Synthesis and anti-HIV activity of carboxylated and drug-conjugated multi-walled carbon nanotubes

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 nanomaterial 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 control the antiviral activity. The more hydrophilic and dispersible oxidized samples, ox-MWCNT and MWCNT-C-CHI360, showed the best results with IC50 values of 11.43 mu g/mL and 4.56 mu g/mL, respectively.