The University of South Australia, School of Pharmacy and Medical Sciences, Adelaide, Australia.
The University of South Australia, Future Industries Institute, Adelaide, Australia.
Toxicol Appl Pharmacol. 2018 Mar 15;343:40-47. doi: 10.1016/j.taap.2018.02.012. Epub 2018 Feb 20.
Zinc pyrithione is an active component incorporated in an extensive range of topically applied commercial products that are used worldwide. Despite its prevalence, no published study has investigated the penetration of zinc from the zinc pyrithione complex into human skin. Zinc is crucial for healthy skin function however an elevated concentration of labile zinc is toxic outside a narrow concentration range. Synchrotron X-ray fluorescence microscopy in conjunction with X-ray absorption near edge structure spectroscopy was used to map the deposition of zinc, quantitate the amount of zinc within the skin and to identify a change in the chemical form of zinc after application. This study has demonstrated a ~3.8 fold increase in zinc concentration within the viable epidermis (VE) after 24 h topical application of zinc pyrithione that increased significantly by ~250 fold after 48 h when compared to control skin. Confocal microscopy using a labile zinc specific dye, ZinPyr-1, showed that zinc pyrithione disrupted the skin cells zinc homeostasis and significantly increased the intracellular zinc concentration leading to cell toxicity. Overall, this study demonstrates that topical application of zinc pyrithione formulations leads to an increase in zinc penetration in human skin, consequently, raising concerns for potential localised toxicity to occur.
吡啶硫酮锌是一种广泛应用于各种局部用商业产品的活性成分，在全球范围内使用。尽管它很普遍，但没有发表的研究调查过锌从吡啶硫酮锌复合物渗透到人体皮肤中。锌对皮肤健康功能至关重要，但在狭窄的浓度范围内，不稳定的锌浓度升高是有毒的。同步加速器 X 射线荧光显微镜结合 X 射线吸收近边结构光谱用于绘制锌的沉积图，定量测定皮肤内的锌含量，并确定应用后锌化学形态的变化。这项研究表明，在 24 小时局部应用吡啶硫酮锌后，活表皮（VE）中的锌浓度增加了约 3.8 倍，与对照皮肤相比，48 小时后锌浓度增加了约 250 倍。使用一种不稳定的锌特异性染料 ZinPyr-1 的共焦显微镜显示，吡啶硫酮锌破坏了皮肤细胞的锌内稳态，并显著增加了细胞内锌浓度，导致细胞毒性。总的来说，这项研究表明，局部应用吡啶硫酮锌制剂会导致锌在人体皮肤中的渗透增加，因此，人们担心会发生局部毒性。
