Abstract

Phenylethyl resorcinol (4-(1-phenylethyl)1,3-benzenediol) (PR) is a new whitening agent that has been found to have the ability to inhibit tyrosinase activity. However, the application of PR is limited by photo instability and poor solubility. PR-loaded nanostructured lipid carriers (PR-NLCs) were prepared by the hot-melted ultrasonic method. Glycerol monostearate and olive oil were selected as the solid lipid and liquid lipid for considering the solubility of PR in liquid lipid and partition coefficient of PR in solid lipid, respectively. The particle size and polydispersity index of PR-NLCs were 57.9 ± 1.3 nm and 0.24 ± 0.01, respectively. The encapsulation efficiency and loading capacity of PR-NLCs were 93.1 ± 4.2% and 8.5 ± 0.4%, respectively. The stability test demonstrated that the incorporation of PR into NLCs conferred excellent physicochemical stability and photo stability for at least three months at 4 °C in the dark and 25 °C under daylight. In vitro release of PR-NLCs revealed a sustained release pattern. Cellular tyrosinase assay showed that PR-NLCs could significantly inhibit tyrosinase activity in melanoma cells, suggesting that NLCs can be used as a biocompatible nanocarrier for the effective delivery of skin whitening agents.

Highlights

  • Phenylethyl resorcinol (4-(1-phenylethyl)1,3-benzenediol) (PR) (Figure 1) is a new whitening agent that has been found to have the ability to inhibit tyrosinase activity [1]

  • Transmission was found thatElectron the addition of a liquid lipidAnalysis to a solid lipid leads to an increase in EE and loading capacity capacity (LC) because of minimizing the leak of images determined that PR-loaded nanostructured lipid carriers (PR-NLCs) are of spherical morphology and did not adhere to each

  • A gloom-like shadow could be seen around the particulate, possibly due to unevenly images determined that of PR-NLCs are of spherical morphology and dida not adhere to each to a groupdyeing of the leakMicroscopy of PR from (TEM)

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Summary

Introduction

Phenylethyl resorcinol (4-(1-phenylethyl)1,3-benzenediol) (PR) (Figure 1) is a new whitening agent that has been found to have the ability to inhibit tyrosinase activity [1]. It is a synthetic compound that is partially derived from natural lightening compounds found in Scotch pine bark. According to research, it is one of the highest tyrosinase inhibitors, 22 times more potent than kojic acid [2]. When directly compared to β-arbutin, PR was shown to be over 100 times as effective at lightening hair. It served as an antioxidant agent—better than vitamin E, vitamin C, and butylated hydroxytoluene. The poor water solubility may limit its absorption, while its photo instability may render the topically applied PR ineffective [3].

Structure
Screening
Determination
Transmission
Fourier-Transform
Stability Test
InNanomaterials
InaVitro
2.10. Cytotoxicity
2.11. Cellular Uptake Study
2.12. Cellular
Materialsand and Methods
Cell Cultures
Screening of Solid and Liquid Lipids
Preparation of PR-NLCs
Measurements of Particle Size and PDI
Determination of EE and LC
HPLC Analysis
TEM Analysis
FT-IR Analysis
3.10. DSC Analysis
3.11. XRD Analysis
3.12. Stability Test
3.13. In Vitro Release Study
3.14. Cytotoxicity Study
3.15. Cellular Uptake Study
3.16. Cellular Tyrosinase Inhibition Assay
Conclusions
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