Lipid structures, such as liposomes or micelles, are of high interest as an approach to support the transport and delivery of active agents as a drug delivery system. However, there are many open questions regarding their uptake and impact on cellular metabolism. In this study, lipid structures were assembled as a supported lipid bilayer on top of biopolymer-coated microcarriers based on the Layer-by-Layer assembly strategy. The functionalized microcarriers were then applied to various human and animal cell lines in addition to primary human macrophages (MΦ). Here, their influence on cellular metabolism and their intracellular localization were detected by extracellular flux analysis and immunofluorescence analysis, respectively. The impact of microcarriers on metabolic parameters was in most cell types rather low. However, lipid bilayer-supported microcarriers induced a decrease in oxygen consumption rate (OCR, indicative for mitochondrial respiration) and extracellular acidification rate (ECAR, indicative for glycolysis) in Vero cells. Additionally, in Vero cells lipid bilayer microcarriers showed a more pronounced association with microtubule filaments than polymer-coated microcarrier. Furthermore, they localized to a perinuclear region and induced nuclei with some deformations at a higher rate than unfunctionalized carriers. This association was reduced through the application of the microtubule polymerization inhibitor nocodazole. Thus, the effect of respective lipid structures as a drug delivery system on cells has to be considered in the context of the respective target cell, but in general can be regarded as rather low.

中文翻译：

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各种细胞系对脂质和聚合物涂层的逐层微载体的微管驱动摄取的代谢反应


脂质结构，例如脂质体或胶束，作为支持活性剂作为药物递送系统的运输和递送的方法而受到高度关注。然而，关于它们的吸收和对细胞代谢的影响还有许多悬而未决的问题。在这项研究中，基于逐层组装策略，脂质结构被组装为生物聚合物包被的微载体顶部的支撑脂质双层。然后，除了原代人巨噬细胞（MΦ）之外，功能化微载体还应用于各种人类和动物细胞系。在这里，分别通过细胞外通量分析和免疫荧光分析检测它们对细胞代谢的影响及其细胞内定位。在大多数细胞类型中，微载体对代谢参数的影响相当低。然而，脂质双层支持的微载体诱导Vero细胞中耗氧率（OCR，指示线粒体呼吸）和细胞外酸化率（ECAR，指示糖酵解）降低。此外，在 Vero 细胞中，脂质双层微载体与微管丝的关联性比聚合物包被的微载体更明显。此外，它们定位于核周区域并以比未功能化载体更高的速率诱导核发生一些变形。通过使用微管聚合抑制剂诺考达唑可以减少这种关联。因此，必须在各个靶细胞的背景下考虑作为药物递送系统的各个脂质结构对细胞的影响，但通常可以认为相当低。