A supramolecular tranexamic acid with enhanced permeability and bioactivity

, the supramolecular interactions within GATA facilitate deeper TA penetration into the skin, achieving >2.5 times improved transdermal permeability than pure TA. Notably, GATA does not damage the skin barrier, with the associated irritation and cytotoxicity significantly lower than that caused by GA. Moreover, compared with TA, GATA has comparable or superior thermal stability, water solubility, anti-glycation, antioxidant, and anti-inflammatory properties. GATA also exhibits excellent skin whitening efficacy. Hence, GATA is a promising alternative to TA, with enhanced permeability, bioactivity, and biosafety, as well as considerable application prospects in transdermal delivery.