Liposome Formulation of Fullerene-Based Molecular Diagnostic and Therapeutic Agents

Abstract

Fullerene medicine is a new but rapidly growing research subject. Fullerene has a number of desired structural, physical and chemical properties to be adapted for biological use including antioxidants, anti-aging, anti-inflammation, photodynamic therapy, drug delivery, and magnetic resonance imaging contrast agents. Chemical functionalization of fullerenes has led to several interesting compounds with very promising preclinical efficacy, pharmacokinetic and safety data. However, there is no clinical evaluation or human use except in fullerene-based cosmetic products for human skincare. This article summarizes recent advances in liposome formulation of fullerenes for the use in therapeutics and molecular imaging.

The first representative of a new family of the bridgehead-modified difluoromethylenated homofullerenes: electrochemical properties and synthetic availability

“…Fullerene compounds exhibit rich redox chemistry; potential values are essential for understanding and predicting the homogeneous redox properties of each particular fullerene derivative as well as the areas of their possible application, e.g., organoelectronics [1][2][3] , medicine [4][5][6][7] , etc. Electronic properties of the fullerene cage can be adjusted via its targeted functionalization with various types of addends or via modification of the cage itself making these compounds very attractive objects.…”

“…[8,9] Thus, the nitrogen atoms in the azafullerene dimer (C 59 N) 2 ensure regiospecific chlorination and alkylation yielding only one isomer of C 59 NCl 5 and C 59 NR 5 containing a pyrrole fragment. [8,10] Similarly, the bridging moieties in the [5,6]-C 60 (CHCN) [11] and in the [5,6]-C 60 NR [8] homofullerene activate the bridgehead positions owing to a steric and -electron density polarization effects.…”

“…0.15 V with respect to the parent fullerenes. [12,15 Contrary to anionic forms of C 60 in which a negative charge is uniformly distributed over the fullerene cage, [5], 16] the negative charge in the anionic species of difluoromethylenated homofullerenes is mainly localized at the bridgehead carbon atoms [12,15] thus providing a possibility for regioselective electrophilic attack. Recently, we have demonstrated that protonation of the electrochemically generated C 60 (CF 2 ) 2-dianion with triflic acid affords a single isomer of C 60 (CF 2 )H 2 which is regioselectively hydrogenated at the bridgehead carbon atoms (see Fig.…”

Nanotechnology platforms in Parkinson’s Disease

“…Also, fullerenes in the form of carboxyfullerenes (C3) showed neuroprotection in Macaque fascicularis monkeys [107]. The technology leveraging the antioxidant properties of fullerenes in the treatment of Parkinson's disease is being commercialized and the leading companies involved are The Bronx Project, Inc. (TBP), Tego BioSciences Corporation (Tego) and Luna Innovations Incorporated (Luna) [108]. In addition to this, cerium oxide (CeO 2 ) is being used for its capability of neutralizing and reducing harmful reactive oxygen species in a redox reaction [102].…”

“…Besides, the clinical translation of research has lead to the development of a number of commercial entities. The Bronx Project, Inc. (TBP), Tego BioSciences Corporation (Tego) and Luna Innovations Incorporated (Luna) [108] are involved in the development of fullerenes for neuroprotection in PD. Parkinson's Pen (by Manus Neurodynamica Ltd.) is another patented technology that uses the changes in handwriting in combination with a sensor device on the pen to analyze the force exerted by each of the fingers, and the changes in handwriting [73].…”