Features of azelaic acid and its mechanism of action


What is Azelaic acid and how does it work?

AA is a carboxylic acid that is formed naturally on normal skin during lipid metabolism and is found in small quantities in the human body. When applied to the skin, AK preparations easily penetrate the epidermis and dermis, with up to 4% of the total dose entering the systemic circulation.

Functions performed by AK on the skin

  • Anti-inflammatory effect – stops the inflammatory process.
  • Antioxidant effect – binds free radicals.
  • Antimicrobial effect (bactericidal) – effective against gram-positive and gram-negative microorganisms, suppresses the transition of C. Acnes to a pathogenic form, retains the skin microbiome (bacterial flora), thereby reducing the load on the immune system.
  • Keratolytic effect - eliminates hyperkeratosis of the mouths of the sebaceous glands follicles.

  • Normalizes the process of differentiation of epidermal cells.
  • Lightening effect - suppresses melanin synthesis by inhibiting the enzyme tyrosinase.
  • Antiandrogenic effect - suppresses the synthesis of type I 5α-reductase, which leads to a decrease in the content of dehydrotestosterone in sebocytes, thereby normalizing the processes of keratinization and sebum secretion.

According to the latest data, AK has an antifungal effect against fungi of the genus Pityrosporum ovale and Candida albicans, which are resistant to antibiotics. Microorganisms do not develop resistance to AK itself even after prolonged exposure.

AZELIQ (gel)

normal, and the existing minor problems promised to be easily eliminated.
But before we come to see a cosmetologist, we were strongly recommended to treat our skin with Azelik gel for at least a month. The price of this product in the pharmacy horrified me. At first we bought a small tube, just tiny, it cost 300 rubles. We had to at least try to see if it would suit our skin. We didn’t find anything bad, so we decided to try to continue the treatment and complete the cleaning process. Therefore, we bought a large tube, which ruined me for 700 rubles.

Gel "Azelik" from "is designed to combat acne. Many, many scary chemical names in the composition indicate that the product is serious and poisonous. For acne, of course. It was not clear to me how the gel should act on acne. It always seemed to me that the only remedy for acne was to squeeze, squeeze, and squeeze again. Steam first and uproot these black dots along with the white rods. This is how they treated them when I was a child. And it helped! And to anoint it, and it all dissolves on its own... a dubious forecast... And at a huge cost. We applied the gel once a day. The manufacturer's note in the instructions about 2.5 cm of gel was completely unclear to me. Do I need to squeeze out a 2.5 cm long strip of gel? But then even a 700-ruble tube won’t be enough for a week. Or maybe you need to apply a 2.5 cm thick layer of gel on your face? No. Nonsense. In general, we just usually applied the gel to the acne areas.

The ointment stung the skin, especially in the first days. The burning sensation indicated that the product was working, and a positive result was very likely. The gel is almost completely odorless. White color. A month passed, no changes occurred on our face. But we have a cleaning ahead of us in the cabin, which should solve everything.

I was not present at the cleansing. But my daughter said that in addition to the use of some special devices, ordinary squeezing also took place. What did I say? You can’t do without this! After this cleaning, our face suffered, there were spots and traces of cleaning left. So far it was not even clear what this process had brought us. I had to wait a week for the skin to calm down to take the final photo. What have we achieved? My daughter likes the result, she says her face has become cleaner. But I don’t see any changes at all. It seems to me that it is as it was. If it got better, it was only a little bit. Therefore, as a result, I am writing - the gel helps, but very little. When buying a product for that kind of money, I expected a better effect, that my face would be cleaner, my skin would be smoother. To be honest, I find it difficult to recommend the product or not. Most likely no. It is much more effective to monitor your skin daily and regularly use regular products to cleanse teenage skin. This way is simpler and more reliable. And buying this product before cleaning, it seems to me, was unnecessary, it’s just commercialism. The effect of this gel does not justify its price.

Peeling with azelaic acid

Study

A study was conducted on the effect of AA, which is part of the surface peeling, on the secretion of sebum in various areas of the face in women.

