Production of drugs that meet the requirements of medicine is developed dynamically and rapidly. Modern pharmacological technologies are aimed at creating drugs with the highest efficacy and safety. Improvement of therapeutic results is achieved via enhancement of the physicochemical properties of drugs. The development of new technologies is associated with more focus on micronization and nanonization of insoluble substances, which enables their transformation to micro- and nanoparticles, thereby increasing solubility of drugs and their permeability through tissue barriers. Now, the most effective method of pharmaceutical micronization is rapid expansion of supercritical solutions (RESS). The efficacy of micronized drugs has been studied in detail by Russian and foreign scientists. The micronization method is widely used in production of drugs for application in various fields of medicine, including topical application in the treatment of dermatological diseases and in cosmetology. Micronization not only increases solubility of a substance but also enhances stability of drugs, which has been demonstrated for retinoids. Acne therapy uses topical preparations represented by micronized azelaic acid, which has certain advantages. Azelaic acid is mainly used to treat acne vulgaris. This is associated with the fact that the acid exhibits pronounced antibacterial, anti-inflammatory, and antiproliferative activities against the main factors of acne pathogenesis and lacks significant adverse reactions typical of other anti-acne drugs. A gel formulation of azelaic acid has been developed whose physicochemical and biological properties as well as quality indicators confirm the rationality of a selected composition for achieving the objective of the present invention and solving the problem of active substance stability. The review presents current literature data on the use of a contemporary micronization technology in the pharmaceutical industry of azelaic acid-based topical drugs for dermatology and cosmetology. The review describes the results of domestic and foreign studies on the development and use of micronized azelaic acid in treatment of acne.