Issue 13, 2016

RGD-modified lipid disks as drug carriers for tumor targeted drug delivery

Abstract

Melittin, the major component of the European bee venom, is a potential anticancer candidate due to its lytic properties. However, in vivo applications of melittin are limited due to its main side effect, hemolysis, especially when applied through intravenous administration. The polyethylene glycol-stabilized lipid disk is a novel type of nanocarrier, and the rim of lipid disks has a high affinity to amphiphilic peptides. In our study, a c(RGDyK) modified lipid disk was developed as a tumor targeted drug delivery system for melittin. Cryo-TEM was used to confirm the shape and size of lipid disks with or without c(RGDyK) modification. In vitro and in vivo hemolysis analyses revealed that the hemolysis effect significantly decreased after melittin associated with lipid disks. Importantly, the results of our in vivo biodistribution and tumor growth inhibitory experiments showed that c(RGDyK) modification increased the distribution of lipid disks in the tumor and the anticancer efficacy of melittin loaded lipid disks. Thus, we successfully achieved a targeted drug delivery system for melittin and other amphiphilic peptides with a good therapeutic effect and low side effects.

Graphical abstract: RGD-modified lipid disks as drug carriers for tumor targeted drug delivery

Article information

Article type
Paper
Submitted
17 Aug 2015
Accepted
02 Mar 2016
First published
03 Mar 2016

Nanoscale, 2016,8, 7209-7216

RGD-modified lipid disks as drug carriers for tumor targeted drug delivery

J. Gao, C. Xie, M. Zhang, X. Wei, Z. Yan, Y. Ren, M. Ying and W. Lu, Nanoscale, 2016, 8, 7209 DOI: 10.1039/C5NR05577F

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