Issue 3, 2015

Tumor extracellular acidity activated “off–on” release of bortezomib from a biocompatible dendrimer

Abstract

A nanoparticle with a specific response to tumor extracellular acidity provides a new option in the design of tumor-targeted delivery systems. In this study, we report such a pH-responsive polymer which realizes an “off–on” release of bortezomib in tumor acidic microenvironments. A dendrimer surface is grafted with a neutral shell to reduce its cellular uptake, and its interior is functionalized with catechol moieties. An anticancer drug, bortezomib, is loaded within the dendrimer interior via a boronate–catechol interaction. The bortezomib-loaded dendrimer is non-toxic to a number of cells under physiological conditions, but kills most of the cells in slightly acidic microenvironments. In vivo studies further prove that the bortezomib-loaded dendrimer significantly inhibits tumor growth while causing minimal systemic toxicity to the animals. Since there are a number of potent anticancer drugs containing the boronate structure, the polymeric vector in this study provides a versatile scaffold to design pH-responsive drug carriers for chemotherapy.

Graphical abstract: Tumor extracellular acidity activated “off–on” release of bortezomib from a biocompatible dendrimer

Supplementary files

Article information

Article type
Paper
Submitted
18 Oct 2014
Accepted
05 Dec 2014
First published
18 Dec 2014

Biomater. Sci., 2015,3, 480-489

Author version available

Tumor extracellular acidity activated “off–on” release of bortezomib from a biocompatible dendrimer

M. Wang, Y. Wang, K. Hu, N. Shao and Y. Cheng, Biomater. Sci., 2015, 3, 480 DOI: 10.1039/C4BM00365A

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