Urey Carlos, Weiss Victor U, Gondikas Andreas, von der Kammer Frank, Hofmann Thilo, Marchetti-Deschmann Martina, Allmaier Günter, Marko-Varga György, Andersson Roland
Department of Surgery, Clinical Sciences Lund, Lund University, Lund, Sweden.
Institute of Chemical Technologies and Analytics, TU Wien, Vienna, Austria.
Int J Pharm. 2016 Nov 20;513(1-2):309-318. doi: 10.1016/j.ijpharm.2016.09.049. Epub 2016 Sep 14.
For drug delivery, characterization of liposomes regarding size, particle number concentrations, occurrence of low-sized liposome artefacts and drug encapsulation are of importance to understand their pharmacodynamic properties. In our study, we aimed to demonstrate the applicability of nano Electrospray Gas-Phase Electrophoretic Mobility Molecular Analyser (nES GEMMA) as a suitable technique for analyzing these parameters. We measured number-based particle concentrations, identified differences in size between nominally identical liposomal samples, and detected the presence of low-diameter material which yielded bimodal particle size distributions. Subsequently, we compared these findings to dynamic light scattering (DLS) data and results from light scattering experiments coupled to Asymmetric Flow-Field Flow Fractionation (AF4), the latter improving the detectability of smaller particles in polydisperse samples due to a size separation step prior detection. However, the bimodal size distribution could not be detected due to method inherent limitations. In contrast, cryo transmission electron microscopy corroborated nES GEMMA results. Hence, gas-phase electrophoresis proved to be a versatile tool for liposome characterization as it could analyze both vesicle size and size distribution. Finally, a correlation of nES GEMMA results with cell viability experiments was carried out to demonstrate the importance of liposome batch-to-batch control as low-sized sample components possibly impact cell viability.
对于药物递送而言,脂质体在大小、颗粒数浓度、低尺寸脂质体伪像的出现情况以及药物包封方面的特性,对于理解其药效学性质至关重要。在我们的研究中,我们旨在证明纳米电喷雾气相电泳迁移率分子分析仪(nES GEMMA)作为分析这些参数的合适技术的适用性。我们测量了基于数量的颗粒浓度,确定了名义上相同的脂质体样品之间的大小差异,并检测到了产生双峰粒度分布的低直径物质的存在。随后,我们将这些发现与动态光散射(DLS)数据以及与不对称流场流分级(AF4)耦合的光散射实验结果进行了比较,由于在检测之前有一个尺寸分离步骤,后者提高了多分散样品中较小颗粒的可检测性。然而,由于方法固有的局限性,无法检测到双峰粒度分布。相比之下,冷冻透射电子显微镜证实了nES GEMMA的结果。因此,气相电泳被证明是一种用于脂质体表征的通用工具,因为它可以分析囊泡大小和大小分布。最后,进行了nES GEMMA结果与细胞活力实验的相关性研究,以证明脂质体批次间控制的重要性,因为低尺寸样品成分可能会影响细胞活力。