Research data:

  • 11 women aged 49-71 years
  • Measuring sebum levels with a sebum meter
  • Peeling course – 5 procedures with an interval of 2 weeks

Results:

Decreased sebum production

even out skin tone,

narrowing of pores,

reduction of inflammatory elements of acne.

How does AK work as part of a peeling?

  • Has a sebum-regulating effect;
  • Evens out skin tone;
  • Works against acne and prevents the appearance of new rashes;
  • Increases skin tone and elasticity;
  • Evens out skin texture.

Summary

Peeling with azelaic acid is ideal for adult skin prone to inflammatory acne and rosacea; Peeling is effective for enlarged pores and oily skin; Azelaine peeling works against age spots.

Acne is one of the most common skin problems, affecting not only teenagers but also adults. The disease may begin in adolescence and subsequently be characterized by a continuous or periodic course, or manifest for the first time in adulthood. Recently, a third type of pathology has been proposed, called recurrent acne - with the onset of acne in adolescence, clinical improvement for a period of time, but then recurrence years later.

It is believed that genetic and hormonal factors contribute to the pathogenesis of late-onset acne. Several possibilities are considered as triggers or aggravating factors, such as exposure to ultraviolet radiation, stress, obesity, dietary disorders, smoking, sleep disorders, use of cosmetics and medications, excessive skin washing, immune system reaction to Cutibacterium acnes, and endocrine system deficiency.

Although milder forms of the disease usually occur in adults, they are quite resistant to treatment - acne tarda is chronic and requires maintenance treatment - in some cases for many years. The search for optimal schemes is still ongoing.

A recent study published in the journal Scientific Reports compared the effectiveness of azelaic acid and pyruvic acid in treating acne in 120 young women.

Azelaic acid has been used to treat acne for a long time. This is a dibasic saturated carboxylic acid, which is sometimes mistakenly put on a par with hydroxy acids, but it has nothing in common with them either in chemical structure, or in properties, or in the mechanism of action in the skin.

The effect of azelaic acid on the skin consists of four main effects - antibacterial, anti-inflammatory, comedolytic and depigmenting. Each of them has its own mechanism of action. Thus, azelaic acid is able to influence the metabolism, enzymatic activity and intracellular pH of microorganisms - both aerobic and anaerobic, and this is associated with a bacteriostatic effect against a wide range of bacteria, including C. acnes. It is interesting to note that azelaic acid has a high affinity for C. acnes, and its concentration inside the bacterial cell can be 90 (!) times higher than in the environment.

The anti-inflammatory effect is partly due to a decrease in the number of cutibacteria, and partly due to direct suppression of the release of pro-inflammatory mediators and reactive oxygen species from skin cells involved in the inflammatory response.

The comedolytic effect is due to the fact that azelaic acid affects the production of sebum lipids in sebocytes and reduces the production of long-chain fatty acids that contribute to the development of acne.

In addition, azelaic acid suppresses the proliferation of basal keratinocytes by inhibiting DNA synthesis and reduces the rate of their maturation, reducing the respiratory function of mitochondria. As a result, with the use of drugs with azelaic acid, the stratum corneum becomes thinner, and the signs of hyperkeratosis become less pronounced, and this is a good prevention of closed comedones.

DNA inhibition under the influence of azelaic acid was also recorded in melanocytes, and this explains the depigmenting effect. In the context of preventing post-inflammatory pigmentation, characteristic of post-acne, the anti-inflammatory effect of azelaic acid is also important.

All these effects are useful for acne, so preparations with azelaic acid are used at different stages of this disease.

Pyruvic acid is a relatively new player in the acne therapy field. It is an α-keto analogue of lactic acid. Due to its low pH value and small size, pyruvic acid passes well through the stratum corneum. When applied topically, pyruvic acid exhibits keratolytic, bactericidal and sebostatic properties. In addition, it is also able to stimulate the formation of new collagen and elastin. Pyruvic acid is used in the treatment of dermatological problems such as acne, superficial scars, photodamage, and pigmentation disorders.

