PAR-2 Blockers: A Key to Lightening Skin and Evening Skin Tone

PAR-2 Blockers To Lighten Skin and Even Skin Tone

Protease-activated receptor 2 (PAR-2) is a receptor in the epidermis of the skin that can be blocked to lighten skin color. Niacinamide is an example of a PAR-2 inhibitor. Blocking this receptor can also help prevent melasma and hyperpigmentation from coming back.

Adding PAR-2 blockers to your skin-lightening regimen is one way to lighten skin faster. We recommend using several types of skin lighteners in your skin care routine to lighten dark spots on the skin. PAR-2 receptor blockers can be used with retinoids and tyrosinase inhibitors and other skin lightening ingredients.

Treating uneven skin tone such as melasma and dark spots is challenging because skin lightening ingredients take 8-16 weeks to work. There is no way to lighten skin overnight, but there are tips to make skin lightening treatments work faster and better such as using skin lightening ingredients from several different categories in your skin care routine. PAR-2 blockers is one of those categories.

To understand how PAR-2 blockers work, you need to now how the skin pigment melanin gets into the skin cells called keratinocytes.

What are PAR-2 Blockers? How do PAR-2 blockers work?

Where is Melanin Produced?

Skin pigment, known as melanin, is made in the melanocyte cell and packaged in melanosomes for delivery to skin cells. One melanocyte provides melanin to 35 or more skin cells in the epidermis. Melanocytes move around in the epidermis and dermis, but for this discussion, we are going to visualize melanocytes located in the bottom of the epidermis of the skin forming an Epidermal Melanin Unit. Each melanocyte looks like an octopus and has long arms that extend between skin cells in the epidermis called keratinocytes.

epidermal melanocyte distribution

The skin pigment melanin, packaged in melanosomes, travels up the arms of the melanocytes and into the 36 + attached keratinocytes. This causes the skin color to darken.

movement of melanosomes in melanocytes in epidermis

Why is a PAR-2 Blocker Important in Skin Lightening Products?

At the connection points between the melanocyte and the keratinocytes, there is a receptor that functions like a locked doorway. This doorway is called the PAR-2 receptor. In order for melanosomes filled with melanin to travel from the melanocyte into the keratinocyte, the PAR-2 doorway must be open. Skin lightening ingredients that block the PAR-2 receptor prevent this movement of the melanosomes, preventing skin pigmentation.1

How To Block The PAR-2 Receptor To Lighten Skin?

Where PAR-2 receptors are in the epidermis.

Skincare ingredients can be used to block the PAR-2 receptor. These function as locks on the PAR-2 doorway which prevent movement of melanin into skin cells. Using a PAR-2 blocking skincare ingredient will prevent skin pigmentation. PAR-2 blockers do not lighten dark skin fast but prevent further pigmentation so it can take over 30 days to see a difference in skin color with skin lighteners. PAR-2 blocking ingredients should be used in combination with tyrosinase inhibitors which prevent the production of melanin, and exfoliants which help desquamate away old skin cells so they can be replaced with newer less pigmented skin cells. Of course, sun protection must be used to prevent the formation of new melanin.

niacinamide is the most popular PAR-2 blocker

What Skincare Ingredients Are PAR-2 Blockers?

The most commonly used PAR-2 blocking cosmeceutical ingredient is niacinamide. Niacinamide has many important functions such as decreasing inflammation, increasing cell energy to help cellular repair processes, and blocking PAR-2. Combine niacinamide in a skin lightening skincare routine with tyrosinase inhibitors, a retinoid, a tinted sunscreen, and exfoliants such as hydroxyacid cleansers and retinoids is the best way to remove dark spots on the skin. Other PAR-2 blockers such as activated soy found in Aveeno products are used to lighten skin. New PAR-2 blockers are being developed to be used in skin lightening products. Stay tuned on social media @SkinTypeSolutions to learn when new PAR-2 blockers come on the market.

List of PAR-2 Blockers

There are not a lot of ingredients that block PAR-2. Here is a list of PAR-2 blocking skin care ingredients:

Niacinamide

Active Soy

Niacinamide structure

Niacinamide

Niacinamide, also known as nicotinamide—an amide form of vitamin B3—has become one of the most popular skin care ingredients.

Clinical studies on niacinamide have shown it can reduce melanosome transfer from melanocytes into keratinocytes by up to 68% in in vitro models. (5)

The blocking of the PAR-2 receptor by niacinamide is reversible and not permanent. (7)

Other research showed that a formulation containing 5% niacinamide, when administered twice daily over an 8-week period, caused noticeable reductions in hyperpigmentation. A combined approach, using 3.5% niacinamide with retinyl palmitate, has been documented to offer similar benefits (6).

Additionally, niacinamide’s role is not limited to pigmentation control. It’s recognized as an effective anti-inflammatory component in skincare.

Niacinamide also gives cell energy to repair DNA damage. At the cellular level, it aids in energy production by influencing the NAD/NADH pathway.

Soy

Paine et al. conducted research on soymilk and its derived proteins: soybean trypsin inhibitor (STI) and the Bowman-Birk inhibitor (BBI). Their findings indicated that these proteins have the capability to inhibit PAR-2 activation, which in turn can lead to skin depigmentation. (4) The effects of these soy-derived proteins can be reversed, ensuring limited side effects. The involvement of the PAR-2 receptor is not only limited to pigmentation; it plays a role in various cellular activities.

