Nikoo™ AXA molecular capsule inclusion compounds refer to inclusion bodies formed by a (drug) molecule being embedded in the cavity structure of another substance molecule (composition), or "molecular capsules". Molecular capsule technology has the advantages of increasing the solubility and dissolution of drugs, covering up the bad smell of drugs and reducing irritation, improving the stability of drugs, and preparing sustained-release preparations.
Nikoo™ AXA molecular capsules are solutions provided by Shumei New Materials for the application problems of azelaic acid using molecular capsule technology. They have the characteristics of good solubility, high utilization rate and low irritation.
The solubility in water at room temperature is more than 20% (zelaic acid effective concentration > 3.0%), and the solubility is significantly improved compared with the traditional method of using azelaic acid.
Nikoo™ AXA molecular capsules with special process packaging solve the solubility problem of the raw material itself, and are suitable for application in multi-scenario products. While ensuring the original efficacy of the product, it also increases the stability of the product system. There is no risk factor data yet, and the normal addition amount generally has no effect on pregnant women.
Anti-acne and antibacterial
Whitening and anti-freckle
Oil control and skin conditioning
Azelaic acid, commonly known as azelaic acid, is a skin care ingredient that dermatologists love. It has many functions such as acne removal, oil control, anti-inflammatory, and whitening, but azelaic acid has a high melting point (109-111 ℃) and low solubility (0.24% solubility in 25℃ water; oil solubility is not good). At present, the application method of azelaic acid includes dissolving it in the oil phase and emulsifying it into a cream after adding an emulsifier. Most of the azelaic acid will re-precipitate and remain on the surface of the skin, unable to be absorbed and effective, and will feel sticky and heavy on the skin, affecting the skin feel; another method of use is to dissolve azelaic acid in an alkaline solution (sodium hydroxide, potassium hydroxide, etc.), and it exists in the solution in the form of potassium azelate, sodium azelate and other ions, which cannot pass through the skin barrier, and the utilization rate of azelaic acid is not high.
The anti-inflammatory mechanism of azelaic acid:
• Inhibits the formation and release of reactive oxygen species, scavenges hydroxyl free radicals and superoxide;
• Inhibits CD36 (fatty acid transporter) and NADPH oxidase (Nox, an enzyme protein that regulates cellular ROS synthesis), ultimately inhibiting MAPK/NF-κB;
• Inhibits the transport of MARK p38 protein kinase and NF-κB;
• Stimulates the expression of PPAR-γ (peroxisome proliferator-activated receptor), thereby inhibiting the transport of NF-κB;
• Inhibits kallikrein 5 (KLK5) in keratinocytes to inhibit antimicrobial peptides, thereby inhibiting the production of pro-inflammatory cytokines and alleviating inflammatory responses.
However, the reactions at the microscopic level are always a bit abstract... Back to real life, the ultimate effect of the above reactions can be reflected in: inhibiting the inflammatory response caused by ultraviolet rays, alleviating the inflammatory response in the clinical treatment of rosacea, etc.
As a broad-spectrum antibacterial solution, azelaic acid has a better bactericidal effect than antibiotics. Some bacteria have shown resistance to antibiotics, but so far azelaic acid has not been found to cause resistance and is effective against methicillin-resistant Staphylococcus aureus.
In fact, the bactericidal mechanism of azelaic acid determines that it is difficult to cause resistance: azelaic acid can enter the bacterial cytoplasm, reduce the intracellular pH value, affect the pH gradient inside and outside the cell membrane, and thus inhibit the synthesis of DNA and protein in the cell.
In clinical trials, topical azelaic acid can significantly reduce the number of Staphylococci and Propionibacterium on the skin surface and in hair follicles.
Whitening effect (difference between azelaic acid and salicylic acid):
Salicylic acid assists in whitening by metabolizing keratin; azelaic acid can directly inhibit melanin production;
Acne treatment effect (difference between azelaic acid and salicylic acid):
Salicylic acid focuses on exfoliation and anti-inflammatory, and is more suitable for acne-type acne, or long-term use to prevent excessive oil, closed comedones, blackheads and other problems; azelaic acid performs very well in sterilization, anti-inflammatory, and oil control, especially the strong sterilization effect is better, and is more suitable for controlling inflammatory red and swollen acne.
References:
1、Clinical studies of 20% azelaic acid cream in the treatment of acne vulgaris. Comparison with vehicle and topical tretinoin. Katsambas A, Graupe K, Stratigos J. Acta Derm Venereol Suppl (Stockh). 1989;143:35-92、Farshi MD, M. (2011). Comparative study of therapeutic effects of 20% azelaic acid and hydroquinone 4% cream in the treatment of melasma. Journal of Cosmetic Dermatology, 10(4).3、Sieber, M., & Hegel, J. (2014). Azelaic acid: Properties and mode of action. Skin Pharmacology and Physiology, 27, 9-17. doi:10.1159/000354888