Abstract
Phenylethyl Resorcinol (PR) is a cosmeceutical skin lightening agent and the purpose of this study was to enhance its stability by using liposomal cream formulation which increases local efficacy and safety. Liposome formulation was prepared by modified ethanol injection method, and it contained soy phosphatidyl choline (SPC), cholesterol (CHO), Tween 80 (TW80) and deoxycholic acid (DA) mixed with 2% PR. The physicochemical properties, skin permeation as well as cellular study were evaluated in order to obtain the optimized formulation. The optimized liposome formulation composed of SPC:TW80:DA (84:16:2.5) and exhibited vesicle size, polydispersity index (PDI) and zeta potential of 286.4±8.04 nm, 0.317±0.03 and -39.20±3.85 mV, respectively. Entrapment efficiency (EE) of liposome formulation was 93.55±0.05%. The vesicle was spherical in shape and showed good physicochemical stability for 4 months. The skin permeation study demonstrated that liposome with a negative charge could result in a high PR skin deposition value of 1732.76±216.24 µg/cm2 after 24 h. Cellular study showed that liposome formulation could inhibit melanin content in B16 melanoma cells and enhance cell viability in HaCaT keratinocyte cells. The optimized PR liposome was incorporated in cream and investigated physicochemical properties, stability and skin permeation. Liposomal PR cream showed a good stability and a superior result than PR cream in skin permeation parameters, as well as in tyrosinase inhibition.
Highlights
Skin pigmentation is a physiological defense against ultraviolet radiation (UVR) and it results in the production and distribution of melanin in epidermis [1,2]
Phenylethyl Resorcinol (PR) is a cosmeceutical skin lightening agent and the purpose of this study was to enhance its stability by using liposomal cream formulation which increases local efficacy and safety
In this study 16 liposome formulations were prepared in different compositions
Summary
Skin pigmentation is a physiological defense against ultraviolet radiation (UVR) and it results in the production and distribution of melanin in epidermis [1,2]. UVR which has specific wavelengths can be divided into 3 types including UVA, UVB and UVC [3]. UVB (280-320 nm) can penetrate into the epidermis and cause skin redness associated with sunburn. UVA (320-400 nm) can penetrate much deeper into the skin and can cause damage to the skin, such as photo aging, skin pigmentation and melasma [4]. Upon exposure to UVR, melanogenesis is increased by activation of the key enzyme tyrosinase, which stimulates melanin production. Melanin can be found in 2 different types; yellow or red (pheomelanin) and brown or black (eumelanin) [5]. Inhibiting tyrosinase activity has generated much interest in several studies
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