These authors contributed equally to this work.
HDL-Mimicking Peptide–Lipid Nanoparticles with Improved Tumor Targeting
Article first published online: 2 DEC 2009
Copyright © 2010 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim
Volume 6, Issue 3, pages 430–437, February 5, 2010
How to Cite
Zhang, Z., Chen, J., Ding, L., Jin, H., Lovell, J. F., Corbin, I. R., Cao, W., Lo, P.-C., Yang, M., Tsao, M.-S., Luo, Q. and Zheng, G. (2010), HDL-Mimicking Peptide–Lipid Nanoparticles with Improved Tumor Targeting. Small, 6: 430–437. doi: 10.1002/smll.200901515
- Issue published online: 27 JAN 2010
- Article first published online: 2 DEC 2009
- Manuscript Revised: 20 OCT 2009
- Manuscript Received: 14 AUG 2009
- cancer therapy;
- tumor targeting
Targeted delivery of intracellularly active diagnostics and therapeutics in vivo is a major challenge in cancer nanomedicine. A nanocarrier should possess long circulation time yet be small and stable enough to freely navigate through interstitial space to deliver its cargo to targeted cells. Herein, it is shown that by adding targeting ligands to nanoparticles that mimic high-density lipoprotein (HDL), tumor-targeted sub-30-nm peptide–lipid nanocarriers are created with controllable size, cargo loading, and shielding properties. The size of the nanocarrier is tunable between 10 and 30 nm, which correlates with a payload of 15–100 molecules of fluorescent dye. Ligand-directed nanocarriers targeting epidermal growth factor receptor (EGFR) are confirmed both in vitro and in vivo. The nanocarriers show favorable circulation time, tumor accumulation, and biodistribution with or without the targeting ligand. The EGFR targeting ligand is proved to be essential for the EGFR-mediated tumor cell uptake of the nanocarriers, a prerequisite of intracellular delivery. The results demonstrate that targeted HDL-mimetic nanocarriers are useful delivery vehicles that could open new avenues for the development of clinically viable targeted nanomedicine.