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

Zhuxian Wang, Yaqi Xue, Tingting Chen, Qunqun Du, Zhaoming Zhu, Yuan Wang, Yufang Wu, Quanfu Zeng, Chunyan Shen, Cuiping Jiang, Zhijun Yang, Hongxia Zhu, Li Liu*, Qiang Liu*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

5 Citations (Scopus)

Abstract

The 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 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 distortion and keratin denaturation. Furthermore, GA+LA micelles exhibited synergistic whitening effect on B16 cells and UVB-exposed C57BL/6 mice. Collectively, GA micelles can enhance penetration of LA to the epidermis mainly via the hair follicles following topical application, and reduce skin pigmentation.

Original languageEnglish
Article number106029
Number of pages13
JournalEuropean Journal of Pharmaceutical Sciences
Volume167
Early online date30 Sep 2021
DOIs
Publication statusPublished - 1 Dec 2021

Scopus Subject Areas

  • Pharmaceutical Science

User-Defined Keywords

  • Co-penetration
  • Glycyrrhiza acid micelles
  • Hair follicles
  • Mechanism of penetration enhancement
  • Topical delivery

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