In this study, Polish experts compared the effectiveness of azelaic and pyruvic acid in the treatment of acne in 120 young women aged 20 to 24 years with mild to moderate acne that had been observed for at least 7 years. All participants were third-year students of the specialty “Cosmetology” at the Opole Medical School, and were randomized into 2 equal groups of 60 people.

In each group, 6 procedures were performed using azelaic and pyruvic acid, respectively, the interval between procedures was 2 weeks.

In the azelaic acid group, a solution containing 16% azelaic acid, 10% mandelic acid and 2% salicylic acid was applied first, and then 16% azelaic acid alone was applied twice (after the previous layer had dried). In the pyruvic acid group, a solution of 50% concentration with a pH of 0.8 was used, which was applied three times, left for about one minute each, and then neutralized. After the procedure, sunscreen was used. Home care during the 12 weeks of the study included only cleansing the skin with micellar water and subsequent application of a regenerating cream.

As a result, both groups showed comparable results in terms of reducing acne severity, but the pyruvic acid group showed a greater reduction in skin oiliness. No side effects were recorded.

The authors conclude that based on the results of their work, pyruvic acid can be recommended to patients with not only acne, but also the problem of severe oily skin.

You can read more about the difference between peeling agents and the peculiarities of their choice for the treatment of various conditions in the book from the series “My specialty is cosmetology,” “Chemical peeling in the practice of a cosmetologist.” And, of course, to everyone who is engaged in acne therapy or is looking for a solution to the problem for themselves, we strongly recommend our bestseller from the same series - “Oily skin, acne and post-acne in the practice of a cosmetologist.”

Source:

Chilicka K., Rogowska AM, Szyguła R., Dzieńdziora-Urbińska I., Taradaj J. A comparison of the effectiveness of azelaic and pyruvic acid peels in the treatment of female adult acne: a randomized controlled trial. Sci Rep 2020; 10(1): 12612.

Antimicrobial action18

According to research, azelaic acid has bacteriostatic and bactericidal activity against a large number of microorganisms, including S. epidermidis, P. acnes, S. aureus, P. granulosum, S. capitis, etc. Bacteria do not develop resistance to AK. In order for azelaic acid to exhibit its antibacterial properties, it must be used for at least 1 month.

The antimicrobial effect of AA is associated with the ability to change the pH level inside bacterial cells. Azelaic acid penetrates into the bacterial cell due to transmembrane ionophore proteins. The lower the pH, the better the absorption of AA by Propionibacterium acnes. Disruption of the transmembrane pH gradient negatively affects bacterial metabolism.

Self-use of azelaine peeling

  1. At home, azelaic acid is used in low concentrations - up to 15%.
  2. A preliminary consultation with a doctor is carried out to determine the type of procedure and identify possible allergic manifestations.
  3. The skin is cleansed and degreased with a glycolic acid-based tonic under sterile conditions.
  4. The delicate areas around the treated areas are protected with Vaseline.
  5. Azelaine peeling is rubbed into the skin with massage movements for 10 minutes, then washed off with chilled water.
  6. After the procedure, moisturizers are used and generally accepted post-care recommendations are followed.

Azelik® is a modern remedy for acne* on the face and body

Only a doctor can select an effective remedy for acne* on the face and body, and this is based on the characteristics of the course of the disease, the depth of the process, the prevalence of the rash, and the severity of the disease9.

Azelik® is a drug for acne* on the face and body, the main active ingredient of which is azelaic acid. The base includes auxiliary components5,7:

  • Emollient squalane. Its microdrops fill the space between the scales of the stratum corneum, which helps soften and moisturize the skin.
  • Dimethicone. This component is a hydrophobic solvent, which promotes better penetration of the drug.
  • N-methyl-pyrrolidone. Promotes better penetration of azelaic acid.

The remedy for acne* and acne on the face must be used twice a day - morning and evening. Azelik® is applied to clean and dry skin5.

*acne

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