How to Formulate with Azelaic Acid

How to Formulate with Azelaic Acid Easily

Azelaic Acid Works Miracles for Your Skin

No one would dispute that Azelaic acid is a miracle and multifunctional cosmetic ingredient in skincare. This gentle acid occurs naturally or by chemical modification of lipids. A small amount shows up on humans' skin naturally through the lipid breakdown process by the yeast, Malassezia spp, that naturally lives on our skin. 

What does azelaic acid do for the skin?

  1. Anti-skin hyperpigmentation: It prevents and fades all forms of hyperpigmentation through its powerful tyrosinase-inhibiting bioactivities. Its keratolytic and skin-exfoliating properties help speed up skin cell turnover and enhance the penetration of itself and other ingredients in the formula, thereby increasing its full-spectrum of skin benefits.

  2. Anti Rosacea:
    The exact cause of Rosacea is unknown. It is believed to relate to genetic, abnormal immuno-response to trigger factors, skin mites, and certain bacteria resulting in skin inflammatory response and skin lesions.      There is no cure but can be managed to slowdown the prograss and make it less noticeable on the skin.
    One of the most commonly used ingredients is Azelaic acid. Azelaic acid provides anti-inflammatory, anti skin mites, anti-microbial properties, and immunomodulating properties. The most effective concentration for management of Rosacea is the products containing 15-20% Azelaic acid for full benefits in management of rosacea skin. 
  3. Anti-Acne skincare:
    Azelaic acid is one of the most effective agents for treating and preventing acne- acne breakouts and managing acne, especially for adult acne due to it gentleness, unselcetive anti microbia function, sebum control, exfoliating, uncloging pores, preventing and fading PIH, and anti inflammatory properties. It is suited for all skin types.
    It also helps to reduce acne scar formation by down grade the inflammatory reaction.
  4. In melasma management: 

    Another skin disease that scientists can't figure out the causes. There are several factors believed to related to melasma: genetic, hormonal, high pigmentation production activities, sun exposure, etc. Underneath the dark patches, there is always an chronic inflammation. Some environmental stimulus, such as UV light, blue light, heat, and mechanical irritants can make this situation worse.

    Do you know, there are estimated 6 million American women have this skin disorder. It can also happens to man.  The incidence is higher in darker skin types. Unfortunately there is no cure, need long term management, and difficult to control.

    Athought this skin disorder doen't cause health problems, the stress it causes troumendous for the patients. Fighting with melasma is a life long battle. Although there are some treatment in doctor's office can bring you an instant improvement, if there is no effective management in place, the dark patches will be back. So finding a safe and effective a long term pigmentation management is critical to keep the hyperpigmentation under control.  

    Topical Azelaic acid is commonly used for management of melasma due to its powerful inhibition in melanin synthesis, anti-inflammatory, and antioxident properties. It is considered safe for long term topical applications and during pregnancy and breastfeeding. 

    Other safe ingredients for long-term management includes tranexamic acid, cysteamine HCl, Niacinamide, Vitamin C, and other natural/or skin identical skin brightening ingredients.
  5. Anti aging skincare:

    As an acid, Azelaic acid inheritantly provide the exfoliating property to resurfacing the skin, speeding up the skin cell turnover rate, brightening the skin tone, and protecting the skin from micro-inflammatory response to the environmental adverse influences due to its antioxidative properties. Those properties are beneficial for antiaging skincare. 

    In antiaging skincare, most of us ignoring the importance of anti inflammatory skincare.     The skin aging is caused by mutiple factors, including natural aging process, internal and external adverse factors. Almost all those factors damage the skin through chronic inflammation. Chronic inflammation is the cause of skin aging. It damages the skin structures, cause skin cells/skin stem cells death, and thinning of the full thickness of skin, epidermis, dermis, and hypodermis, and eventually cause all signs of skin aging, including fine lines, wrinkles, skin sagging, hollo effect around the eyes, etc. 

    Azelaic acid is appreciated in antiaging skin care due to its fast acting in skin resurfacing/exfoliating to create a smooth and radiant skin texture; its antioxidant helps to prevent the skin from oxidative stress, and anti inflammatory property helps to reduce the damages caused by internal and external adverse factos.

    Because it is gentle and effective ingredient and suited for all skin types. Its hyperpigmentation property helps to fade dark spots, even the skin tone, and gives the skin a much younger appearance. It is love by professionals, formulators, and Diyers. Those are the true reasons more and more Azelaic acid or its derivatives appear in a lot of antiaging products from big brands.

Concentration Matters:

As you can see, Azelaic acid has its unshakeable position in skincare. At lower concentrations (≤10%), It is used as an antiaging agent; At higher concentrations (15-20%), it acts as an immunomodulator and anti-inflammatory and antimicrobial, and skin-brightening agent for specific skin concerns, as mentioned above. 

