e biodistribution and pharmacokinetic evaluation of choline-bound gold nanoparticles in a human prostate tumor xenogra model Abstract Purpose: Gold nanoparticles (GNPs) have attracted signi cant attention in the treatment of cancer due to their potential as novel radiation enhancers, particularly when functionalized with various targeting ligands. e aim of this study was to assess the biodistribution and pharmacokinetic characteristics of a novel choline-bound GNP (choline-GNP) stabilized with polyethelenimine (PEI).Methods: Choline bound to 27 nm diameter GNPs was characterized using transmission electron microscopy (TEM), X-ray photoelectron spectroscopy (XPS) and Fourier transform infrared spectroscopy (FTIR). Toxicity of choline-GNPs was examined on DU-145 prostate cancer cells using an MTT assay. Using balb/c mice bearing ank DU-145 prostate tumors, choline-GNPs bio-distribution was measured using inductively coupled mass spectroscopy (ICP-MS). Blood, heart, lung, liver, spleen, brain, kidney and tumor gold content were examined at multiple time points over a 24-hour period a er tail vein injection.Results: An MTT assay using DU-145 prostate cancer cells yielded a 95% cell viability 72 hours a er choline-GNP administration. e tumor GNP area under the concentrationtime curve during the rst 4 hours (AUC0-4) was 2.2 ”g/ml h, representing 13% of the circulating blood GNP concentration over the same time period. e maximum intratumor GNP concentration observed was 1.4% of the injected dose per gram of tumor tissue (%ID/g) one hour post injection.Conclusions: GNPs functionalized with choline demonstrates a viable future nanoparticle platform with increased intra-tumor uptake as compared to unconjugated GNPs. Decreased intra-hepatic accumulation appears to be the reason for the improved systemic bioavailability. e next logical translational investigation will incorporate external beam radiation with the observed maximum intra-tumor uptake.