Nano-Oncology Unit, Health Research Institute of Santiago de Compostela (IDIS), SERGAS, Santiago de Compostela, Spain; GIGA-CRC In Vivo Imaging, Centre de Recherches du Cyclotron, Université de Liège - ULiège, Liège, Belgium.
GIGA-CRC In Vivo Imaging, Centre de Recherches du Cyclotron, Université de Liège - ULiège, Liège, Belgium.
Colloids Surf B Biointerfaces. 2020 Apr;188:110793. doi: 10.1016/j.colsurfb.2020.110793. Epub 2020 Jan 13.
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 (F), a radioisotope regularly used in clinic. [F]fluoride was produced by the cyclotron and was incorporated into 4-[F]fluorobenzamido-N-ethylmaleimide ([F]FBEM), which was coupled next to the emulsions previously functionalized with a thiol group, via inclusion of either a thiol-PEG-lipid (SH-PEG-C), or a peptide-PEG-lipid (Cys-Pro-Ile-Glu-Asp-Arg-Pro-Met-Cys-PEG-C) 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.
由可生物降解和生物相容的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，我们试图探索一种新的放射性标记螯合策略，用于氟-18（F）标记可生物降解的神经鞘磷脂纳米乳液，F 是一种经常在临床中使用的放射性同位素。[F]氟化物由回旋加速器产生，并与先前用巯基官能化的乳液结合，通过包含硫醇-PEG-脂质（SH-PEG-C）或肽-PEG-脂质（Cys-Pro-Ile-Glu-Asp-Arg-Pro-Met-Cys-PEG-C）衍生物，偶联到 4-[F]氟苯甲酰胺-N-乙基马来酰亚胺（[F]FBEM）上。通过简单的共轭化学，在不使用有机溶剂的情况下，快速有效地获得了放射性标记的乳液，并根据粒径、多分散性、表面电荷、pH 值和渗透压进行了表征。在 BALB/c 小鼠中进行的 PET 成像和生物分布研究允许获得放射性标记乳液的药代动力学，并确定清除途径。总之，我们证实了这项新技术在用于 PET 成像诊断的脂质药物纳米系统放射性标记中的潜力。
