Synthesis and anti-HIV activity of carboxylated and drug-conjugated multi-walled carbon nanotubes Daniela Iannazzo a, * , Alessandro Pistone a , Signorino Galvagno a , Stefania Ferro b, * , Laura De Luca b , Anna Maria Monforte b , Tatiana Da Ros c , Caroline Hadad c , Maurizio Prato c , Christophe Pannecouque d a Department of Electronic Engineering, Industrial Chemistry and Engineering, University of Messina, Contrada Di Dio, I-98166 Messina, Italy b Department of Pharmaceutical Sciences and Health Products, University of Messina, Viale Annunziata, I-98168 Messina, Italy c Department of Pharmaceutical and Chemical Sciences, University of Trieste, Piazzale Europa 1, I-34127 Trieste, Italy d Rega Institute for Medical Research, Katholieke Universiteit Leuven, Minderbroedersstraat 10, B-3000 Leuven, Belgium ARTICLE INFO Article history: Received 1 July 2014 Accepted 3 November 2014 Available online xxxx ABSTRACT Carbon nanotubes have attracted particular attention in antiviral therapy and recently have been explored as HIV inhibitors through structure-based design. In order to prove their in vitro ability to interact with viral enzymes and to act as HIV inhibitors, we have studied the antiviral potentiality of highly hydrophilic and dispersible carboxylated multi-walled carbon nanotubes (ox-MWCNT) and the activity exerted by the same nano- material bearing antiretroviral drugs and hydrophilic functionalities. The antiretroviral drugs chosen for this study were two newly synthesized benzimidazolones, CHI360 and CHI415, belonging to a series of active non-nucleoside reverse transcriptase inhibitors (RTI), and lamivudine (3TC), a known antiretroviral nucleoside agent, currently used in anti-HIV therapy. From this study, the physicochemical properties of these nanomaterials, namely hydrophilicity and dispersibility, emerged as the most relevant features able to con- trol the antiviral activity. The more hydrophilic and dispersible oxidized samples, ox- MWCNT and MWCNT-C-CHI360, showed the best results with IC 50 values of 11.43 lg/mL and 4.56 lg/mL, respectively. Ó 2014 Elsevier Ltd. All rights reserved. 1. Introduction The use of nanomaterials in medicine raises high expecta- tions for human health and nanotechnology is already con- tributing to the development of new drugs, biologics, and medical devices [1,2]. The improvement of existing therapeu- tics has the potential to give promising solutions to many illnesses, aiming for a better, more efficient and affordable healthcare [3,4]. Mankind is still fighting against a high num- ber of serious and complex illnesses like cancer, cardiovascu- lar diseases, multiple sclerosis, Alzheimer’s and Parkinson’s disease, diabetes as well as different kinds of serious inflam- matory or infectious diseases such as Acquired Immune Defi- ciency Syndrome (AIDS). Human immunodeficiency virus http://dx.doi.org/10.1016/j.carbon.2014.11.007 0008-6223/Ó 2014 Elsevier Ltd. All rights reserved. * Corresponding authors: Fax: +39 090 3977464 (D. Iannazzo). E-mail addresses: diannazzo@unime.it (D. Iannazzo), sferro@unime.it (S. Ferro). CARBON xxx (2014) xxx – xxx Available at www.sciencedirect.com ScienceDirect journal homepage: www.elsevier.com/locate/carbon Please cite this article in press as: Iannazzo D et al. Synthesis and anti-HIV activity of carboxylated and drug-conjugated multi-walled carbon nanotubes. Carbon (2014), http://dx.doi.org/10.1016/j.carbon.2014.11.007