Hydroquinone alternative with penetration enhancement improves facial hyperpigmentation

Key takeaways:

• The multimodal combination effectively reduced target spot and overall facial dyspigmentation as early as 4 weeks.
• No cutaneous toxicities were observed.

NEW ORLEANS — A combination of tranexamic acid, niacinamide, hexylresorcinol and licorice root was effective in improving overall facial dyspigmentation with an excellent tolerability profile, according to a poster presentation here.

Ever since the gold standard ingredient for skin pigmentation, hydroquinone, was removed from the over-the-counter markets, researchers have been looking for alternative treatment options for facial dyspigmentation, according to study authors Zoe Diana Draelos, MD, of Dermatology Consulting Services, and Isabel Diaz, of Colgate-Palmolive Company.

“Dyspigmentation of the face [is] a common challenging problem for the dermatologist and cosmetic formulator,” Draelos and Diaz wrote in their poster presented at the American Academy of Dermatology Annual Meeting. “There is a challenge to develop topical formulations utilizing other ingredients that inhibit melanin formation.”

In this study, the efficacy of a multimodal combination of tranexamic acid, niacinamide and licorice root penetration enhanced with hexylresorcinol was evaluated when used on mild to moderate facial dyspigmentation.

Fifty women aged 18 years and older with mild to moderate facial dyspigmentation were enrolled and 48 completed the study. Participants applied the serum twice daily on the entire face for 16 weeks.

Results showed that the target spots of hyperpigmentation significantly improved at weeks 4, 8, 12 and 16 (P < 0.001). At week 4, investigators also observed decreased pigment intensity (P < .001), target spot size (P = .031), sallowness of the face (P = .031), absence of facial brightness (P < .001) and absence of clarity (P < .001).

Even with further penetration, which was achieved with the hydroxy acids lactic acid and gluconolactone, the safety profile maintained excellent tolerability.

Small amounts of irritation were minimized by the chamomile derivative bisabolol, and no cutaneous toxicities were observed, making this serum safe for long-term use, according to the researchers.

“Undesirable melanin production is best addressed through a multimodal approach with penetration enhancement to reach the target site for melanin production at the dermal/epidermal junction,” Draelos and Diaz wrote.

“The multimodal combination of tranexamic acid, niacinamide, hexylresorcinol, and licorice was effective in reducing target spot and overall facial dyspigmentation as early as 4 weeks with continued improvement noted up to 16 weeks with twice daily use,” they concluded.