A Review of Oral Therapies for the Treatment of Skin Hyperpigmentation

Abstract

This review article examines evidence supporting the use of oral therapies in treating idiopathic, actinic, and metabolically induced skin hyperpigmentation. A thorough review of the literature regarding oral treatments for hyperpigmentation was systematically conducted through PubMed. Keywords used in the primary search include “Hyperpigmentation,” “Melanosis” or “Melasma,” “Lightening,” “Oral,” and “Therapeutics.” The search was limited to the English language, and no timeframe restrictions were implemented. Numerous orally administered therapies have been proposed for the treatment of skin hyperpigmentation. There is an abundant body of literature demonstrating the efficacy of orally administered tranexamic acid, glutathione, isotretinoin, and proanthocyanidin. It is reasonable to expect that the most effective oral therapies will address known underlying causes of hyperpigmentation such as thyroid disease, diabetes, and hormonal imbalance. Improvement due to oral therapy of otherwise unresponsive skin hyperpigmentation or hyperpigmentation of unknown cause is less predictable. This review is limited by the strength of evidence contained within the available studies. Clinical studies investigating the treatments discussed within this article are limited in number, at times lack blinding in the study design, and are based on small sample sizes. Based on existing research, the most promising oral remedies for hyperpigmentation appear to be tranexamic acid, glutathione, isotretinoin, and proanthocyanidin. Additional studies to better establish safety and efficacy are necessary.

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“…Over many years, glycyrrhizin, which is comparable to corticosteroids in terms of pharmacological efficacy but with fewer and less severe adverse effects, has been used to treat a number of dermatological disorders efficiently. According to previous research, glycyrrhizin has a variety of effects, including anti-inflammatory, antiviral (Shimshak et al, 2022), anti-allergy, anti-carcinogenesis, and antithrombin properties. The inhibition of monocyte migration and induction of apoptosis is a plausible explanation for the mechanism of glycyrrhizin therapy in Riehl's melanosis.…”

Efficacy and safety of a facial serum and a mask containing salicylic acid and lipohydroxy acid in acne management: A randomized controlled trial

“…7,8 Combining retinoids with other topical agents, procedures and oral therapies is also recommended. 7 Although some of these agents could effectively prevent PIE and/ or PIH, 9 clinical studies addressing their use are limited and often biased by small sample sizes. Moreover, the question of combining various skin care products and cosmetics that may also stimulate hyperpigmentation is rarely addressed.…”

Tetrahedral framework nucleic acid loaded with glabridin: A transdermal delivery system applicated to anti‐hyperpigmentation

“…TYR and TYR‐related proteins (TRP‐1 and TRP‐2) are transported from the nucleus to melanosomes at an early stage and catalyse the synthesis of melanin. 17 , 18 , 19 Specifically, melanin synthesis in the human body begins with l ‐tyrosine, which is finally converted to melanin through complex processes. In this pathway, TYR converts l ‐tyrosine to dopaquinone (DQ).…”

“…TYR and TYR-related proteins (TRP-1 and TRP-2) are transported from the nucleus to melanosomes at an early stage and catalyse the synthesis of melanin. [17][18][19] Specifically, melanin synthesis in the human body Jiajun He and Wen Chen contributed equally to this work.…”