Aim
To develop lipid nano-antiretrovirals (LNAs) for the treatment of HIV-infected macrophages. Materials &
Conclusion
These findings demonstrate the potential of LNAs for the treatment of infected macrophages, which are key players in HIV reservoirs.
Methods
LNAs were prepared with docosahexaenoic acid to facilitate brain penetration and surface-decorated with folate considering that infected macrophages often overexpress folate receptors.
Results
Folate-decorated LNAs loading rilpivirine (RPV) were efficiently taken up by folate receptor-expressing cell types including activated macrophages. The intracellular Cmax of the RPV-LNAs in activated macrophages was 2.54-fold and the area under the curve was 3.4-fold versus free RPV, translating to comparable or higher (p < 0.01; RPV ≤6.5 ng/ml) activities against HIV infectivity and superior protection (p < 0.05) against HIV cytotoxicity. LNAs were also effective in monocyte-derived macrophages.