Patil S, Singh P, Sarasour K, Maibach H
Department of Dermatology, School of Medicine, University of California, San Francisco 94143, USA.
J Pharm Sci. 1995 Oct;84(10):1240-4. doi: 10.1002/jps.2600841018.
Sodium lauryl sulfate (SLS) is known to penetrate skin and cause cutaneous irritation. Some of these effects have been well-defined using bioengineering techniques. In this study, the ability of SLS to penetrate skin was quantified in a hairless rat model. In addition, local deep tissue penetration and systemic exposure to SLS were also evaluated to assess the toxic potential of topically applied SLS. SLS was observed to penetrate directly to a depth of about 5-6 mm below the applied site. Systemic redistribution was predominantly responsible in determining concentrations of SLS in tissues deeper than 5-6 mm. Epidermal concentrations of SLS after application of 1% (34 mM) aqueous SLS solution for 24 h were above the threshold levels which are known to evoke typical skin irritation responses. Deeper underlying tissues including dermis, subcutaneous, and muscle may also be exposed to high levels of SLS. Topically applied SLS was also observed in blood and contralateral tissues but the observed levels were not likely to elicit any systemic side effects at these doses. Traces of SLS were observed in tissues 7 days after single 24 h application of SLS, which supports the prolonged barrier disruption data generated using conventional bioengineering techniques. Cumulative treatment of SLS significantly increased the concentration of this compound in the underlying epidermis. The known preferential affinity of SLS for skin lipids and proteins was further confirmed by both in vitro and in vivo results. However, in vitro studies failed to predict the underlying tissue toxicity of SLS under the patch site when compared to the in vivo results. Such quantitative pharmacokinetic-pharmacodynamic correlations may be useful predictors for effective use of surfactants as penetration enhancers in cosmetic, pharmaceutical, and industrial applications.
月桂醇硫酸酯钠(SLS)已知可穿透皮肤并引起皮肤刺激。其中一些影响已通过生物工程技术得到明确界定。在本研究中,在无毛大鼠模型中对SLS穿透皮肤的能力进行了量化。此外,还评估了局部深层组织渗透和全身暴露于SLS的情况,以评估局部应用SLS的潜在毒性。观察到SLS直接穿透至涂抹部位下方约5 - 6毫米的深度。全身再分布在决定深度超过5 - 6毫米的组织中SLS的浓度方面起主要作用。在涂抹1%(34 mM)的SLS水溶液24小时后,表皮中SLS的浓度高于已知会引发典型皮肤刺激反应的阈值水平。更深层的底层组织,包括真皮、皮下组织和肌肉,也可能暴露于高水平的SLS中。在血液和对侧组织中也观察到了局部应用的SLS,但在这些剂量下观察到的水平不太可能引发任何全身副作用。在单次24小时应用SLS 7天后,在组织中观察到了痕量的SLS,这支持了使用传统生物工程技术产生的屏障破坏持续时间的数据。SLS的累积处理显著增加了该化合物在底层表皮中的浓度。体外和体内结果进一步证实了SLS对皮肤脂质和蛋白质已知的优先亲和力。然而,与体内结果相比,体外研究未能预测贴片部位下方SLS对底层组织的毒性。这种定量的药代动力学 - 药效学相关性可能是在化妆品、制药和工业应用中有效使用表面活性剂作为渗透促进剂的有用预测指标。