The targeted delivery of a hydrophilic Tripeptide-3 to the skin using microemulsions or nanoemulsions for facial oil reduction was the focus of this study. The impact factors affecting oil/water transparent dispersion formation, such as the surfactant system, HLB value, and co-solvent, were identified through the water titration method and pseudoternary phase diagram plots. The interfacial tension between caprylic/capric triglyceride (CCT oil) and water was significantly reduced by the surfactant/co-surfactant combination (Smix) of Cremophore® RH40 and a double-tails co-surfactant, polyglycerol-3-diisostearate, at an HLB of 13 together with a water-to-co-solvent (PG) ratio of 1:1. A two-level full factorial design of experiment (FFD-DoE) emphasized the independent variables of the HLB value, co-solvent, and CCT oil contents affecting the optimal compositions for micro- or nanoemulsion formation. The low-energy spontaneous emulsification of the optimized combination at a low Smix content (10%) yielded the translucent oil-in-water Tripeptide-3 nanoemulsions with an internal droplet size of 25.7 ± 1.20 nm, a narrow polydispersity index of 0.237 ± 0.129, and 70.6 ± 0.58% transmittance. The in vitro skin permeation study revealed a significantly higher skin penetration and retention of the Tripeptide-3 nanoemulsions compared to the high surfactant microemulsions and coarse emulsions. Skin irritation and oil control efficacy were evaluated in healthy volunteers before and after product application for 28 days. The obtained nanoemulsions not only decreased sebum production but also enhanced skin moisture levels. In conclusion, the meticulously designed nanoemulsions, incorporating suitable excipients, show a promising delivery system for hydrophilic peptides to control sebum overproduction in oily facial skin.

中文翻译：

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用于局部递送 Tripeptide-3 的微乳液和纳米乳液：从实验设计到面部皮肤的抗皮脂功效

使用微乳液或纳米乳液将亲水性 Tripeptide-3 有针对性地递送至皮肤以减少面部油脂是本研究的重点。通过水滴定法和伪三元相图确定了影响油/水透明分散体形成的因素，如表面活性剂体系、HLB值和助溶剂。 Cremophore® RH40 和双尾辅助表面活性剂聚甘油-3-二异硬脂酸酯的表面活性剂/辅助表面活性剂组合 (Smix) 显着降低了辛酸/癸酸甘油三酯（CCT 油）和水之间的界面张力（HLB） 13，水与助溶剂 (PG) 的比例为 1:1。两级全因子实验设计 (FFD-DoE) 强调了 HLB 值、共溶剂和 CCT 油含量的自变量影响微乳液或纳米乳液形成的最佳组合物。优化组合在低 Smix 含量 (10%) 下的低能自发乳化产生半透明水包油 Tripeptide-3 纳米乳液，其内部液滴尺寸为 25.7 ± 1.20 nm，窄多分散指数为 0.237 ± 0.129 ，和 70.6 ± 0.58% 透射率。体外皮肤渗透研究表明，与高表面活性剂微乳液和粗乳液相比，Tripeptide-3 纳米乳液具有显着更高的皮肤渗透性和保留性。在健康志愿者中评估使用产品前后 28 天的皮肤刺激和控油功效。获得的纳米乳液不仅减少皮脂产生，而且提高皮肤水分含量。总之，精心设计的纳米乳液，结合合适的赋形剂，显示出一种有前途的亲水肽递送系统，可以控制油性面部皮肤的皮脂过量产生。