Role of physicochemical properties of coating ligands in receptor-mediated endocytosis of nanoparticles

A fundamental understanding of the receptor-mediated endocytosis is of great importance in biomedicine. In this paper, we systematically investigate the effect of the properties of coating ligands on the cellular uptake of nanoparticles by using dissipative particle dynamics, and find that the strength of the receptor-ligand interaction, the ligand density and length as well as its rigidity can strongly affect the final equilibrium in the receptor-mediated endocytosis. Interestingly, it is found that the particle decorated with longer ligands is more likely to attach to the membrane, while it is harder to be totally engulfed. Increasing the ligand density and rigidity which enhances the uniform distribution of ligands on the particle may lead to the total engulfment. Further, we also show that the particle can be totally engulfed if one can reasonably design the hydrophobic/lipophobic properties of ligands. The present study shows that not only the chemical but also the physical parameters of ligands can govern the nanoparticle-cell interaction, which may give some significant insights into future nanoparticle design in drug delivery. (C) 2012 Elsevier Ltd. All rights reserved.