A Novel Fullerene-Based Drug Delivery System Delivering Doxorubicin for Potential Lung Cancer Therapy

We developed an attractive method to prepare a fullerene-based (C82) drug delivery system modified with doxorubicin (DOXO) and cyclic RGD motif (DOXO-C82-cRGD) for potential clinic use treating solid tumors, lung cancers. The DOXO-C82-cRGD nanoparticles with a diameter of ~1.7 nm were prepared and the chemical structure was confirmed with MALDI-TOF, dynamic light scattering (DLS), and X-ray photoelectron spectroscopy (XPS). The DOXO-C82-cRGD nanoparticles showed great stability in phosphate buffer solution (PBS) and were also stable in low concentration of thiols (20 μM). On the contrary, the high concentration of thiols (10 mM) remarkably enhanced the deconjugation of DOXO-C82-cRGD. The in vitro results demonstrated that DOXO-C82-cRGD nanoparticles showed great preferential cellular uptake in non-small lung cancer cells as compared with DOXO-C82 and particularly, DOXO. Moreover, the cell viability results suggested that DOXO-C82-cRGD had significant cytotoxicity to cells at low dose. Apparently, the DOXO-C82-cRGD nanoparticles showed strong in vitro anti-tumor ability. Our study certainly provide a novel drug delivery system for preparing DOXO-contained vehicles for solid tumor therapy in clinic.