Background: HIV/AIDS is a macrophage resident infection localized in
the reticuloendothelial system and remote locations of brain and bone marrow. We
present core shell nanoparticles of gold(AuNPs) and nevirapine(NVP) for targeted
delivery to the multiple HIV reservoirs. The aim of the study was to design core shell
NVP loaded AuNPs with high drug loading and to evaluate biodistribution of the
nanoparticles in possible HIV reservoirs in vivo. A specific objective was to assess
the possible synergy of AuNPs with NVP on anti-HIV activity in vitro.
Method: Core shell nanoparticles were prepared by double emulsion solvent evaporation
method and characterized.
Results: Glyceryl monostearate-nevirapine-gold nanoparticles(GMS-NVP-AuNPs)
revealed high entrapment efficiency (>70%), high loading (~40%), particle size <250 nm and zeta potential
-35.9± 1.41mv and exhibited sustained release with good stability. Surface plasmon resonance
indicated shell formation while SEM coupled EDAX confirmed the presence of Au. TEM confirmed
formation of spherical core shell nanoparticles. GMS-NVP-AuNPs revealed low hemolysis (<10 %) and
serum stability upto 6 h. GMS-NVP-AuNPs exhibited rapid, high and sustained accumulation in the
possible HIV reservoir organs, including the major organs of liver, spleen, lymph nodes, thymus and
also remote locations of brain, ovary and bone marrow. High cell viability and enhanced uptake in
PBMC’s and TZM-bl cells were observed. While uptake in PBMC’s proposed monocytes/macrophages
enabled brain delivery. GMS-NVP-AuNPs demonstrated synergistic anti-HIV activity.
Conclusion: The superior anti-HIV activity in vitro coupled with extensive localization of the nanoparticles
in multiple HIV reservoirs suggests great promise of the core shell GMS-NVP-AuNPs for improved
therapy of HIV.