Skin Lightening Ingredients

Skin lightening, bleaching, and whitening involves a using products with a variety of active ingredients that synergistically work to slow the production of melanin. Most skin lightening products work on the epidermal superficial layer of the skin by reducing or blocking some production of melanin. As melanin production is slowed, hyperpigmentation fades, and skin tone ultimately evens out.

The following informational list of active ingredients includes only some of the top components used in skin lightening products. It is not an exhaustive list. There are a plethora of other chemical and natural components that aid in lightening of superficial hyperpigmentation. The following list gives examples of active ingredients used in treating hyperpigmentation at every level of its synthesis.


Retinoids are functional equivalents of Vitamin A. Retinoids are commonly used as treatments for the improvement of acne, post inflammatory hyperpigmentation, and photo damage.

Retinoids work by inhibiting the enzyme, tyrosinase, responsible for stimulating the melanocyte to produce melanin. Retinoids also work to accelerate epidermal cell turnover to aid in absorption of other skin lightening ingredients, and speed cell turnover of hyperpigmented areas.


Retinoids are available by prescription only. Retinoids are available by prescription in a variety of forms and concentrations. Adverse side effects include dryness, burning, stinging, scaling, and flaking. Retinoid irritation and sensitivity may lead to post inflammatory hyperpigmentation, exasperating the problem of hyperpigmentation. Retinoids are usually found in skin lightening products together with a corticosteroid and hydroquinone.


Hydroquinone is used as a topical ingredient for the inhibition of melanin production. Hydroquinone is the most frequently used first step in skin lightening treatment of hyperpigmentation. Hydroquinone is proven successful in blocking the synthesis and production of melanin.

Topical hydroquinone is available over the counter in cosmetic concentrations up to 2%, or by prescription concentrations up to 4%. Higher concentrations of hydroquinone result in greater efficacy, however, the higher the concentration, the greater the risk of irritation.

Topical hydroquinone is considered an effective skin lightening product agent when used correctly under proper physician supervision. Hydroquinone is often prescribed in formulation with a retinoid to aid in absorption, and a corticosteroid as an anti-inflammatory.


However, hydroquinone is considered a controversial ingredient when used without proper physician supervision, when used in excessively high dosage, and when used with frequent prolonged usage. Topical hydroquinone can cause skin irritation and sensitivity when applied in high concentrations, has caused medical concerns as a potential carcinogenic risk, and been reported to induce blue-black hyperpigmentation or exogenous ochronosis lesions.

Adding to the controversy surrounding hydroquinone, some countries have banned over the counter sales of hydroquinone. However, sales of over the counter 2% hydroquinone are still available in the United States. The Food and Drug Administration (FDA) is currently pending a review of the research and data on hydroquinone and products containing hydroquinone.


Arbutin is a botanically derived compound that is extracted from the leaves of a variety of plants, including the bearberry plant. It is commonly referred to as bearberry extract. Arbutin is a naturally occurring hydroquinone glucoside, a plant molecule with a glucose derivative, and is used to inhibit melanin production and lighten hyperpigmentation.

The active component of Arbutin, the hydroquinone component, is released slowly and is a milder and less irritating controlled form of hydroquinone. Arbutin is often used in skin lightening products as a replacement ingredient for the controversial hydroquinone.


Arbutin is considered a safe alternative to hydroquinone and doesn’t appear to have any side effects. However, it is a glucosylated form of hydroquinone and may carry similar risks.

Azelaic Acid

Azelaic acid is a highly selective lightening ingredient. Azelaic acid appears to only lighten hyperactive melanocytes, with minimal effects on normal melanocyte production.

Azelaic acid is used in skin lightening products with well-tolerated concentrations of 15% to 20%, and with transient and minor irritation.


The only apparent disadvantage to having azelaic acid in a skin lightening product, is the possibility for minor and transient irritation.

Kojic Acid

Kojic acid is derived from fungus, and acts as a melanin inhibitor at the melanocyte site of production to lighten hyperpigmentation.

Kojic acid is most often used in in skin lightening products in combination with glycolic acid and/or hydroquinone. The synergetic combination of 2% kojic acid, 10% glycolic acid, and 2% hydroquinone showed superior lightening results in clinical trials.


Kojic acid can potentially cause allergic reactions, irritating contact dermatitis, and sensitization with only moderate depigmentation results. Kojic acid appears to have only moderate lightening results when used alone in a skin lightening product.

Vitamin C

Vitamin C (l-ascorbic acid) is derived and extracted from citrus fruits, and has a prominent role in antioxidant health and wellbeing.

Vitamin C not only supports skin lightening, but it has anti-inflammatory properties that counteract hyperpigmentation formed from inflammation. It is also well tolerated as part of a skin lightening product ingredient, and is topically safe.


Vitamin C promptly oxidizes when exposed to air, rapidly decreasing its topical efficacy, and because of its instability, is difficult to store.

Alpha Hydroxy Acids (AHA)

AHAs are weak organic acids that are used to treat dry skin and acne by promoting exfoliation, and stimulating new skin growth.

Glycolic acid is an AHA derived from sugar cane. Glycolic acids in skin lightening products help to remove superficial layers of the epidermis, which enhances the penetration of melanin inhibiting products, and increases the rapidity of pigment loss through epidermal cell turnover.


Glycolic acid is an irritant and may cause sun sensitivity. Sunscreen is recommended when using any skin lightening product with glycolic acid or any other AHA.


In review, the most efficacious methods of treating hyperpigmentation are skin lightening products that use a combination of active ingredients. Using a skin lightening product that inhibits melanin production and stimulates cell turnover contributes to the most successful skin-lightening regimen.

Each active ingredient has benefits as well as disadvantages in their use. The key to healthy and even toned skin is patience, and finding the active ingredients in a skin lightening product that are best suited for your individual skin type.

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