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Superior even skin tone and anti-ageing benefit of a combination of 4-hexylresorcinol and niacinamide.


ABSTRACT:

Objectives

To demonstrate the synergistic effect of 4-hexylresorcinol (4-HR) with niacinamide in boosting anti-melanogenic efficacy in vitro and establish the in vivo efficacy and safety of the combination in a human trial.

Methods

Primary human epidermal melanocytes and 3D pigmented skin equivalents were treated with 4-HR, niacinamide, and their combinations for their effect on pigmentation. This was followed by a randomized, double-blind, split-face clinical study in Chinese subjects, and effects on skin tone, hyperpigmentation, fine lines and wrinkles, hydration, and skin firmness were measured for a 12-week study period.

Results

In vitro tyrosinase enzyme activity studies showed that 4-HR is one of the most potent tyrosinase inhibitors. The combination of 4-HR and niacinamide showed a synergistic reduction in melanin production in cultured melanocytes and lightened the 3D skin equivalent model. In vitro as well as in the human trial, the combination of 4-HR and niacinamide showed significantly improved efficacy over niacinamide alone on hyperpigmentation spots as measured by L*, the visual appearance of fine lines and wrinkles in crow's feet and perioral area and skin firmness, with no product-related adverse events.

Conclusions

A formulation containing a combination of 4-HR and niacinamide delivered superior skin tone and anti-ageing benefits significantly better than niacinamide alone with no adverse events. This study demonstrates that a product designed to affect multiple pathways of melanogenesis, inflammation, and ageing may provide an additional treatment option, beyond hydroquinone and retinoids, for hyperpigmentation and ageing.

SUBMITTER: Shariff R 

PROVIDER: S-EPMC9305876 | biostudies-literature | 2022 Feb

REPOSITORIES: biostudies-literature

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Publications

Superior even skin tone and anti-ageing benefit of a combination of 4-hexylresorcinol and niacinamide.

Shariff Rezwan R   Du Yaping Y   Dutta Maitreyee M   Kumar Satish S   Thimmaiah Sreenivasa S   Doraiswamy Chandraprabha C   Kumari Annu A   Kale Vaidehi V   Nair Nirmala N   Zhang Shuliang S   Joshi Manoj M   Santhanam Uma U   Qiang Qiu Q   Damodaran Anita A  

International journal of cosmetic science 20220201 1


<h4>Objectives</h4>To demonstrate the synergistic effect of 4-hexylresorcinol (4-HR) with niacinamide in boosting anti-melanogenic efficacy in vitro and establish the in vivo efficacy and safety of the combination in a human trial.<h4>Methods</h4>Primary human epidermal melanocytes and 3D pigmented skin equivalents were treated with 4-HR, niacinamide, and their combinations for their effect on pigmentation. This was followed by a randomized, double-blind, split-face clinical study in Chinese sub  ...[more]

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