Size-dependent EPR effect of polymeric nanoparticles on tumor targeting

Citation:

H. Kang, S. Rho, W. R. Stiles, S. Hu, Y. Baek, D. W. Hwang, S. Kashiwagi, M. S. Kim, and H. S. Choi. 2020. “Size-dependent EPR effect of polymeric nanoparticles on tumor targeting.” Adv Healthc Mater, 9, Pp. e1901223. Publisher's Version

Abstract:

Passive targeting of large nanoparticles by the enhanced permeability and retention (EPR) effect is a crucial concept for solid tumor targeting in cancer nanomedicine. There is, however, a trade-off between the long-term blood circulation of nanoparticles and their nonspecific background tissue uptake. To define this size-dependent EPR effect, near-infrared fluorophore-conjugated polyethylene glycols (PEG-ZW800s; 1-60 kDa) are designed and their biodistribution, pharmacokinetics, and renal clearance are evaluated in tumor-bearing mice. The targeting efficiency of size-variant PEG-ZW800s is investigated in terms of tumor-to-background ratio (TBR). Interestingly, smaller sized PEGs (20 kDa, 13 nm) accumulate highly in major organs, including the lungs, liver, and pancreas. Among those tested, 20 kDa PEG-ZW800 exhibits the highest TBR, while excreting unbound molecules to the urinary bladder. This result lays a foundation for engineering tumor-targeted nanoparticles and therapeutics based on the size-dependent EPR effect.
Last updated on 06/13/2022