Introduction: Tranexamic acid is used for the treatment of hyperpigmentation, and the topical route is the most favorable route for its administration. Tranexamic acid lowers plasmin and tyrosinase, which reduces melanin and skin hyperpigmentation. Low penetration through the outer layer of skin and low availability at target melanocyte cells limit tranexamic acid topical administration. Different novel delivery systems like liposomes, microneedles, topical beads, and microparticles can help in overcoming these limitations.
Areas covered: The mechanism of action of tranexamic acid and novel delivery systems for its topical delivery have been discussed. Further, patents related to the topical delivery of tranexamic acid and clinical trials undertaken to analyze their potential have been discussed.
Expert opinion: Targeting tranexamic acid in the epidermal layer makes more amount of drug available for action on melanocytes, the target site for tranexamic acid. Novel drug delivery formulations like liposomes, solid lipid nanoparticles, nano-lipidic carriers, and topical beads have the potential of achieving epidermal targeting. Epidermal targeting of tranexamic acid can help in the superior delivery of the drug, making its topical treatment more efficient.
Keywords: Epidermal targeting; hyperpigmentation disorders; melasma; nano drug delivery systems; topical drug delivery; tranexamic acid.