Right on target: An in vivo tumor‐targeting strategy using nanoparticles has been developed. An unnatural sialic acid (green, see scheme) with azide groups is artificially generated on the target site by metabolic glycoengineering. These groups then effectively enhance the accumulation of nanoparticles in the target tumor site by an in vivo bioorthogonal copper‐free click reaction.

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Gold nanoprobe: Heparin–DOPA‐coated gold nanoparticles (HEPA–AuNPs) showed low toxicity, prolonged stability, and an enhanced X‐ray absorption coefficient in vitro. In vivo microCT images showed that HEPA–AuNPs produced enhanced liver‐specific CT images compared with iodine‐based contrast agents, thus highlighting its potential as a novel, liver‐specific CT imaging agent (see figure).

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Colon cancer is the second leading cause of cancer-related death in the United States. The considerable mortality from colon cancer is due to metastasis to other organs, mainly the liver. In the management of colon cancer, early detection and targeted therapy are crucial. In this study, we aimed to establish a versatile theranostic system for early tumor detection and targeted tumor therapy by using poly(ethylene glycol)-conjugated hyaluronic acid nanoparticles (P-HA-NPs) which can selectively accumulate in tumor tissue. For the diagnostic application, a near-infrared fluorescence (NIRF) imaging dye (Cy 5.5) was chemically conjugated onto the HA backbone of P-HA-NPs. After intravenous injection of Cy5.5-P-HA-NPs into the tumor-bearing mice, small-sized colon tumors as well as liver-implanted colon tumors were effectively visualized using the NIRF imaging technique. For targeted therapy, we physically encapsulated the anticancer drug, irinotecan (IRT), into the hydrophobic cores of P-HA-NPs. Owing to their notable tumor targeting capability, IRT-P-HA-NPs exhibited an excellent antitumor activity while showing a reduction in undesirable systemic toxicity. Importantly, we demonstrated the theranostic application using Cy5.5-P-HA-NPs and IRT-P-HA-NPs in orthotopic colon cancer models. Following the systemic administration of Cy5.5-P-HA-NPs, neoplasia was clearly visualized, and the tumor growth was effectively suppressed by intravenous injection of IRT-P-HA-NPs. It should be emphasized that the therapeutic responses could be simultaneously monitored by Cy5.5-P-HA-NPs. Our results suggest that P-HA-NPs can be used as a versatile theranostic system for the early detection, targeted therapy, and therapeutic monitoring of colon cancer.

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