Functionalized Lipopeptide Micelles as Highly Efficient NMR Depolarization Seed Points for Targeted Cell Labelling in Xenon MRI

• DOI: 10.1002/adbi.201900251
• Publication Date: 2020-01-02T07:08:29Z
• Authors: Matthias Schnurr; Ines Volk; Heike Nikolenko; Lars Winkler; Margitta Dathe; Leif Schröder
• Keywords: Lipopeptide

Abstract Improving diagnostic imaging and therapy by targeted compound delivery to pathological areas across biological barriers is of urgent need. A lipopeptide, P‐CrA‐A2, composed a highly cationic peptide sequence (A2), an N‐terminally attached palmitoyl chain (P) cryptophane molecule (CrA) for preferred uptake into blood–brain barrier (BBB) capillary endothelial cells, was generated. CrA allows reversible binding Xe NMR detection with hyperpolarized nuclei. The lipopeptide forms size‐optimized micelles diameter about 11 nm at low micromolar concentration. Their high local payload has strong switchable impact on the bulk magnetization through Hyper‐CEST detection. Covalent fixation does not impede micelle formation hamper its host functionality but simplifies access hosts inducing saturation transfer. magnetic resonance (MRI) distinguishing BBB cells from control aortic small volume sevenfold improved CrA‐loading density compared liposomal carriers cell labelling minimally invasive (≈16 000‐fold more efficient than 19 F labelling). Thus, these nanoscopic particles combine selectivity human brain great sensitivity MRI might be potential tool in diagnostics.