Iron oxide nanoparticles served as the primary carrier to increase drug loading in macrophages

The specific chemotaxis of macrophages to inflammatory site makes them good candidate for inflammation drug delivery. However, the loading capacity of free drug is low. The goal of the manuscript is to enhance the loading capacity by encapsulating drug onto iron oxide nanoparticles (IONPs) and investigate the size effect on the cellular uptake. IONPs with different sizes (10 nm, 70 nm, and 200 nm) were synthesized. The loading capacities of model drug protoporphyrin IX (PPIX) on different sized IONPs were studied, showing similar loading capacity. However, the cellular internalization of PPIX loaded IONPs (Fe₃O₄-PPIX) was quite different. 70 nm IONPs indicated maximum uptake by the macrophages. The results also demonstrate that the IONPs could significantly improve the loading capacity when compared with free drug. All the three sized nanoparticles demonstrated minimal effects on cellular viability and would not induce the polarization of macrophages. This study not only provides an efficient method to increase the drug loading capacity in macrophages, but also indicates the optimal size of nanoparticles for cellular uptake.