Lamivudine-conjugated and efavirenz-loaded G2 dendrimers: Novel anti-retroviral nano drug delivery systems.

Infection with human immunodeficiency virus (HIV)-1 causes immunological disorders and death worldwide which needs to be further assisted by novel anti-retroviral drug delivery systems. Consequently, finding newer anti-retroviral pharmaceuticals by using biocompatible, biodegradable nanomaterials comprising a nanoparticle as core and a therapeutic agent is of high global interest. In this experiment, a second generation of a negatively charged nano-biopolymer linear globular G2 dendrimer was carefully conjugated and loaded with well-known anti-HIV drugs lamivudine and efavirenz, respectively. They were characterised by a variety of analytical methods such as Zetasizer, Fourier-transform infrared spectroscopy, elemental analysis and liquid chromatography-mass spectroscopy. Additionally, conjugated lamivudine and loaded efazirenz with globular PEGylated G2 dendrimer were tested on an HEK293 T cell infected by single-cycle replicable HIV-1 virion and evaluated using XTT test and HIV-1 P24 protein load. The results showed that lamivudine-conjugated G2 significantly decreased retroviral activity without any cell toxicity. This effect was more or less observed by efavirenz-loaded G2. These nano-constructs are strongly suggested for further in vivo anti-HIV assays.