Abstract

Plants with high amounts of antioxidants may be a promising therapy for preventing and curing UV-induced oxidative skin damage. The objective of this study was to verify the efficacy of topical formulations containing dissolved and suspended Silybum marianum extract against UVB-induced oxidative stress in guinea pig and HaCaT keratinocytes. Herbal extract was dissolved in Transcutol HP (TC) and sucrose-esters were incorporated as penetration enhancers in creams. Biocompatibility of compositions was tested on HeLa cells and HaCaT keratinocytes as in vitro models. Transepidermal water loss (TEWL) tests were performed to prove the safety of formulations in vivo. Drug release of different compositions was assessed by Franz diffusion methods. Superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPx) and lipid peroxidation (MDA) activities were evaluated before and after UVB irradiation in a guinea pig model and HaCaT cells. Heme oxygenase-1 (HO-1) enzyme activity was measured in the epidermis of guinea pigs treated by different creams before and after UVB irradiation. Treatment with compositions containing silymarin powder (SM) dissolved in TC and sucrose stearate SP 50 or SP 70 resulted in increased activities of all reactive oxygen species (ROS) eliminating enzymes in the case of pre- and post-treatment as well. Reduction in the levels of lipid peroxidation end products was also detected after treatment with these two compositions. Post-treatment was more effective as the increase of the activity of antioxidants was higher. Lower HO-1 enzyme levels were measured in the case of pre- and post-treatment groups compared to control groups. Therefore, this study demonstrates the effectiveness of topical formulations containing silymarin in inhibiting UVB irradiation induced oxidative stress of the skin.

Highlights

  • Silybum marianum (Milk thistle) is a well-known medicinal plant that has been used for centuries as a herbal medicine for the treatment of liver-related diseases [1]

  • Our results showed the was better from compositions containing sucrose stearate

  • Silymarin topical formulations containing different surfactants and penetration enhancers with high bioavailability were designed. These preparations showed higher antioxidant activity against UVB-induced oxidative stress in guinea pig and HaCaT cells as preand post-treatment compared to controls

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Summary

Introduction

Silybum marianum (Milk thistle) is a well-known medicinal plant that has been used for centuries as a herbal medicine for the treatment of liver-related diseases [1]. Flavonolignan and non-flavonolignan components were separated from the Silybum marianum complex by a high performance liquid chromatography/tandem mass spectrometry (HPLC-MS/MS) method [3]. The major bioactive flavonolignans include silychristins A and B, silydianin, silybin A and B, isosilybin A and B. Three additional components were detected and partly separated, presumably two silybin stereoisomers and one isosilybin stereoisomer [4]. These components possess a wide range of antioxidant, cell regenerating and anticancer effects in the case of peroral application. Several articles have dealt with the topical application of Silybum marianum extract, mainly on the protective effects of silymarin and silybin against UVB-induced skin damage [6]

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