Abstract
This study introduces multifunctional lipid nanoparticles (LNPs), mimicking the structure and compositions of low-density lipoproteins, for the tumor-targeted co-delivery of anti-cancer drugs and superparamagnetic nanocrystals. Paclitaxel (4.7 wt%) and iron oxide nanocrystals (6.8 wt%, 11 nm in diameter) are co-encapsulated within folate-functionalized LNPs, which contain a cluster of nanocrystals with an overall diameter of about 170 nm and a zeta potential of about -40 mV. The folate-functionalized LNPs enable the targeted detection of MCF-7, human breast adenocarcinoma expressing folate receptors, in T2-weighted magnetic resonance images as well as the efficient intracellular delivery of paclitaxel. Paclitaxel-free LNPs show no significant cytotoxicity up to 0.2 mg mL-1, indicating the excellent biocompatibility of the LNPs for intracellular drug delivery applications. The targeted anti-tumor activities of the LNPs in a mouse tumor model suggest that the low-density lipoprotein-mimetic LNPs can be an effective theranostic platform with excellent biocompatibility for the tumor-targeted co-delivery of various anti-cancer agents.
| Original language | English |
|---|---|
| Pages (from-to) | 222-231 |
| Number of pages | 10 |
| Journal | Small |
| Volume | 11 |
| Issue number | 2 |
| DOIs | |
| State | Published - Jan 14 2015 |
Funding
J. Y. Lee and J.‐H. Kim contributed equally to this work. The authors deeply appreciate Mr. Geunho Im for the technical help during the animal imaging experiments for the MR imaging studies. This study was supported by a grant from the Korea Health Technology R&D Project, Ministry of Health & Welfare (A111552), the National Research Foundation (NRF) (2010–0029410), and Converging Research Center (2009–0082276) funded by the NRF of the Republic of Korea.