Vidlářová Lucie, Hanuš Jaroslav, Veselý Martin, Ulbrich Pavel, Štěpánek František, Zbytovská Jarmila
Department of Chemical Engineering, University of Chemistry and Technology Prague, Technická 3, 166 28 Prague 6, Czech Republic.
Department of Organic Technology, University of Chemistry and Technology Prague, Technická 3, 166 28 Prague 6, Czech Republic.
Eur J Pharm Biopharm. 2016 Nov;108:289-296. doi: 10.1016/j.ejpb.2016.07.016. Epub 2016 Jul 20.
The aim of this study was to follow the skin penetration of a model lipophilic compound (Nile red) delivered by nanoparticulate carriers, the so-called lipid nanocapsules. The nanocapsules consisting of an oil core stabilized by amixture of surfactants were prepared by the phase inversion temperature method. Varying the particle composition (the oil/surfactant ratio) nanoparticles of different size were prepared and characterized. The penetration profile of Nile red delivered into the porcine skin by the nanoparticles compared to non-particulate samples was determined using fluorescence microscopy combined with a novel, statistically robust quantitative image analysis method. This study demonstrated that lipid nanoparticles promoted the skin penetration of encapsulated Nile red in comparison with all the non-particulate samples. Nile red delivered by the lipid-based nanoparticles was able to diffuse across the stratum corneum and partition itself uniformly in the epidermis. No relationship between Nile red penetration into the skin and the particle size was found. Moreover, the presence of sodium chloride in the water phase had a negative impact on the Nile red penetration into the skin. The results indicate that the physico-chemical circumstances of the nanoparticulate formulation play the major role in the penetration of lipophilic substances into the skin.
本研究的目的是追踪由纳米颗粒载体（即所谓的脂质纳米囊）递送的模型亲脂性化合物（尼罗红）的皮肤渗透情况。通过相转变温度法制备了由油核和表面活性剂混合物稳定的纳米囊。通过改变颗粒组成（油/表面活性剂比例）制备并表征了不同尺寸的纳米颗粒。使用荧光显微镜结合一种新颖的、具有统计学稳健性的定量图像分析方法，测定了纳米颗粒与非颗粒样品相比将尼罗红递送至猪皮肤中的渗透情况。本研究表明，与所有非颗粒样品相比，脂质纳米颗粒促进了包封的尼罗红的皮肤渗透。基于脂质的纳米颗粒递送的尼罗红能够扩散穿过角质层并在表皮中均匀分布。未发现尼罗红渗透到皮肤中与颗粒大小之间存在关联。此外，水相中氯化钠的存在对尼罗红渗透到皮肤中具有负面影响。结果表明，纳米颗粒制剂的物理化学环境在亲脂性物质渗透到皮肤中起主要作用。
