Nanoliposome Use to Improve the Stability of Phenylethyl Resorcinol and Serve as a Skin Penetration Enhancer for Skin Whitening
Huan Xia, Yan Tang, Rufei Huang, Jinlian Liang, Siying Ma, Derong Chen, Yuqing Feng, Yaling Lei, Qi Zhang, Yan Yang, Yadong Huang
Abstract
Phenylethyl resorcinol (PR) is a potent tyrosinase inhibitor and a cosmeceutical skin lightening agent. However, the application of PR is limited by photoinstability and poor solubility. In this study, we formulated and optimized phenylethyl resorcinol loaded nanoliposomes (PR-NLPs) to improve the stability and effective delivery of PR. PR-NLPs were prepared by the ethanol injection method and optimized by a single factor experimental and Box–Behnken design. In addition, Diethylamino Hydroxybenzoyl Hexyl Benzoate (DHHB) as the UBA absorber was added to PR-NLPs, which significantly improved the photostability of PR. The mean size, polydispersity index (PDI), and zeta potential of the optimized PR-NLPs were 130.1 ± 3.54 nm, 0.225 ± 0.02, and −43.9 ± 3.44 mV, respectively. The drug encapsulation efficiency (EE) and loading efficiency (LC) of PR-NLPs were 96.81 ± 3.46% and 8.82 ± 0.6%, respectively. These PR-NLPs showed good physicochemical stability for 3 months at 4 °C and 25 °C in the dark. They showed typical sustained and prolonged drug-release behavior in vitro. The in vitro cytotoxicity assay and cellular uptake demonstrated that the PR-NLPs had excellent biocompatibility and cell transport ability. It significantly inhibited tyrosinase activity and reduced melanin production in B16F10 cells at concentrations of 20 or 30 μg/mL. Moreover, the PR-NLPs enhanced the PR into the skin. These results indicate that PR-NLPs can be used as a nanocarrier to improve the transdermal delivery of PR.