Lamivudine-Conjugated and Efavirenz-Loaded G2 Dendrimers: Novel Anti-Retroviral Nano Drug Delivery Systems Publisher



Pargoo EM¹ ; Aghasadeghi MR² ; Parivar K¹ ; Nikbin M³ ; Rahimi P² ; Ardestani MS⁴
Source: IET Nanobiotechnology Published:2021

Abstract

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. © 2021 The Authors. IET Nanobiotechnology published by John Wiley & Sons Ltd on behalf of The Institution of Engineering and Technology.