PEGylation and zwitterionization, which are used in minimizing serum protein adsorption and nonspecific reticuloendothelial system (RES) uptake of nanoparticles (NPs), have a distinct impact on tumor targeting of luminescent gold nanoparticles (AuNPs), although both strategies provide AuNPs with effective renal clearance. The renal-clearable NIR-emitting PEGylated AuNPs was synthesized through a facile one-step method, and these NPs exhibit photophysical properties and core size almost identical to the zwitterionic glutathione coated AuNPs (GS-AuNPs). Systematic studies of the renal clearance, pharmacokinetics, and passive tumor targeting of PEG-AuNPs and GS-AuNPs in mice bearing MCF-7 tumors showed that the PEG-AuNPs can effectively target tumors with an efficiency three times higher than that of the GS-AuNPs, although the two of them exhibited comparable low RES uptake. The high tumor-targeting efficiency of the PEG-AuNPs is fundamentally a result of the fact that PEGylation can enhance the enhanced permeability and retention (EPR) effect of renal-clearable luminescent AuNPs relative to zwitterionization by increasing their retention time and concentration in the blood. However, the limitation of PEGylation in tumor imaging is that it took much longer for the PEG-AuNPs to reach the desired contrast index threshold than it took the zwitterionic GS-AuNPs because of the slow tumor accumulation and normal-tissue clearance of the PEG-AuNPs. These differences suggest that appropriate surface chemistries for NPs should be rationally selected upon their exact applications in cancer diagnosis and therapy.   Reference:J.B. Liu, M.X. Yu, X.H. Ning, C. Zhou, S.Y. Yang, and J. Zheng, Angew. Chem. Int. Ed. , 2013, DOI:10.1002/anie.201304465.J.B. Liu, M.X. Yu, C. Zhou, S.Y. Yang, X.H. Ning, and J. Zheng, J. Am. Chem. Soc. , 2013, 135(13), 4978-4981.J.B. Liu, M.X. Yu, C. Zhou, and J. Zheng, Mater. Today , 2013, accepted.

PEGylation and zwitterionization: Pros and cons in the renal clearance and tumor targeting of near-IR-emitting gold nanoparticles

247th National Meeting (2014)

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