A Comparative, Randomized, Double-Blinded, and Vehicle-Controlled Study for the Reduction in Facial Pigmentation after Treatment with both Tranexamic Acid and Tranexamic Acid Ethyl Ester

Abstract

Alaa A. Ali, Zaid Mahdi Jaber Al-Obaidi, Ayad M.R. Raauf, Hasanain Shakir Mahmood.

Background: Tranexamic acid is used to treat or prevent excessive blood loss. Moreover, tranexamic acid is reported to treat the UV light-induced hyperpigmentation. Several tranexamic acid esters were approved to have topical skincare, however, tranexamic acid ethyl ester was not. In this work, a vehicle-controlled, double-blinded, and randomized clinical study was conducted for both tranexamic acid and its synthesized ethyl ester.
Methods: a well-established protocol was adopted to synthesize ethyl-4-(Aminomethyl)Cyclohexanecarboxylate from tranexamic acid and ethanol. Three gel preparations were applied. These contained tranexamic acid, tranexamic acid ethyl ester, and vehicle (gel base). These three prepared gels were applied to thirty-six subjects of three equally-divided groups for thirty days’ period.
Results: The synthesis shows 90% yield with purity > 99.7%. While the clinical findings were significant for both tranexamic acid (P = .01) and tranexamic acid ethyl ester (P < .001) whereas it was insignificant for the gel vehicle (P = .176).
Conclusion: The authors concluded that both tranexamic acid and tranexamic acid ethyl ester topical gels are considered favourable choices to counteract facial hyperpigmentation.