Department of Pharmaceutical Sciences, Università degli Studi di Milano, Via G. Colombo 71, 20133, Milan, Italy.
Drug Deliv Transl Res. 2018 Apr;8(2):414-421. doi: 10.1007/s13346-017-0390-7.
The use of nanoemulsions in cosmetic products has been enlarged in the last decades because of several formulative advantages (e.g., the improved self-life stability, better texture properties). In addition, nanoemulsions seemed to improve the penetration of active ingredients through the human skin, comparing to conventional emulsion. In this contest, the risk of a higher systemic exposure of consumer to active ingredients, due to the ability of nanoemulsion to enhance permeation, results a critical attribute that should be evaluated for assuring the consumer safety. The aim of this work was the evaluation of how an oil-in-water (O/W) nanoemulsion can influence the in vitro skin permeation profiles of two model active ingredients with different polarity (i.e., caffeine and ethyl ximenynate). Preliminarily, since both selected molecules influenced the physical stability of nanoemulsion, formulative studies were carried out to identify the most stable formulation to perform in vitro permeation studies. The overall results demonstrated that nanoemulsions could significantly influence the permeation profiles of molecules as a function of their physicochemical properties. In particular, O/W nanoemulsions significantly improved the permeation profiles of apolar active ingredients in comparison to conventional emulsions, whereas no differences were observable for polar molecules. Considering such findings, it is worth observing that there is room for reconsidering the risk assessment of nanoemulsion-based cosmetic products.
在过去的几十年中,由于具有许多制剂优势(例如,改善了自保质期稳定性,更好的质地特性),纳米乳液在化妆品产品中的使用得到了扩大。此外,纳米乳液似乎比常规乳液更能促进活性成分渗透人体皮肤。在这种情况下,由于纳米乳液增强渗透的能力,消费者接触活性成分的全身暴露风险更高,这是一个关键属性,需要进行评估以确保消费者安全。本工作的目的是评估水包油(O/W)纳米乳液如何影响两种具有不同极性的模型活性成分(即咖啡因和乙基丁香酚)的体外皮肤渗透曲线。初步研究表明,由于所选的两种分子均会影响纳米乳液的物理稳定性,因此进行了制剂研究以确定最稳定的配方来进行体外渗透研究。总体结果表明,纳米乳液可以根据其物理化学性质显著影响分子的渗透曲线。特别地,与常规乳液相比,O/W 纳米乳液显著改善了非极性活性成分的渗透曲线,而极性分子则没有观察到差异。考虑到这些发现,值得观察的是,有必要重新考虑基于纳米乳液的化妆品产品的风险评估。