oil from Fructus (EOFAZ) lipid microspheres (EOFAZ@LM) for cardiovascular therapy.

METHODS

EOFAZ@LM was developed by leveraging the volatilization of EOFAZ and integrating it with the oil phase of LM, followed by surface modification with cell-penetrating peptide R8 to target the site of vascular endothelial injury. The therapeutic effects of this formulation in alleviating lipopolysaccharide-induced vascular endothelial inflammation were evaluated by assessing mitochondrial membrane potential (MMP), intracellular reactive oxygen species (ROS) levels, as well as inflammatory factors interleukin-6 (IL-6) and interleukin-1 (IL-1) levels.

RESULTS

EOFAZ@LM effectively delivered EOFAZ to the site of injury and specifically targeted the mitochondria in vascular endothelial cells, thereby ameliorating mitochondrial dysfunction through regulation of MMP and reduction of intracellular ROS levels. Moreover, it attenuated the expression levels of IL-6 and IL-1, exerting protective effects on the vascular endothelium.

CONCLUSION

Our findings highlight the significant therapeutic potential of EOFAZ@LM in cardiovascular therapy, providing valuable insights for developing novel dosage forms utilizing EOFAZ for effective treatment against cardiovascular diseases.