Abstract

BackgroundHyperpigmentation is a skin disorder characterized by elevated production of melanin. Current treatment approaches mainly rely on the application of skin lightening chemicals, most of which have safety issues. Efficacy of delivery of the active ingredients to the target organ has also been a challenge. Transdermal based drug delivery platform has been shown to improve drug bioavailability, avoiding the hepatic first pass metabolism, decrease gastrointestinal side effects, and eventually enhance patient compliance.ResultsThis article explores the utilization of micellar transdermal delivery technology to improve skin penetration and efficacy of arbutin, a hyperpigmentation agent. The suppression efficacy of cellular melanin production versus cell viability of four active ingredients commonly used in skin lightening products, namely allantoin, arbutin, glycolic acid, and hyaluronic acid were first compared. Arbutin was selected for the micellar delivery studies base on its comparatively low cytotoxicity and better performance in reducing melanin production. Micellar Arbutin cream was formulated using Urah® proprietary micellar technology and was assessed for its cellular melanin suppression efficacy and skin penetration capacity.ConclusionThe results show that micellar arbutin cream improved both the delivery and cellular melanin suppression, suggesting that micellar transdermal delivery may have potential application in addressing hyperpigmentation skin disorders.Graphical abstractTransdermal delivery of arbutin with micelles for melanin production suppression.Electronic supplementary materialThe online version of this article (doi:10.1186/s13104-016-2047-x) contains supplementary material, which is available to authorized users.

Highlights

  • Hyperpigmentation is a skin disorder characterized by elevated production of melanin

  • Melanin suppression activity and cytotoxicity Allantoin, arbutin, glycolic acid, and hyaluronic acid were firstly compared for their suppression of melanin production in B16-F10 mouse melanoma cells

  • The daily imaging suggested that the lower melanin amounts observed for glycolic and hyaluronic acids were due to the decrease of cell viability (Additional file 1: Figure S2)

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Summary

Introduction

Hyperpigmentation is a skin disorder characterized by elevated production of melanin. Melanin formation in skin cells can be reduced or blocked by some chemicals which are the common active ingredients in skin lightening products [4, 5]. To reach the skin cells, the chemicals have to pass through the stratum corneum, which acts as highly resistant lipid barrier to penetration of foreign molecules into the skin [8]. In both the pharmaceutical and cosmetic fields, significant efforts have been put forth in attempts to overcome the barrier of the stratum corneum in order to deliver topically functional agents into the skin.

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