Low-density lipoprotein-mimicking nanoparticles for tumor-targeted theranostic applications.

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.

• Authors: Jeong Yu Lee, Jin-Ho Kim, Ki Hyun Bae, Mi Hwa Oh, Youngwook Kim, Jee Seon Kim, Tae Gwan Park, Keunchil Park, Jung Hee Lee, Yoon Sung Nam
• Journal: Small (Weinheim an der Bergstrasse, Germany) (Small) Vol. 11 Issue 2 Pg. 222-31 (Jan 14 2015) ISSN: 1613-6829 [Electronic] Germany
• PMID: 25137631 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Chemical References

• Lipoproteins, LDL

Topics

• Animals
• Cell Cycle
• Humans
• Lipoproteins, LDL (administration & dosage)
• MCF-7 Cells
• Magnetic Resonance Imaging
• Mice
• Microscopy, Atomic Force
• Microscopy, Electron, Transmission
• Nanoparticles
• Neoplasms (therapy)