One of the biggest challenges faced by formulators of skin lightening products is choosing which actives to add to the products.

When we consider the options available on the market, offered by raw material suppliers, R&D teams know that adding only one active will not be enough to increase sales for a product.

Despite being an excellent lightening agent, hydroquinone is forbidden for use in cosmetics in many countries, so we are always searching for alternatives with the same effectiveness.

Cosmetic Skin Lightening Actives

Formerly, the actives available for treating spots were the famous tyrosinase enzyme inhibitors, such as kojic acid and arbutin. Inhibiting the tyrosinase enzyme is an effective way to lighten skin since this reduces the cascade process of melanin production. However, many products available on the market already adopted this concept and, in order to stand out from the competition, a product needs more than one mechanism. There are currently more than 20 different mechanisms and cosmetic actives available for skin lightening. Including all these mechanisms and actives in a single product is a complicated task, but it is possible to add a number of them.

An effective treatment is to add lighteners to sunscreen products, but not many companies do this. For example, think of a cosmetic treatment consisting of a lightening night cream with five actives from different mechanisms associated with a sunscreen with five more actives. This would provide 10 different actives and a number of different mechanisms, considerably increasing the chance of a successful treatment when compared to a product with one single mechanism.

Among the lightening mechanisms available, I would like to highlight Oligopeptide-34 that has the ability to inhibit an important transcription factor known as Melanogenesis Associated Transcription Factor (MITF). MITF is responsible for the synthesis of tyrosinase and other enzymes that are essential for the process of melanin production.

Another active that is able to inhibit melanin production early in the process is Pancratium Maritimum extract. It has been proven that this active can inhibit a prohormone known as Proopiomelanocortin (POMC) and it also has a skin lightening effect. Inhibiting POMC is essential, since this prohormone is converted into alfa–MSH (melanocyte-stimulating hormone) that is later bound to melanocyte membrane receptor, initiating a reaction that stimulates melanin production.

An active that has the ability to inhibit alfa-MSH is resveratrol. There are also important factors that are secreted by Keratinocytes and increase dendrite formation and melanogenesis, such as Stem Cell Factor (SCF) and Endothelin-1. SCF can also be reduced through the use of resveratrol, and Endithelin-1 could be inhibited by Bellis Perennis (Daisy) Flower Extract.

It is important to remember that inflammation and the formation of reactive oxygen species (ROS) can cause the appearance of spots, since they induce melanin production. Published studies have shown that the use of bisabolol is an effective treatment for skin lightening. Regarding the inhibition of ROS, results from a comparative study between vitamin C (ascorbic acid) and hydroquinone have shown good efficacy of vitamin C.

I would like to highlight another useful active: niacinamide. In a comparative study with hydroquinone 4 percent, it has shown the same efficacy in patients with melasma.  This active is able to inhibit a glycoprotein known as PMEL-17, involved in the process of melanin production. When used in concentrations of 4 percent, niacinamide has a powerful lightening effect.

As we can see, there is no single way to develop a lightening product. We need to research all technology available and assess each different action mechanism. This will allow us to formulate a product with higher efficacy and provide marketing teams with arguments to create attractive marketing claims to increase sales.