Glycyrrhiza acid micelles loaded with licochalcone A for topical delivery: co-penetration and anti-melanogenic effect

Eur J Pharm Sci. 2021 Sep 30:106029. doi: 10.1016/j.ejps.2021.106029. Online ahead of print.ABSTRACTThe co-penetration of micellar vehicles and the encapsulated drugs into the skin layers, as well as the mechanisms underlying the penetration enhancement have not been clearly elucidated. We developed licochalcone A (LA)-loaded glycyrrhiza acid (GA) (GA+LA) micelles for topical delivery of LA into the epidermis. The in vitro release, in vitro co-penetration, penetration pathways, mechanism of interaction between skin and the micelles, and the in vitro and in vivo whitening effect of GA+LA micelles were evaluated. Co-penetration and penetration pathways were visualized on the abdominal skin of rats model with confocal laser scanning microscopy (CLSM) using a nile blue A-labeled GA (GA-NB). We found that GA significantly increased the transport of LA into the skin predominantly via the hair follicles and GA mainly accumulated in the SC and epidermis, while LA was localized in the epidermis and dermis. Moreover, 73.4% of the LA deposited into the epidermis within 12 h and approximately 9.32% of the LA permeated across the SC in the form of entire micelles within 24 h. GA-NB+LA micelles disaggregated and accumulated in the specific skin layers, and the LA released from the carrier penetrated into deeper layers. Moreover, the GA+LA micelles promoted drug penetration via intracellular or intercellular routes by loosening the skin surface and enhancing fluidization through lipid disto...
Source: European Journal of Pharmaceutical Sciences - Category: Drugs & Pharmacology Authors: Source Type: research