Several studies have illustrated the ability of these agents to inhibit melanosome transfer, reducing pigmentation. These effects were tested both in the lab and on living organisms. In one experiment involving dark-skinned Yucatan microswine, the application of soybean extract led to visibly lighter skin. A key observation was that only fresh soymilk had this effect, whereas pasteurized soymilk did not. This indicates that a component in the fresh milk, likely the STI, is the active ingredient in depigmentation. Moreover, the use of soymilk showed protective properties against UVB-induced skin darkening. Human trials also confirmed a reduction in pigmented spots after the application of soybean extract. (11)

Another study delved into the effectiveness of a moisturizer containing non-denatured STI and BBI. For this study, 65 women aged 30 to 61 with varying skin conditions were enrolled. They were treated with the moisturizer or a control substance twice a day for 12 weeks. The results showed significant improvements in several skin attributes, including pigmentation, texture, and overall appearance. (9)

Beyond its depigmentation capabilities, soy also contains isoflavones. These possess antioxidant properties and have been associated with potential cancer-preventing benefits.

DQH Can I use salicylic acid first and then vitamin C? It’s easy to create a skincare routine, but knowing how to use it is another thing entirely. In most cases, if you’re not getting the desired skin results, it could be due to the layering of conflicting ingredients. So, is it possible that salicylic acid and vitamin C are such ingredients? Or are these active ingredients the duo that’s been missing from your skincare routine? If you want answers, stick around because today we are going to explain the benefits of salicylic acid and vitamin C and how they can be used in your daily life. What are the benefits of salicylic acid for skin? Salicylic acid is one of the most commonly used beta hydroxy acids and is favored by many people with oily, acne-prone skin. This acid is derived from willow bark, and unlike its water-soluble relatives (called alpha-hydroxy acids), salicylic acid is oil-soluble, which means it can penetrate deeper into the lower layers of the skin. Once it reaches the lower layers, it can help unclog pores of excess sebum, dirt, bacteria, debris, and impurities. This results in clearer skin tones and greater definition. Not only does salicylic acid benefit the underlying layers, but the outer surface of the skin benefits as well. When applied to the skin, salicylic acid removes the buildup of dead skin cells. This is accomplished by breaking the bonds that hold dead cells to the surface. Over time, this can cause the complexion to look dull and prone to acne, blackheads, and other blemishes. If you’d like to learn more about salicylic acid and how it can improve your skin, check out this dedicated blog post from a beauty insider. What are the benefits of vitamin C for skin? Vitamin C is considered one of the most powerful antioxidants, which means it is very effective at fighting free radicals and preventing them from causing further skin damage. Examples of free radicals include pollution, central heating, UV rays and harsh climate. They attack proteins, fats and cell membranes as soon as they come into contact with the skin, causing signs of premature aging such as fine lines and wrinkles as well as hyperpigmentation, flaky patches of skin and loss of elasticity. Many people usually prefer to use vitamin C in their morning routine as this ingredient gives the complexion a radiant glow. You’ll also find that vitamin C can target areas of hyperpigmentation, plumping the skin and reducing the appearance of fine lines and wrinkles. The thing about vitamin C is that there are a lot of outdated studies going back to the 1950s that describe vitamin C as an unstable skin component. Thanks to improvements in modern technology, this is no longer the case as all products now contain a stable form of vitamin C. Visit The Beauty Insider to learn more about vitamin C. So please check out our blog post. Can I use salicylic acid first and then vitamin C? Yes, you absolutely can. In fact, it’s thought that using salicylic acid before using vitamin C ensures it penetrates faster and works faster. This is an efficient way to utilize two power sources, and the reason has to do with pH. For example, the skin’s natural pH is about 4.7, making it slightly acidic. Salicylic acid and vitamin C are also both acidic, and you’ll find that vitamin C is absorbed quickly into the skin. Therefore, using salicylic acid beforehand can increase the acidity of the skin and allow vitamin C to penetrate into the skin faster. While this is considered an effective way to combine two powerful ingredients, you need to be aware of your skin type and how it reacts to certain active ingredients. Even people with perfect, normal skin can experience skin sensitivity and irritation. Therefore, always consult a doctor or dermatologist before using any new products on your skin. It’s also important to follow skin application rules. In this case, you need to use the product correctly to ensure you get the best results for your skin. If you’re not sure what I mean, the basic rule for skin is to start with the thinnest consistency and work your way up to the thickest consistency. This prevents a barrier from forming on the surface, preventing other active ingredients from penetrating the skin. Can I use salicylic acid at night and vitamin C in the morning? Yes, absolutely, this is considered the most effective way to get returns without any adverse side effects. This is because there is enough time between applications to ensure that the skin’s pH levels return to balance. You’ll also find that Vitamin C is rich in antioxidants and is perfect for use in the morning to ensure your skin is protected and looking its healthiest. Due to the small size of salicylic acid molecules, it is an acid that is able to reach the deepest parts of the skin. While this is effective at keeping skin clear, it also increases the risk of irritation and photosensitivity. Therefore, many people prefer to use powerful BHAs in their evening routine without exposure to UV rays, pollution, or harsh weather. Warning: If you avoid using sunscreen every day, none of these ingredients will do what your skin needs. The combination of chemical peels and powerful ingredients increases the risk of further damage to the skin’s surface. Use SPF 50 every day to keep your skin protected and your lipid barrier healthy, even on cloudy days, keeping your skin in top condition.

Related Articles

Ad Blocker Detected