Gledovic Ana, Janosevic Lezaic Aleksandra, Nikolic Ines, Tasic-Kostov Marija, Antic-Stankovic Jelena, Krstonosic Veljko, Randjelovic Danijela, Bozic Dragana, Ilic Dusan, Tamburic Slobodanka, Savic Snezana
Department of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, University of Belgrade, 11121 Belgrade, Serbia.
Department of Physical Chemistry and Instrumental Methods, Faculty of Pharmacy, University of Belgrade, 11121 Belgrade, Serbia.
Nanomaterials (Basel). 2021 Jan 15;11(1):217. doi: 10.3390/nano11010217.
This study focuses on the development of biocompatible oil-in-water (O/W) nanoemulsions based on polyglycerol esters, as promising carriers for natural actives: red raspberry seed oil-RO and hydro-glycolic fruit extracts from red raspberry-RE and French oak-FE. Nanoemulsions were obtained via phase inversion composition (PIC) method at room temperature by dilution of microemulsion phase, confirmed by visual appearance, percentage of transmittance, microscopic, rheological and Differential Scanning Calorimetry (DSC) investigations. The results have shown that the basic RO-loaded formulation could be further enriched with hydro-glycolic fruit extracts from red raspberry or French oak, while keeping a semi-transparent appearance due to the fine droplet size (Z-ave: 50 to 70 nm, PDI value ≤ 0.1). The highest antioxidant activity (~92% inhibition of the DPPH radical) was achieved in the formulation containing both lipophilic (RO) and hydrophilic antioxidants (FE), due to their synergistic effect. The nanoemulsion carrier significantly increased the selective cytotoxic effect of RO towards malignant melanoma (Fem-X) cells, compared to normal human keratinocytes (HaCaT). In vivo study on human volunteers showed satisfactory safety profiles and significant improvement in skin hydration during 2 h after application for all nanoemulsions. Therefore, polyglycerol ester-based nanoemulsions can be promoted as effective carriers for red raspberry seed oil and/or hydro-glycolic fruit extracts in topical formulations intended for skin protection and hydration.
本研究聚焦于基于聚甘油酯的生物相容性水包油(O/W)纳米乳液的开发,该纳米乳液有望成为天然活性成分的载体,这些活性成分包括红树莓籽油(RO)、红树莓的水醇提取物(RE)和法国橡木提取物(FE)。通过微乳液相稀释,在室温下采用相转变组成(PIC)方法获得纳米乳液,并通过外观、透光率百分比、显微镜观察、流变学和差示扫描量热法(DSC)研究进行确认。结果表明,基本的负载RO的配方可以进一步添加红树莓或法国橡木的水醇提取物,同时由于液滴尺寸细小(Z-ave:50至70nm,PDI值≤0.1)而保持半透明外观。由于亲脂性(RO)和亲水性抗氧化剂(FE)的协同作用,在同时含有这两种抗氧化剂的配方中实现了最高的抗氧化活性(对DPPH自由基的抑制率约为92%)。与正常人角质形成细胞(HaCaT)相比,纳米乳液载体显著增强了RO对恶性黑色素瘤(Fem-X)细胞的选择性细胞毒性作用。对人类志愿者的体内研究表明,所有纳米乳液在应用后2小时内均显示出令人满意的安全性,且皮肤水合作用有显著改善。因此,基于聚甘油酯的纳米乳液可作为红树莓籽油和/或水醇水果提取物在用于皮肤保护和保湿的局部制剂中的有效载体进行推广。