Abstract
d-Glucosamine (DG) was conjugated to a core-cross linked polymeric micelle (CCPM) system equipped with both a near-infrared fluorophore (NIRF) and a gamma emitter (111In). The resultant nano-scale tumor-targeting imaging tracer, 111In-DG-NIRF-CCPM, selectively accumulated in a human epithelial carcinoma A-431 xenograft model in mice. At 24 hrs post injection, the tumor uptake was 2.62 ± 0.80 % of the injected dose per gram of tissue (%ID/g). Tumors were clearly delineated in both single-photon emission computed tomography (SPECT) and optical imaging. The results suggest that the prepared imaging tracer is a promising agent for tumor diagnosis.
Highlights
Optical imaging is a relatively new molecular imaging modality that offers non-invasive, real-time and high-sensitivity imaging of fluorophores embedded in diseased tissues [1,2]
We recently reported the synthesis of 68Ga- and 111In-labeled DG for the positron emission tomography (PET) and single-photon emission computed tomography (SPECT) imaging of tumors [14,15,16]
About 70% of the NCS-Bz-DTPA was attached to the near-infrared fluorophore (NIRF)-core-cross linked polymeric micelle (CCPM)
Summary
Optical imaging is a relatively new molecular imaging modality that offers non-invasive, real-time and high-sensitivity imaging of fluorophores embedded in diseased tissues [1,2]. We investigated whether the surface of CCPM can be further modified with sugar molecules to improve its pharmacokinetics profile and minimize its non-tumor uptake [9]. We recently reported the synthesis of 68Ga- and 111In-labeled DG for the positron emission tomography (PET) and SPECT imaging of tumors [14,15,16]. Those studies have showed that DG attached to a bulky moiety still preserved its biological functions. We conjugated DG to the CCPM surface via a succinate linker, and investigated its performances regarding the tumor targeting, in vitro and in vivo stability, biodistribution, and dual gamma and NIRF optical imaging. Further studies are needed to improve the drug targeting efficiency with dual-labeled CCPM for molecular imaging
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