卵磷脂纳米乳剂对皮肤的影响：短期细胞毒性MTT和BrdU研究，表面活性剂和添加剂对皮肤的渗透以及姜黄素的递送。,International Journal of Pharmaceutics

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卵磷脂纳米乳剂对皮肤的影响：短期细胞毒性MTT和BrdU研究，表面活性剂和添加剂对皮肤的渗透以及姜黄素的递送。
International Journal of Pharmaceutics ( IF 5.3 ) Pub Date : 2020-03-09 , DOI: 10.1016/j.ijpharm.2020.119209
Claudia Vater ₁ , Victoria Hlawaty ₂ , Patricia Werdenits ₂ , Małgorzata Anna Cichoń ₃ , Victoria Klang ₂ , Adelheid Elbe-Bürger ₃ , Michael Wirth ₂ , Claudia Valenta ₁

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表面活性剂是乳剂，洗发剂或沐浴露中的药物和化妆品制剂中的重要成分。由于传统的乳化剂（如十二烷基硫酸钠）因其对皮肤的刺激性而声名狼藉，因此人们正在研究天然存在的卵磷脂作为一种潜在的替代品。因此，制备了有和没有药物姜黄素的基于卵磷脂的纳米乳剂，以其伤口愈合特性而闻名，并根据其粒径，多分散指数（PDI）和ζ电位进行了表征，并与基于SDS的制剂进行了比较。使用两种不同的细胞活力测定法（BrdU和EZ4U），使用原代人角质形成细胞和成纤维细胞评估了所产生的空白纳米乳剂的体外毒性。进一步，我们使用结合的ATR-FTIR /胶带剥离实验研究了部署的表面活性剂和油组分的渗透曲线，并在胶带剥离-UV / Vis实验中证实了基于卵磷脂的纳米乳液将姜黄素递送至角质层的能力。所有制造的纳米乳剂均显示出250 nm以下的液滴尺寸，并具有令人满意的PDI和zeta电位值。用人类皮肤细胞进行的活力测定清楚地表明，基于卵磷脂的纳米乳剂优于基于SDS的制剂。ATR-FTIR测试表明，卵磷脂和油脂成分残留在角质层的表层，表明皮肤刺激的风险较低。离体胶带剥离实验表明，纳米乳液中所用的油的种类似乎影响姜黄素渗透至角质层的深度。

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Effects of lecithin-based nanoemulsions on skin: short-time cytotoxicity MTT and BrdU studies, skin penetration of surfactants and additives and the delivery of curcumin.

Surfactants are important ingredients in pharmaceutical and cosmetic formulations, as in creams, shampoos or shower gels. As conventional emulsifiers such as sodium dodecyl sulfate (SDS) have fallen into disrepute due to their skin irritation potential, the naturally occurring lecithins are being investigated as a potential alternative. Thus, lecithin-based nanoemulsions with and without the drug curcumin, known for its wound healing properties, were produced and characterised in terms of their particle size, polydispersity index (PDI) and zeta potential and compared to SDS- based formulations. In vitro toxicity of the produced blank nanoemulsions was assessed with primary human keratinocytes and fibroblasts using two different cell viability assays (BrdU and EZ4U). Further, we investigated the penetration profiles of the deployed surfactants and oil components using combined ATR-FTIR/tape stripping experiments and confirmed the ability of the lecithin-based nanoemulsions to deliver curcumin into the stratum corneum in tape stripping-UV/Vis experiments. All manufactured nanoemulsions showed droplet sizes under 250 nm with satisfying PDI and zeta potential values. Viability assays with human skin cells clearly indicated that lecithin-based nanoemulsions were superior to SDS-based formulations. ATR-FTIR tests showed that lecithin and oil components remained in the superficial layers of the stratum corneum, suggesting a low risk for skin irritation. Ex vivo tape stripping experiments revealed that the kind of oil used in the nanoemulsion seemed to influence the depth of curcumin penetration into the stratum corneum.

更新日期：2020-03-09

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