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.
Highlights
The discovery of a spherical crystal form of carbon, bound by single and double bonds that form a three-dimensional geodesic spheroidal crystal, named fullerenes or buckminsterfullerene, by Curl, Kroto, and Smalley in 1985 opened a new field of science—nanotechnology [1]
The results demonstrated that the liposome formulation of amphiphilic fullerene amphiphilic liposomal malonylfullerene (ALM) is capable of preferentially accumulating in the inflamed synovial joints
Fullerenes, often dubbed carbon nanomaterials, are small molecules, similar in molecular size and volume to steroids, making them ideal molecular platforms to serve as ligands to enzymes and receptors
Summary
The discovery of a spherical crystal form of carbon, bound by single and double bonds that form a three-dimensional geodesic spheroidal crystal, named fullerenes or buckminsterfullerene, by Curl, Kroto, and Smalley in 1985 opened a new field of science—nanotechnology [1]. Pharmaceutics 2013, 5 organic molecules such as steroid hormones and peptide alpha helices—an important property from the drug design and development perspective Because of their spherical shape and their one nanometer size, fullerenes are often denoted as buckyballs or carbon nanomaterials. The metal inside the cage is not accessible for replacement such as transmetallation with endogenous ions, making it far more stable and inert than traditional metal chelates that are used in contrast-enhanced medical imaging. This property has been exploited recently in encapsulating gadolinium for use as MRI contrast agents, and radioactive isotopes for use in nuclear medicine including radiotherapy and nuclear imaging (PET and SPECT).
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