Abstract

The skin-whitening agent, deoxyArbutin, is a potent tyrosinase inhibitor that is safer than hydroquinone and arbutin. However, it is thermolabile in aqueous solutions, where it decomposes to hydroquinone. Pharmaceutical and cosmetic emulsions are normally oil-in-water (o/w) or water-in-oil (w/o) systems; however, emulsions can be formulated with no aqueous phase to produce an anhydrous emulsion system. An anhydrous emulsion system could offer a stable vehicle for compounds that are sensitive to hydrolysis or oxidation. Therefore, to enhance the stability of deoxyArbutin in formulations, we chose the polyol-in-silicone, anhydrous emulsion system as the basic formulation for investigation. The quantity of deoxyArbutin and the accumulation of hydroquinone in both hydrous and anhydrous emulsions at various temperatures were analyzed through an established high performance liquid chromatographic (HPLC) method. The results indicated that water increased the decomposition of deoxyArbutin in the formulations and that the polyol-in-silicone, oil-based, anhydrous emulsion system provided a relatively stable surrounding for the deoxyArbutin that delayed its degradation at 25 °C and 45 °C. Moreover, the composition of the inner hydrophilic phase, containing different amounts of glycerin and propylene glycol, affected the stability of deoxyArbutin. Thus, these results will be beneficial when using deoxyArbutin in cosmetics and medicines in the future.

Highlights

  • IntroductionThe biosynthesis of melanin in melanocytes might be affected by cellular tyrosinase activity [1,2]

  • Tyrosinase is an enzyme with a copper center that is widely expressed in many life forms and is mainly involved in the formation of pigments, such as melanin and other polyphenolic compounds.The biosynthesis of melanin in melanocytes might be affected by cellular tyrosinase activity [1,2]

  • We used an established high performance liquid chromatographic (HPLC) method to confirm the quantity of deoxyArbutin and hydroquinone in these formulations at various temperatures

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Summary

Introduction

The biosynthesis of melanin in melanocytes might be affected by cellular tyrosinase activity [1,2]. Investigation into depigmentation mechanisms and the clinical aspects of skin whitening agents is very important [3,4]. Various compounds have demonstrated inhibitory effects on melanogenesis through inhibition of the enzymatic activity of tyrosinase [5,6,7]. Hydroquinone (Figure 1A) and deoxyArbutin (dA; Figure 1B) are both potent skin-whitening agents that are capable of suppressing the function of tyrosinase. DeoxyArbutin (4-[(tetrahydro-2H-pyran-2-yl)oxy]phenol) was first shown by Boissy et al to exhibit greater inhibition of tyrosinase activity and to be safer than hydroquinone and arbutin [8]. Enhancing the stability of this skin-whitening agent is important for its development

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