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 Knowledge drop: In your 20s, your skin cell turnover decreases. (Cell turnover is a key component in keeping your skin youthful.) You know what else slows down? Your collagen production. Starting in your 20s, collagen decreases by about 1 percent per year. Should you want to prevent fine lines and wrinkles, start by eliminating behaviors that contribute to premature aging. “If it’s bad for you, it’s bad for your skin,” says dermatologist Michel Somenek. “Cigarette smoking reduces blood flow to the skin and causes premature wrinkling and a dull skin texture. Making the repeated pursed motion to inhale can also cause smoker’s lines. Alcohol and recreational drugs are toxins for the skin that damage its cellular structure and DNA,” Somenek tells us. “The faster you eliminate vices while you are young, the better chance your skin and body have to recuperate.” Also, adopting an anti-aging routine in your 20s is key. After all, the best offense is a good defense. We spoke to Somenek and experts Joshua Ross and Audrey Kunin to find out more. Keep reading for the best anti-aging products for your 20s, according to skincare professionals. Sunscreen “We all know that the sun is the number one cause of skin aging and starting the prevention in your 20s is very important,” Ross says. “The majority of your sun damage won’t start to appear until you’re in your 30s, so don’t wait until you see it surface or you’ll be behind the curve. Stay ahead of it with a good-quality zinc-based sunscreen worn daily.” Farmacy Green Defense Daily Mineral Sunscreen An invisible sunscreen with SPF 30, plus botanical extracts meant to protect skin with tons of antioxidants. Bonus: It’s clean and fine to use under makeup. Bareminerals Complexion Rescue™ Tinted Moisturizer Broad Spectrum SPF 30 Although we recommend you use your SPF and moisturizer separately, we also understand moments when you don’t have time or energy for that extra step. For those times, this bareMinerals moisturizer is a great thing to have on hand. Vitamin C Serum “A great introduction to anti-aging is to start with a vitamin C serum in your morning skincare routine,” Ross says. “It’s a powerful antioxidant that will neutralize free radicals and brighten the skin.” He adds that it’s a great way to counteract the effects of the sun’s harmful rays, which, as previously mentioned, are among the biggest causes of premature aging. Drunk Elephant C-Firma™ Vitamin C Day Serum The Drunk Elephant C-Firma is a lightweight serum that promises to give skin a glow by combining the brightening powers of vitamin C with ferulic acid, l-ascorbic acid, and vitamin E. The included sodium hyaluronate is meant to replace hydration loss, so you shouldn’t have to deal with any irritation. Sunday Riley C.E.O. Rapid Flash Brightening Serum This potent serum is jam-packed with vitamin C (15 percent, to be exact), which means it’s a potential superstar at both brightening skin and dousing it in antioxidants. Peptides Using peptides on your skin has many benefits, says Somenek. “The skin barrier is what defends the body against pollution, UV rays, bacteria, and toxins. It can be damaged by several everyday factors. Using topical peptides aids in building a stronger barrier,” he says. “Peptides comprise elastic fibers, which are a type of protein. These fibers help to make skin appear taut and firm. Peptides can also help repair damaged skin, relieve inflammation, and even out skin tone. Some peptides can kill acne-causing bacteria that is common in 20-somethings.” Kunin agrees, saying, “Peptides are an excellent entry point for supporting collagen.” She recommends looking for face and eye treatments that contain these collagen-boosting powerhouses. Charlotte Tilbury Magic Eye Rescue Cream This Charlotte Tilbury super-emollient eye cream has a base of coconut oil and shea butter (read: it’s incredibly hydrating). Botanicals plus peptides are meant to help reduce dark circles and boost collagen, respectively. This creamy moisturizer serves up potent collagen-boosting peptides and pycnogenol, and antioxidant-rich vitamin C. “Instead of sitting on top of the skin, peptides penetrate the outer layer so they go deep. The ‘signals’ they send tell the cells to produce elastin and collagen, which are needed for youthful-looking skin,” explains Somenek. At-Home Peel Pads Remember that skin cell turnover fiasco we talked about earlier? One way to help support it is by exfoliating. “Exfoliation is important to help keep skin fresh and luminous,” Kunin says. She recommends using at-home peel pads as an easy and effective way to exfoliate. “The goal in your 20s is to fight the slowing pace of cell turnover. It is wise to use products that gently exfoliate, yet still remove oil and other impurities. Products that have Alpha Hydroxy Acids (AHA) or Beta Hydroxy Acids (BHA) are a good choice.” According to Somenek, you should only exfoliate two to three times a week. “People of all ages are guilty of over-exfoliating and that can be too much of a good thing,” he says. Dermadoctor Kakadu C Intensive Vitamin C Peel Pad A few swipes of this Derma Doctor powerful peel pad promise to leave your skin glowing and smooth, thanks to the seven (yes, seven) types of chemical exfoliants, including AHA and BHA. It also contains vitamin C via Kakadu plum extract for added brightening and antioxidant protection. KEY INGREDIENTS Kakadu plum extract is sourced from the Kakadu plum, a fruit grown in northern Australia. It contains vitamin C, which restores the skin’s natural barrier, increases collagen production, and soothes irritation. Dr. Dennis Gross Skincare Alpha Beta® Universal Daily Peel Pads These are the gold standard of peel pads, with a cult following and over 900 five-star reviews on Sephora. They’re easy to use and contain a blend of anti-aging exfoliating acids. Emollient Night Cream “In your 20s, you need to start upping the hydration in your skincare routine. You may have been cautious of over-moisturizing because of acne in your teens, but as you enter your 20s, your skin transitions and becomes drier,” Ross says. “I recommend an emollient night cream added into your evening skincare regimen.” “Twenty-somethings need to make sure that they are not using creams that will clog their pores and cause excess oil production,” says Somenek. Opt for non-comedogenic products. Cerave Skin Renewing Night Cream One great choice is the CeraVe Skin Renewing Night Cream, which is a non-comedogenic night cream that leaves skin soft and glowy. It combines the moisturizing powers of ceramides and hyaluronic acid. RoC Retinol Correxion Max Hydration Creme “The best night cream ingredients contain retinol, benzoyl peroxide, and/or salicylic acid or hyaluronic acid. The goal is to moisturize, yet remove excess oil,” says Somenek. This Roc Retinol Correxion cream fits the bill as it contains both hyaluronic acid and retinol so it promises to moisturize while also being non-comedogenic.

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