Fullerene C(60) as a multifunctional system for drug and gene delivery. Nanoscale 3:4035-4041

Center of Excellence for Nanostructured Materials (CENMAT), Department of Chemical and Pharmaceutical Sciences, and INSTM, Unit of Trieste University of Trieste, Piazzale Europa 1, 34127 Trieste, Italy.
Nanoscale (Impact Factor: 7.39). 09/2011; 3(10):4035-41. DOI: 10.1039/c1nr10783f
Source: PubMed


The fullerene family, and especially C(60), has delighted the scientific community during the last 25 years with perspective applications in a wide variety of fields, including the biological and the biomedical domains. Several biomedical uses have been explored using water-soluble C(60)-derivatives. However, the employment of fullerenes for drug delivery is still at an early stage of development. The design and synthesis of multifunctionalized and multimodal C(60) systems able to cross the cell membranes and efficiently deliver active molecules is an attracting challenge that involves multidisciplinary strategies. Promising results have emerged in the last years, bringing fullerenes again to the front of interest. Herein, the state of the art of this emerging field is presented and illustrated with some of the most representative examples.

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    • "C 60 fullerene nanoparticles can also act as physiologically active compounds constraining functional activity of neoplastic cells and, at the same time, inhibiting side effects of chemotherapeutic drugs on organism. In order to improve the biodistribution of anticancer drugs, C 60 fullerene is now considered as one of the most effective drug carriers[17]. The complexation of C 60 fullerene with well-established drug molecules has been a representative strategy to impart C 60 fullerenespecific properties for improved formulation[10,15]. "
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    ABSTRACT: With an aim to elucidate the effects of C60 fullerene complexed with antibiotic doxorubicin (Dox) on model bilipid membranes (BLM), the investigation of the electrical properties of BLM under the action of Dox and C60 fullerene, and of their complex, C60+ Dox,was performed. The complex aswell as its components exert a clearly detectable influence on BLM, which is concentration-dependent and also depends on phospholipid composition. The mechanism of this effect originates either from intermolecular interaction of the drug with fatty-acid residues of phospholipids, or from membranotropic effects of the drug-induced lipid peroxidation, or from the sum of these two effects. By fluorescence microscopy the entering of C60 + Dox complex into HeLa cells was directly shown.
    Full-text · Article · Feb 2016
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    • "Fullerenes are a class of carbon allotropes with unique and tuneable properties (superconductivity, ferromagnetism, sorption, among others), which makes them of particular interest in different fields of application, such as medicine (Montellano et al., 2011), material sciences, (Goyal et al., 2005), energy (Brabec et al., 2010) and personal care products (Benn et al., 2011). Currently, fullerenes are produced on a small-scale, around 10 T/year in the US and a similar output in Europe (Piccinno et al., 2012). "
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    ABSTRACT: In the present work, a new analytical approach is proposed for the analysis of seven fullerenes (C60, C70, N-methylfulleropyrrolidine, [6,6]-phenyl C61 butyric acid methyl ester, [6,6]-thienyl C61 butyric acid methyl ester, C60 pyrrolidine tris-acid ethyl ester and [6,6]-phenyl C71 butyric acid methyl ester fullerenes) in soils and sediments. This procedure combines an ultrasound-assisted solvent extraction (UAE) with toluene followed by liquid chromatography (LC), using a pyrenylpropyl group bonded silica based column, coupled to a high-resolution mass spectrometer (HRMS) using atmospheric pressure photoionisation (APPI) in negative ion mode. The analytical performance for fullerene separation of the pyrenylpropyl group bonded silica column was compared to the C18 column. For the ultra-trace analysis of fullerenes in complex environmental samples, the use of the APPI source and the use of the electrospray ionisation (ESI) source were compared. Using this approach for the analysis of fullerenes in complex matrices, a series of advantages, in terms of sensitivity and specificity, have been demonstrated. The method limits of detection (MLOD) and the method limits of quantification (MLOQ) in soils and sediments ranged from 0.022 to 0.39pg/g and from 0.072 to 1.3pg/g, respectively. Recoveries were between 68 and 106%. The analytical method was applied in order to assess the occurrence of selected fullerenes in 45 soils of Sul Catarinense (Santa Catalina State, Brazil) and 15 sediments from the Tubarão River, presenting different pressures of contamination: a coal-combustion power plant, car exhaust, coal mining industry and wastewater effluents. C60 and C70 fullerenes have been detected at concentrations ranging from the MLOD to 0.150ng/g. None of the functionalised fullerenes were detected in any of the samples. Combustion processes, in particular car exhaust, were identified as the main source of fullerenes. However, the potential degradation of residual concentrations of engineered fullerenes to more stable forms, such as C60 and C70, should also be considered. Copyright © 2014 Elsevier B.V. All rights reserved.
    Full-text · Article · Feb 2015 · Science of The Total Environment
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    • "To solve the dilemma on the optimal sizes for lung-targeted delivery, stable submicrometer-sized complex prepared prior to intravenous injection must grow into micrometer-sized particles under physiological conditions, release drugs at lung capillaries, and escape from the lung when the drug delivery is complete. In light of the diverse aggregation behavior of fullerenes in water14, their ability to protect DNA from degradation, and in vitro and in vivo gene delivery151617, we hypothesized that a cationic fullerene could serve as a carrier for the delivery of small interfering RNA (siRNA) for RNA interference (RNAi) therapeutics in vivo1819. We report here on the lung-specific delivery of siRNA using a cationic fullerene, tetra(piperazino)fullerene epoxide (TPFE) (Fig. 1)20. "
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    ABSTRACT: The efficient treatment of lung diseases requires lung-selective delivery of agents to the lung. However, lung-selective delivery is difficult because the accumulation of micrometer-sized carriers in the lung often induces inflammation and embolization-related toxicity. Here we demonstrate a lung-selective delivery system of small interfering RNA (siRNA) by controlling the size of carrier vehicle in blood vessels. The carrier is made of tetra(piperazino)fullerene epoxide (TPFE), a water-soluble cationic tetraamino fullerene. TPFE and siRNA form sub-micrometer-sized complexes in buffered solution and these complexes agglutinate further with plasma proteins in the bloodstream to form micrometer-sized particles. The agglutinate rapidly clogs the lung capillaries, releases the siRNA into lung cells to silence expression of target genes, and is then cleared rapidly from the lung after siRNA delivery. We applied our delivery system to an animal model of sepsis, indicating the potential of TPFE-based siRNA delivery for clinical applications.
    Full-text · Article · May 2014 · Scientific Reports
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