pH-Controlled Delivery of Doxorubicin to Cancer Cells, Based on Small Mesoporous Carbon Nanospheres

Mesoporous carbon nanospheres (MCNs) with small diameters of ≈90 nm are developed as an efficient transmembrane delivery vehicle of an anticancer drug, doxorubicin (DOX). MCNs exhibit a high loading capacity toward DOX due to hydrophobic interactions and the supramolecular π stacking between DOX and the carbonaceous structures, on which the pH-dependent drug release are successfully achieved. Specifically, DOX can be loaded onto MCNs in basic solution and in a physiological pH range, while release occurs in acidic solution in its ionized state. By effective passive and active targeting, MCNs can be readily internalized into HeLa cells, where the carried DOX can be efficiently released in the acidic microenvironment of the tumors for further therapy. The endocytosis and cytotoxicity of DOX@MCNs toward HeLa cells are investigated by confocal microscopy and MTT assay. This smart pH-dependent drug loading and release property of DOX@MCNs makes it possible to reduce the cytotoxicity to normal tissues during circulation in the body since the normal physiological pH is ≈7.4.