Study of a potential drug delivery system based on carbon nanoparticles: effects of fullerene derivatives in MCF7 mammary carcinoma cells

• Published in: Journal of nanoparticle research : an interdisciplinary forum for nanoscale science and technology Vol. 14; no. 4; pp. 1 - 13
• Main Authors: Lucafò, Marianna, Pacor, Sabrina, Fabbro, Chiara, Da Ros, Tatiana, Zorzet, Sonia, Prato, Maurizio, Sava, Gianni
• Format: Journal Article
• Language: English
• Published: Dordrecht Springer Netherlands 01.03.2012; Springer Nature B.V
• Subjects: Characterization and Evaluation of Materials; Chemistry and Materials Science; Cytotoxicity; Inorganic Chemistry; Lasers; Materials Science; Nanoparticles; Nanotechnology; Optical Devices; Optics; Photonics; Physical Chemistry; Research Paper; Fullerene; Cytotoxicity; Cellular uptake; Nanoparticle; Nanomedicine; Anticancer drug delivery
• ISSN: 1388-0764; 1572-896X
• DOI: 10.1007/s11051-012-0830-8

Fullerenes (C 60 ) represent important carbon nanoparticles, widely investigated for diagnostic and therapeutic uses, mainly because they are characterized by a small size (between 7 and 10 Å) and a large surface area. The cytotoxicity of two fullerene derivatives, functionalized by 1,3-dipolar cycloaddition of azomethine ylides to the C 60 cage ( 1 and 2 ), the mechanism of cellular uptake (studied with a fluorescein-bearing derivative of 1 , hereafter called derivative 3 ), and the intracellular distribution are the subject of this work. Cell cytotoxicity on human mammary carcinoma cell line (MCF7), evaluated with the MTT test and further confirmed by a flow cytometry approach with DiOC 6 and PI probes, showed that derivative 1 was free of necrotic or apoptotic effects even after a long lasting cell exposure. Cell uptake and internalization of derivative 3 reach their zenith within 12 h after treatment, with a tendency to persist up to 72 h; this process was evaluated by flow cytometry and confirmed by confocal microscopy. Thus, it appears that a compound such as derivative 1 may be unspecifically taken up by MCF7 cells, in which it distributes throughout the cytoplasm, apparently avoiding any co-localization within the nucleus and secretory granules. These results suggest a strong interaction between the tested fullerene and mammalian cells and a significant ability of this compound to enter tumor cells, therefore resulting to be a suitable vector to deliver anticancer agents to tumor cells.