Characterization and topical delivery of phenylethyl resorcinol.

Abstract

Phenylethyl resorcinol (PR) has been used widely in the personal care industry as a novel skin lightening ingredient. Surprisingly, there is only limited information describing the physicochemical properties of this active. Therefore, the primary objective of this study was to perform a comprehensive characterization of PR. A secondary objective was to investigate the delivery of this molecule to mammalian skin. Phenylethyl resorcinol was characterized using differential scanning calorimetry (DSC), thermogravimetric analysis (TGA) and nuclear magnetic resonance (NMR). A new high-performance liquid chromatographic (HPLC) method for analysis of PR was developed and validated. The log P (octanol water partition coefficient), value, solubility and short-term stability of PR in a series of vehicles were also determined using HPLC. The evaporation of the selected vehicles was examined using dynamic vapour sorption (DVS). The permeation profiles of PR were investigated under finite dose conditions in porcine and human skin. The melting point of PR was determined to be 79.13°C and the measured log P (octanol water partition coefficient) at 21°C was 3.35±0.03. The linearity of the HPLC analytical method was confirmed with an r2 value of 0.99. Accuracy of the method was evaluated by average recovery rates at three tested concentrations, and the values ranged from 99 to 106%. The limit of detection (LOD) and limit of quantification (LOQ) were 0.19 and 0.57μgmL-1 , respectively. The solubility of PR in PG, DMI, glycerol was within the range of 367 to 877mgmL-1 . The stability of PR in tested solvents was also confirmed by the 72h stability studies. From the DVS studies, 70-125% of applied formulations were recovered at 24h. The permeation through porcine skin at 24h ranged from 4 to 13μgcm-2 , while the corresponding amounts of PR delivered through human skin were 2 to 10μgcm-2 . The physicochemical properties of PR confirm it is suitable for dermal delivery. In this study, propylene glycol was the most promising vehicle for PR delivery to human skin. Future work will expand the range of vehicles studied and explore the percutaneous absorption from more complex formulations.