Bai, De, Chen, Haowei, Liu, Lijuan, Xiang, Nanxi, Zhang, Jichuan, Wu, Chengyu, Zhang, Jiaheng, and Wang, Fang
Ionic liquid microcapsules for the topical delivery of pterostilbene: Enhanced transdermal delivery and anti-wrinkle and skin brightening effects. [Display omitted] • In this study, we used a supramolecular solvent for microencapsulation, and successfully prepared a PTB-loaded ionic liquid microcapsule (denoted Mat-IL-MicCap@PTB), which effectively resolved the poor stability and low bioavailability of PTB. Further, transdermal experiments showed that the microcapsules improved the permeation and retention of the active component. In vitro experiments confirmed that the microcapsules reduced the irritation and side effects of PTB, and they not only achieved a lasting antioxidant effect but also inhibited the production of melanin, attenuated fine lines, and enhanced skin elasticity and health. Therefore, Mat-IL-MicCap@PTB is a feasible carrier for transdermal delivery and synergistic skin care, providing an effective strategy for improving the transdermal delivery of various dermatological drugs. • The particle size and polydispersity index (PDI) of Mat-IL-MicCap@PTB, as measured by DLS, were 154.5 ± 3.4 nm and 0.178, respectively, indicating that the obtained microcapsule had a uniform particle size distribution without aggregation into large particles. The encapsulation efficiency was found to be 99.7 ± 0.3 %. • Cell viability suggest that Mat-IL-MicCap@PTB has almost no harmful effect on healthy cells. Notably, the inhibitory effect of Mat-IL-MicCap@PTB on G361 cells was significantly greater than that of Free PTB, which is consistent with reported results for lipid nanoparticles and nanostructured lipid carriers. • The results of transdermal experiment showed that skin retention of Mat-IL-MicCap@PTB was higher than that of Free PTB at different time points. After 8 h of reaction, the skin retention of Mat-IL-MicCap@PTB was 7.7-times higher than that of Free PTB. • In addition, the use of Mat-IL-MicCap@PTB resulted in a significant increase in the UVA-induced type-I collagen content at concentrations of 0.0156%, 0.0313%, and 0.0625% (v/v). Notably, Mat-IL-MicCap@PTB increased the type-I collagen content in fibroblasts more significantly than Free PTB, indicating that the former has better anti-wrinkle and skin-tightening effects. • Clinical trials indicated that the synthesized Mat-IL-MicCap@PTB increased skin firmness and elasticity and inhibited wrinkle formation without adverse effects, such as irritation or toxicity to the skin. • In summary, it was concluded that Mat-IL-MicCap@PTB has high clinical safety and outstanding clinical efficacy in terms of antioxidant, anti-wrinkle, moisturizing, brightening, and repair properties. Pterostilbene (PTB) is a hydrophobic compound derived from plants in the Astragalus family. PTB possesses remarkable skin brightening and antioxidant properties. However, delivery methods for PTB require enhancement, and this can be achieved by formulating suitable carriers. In this study, we prepared ionic liquid microcapsules containing PTB by using a microencapsulation technique based on a matrine and cocinic acid ([Mat][Coc]) ionic liquid. The particle size of the microcapsules was 154.5 ± 3.42 nm, and the encapsulation efficiency was as high as 99.7 %. Further, the PTB-loaded ionic liquid microcapsules had good biocompatibility, enhanced skin retention (7.7-times higher than that of free PTB), and improved skin penetration without damaging the skin structure. Clinical testing with human subjects revealed that the microcapsule emulsion reduced fine lines and brightened skin tone. Therefore, PTB-loaded ionic liquid microcapsules have promise for use in cosmetic formulations and applications in transdermal drug delivery and efficacy enhancement. [ABSTRACT FROM AUTHOR]