Azelaic Acid Drawbacks

Unfortunately, Azelaic acid is one of the most challenging ingredients to work with, even for professionals, primarily due to its very low water solubility (0.21%), tendency to recrystallize in finished products, and tendency to destabilize formulations.

For these reasons, it is often found in many products at the concentration that is too low to provide any visibe benefits. For higher concentrations, it takes time, money, and experience to handle it properly. 

However, if you are experiencing rosacea, melasma, acne, or other skin hyperpigmentation, low concentrations are insufficient to address these conditions. People with those skin conditions may have tried many products on the market. Ultimately, most of you have to take matters into your own hands and find a solution that taylor to your skin needs. Many even start making DIY products that perform better than what you can find for long time battle with those conditions.

Three Major Challenges when Formulating with AZA: 


Its water solubility Issue:
Azelaic acid has very low water solubility (0.21%). It doesn't dissolve readily in water. Applying heat or adjusting pH may help temporarily, in which needle-like crystals form throughout the finished products, undoing all your effort.  

Solvent in High Concentration:
In the past, to address solubility issues, larger amounts of solvent(s) were often used to achieve the desired concentrations and to stabilize the formula. High concentrations of solvents usually cause skin irritation and other unpredictable side effects. Sometimes these solvents can worsen skin conditions. 

Recrystallization Issue:
Recrystallization is the most common formulation problem with Azelaic acid, even for experienced formulators. It takes significant effort, time, and testing to develop a stable formula. 

Azelaic acid is easy to formulate with:

The cosmetics industry has changed dramatically over the past 10 years. It has accelerated over the past couple of years. Many new methods and ingredients have been developed to handle difficult yet indispensable raw materials, such as azelaic acid. Now there are at least two azelaic acid derivatives that effectively address those 3 challenges. Working with AZA derivatives becomes effortless.

DF-AZA60:

60% Azelaic Acid water-soluble powder, developed for Dermafactors LLC. The product contains 60% pure azelaic acid and 40% skin-protecting and skin-delivery agents. It works exactly like azelaic acid but makes your diy projects som much easier and other components not only provide not only significant improvement in solubility but also skin protection and penetration benefits. DF-AZA60 forms an effective skin-delivery system for itself and other active ingredients in the formulas. 

I made a 15% azelaic acid toner with a straightforward formula as follows:
  1. 25% DF-AZA60
  2. 1% DF-PE9010
  3. Add water to 100%
— Add all ingredients to a clean container and mix well. It is a cold process. No heat or solvent necessary. You can certainly modify this simple formula by adding other compatible ingredients to suite your skin needs.

This water-like, oil-free formula leaves skin non-tacky and non-sticky after use. It can be used alone or layered with other skincare products without irritating or adding any stress to the skin.

This formula delivers 15% azelaic acid to the skin, providing full-spectrum benefits for problematic skin. It is suited for someone who doesn’t want their skin routine disturbed by using too many products or too complicated skincare routine. 

Potassium Azeloyl Diglycinate (PAD):

If you are deep into skincare, you may have already noticed that this new 5-star noble ingredient is increasingly featured in products from leading brands. Potassium Azeloyl Diglycinate is a chemically modified Azelaic acid designed to eliminate water solubility, recrystallization, and poor skin penetration issues, with added critical skin benefits in supporting skin healing and regeneration—the two components used for the modification, potassium and glycine, are both skin-identical ingredients.

As a salt form of Azelaic acid with a lower pH than its original form, Pad penetrates the skin more readily and effectively. Additionally, it enhances the other active ingredient’s skin penetration (2-10%) and works effectively while being extremely skin-friendly. Formulate at higher concentrations; a little heat is recommended for complete dissolution in water.

After Pad penetrates the skin, its molecules release three components: Azelaic acid, potassium, and glycine. In its original form, Azelaic acid provides the skin with full-spectrum benefits, including antiaging, anti-inflammatory, anti-pigmenting, and antimicrobial properties. It is a glycine derivative. Provide critical support for skin healing and regeneration, as skin's Natural Moisturizing Factors (NMFs), potassium, and glycine greatlysignificantlye deep skin hydration, normalize skin bio-activities, and stabilize the balance of the skin microbiome. 
The only drawbacks are their cost and scarcity.

I have made a simple toner with this ingredient to determine the best way to use it. Here is what I used: 
PAD 5%
Glycerin 5%
DF-PE9010 1%
Supper Low molecular weight Hyaluronic acid 1%
Add water to 100%.
Tips:
I found that adding PAD a little at a time while stirring (be patient) or applying a little heat helps dissolve this ingredient easily, and no recrystallization was observed up to 10%.

 

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