Tumor targeting efficiency of bare nanoparticles does not mean the efficacy of loaded anticancer drugs: Importance of radionuclide imaging for optimization of highly selective tumor targeting polymeric nanoparticles with or without drug
- Tumor targeting efficiency of bare nanoparticles does not mean the efficacy of loaded anticancer drugs: Importance of radionuclide imaging for optimization of highly selective tumor targeting polymeric nanoparticles with or without drug
- 이범석; 박경순; 박상진; 김기철; 김효정; 이상주; 길희섭; 오승준; 지대윤; 김광명; 최귀원; 권익찬; 김상윤
- NAcHis-GC; Biodistributions; Gamma camera; Near-infrared fluorescence; Non-invasive imaging; Drug delivery
- Issue Date
- Journal of controlled release
- VOL 147, NO 2, 253-260
- The better understanding of polymeric nanoparticles as a drug delivery carrier is a decisive factor to get more
efficient therapeutic response in vivo. Here, we report the non-invasive imaging of bare polymeric
nanoparticles and drug-loaded polymeric nanoparticles to evaluate biodistribution in tumor bearing mice. To
make nano-sized drug delivery carrier, glycol chitosan was modified with different degrees of hydrophobic
N-acetyl histidine (NAcHis-GC-1, -2, and -3). The biodistribution of polymeric nanoparticles and drug was
confirmed by using gamma camera with 131I-labeled NAcHis-GC and 131I-labeled doxorubicin (DOX) and by
using in vivo live animal imaging with near-infrared fluorescence Cy5.5-labeled NAcHis-GC. Among bare
nanoparticles, NAcHis-GC3 (7.8% NAcHis content) showed much higher tumor targeting efficiency than
NAcHis-GC1 (3.3% NAcHis content) and NAcHis-GC2 (6.8% NAcHis content). In contrast, for drug-loaded
nanoparticles, DOX-NAcHis-GC1 displayed two-fold higher tumor targeting property than DOX-NAcHis-GC3.
These data imply that the biodistribution and tumor targeting efficiency between bare and drug-loaded
nanoparticles may be greatly different. Therapeutic responses for NAcHis-GC nanoparticles after drug
loading were also evaluated. In xenograft animal model, we could find out that DOX-NAcHis-GC1 with higher
tumor targeting of DOX has more excellent therapeutic effect than DOX-NAcHis-GC3 and free DOX. These
results mean that the hydrophobic core stability might be a critical factor for tumor targeting efficiency of
nanoparticles. The present study indicates that by using molecular imaging, we can select more appropriate
nanoparticles with the highest tumor targeting properties, leading to exerting more excellent therapeutic
results in cancer therapy.
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