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Non-invasive medical imaging techniques such as positron emission tomography (PET) imaging are powerful platforms to track the fate of radiolabeled materials for diagnostic or drug delivery applications. Polymer-based nanocarriers tagged with non-standard PET radionuclides with relatively long half-lives (e.g. 64 Cu: t 1/2 = 12.7 h, 76 Br: t 1/2 = 16.2h, 89 Zr: t 1/2 = 3.3 d, 124 I: t 1/2 = 4.2 d) may greatly expand applications of nanomedicines in molecular imaging and therapy. However, radiolabeling strategies that ensure stable in vivo association of the radiolabel with the nanocarrier remain a significant challenge. In this study, we covalently attach radioiodine to the core of pre-fabricated nanocarriers. First, we encapsulated polyvinyl phenol within a poly(ethylene glycol) coating using Flash NanoPrecipitation (FNP) to produce stable 75 nm and 120 nm nanocarriers. Following FNP, we radiolabeled the encapsulated polyvinyl phenol with 125 I via electrophilic aromatic substitution in high radiochemical yields (&gt; 90%). Biodistribution studies reveal low radioactivity in the thyroid, indicating minimal leaching of the radiolabel in vivo . Further, PEGylated [ 125 I]PVPh nanocarriers exhibited relatively long circulation half-lives (t 1/2 α = 2.9 h, t 1/2 β = 34.9 h) and gradual reticuloendothelial clearance, with 31% of injected dose in blood retained at 24 h post-injection.

Biodistribution and fate of core-labeled125I polymeric nanocarriers prepared by Flash NanoPrecipitation (FNP)

Biodistribution and fate of core-labeled¹²⁵I polymeric nanocarriers prepared by Flash NanoPrecipitation (FNP)