A supramolecular synergistic antibacterial strategy involving direct complexation of a commercial antibacterial agent, azelaic acid (AzA) by a cationic pillar[5]arene (WP5A) is described. The formation of AzA/WP5A complex could exert synergistic antibacterial effect, leading to promote wound healing efficacy and reduce bacterial burden on S. aureus-infected mice models.