A supramolecular tranexamic acid with enhanced permeability and bioactivity

Area of Science:

• Biomedical Engineering
• Materials Science
• Dermatology

Background:

• Tranexamic acid (TA) is recognized for its bioactivities but faces limited skin penetration due to its hydrophilic nature.
• Developing effective transdermal delivery systems for hydrophilic compounds like TA is crucial for biomedical and cosmetic applications.

Purpose of the Study:

• To design and characterize a supramolecular complex of tranexamic acid (TA) and glycolic acid (GA), termed GATA, to overcome TA's poor skin permeability.
• To evaluate the transdermal permeability, bioactivity, and biosafety of GATA compared to pure TA and GA.

Main Methods:

• Supramolecular complex formation via non-covalent interactions between TA and GA.
• Multidimensional characterization including single crystal analysis and computer-aided simulations.
• In vitro assessment of transdermal permeability, skin irritation, cytotoxicity, and bioactivities (anti-glycation, antioxidant, anti-inflammatory).

Main Results:

• GATA demonstrated >2.5 times improved transdermal permeability compared to pure TA.
• GATA exhibited significantly lower skin irritation and cytotoxicity than GA, without damaging the skin barrier.
• GATA showed comparable or superior thermal stability, water solubility, and bioactivities to TA, along with excellent skin whitening efficacy.

Conclusions:

• GATA represents a promising supramolecular alternative to TA for transdermal delivery.
• The enhanced permeability, bioactivity, and biosafety profile of GATA suggest significant potential in cosmetic and biomedical fields.
• GATA's design overcomes the limitations of TA's hydrophilicity, paving the way for improved topical treatments.