ROS Response Lipid-Coated Hollow Mesoporous Silica Nanoparticles Loading Glabridin for Anti-Pigmentation

Glabridin is one of the most effective whitening agents for treatment of skin pigmentation, while its poor solubility, and instability limit its cosmetic exploitation. In this paper, to efficiently enhance transdermal delivery and anti-pigmentation, a novel ROS-responsive delivery device by integrating the cell penetrating peptide polyarginine-R8 and ROS-responsive thioether phosphatidylcholines (T-PCs) within lipid-coated hollow mesoporous silica nanoparticles (HMSNs) with amino groups inside has been designed, in which whitening agent Glabridin could be controllably released by ROS-trigger. The nanocarrier (Glabridin@HTLB-R8) is prepared by modifying HMSNs with amino groups to enhance the loading of Glabridin, followed by envelop of T-PCs-grafted lipid bilayer which act as ROS-responsive trigger for controlling drug release. In vitro , Glabridin@HTLB-R8 rapidly penetrated into keratinocytes and melanocytes and exhibited the strongest photoprotection and anti-pigmentation activity. And in vivo experiments demonstrated that this novel ROS-responsive nanocarriers loading Glabridin achieve significant improvement hyperpigmentation via inhibiting tyrosinase and scavenging reactive oxygen species. This study provides a promising platform for the design and fabrication of multifunctional nanoparticles, which is potentially useful for cosmetic industry.