ja8b09582_si_002.cif (6.25 MB)

Visualizing Kinetically Robust CoIII4L6 Assemblies in Vivo: SPECT Imaging of the Encapsulated [99mTc]TcO4 Anion

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posted on 2018-11-28, 00:00 authored by Benjamin P. Burke, William Grantham, Michael J. Burke, Gary. S. Nichol, David Roberts, Isaline Renard, Rebecca Hargreaves, Christopher Cawthorne, Stephen J. Archibald, Paul J. Lusby
Noncovalent encapsulation is an attractive approach for modifying the efficacy and physiochemical properties of both therapeutic and diagnostic species. Abiotic self-assembled constructs have shown promise, yet many hurdles between in vitro and (pre)­clinical studies remain, not least the challenges associated with maintaining the macromolecular, hollow structure under nonequilibrium conditions. Using a kinetically robust CoIII4L6 tetrahedron we now show the feasibility of encapsulating the most widely used precursor in clinical nuclear diagnostic imaging, the γ-emitting [99mTc]­TcO4 anion, under conditions compatible with in vivo administration. Subsequent single-photon emission computed tomography imaging of the caged-anion reveals a marked change in the biodistribution compared to the thyroid-accumulating free oxo-anion, thus moving clinical applications of (metallo)­supramolecular species a step closer.