Arbutin is a derivative of hydroquinone naturally found in some evergreen plants. As a derivative of hydroquinone, arbutin is banned in dietary aids because of toxicity. However, it is considered a non-phenol alternative to hydroquinone for dermatologic and cosmetic use. In topical applications, arbutin reduces pigmentation in the skin and has been used as a skin-lightening agent since the 1960s. Currently arbutin is combined with other active ingredients in skin-care regimens to treat dark patches from sun exposure, freckles, liver spots and age spots.
Arbutin is extracted from the leaves of various types of plants, most notably the bearberry plant (Arctostaphylas uva-ursi), cranberries and blueberries, as well as in wheat and pear skins. Arbutin is converted by the body to hydroquinone, which is a type of phenol with disinfecting and diuretic properties. Arbutin was found in teas, tinctures and capsules as bearberry extracts or uva ursi extracts for weight control and menstruation aids before an FDA ban in 1990. Currently, arbutin is available in topical formulations for skin lightening because of little to no systemic absorption.
Arbutin is a derivative of hydroquinone. Like hydroquinone, it has an antibacterial effect and interferes with cell processes. When taken internally, toxicity can result and changes in heart rate and gastrointestinal damage can occur. When applied topically, arbutin produces similar but milder effects as phenol (hydroquinone) on skin tissue. Arbutin interferes with the production of pigment in cells (melanin), thereby preventing the formation and enhancing the breakdown of melanin. Topical application of arbutin produces less toxicity and irritation than phenol.
Arbutin is currently an active ingredient in skin-lightening products because of its effect on melanin. In topical formulations, the effect of arbutin is localized and penetration into deeper layers of the skin is limited. Results are dependent on dose and frequency of application, as arbutin reduces the amount of melanin in the skin layer. Arbutin can be combined with other agents that help penetration into deeper skin layers or aid skin repair to correct hyperpigmented conditions for even skin tone.
In topical formulations, the effects of arbutin are localized and dose-dependent, which provides control in managing the extent of skin lightening. Products containing arbutin can be used according to the severity of hyperpigmentation, and lower doses and reduced frequency can be employed to fine-tune skin tone. Since arbutin has limited penetration and little to no systemic absorption, use of arbutin-containing products can be stopped to allow normalized skin cells to grow (without overstimulated melanin).
Topical use of arbutin is considered to be safe and effective. Since arbutin is included in various skin products, consideration regarding the effects of the other ingredients is recommended. Prolonged use of arbutin may produce uneven pigmentation such as patches of skin with no pigmentation because its effect is localized.