Shiseido Develops New Ingredients That Dramatically Improve Skin Penetration of Drugs

 Shiseido has developed the world's first infusion-promoting ingredient that dramatically increases the penetration rate of drugs while also ensuring skin safety by applying the phenomenon in which normally solid substances interact with specific molecules to liquefy. Developed. In order to quickly penetrate the drug to the target site of action in the skin, it was necessary to lower the barrier function of the skin, and there was an issue with safety on the skin. However, by utilizing the introductory component developed this time, it has become possible to efficiently penetrate the drug while maintaining safety. Some of the results of this research were presented at the 32nd International Federation of Cosmetic Engineers Association London 2022.

This research was conducted with the approach of "Functionality/Japan Quality" of Shiseido's unique R&D philosophy "DYNAMIC HARMONY". With the newly developed introductory ingredient, we aim to realize functional and effective skin care products with excellent permeability as well as high quality that pursues gentleness to the skin.

In recent years, one of the expectations of customers has been the realization of the extremely high effectiveness of quasi-drugs. In order to achieve this goal, we are working day and night to develop unique ingredients and research into active ingredients, and our strength lies in the field of drug development. However, in order to further increase its value, we believe that it is also important to strengthen the technology to quickly deliver more of the active ingredients to the target areas deep in the skin.

On the skin surface, there is a layer that has a high affinity for oil and has the property of repelling water. On the other hand, many of the agents used in cosmetics are designed to have a high affinity with the base water, so they repel water. Due to its nature, it is difficult to penetrate the skin, and drug introduction accelerators have been developed for some time. The introduction enhancer promotes the penetration of the drug, but on the other hand, it has a surfactant-like structure and properties, so it penetrates the stratum corneum and lowers the lipid barrier function, and further penetrates deep into the skin. Problems such as the transduction promoter damaging cells remained unsolved.

In developing a new introduction accelerator, we focused on a new type of liquid called an "ionic liquid," which becomes liquid at a temperature lower than the melting point of the original substance by combining substances with high melting points. Alkylbetaine, which is commonly used as an introduction accelerator, was combined with various substances, and after examining more than 100 combinations and their blending ratios, it was found that the combination of alkylbetaine and xylitol liquefied. Furthermore, an excellent permeation promotion effect into the skin was recognized. Next, we evaluated the penetration promoting effect of 4MSK, a whitening agent, using human skin.

Next, we investigated how to not only enhance the penetration promotion effect of the drug, but also improve the safety of the skin. Xylitol covers part of the structure of substances that are generally thought to damage skin cells, thereby mitigating damage to cells. The stimulating component AB/XY complex was exposed to living skin cells and cell viability was observed. Despite the fact that the experiment was conducted under experimental conditions in which it was difficult for cells to survive with the transduction promoter alone, the number of cells that lost mitochondrial activity even after exposure to the new transduction promoter AB/XY complex complex was small.