Abstract

Multifunctional high boron content MOFs nano-co-crystals were assembled and architected for precise boron neutron capture therapy (BNCT) of brain glioma. Zirconium and mesotetra(4-carboxyphenyl)porphyrin are screened and determined to structure stable (Zr-TCPP) MOFs. The MOFs binding boron acids formed 100.20 ± 6.72 nm co-crystal structures (MNCs), which contained 42.50 % boric acid (m/m), had excellent stability, superior colloid dispersion, and excellent biocompatibility. Importantly, they could cross the brain-blood barrier, selectively target brain tumors, and deliver a high boron dose of 67.50 ± 4.20 µg [10B] g−1. Inductively coupled plasma mass spectrometry showed an excellent tumor-to-normal tissue boron ratio of 6.20 ± 0.90 and tumor-to-blood boron ratio of 3.80 ± 0.35. The MNCs also had intrinsic fluorescence and Zr89 positron emission tomography imaging capabilities, which can accurately trace and quantify MNCs in vitro and in vivo. Therefore, a significantly antitumor efficiency was achieved in BNCT for glioma in model mice by imaging location of precise space-time.

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