Alpha-Arbutin

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Working concentrations

About this ingredient

Alpha-Arbutin is a synthetic α-isomer of arbutin, a glycoside derivative of hydroquinone. About an order of magnitude more active than β-arbutin at the same safety profile thanks to a spatial configuration that fits the tyrosinase active site. Mechanism. Competitive tyrosinase inhibitor – the key enzyme in melanin synthesis. Suppresses conversion of L-tyrosine to L-DOPA. Unlike hydroquinone, does not damage melanocytes or cause exogenous ochronosis on long-term use. Release of free hydroquinone from α-arbutin is minimal – less than 0.005% of the dose (Migas 2015). Where applied. Depigmenting serums and creams (1–4%, most often 2%). The Ordinary Alpha Arbutin 2% + HA, Sesderma Azelac Ru, Mesoestetic, Martiderm DSP-Bright, SkinCeuticals. In Spain often paired with azelaic acid, retinol, niacinamide. Evidence base. Boissy 2005 (n=22, 12 weeks, 1%) showed 25% VAS reduction in melasma. Hamed 2006 compared 1% α-arbutin with 4% hydroquinone: comparable effect (35% vs 41% MASI reduction) with less irritation from α-arbutin. Garcia 2018 (n=30, 12 weeks, 2% + 4% niacinamide) – 42% melasma reduction. Safety. SCCS in 2015 rated α-arbutin as safe at up to 2% in facial leave-on. Does not photosensitize, does not cause exogenous ochronosis. Irritation is rare. Pregnancy and lactation – use with caution. Direct pregnancy data are scarce. Theoretical risk: release of micro-doses of hydroquinone, classed FDA category C in pregnancy. Alternative for gestational melasma: azelaic acid 15–20% (pregnancy-approved) plus SPF 50+. Particularly suitable for. Melasma, post-inflammatory hyperpigmentation, lentigo, uneven tone. Standard course – 12 weeks with daily SPF 50+. Combined with niacinamide, azelaic acid, and vitamin C for additive effect.

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