Skin Lightening Efficacy of Tranexamic Acid in Topical Delivery Systems

The off-label use of oral Tranexamic Acid (TA) has been proven to be an effective treatment for melasma, a commonly acquired skin hyperpigmentation disorder.Topical TA was introduced as a cosmetic skin lightening product in recent years.However, topical TA often does not achieve clinically significant lightening of melasma.It has been postulated that topical TA does not have good skin permeation properties, therefore, delivery systems have been deployed to improve the skin permeability of TA across the skin barrier.Using an in vitro 3D skin model (MelanoDerm, MatTek), the skin lightening effects of TA encapsulated in poly lactic co-glycolic acid (PLGA) polymer and TA in liposomes were compared against the lightening effect of free TA.The melanin content of MelanoDerm skin models subjected to the three TA variants was assessed, and images of the skin models were captured after 21 days of application.Liposomal-TA and PLGA-TA were found to be superior to free TA molecules in terms of greater reduction in melanin content.Liposomal-TA was deemed to be superior to PLGA-TA since it achieved a similar lightening effect with half the amount of TA in the liposomal delivery system.