Melasma is a chronic recurrent, acquired hyper-melanosis that arises exclusively in sun-exposed areas. With a high recurrence rate, melasma presents a great therapeutic challenge. Conventionally, the cornerstones of melasma therapies have been topical whitening agents and stringent photoprotection. Chemical peels, dermabrasion, and laser treatments are other adjuvant treatment modalities that have shown limited efficacy. There has recently been a growing interest in investigating the impacts of tranexamic acid (TA) on melasma and has shown promise. tranexamic acid has been investigated for melasma treatment in a variety of formulas, which include topical, intradermal (ID), and oral administration, with oral formulations showing the highest albeit transient benefit. Topical therapy is often recommended over systemic therapy for hyperpigmentation illnesses because it delivers medicine directly to the diseased area, leading to fewer side effects and improved patient compliance. Throughout this brief review, we explain the various regimens of TA for melasma, as well as other suggested research directions with an emphasis on nanotechnology that should be pursued in the future.