2012 • In Düzgüneş, Nejat (Ed.) Methods in Enzymology: Nanomedicine — Cancer, Diabetes, and Cardiovascular, Central Nervous System, Pulmonary and Inflammatory Diseases
[en] The destruction of the neovessels in solid tumors can cause the death of tumor cells resulting from the lack of oxygen and nutrients. Peculiarities of the tumor vasculature, however, also position angiogenic endothelial cells as obvious targets to address cytotoxic drugs into the tumor. In particular, the identification of a three-amino acids sequence, arginine-glycine-aspartate (RGD), as a fundamental recognition site for proliferating endothelial attachment to the extracellular matrix leads to the development of tumor-targeting ligands for nanoparticles. The RGD peptide can target the αvβ3 integrin overexpressed by the tumor endothelium, and thereby increases the accumulation of drug-loaded RGD-grafted nanoparticles. RGD-nanoparticles may thus extravasate more efficiently and enter the tumor via the enhanced permeability and retention (EPR) effect. This combination of active and passive processes leads to the penetration of nanoparticles into the tumor tissue, followed by cellular uptake and intracellular delivery of the cytotoxic payload. Since cancer cells may also express αvβ3 integrin, the entrapping of RGD-nanoparticles into the tumor interstitial fluid may yet be facilitated through direct binding to cancer cells. Here, we describe methods used for the preparation of RGD-nanoparticles and for the validation of their potential of tumor endothelium targeting both in vitro and in vivo. We also illustrate how RGD-nanoparticles may be more suited than nontargeted modalities for the tumor delivery of poorly soluble and/or highly cytotoxic drugs, using different mouse tumor xenograft models.
Research Center/Unit :
Center for Education and Research on Macromolecules (CERM)
Disciplines :
Chemistry Materials science & engineering
Author, co-author :
Danhier, Fabienne; Université catholique de Louvain (UCL), Brussels, Louvain Drug Research Institute, Pharmaceutics and Drug Deliv (LDRI)
Pourcelle, Vincent; Université catholique de Louvain (UCL), Institute of Condensed Matter and Nanosciences (IMCN)
Marchand-Brynaert, Jacqueline; Université catholique de Louvain (UCL), Institute of Condensed Matter and Nanosciences (IMCN)
Jérôme, Christine ; University of Liège - ULiège > Department of Chemistry > Center for Education and Research on Macromolecules (CERM)
Feron, Olivier; Université Catholique de Louvain, Institute of Experimental and Clinical Research, Pole of Pharmacology, Brussels
Préat, Véronique; Université catholique de Louvain (UCL), Brussels, Louvain Drug Research Institute, Pharmaceutics and Drug Deliv (LDRI)
Language :
English
Title :
Targeting of tumor endothelium by RGD-grafted PLGA-nanoparticles
Publication date :
2012
Main work title :
Methods in Enzymology: Nanomedicine — Cancer, Diabetes, and Cardiovascular, Central Nervous System, Pulmonary and Inflammatory Diseases
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