Preparation and cellular targeting study of VEGF-conjugated PLGA nanoparticles

Abstract

Vascular endothelial growth factor receptor (VEGFR) is over-expressed on a variety of tumour cells and tumour neovasculature, and so becomes well-documented target for cancer treatment. This study was designed to evaluate the cellular targeting and anti-tumor potency of VEGF-conjugated nanoparticles (VEGF-NPs). The poly-lactic-co-glycolic acid nanoparticles were prepared using the emulsion-solvent evaporation method and the VEGF was conjugated on surface of nanoparticles by covalent coupling method. The obtained particles were found to be of spherical shape exhibiting a size of 710 nm and VEGF conjugation efficiency was 16.6%. The results in vitro test showed that VEGF-NPs were more associated to Human Umbilical Vein Endothelial Cells by binding to VEGFR. In vitro cell proliferation test, IC₅₀ showed the superior antiproliferative activity of paclitaxel-loaded VEGF-NPs over unconjugated nanoparticles and native paclitaxel due to higher cellular association on tumour cells. So, the VEGF-NPs offer a promising active targeting carrier for tumour selective treatment.

• Nanoparticles
• paclitaxel
• poly-lactic-co-glycolic acid
• tumor targeting
• vascular endothelial growth factor

Declaration of interest

This work was supported by National Natural Science Foundation of China (grant nos. 81 302 737). The authors report no conflicts of interest. The authors alone are responsible for the content and writing of the article.