Organic nanoparticles made out of biodegradable and biocompatible materials have attracted increased attention in the therapeutic and diagnostic fields. In this study, we attempted to explore a new radiolabelling chelating free strategy for biodegradable sphingomyelin nanometric emulsions with fluorine-18 (18F), a radioisotope regularly used in clinic. [18F]fluoride was produced by the cyclotron and was incorporated into 4-[18F]fluorobenzamido-N-ethylmaleimide ([18F]FBEM), which was coupled next to the emulsions previously functionalized with a thiol group, via inclusion of either a thiol-PEG-lipid (SH-PEG12-C18), or a peptide-PEG-lipid (Cys-Pro-Ile-Glu-Asp-Arg-Pro-Met-Cys-PEG8-C18) derivative. Radiolabelled emulsions were obtained in a rapid and efficient fashion through facile-conjugated chemistry without the use of organic solvents, and characterized in terms of size, polydispersity, surface charge, pH, and osmolarity. PET imaging and biodistribution studies in BALB/c mice allowed obtaining the pharmacokinetics of the radiolabelled emulsions and determining the clearance pathways. Altogether, we confirmed the potential of this new technique for the radiolabelling of lipid-based drug nanosystems for application in PET imaging diagnosis.

中文翻译：

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用氟18对脂质基纳米载体进行放射性标记，以在体内通过PET进行跟踪。

由可生物降解和生物相容性材料制成的有机纳米颗粒在治疗和诊断领域引起了越来越多的关注。在这项研究中，我们尝试探索一种新的无放射性螯合策略，用于可生物降解的鞘磷脂纳米乳液与氟18（18F）（一种经常在临床上使用的放射性同位素）。回旋加速器产生[18F]氟化物，并掺入4- [18F]氟苯甲酰胺基-N-乙基马来酰亚胺（[18F] FBEM）中，然后通过包含硫醇将其与先前被巯基官能化的乳液偶联-PEG-脂质（SH-PEG12-C18）或肽-PEG-脂质（Cys-Pro-Ile-Glu-Asp-Arg-Pro-Met-Cys-PEG8-C18）衍生物。放射性标记的乳液是通过快速共轭化学快速有效地获得的，无需使用有机溶剂，并以尺寸，多分散性，表面电荷，pH和摩尔渗透压浓度为特征。在BALB / c小鼠中进行PET成像和生物分布研究可获取放射性标记乳剂的药代动力学并确定清除途径。总而言之，我们确认了这项新技术在基于脂质的药物纳米系统的放射性标记中的潜力，可用于PET影像诊断。