Nanoliposome Use to Improve the Stability of Phenylethyl Resorcinol and Serve as a Skin Penetration Enhancer for Skin Whitening

Huan Xia,Siying Ma,Jinlian Liang,Yadong Huang,Derong Chen,Yaling Lei,Yan Yang,Yuqing Feng,Qi Zhang,Rufei Huang,Yan Tang

doi:10.3390/coatings12030362

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.

Highlights

Introduction iationsWhitening is a goal that most people have been pursuing, especially Asians
The mean size and encapsulation efficiency of liposomes are influenced by lecithin, cholesterol, phenylethyl resorcinol, the volume ratios of nonsolvent and solvent volume ratios, and Tween 80
We successfully developed a nanoliposome to facilitate the delivery of Phenylethyl resorcinol (PR)

Summary

Introduction

Whitening is a goal that most people have been pursuing, especially Asians. According to Global Industry Analysts, Inc (GIA), the global market for skin whitening agents will reach $23 billion by 2020 [1], which will make whitening cosmetics become the focus of attention of cosmetics companies. Various inhibitors of melanogenesis-related enzymes have been identified for whitening effects and the control of skin pigmentation in the medicine and cosmetic industries. Melanin is the primary pigment responsible for the color of human skin. Melanogenesis is a process in which melanin is produced within melanocytes and subsequently transferred to adjacent keratinocytes to protect keratinocytes from UV light [2]. Overproduced melanin leads to various skin pathological problems, such as chloasma, age spots, freckles, and pigmentation caused by inflammation [3]

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Results

Conclusion