A Systematic comparison of in vitro cell uptake and in vivo biodistribution for three classes of gold nanoparticles with saturated PEG coatings.

A great deal of attention has been focused on nanoparticles for cancer therapy, with the promise of tumor-selective delivery. However, despite intense work in the field over many years, the biggest obstacle to this vision remains extremely low delivery efficiency of nanoparticles into tumors. Due to the cost, time, and impact on the animals for in vivo studies, the nanoparticle field predominantly uses cellular uptake assays as a proxy to predict in vivo outcomes.

Coating Metal Nanoparticle Surfaces with Small Organic Molecules Can Reduce Nonspecific Cell Uptake.

Elucidation of mechanisms of uptake of nanoparticles by cells and methods to prevent this uptake is essential for many applications of nanoparticles. Most recent studies have focused on the role of proteins that coat nanoparticles and have employed PEGylation, particularly dense coatings of PEG, to reduce protein opsonization and cell uptake. Here we show that small molecule coatings on metallic nanoparticles can markedly reduce cell uptake for very sparsely PEGylated nanoparticles.

Impact of Cross-Linker Valency on Gold Nanoparticle Aggregate Formation and Cellular Uptake.

Synthesis of spherical, biocompatible nanoparticle aggregates using a small molecular cross-linker is a simple and flexible approach for the controlled assembly of gold nanoparticles. This strategy can be extended to a variety of cross-linkers, making it possible to the test the effect of cross-linker properties on aggregate formation and physicochemical properties. Here, we synthesized aggregates using a series of structurally homologous cross-linkers with differing valencies.