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无乳化剂乳液递送咖啡因和 α-生育酚至人体皮肤的效率。

Efficiency of emulsifier-free emulsions in delivering caffeine and α-tocopherol to human skin.

机构信息

EA 6295 Nanomédicaments et Nanosondes, Université de Tours, Tours, France.

GENIALIS, Henrichemont, France.

出版信息

Int J Cosmet Sci. 2023 Jun;45(3):329-344. doi: 10.1111/ics.12837. Epub 2023 Mar 29.

Abstract

OBJECTIVE

Increasing consumer demand for natural and environmentally friendly products is driving the cosmetic industry to seek greener and safer processes. High-frequency ultrasound technology (HFUT) stabilizes emulsions without adding emulsifying surfactants (ES). In this work, the formulation characteristics of an HFUT-treated emulsion and a Reference emulsion were compared for both caffeine and α-tocopherol.

METHODS

A comparison was made between ES-free emulsions and the Reference emulsions based on droplet size, viscosity, pH and rheology behaviour for both active cosmetic ingredients. The permeation of caffeine and the skin retention of α -tocopherol were studied in vitro using Franz diffusion cells on human skin biopsies, considered the gold standard for permeation assays.

RESULTS

The formulations developed were stable and showed suitable droplet size distribution. In the case of ES-free emulsions, the average droplet size was inferior to 1.5 μm regardless of the polarity of the active. All formulations presented a shear-thinning pseudoplastic behaviour, an attribute usually desired for cosmetic products. The skin permeation studies showed that in the case of caffeine (model hydrophilic molecule), the ES-free emulsion presented a delivery capacity similar to that of the Reference emulsion. However, for α-tocopherol (highly lipophilic model molecule), differences were observed in the distribution of the active in the stratum corneum with an advantage for the Reference emulsion, probably due to the impact of surfactants on the SC lipids.

CONCLUSION

This work demonstrates that HFUT is a reliable tool that is able to prepare stable ES-free emulsions loaded with hydrophilic or lipophilic active ingredients. Skin permeation studies confirm that the emulsions produced by HFUT promote the delivery of the actives to the human skin. In the case of α-tocopherol, the delivery efficiency was lower than with the Reference emulsion, especially in the SC layers, due to the absence of surfactants. Nevertheless, the ES-free emulsion still represents a good compromise between efficacy and the need for green cosmetics in the market.

摘要

目的

消费者对天然和环保产品的需求不断增加,推动着化妆品行业寻求更绿色、更安全的工艺。高频超声技术(HFUT)可以在不添加乳化剂(ES)的情况下稳定乳液。在这项工作中,比较了 HFUT 处理的乳液和参考乳液的配方特性,分别针对咖啡因和 α-生育酚这两种活性成分。

方法

比较了无 ES 乳液和参考乳液在两种活性成分的粒径、粘度、pH 值和流变行为方面的差异。使用Franz 扩散细胞在人体皮肤活检上进行体外渗透实验,以评估咖啡因的渗透和 α-生育酚在皮肤中的保留情况,皮肤活检被认为是渗透实验的金标准。

结果

所开发的配方是稳定的,且表现出适宜的粒径分布。对于无 ES 乳液,无论活性成分的极性如何,平均粒径都小于 1.5μm。所有配方均表现出剪切稀化的假塑性行为,这是化妆品产品通常所期望的特性。皮肤渗透研究表明,对于咖啡因(模型亲水分子),无 ES 乳液的递送能力与参考乳液相似。然而,对于 α-生育酚(高亲脂性模型分子),在角质层中活性物质的分布存在差异,参考乳液具有优势,这可能是由于表面活性剂对 SC 脂质的影响。

结论

这项工作表明,HFUT 是一种可靠的工具,能够制备稳定的、负载亲水或亲脂性活性成分的无 ES 乳液。皮肤渗透研究证实,HFUT 制备的乳液能够促进活性物质向人体皮肤的递送。对于 α-生育酚,递送效率低于参考乳液,尤其是在 SC 层,这是由于缺乏表面活性剂。然而,无 ES 乳液在市场对功效和绿色化妆品的需求之间仍然是一个很好的折衷方案。

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