C60 Fullerene Derivatized Nanoparticles and their Application to Therapeutics

Chun-Mao Lin, Tan-Yi Lu

doi:10.2174/187221012800270135

Abstract

Fullerenes can be formed into many new materials and devices. They have a wide range of applications in medicine, electronics, biomaterials, and energy production. An overview of the nanostructure and the physical and chemical characteristics of fullerene-drug derivatives is given. The biological behavior of fullerene derivatives shows their potential to medical application fields because C60 is rapidly absorbed by tissues and is excreted through urinary tract and enterons, which reveals low toxicity in vitro and in vivo studies. Nanomedicine has become one of the most promising areas of nanotechnology, while many have claimed its therapeutic use against cancer, human immunodeficiency virus (HIV), and neurodegenerative disorders. Water-soluble C60 fullerene derivatives that come from chemical modification largely enhance the biological efficacy. The blood-brain barrier (BBB) is a physical barrier composed of endothelial tight junctions that restrict the paracellular permeability. A major challenge facing neuropharmacology is to find compounds that can be delivered into the brain through the bloodstream. Fullerene C60 was demonstratively able to cross the BBB by hybridizing a biologically active moiety dyad, which provides a promising clue as a pharmacological therapy of neural disorders.

Keywords: C60 Fullerene, autophagy, blood brain barrier, fulleropyrrolidine-xanthine dyad, fullerene dyad, nanomedicine, neurodegenerative disease, neuroprotective, PTX-C60-2, PEG-C60-3, tetrahedral sites, C60(1, 4-hydroquinone), Metal-intercalate, Osmylation, Covalent attaching