Fullerene C₆₀ as a multifunctional system for drug and gene delivery.
ABSTRACT 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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ABSTRACT: Fullerenes are among the strongest antioxidants and are characterized as "radical sponges." The research on biomedicinal applications of fullerenes has achieved significant progress since the landmark publication by Friedman et al in 1993. Fullerene-biomolecule conjugates have become an important area of research during the past 2 decades. By a thorough literature search, we attempt to update the information about the synthesis of different types of fullerene-biomolecule conjugates, including fullerene-containing amino acids and peptides, oligonucleotides, sugars, and esters. Moreover, we also discuss in this review recently reported data on the biological and pharmaceutical utilities of these compounds and some other fullerene derivatives of biomedical importance. While within the fullerene-biomolecule conjugates, in which fullerene may act as both an antioxidant and a carrier, specific targeting biomolecules conjugated to fullerene will undoubtedly strengthen the delivery of functional fullerenes to sites of clinical interest.International Journal of Nanomedicine 01/2014; 9:77-92. · 3.46 Impact Factor
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ABSTRACT: Fullerene has shown great potential both in drug delivery and photodynamic therapy. Herein, we developed doxorubicin (DOX)-loaded PEI-derivatezed fullerene (C60-PEI-DOX) to facilitate combined chemotherapy and photodynamic therapy in one system, and DOX was covalently conjugated onto C60-PEI by the pH-sensitive hydrazone linkage. The release profiles of DOX from C60-PEI-DOX showed a strong dependence on the environmental pH values. The biodistributions of C60-PEI-DOX were investigated by injecting Qds (CdSe/ZnS) labeled conjugates (C60-PEI-DOX/Qds) into tumor-bearing mice, and C60-PEI-DOX/Qds showed a higher tumor targeting efficiency compared with Qds alone. Compared with free DOX in an in vivo murine tumor model, C60-PEI-DOX afforded higher antitumor efficacy without obvious toxic effects to normal organs owing to its good tumor targeting efficacy and 2.4-fold higer DOX released in tumor than in the other tissues. Besides, in this work, C60-PEI-DOX also showed a high antitumor efficacy of photodynamic therapy. The ability of C60-PEI-DOX nanoparticles to combine the local specific chemotherapy with external photodynamic therapy significantly improved the therapeutic efficacy of cancer treatment, and the combined treatment demonstrated a synergistic effect. These results suggest that C60-PEI-DOX may be promising for high treatment efficacy with minimal side effects in future therapy.Acta biomaterialia 11/2013; · 5.09 Impact Factor
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ABSTRACT: In this work we have studied the well-known "Buckminsterfullerene" C60 containing different amounts, from one to four molecules, of sodium radio-iodide (Na(131)I), with density functional theory geometrical optimizations and molecular dynamics at 310 K and atmospheric pressure. We found that nanocapsules with the radioactive content Na(131)I@C60, 2Na(131)I@C60 and 3Na(131)I@C60 are stable. Furthermore, the C60 fullerene undergoes expansion when the number of sodium radio-iodide molecules inside increases. Utilizing the Mulliken charge distribution analysis it was shown that a small charge transfer occurs from iodine to fullerene's carbon atoms. This produces repulsion which increases bond lengths thus the structure is weakened while the binding energy per atom decreases. For the case in which the fullerene initially contains four sodium radio-iodide molecules the expansion is greater than that which the structure can withstand. So the fullerene breaks and releases its contents. This result leads us to conclude that the fullerene can encapsulate up to three molecules of sodium radio-iodide.Journal of Molecular Modeling 03/2014; 20(3):2130. · 1.98 Impact Factor