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Nanomedicine. 2013 Nov;9(8):1263-73. doi: 10.1016/j.nano.2013.05.003. Epub 2013 May 13.

Macrophage folate receptor-targeted antiretroviral therapy facilitates drug entry, retention, antiretroviral activities and biodistribution for reduction of human immunodeficiency virus infections.

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  • 1Department of Pharmacology and Experimental Neuroscience, University of Nebraska Medical Center, Omaha, NE, USA. Electronic address:


Macrophages serve as vehicles for the carriage and delivery of polymer-coated nanoformulated antiretroviral therapy (nanoART). Although superior to native drug, high drug concentrations are required for viral inhibition. Herein, folate-modified ritonavir-boosted atazanavir (ATV/r)-encased polymers facilitated macrophage receptor targeting for optimizing drug dosing. Folate coating of nanoART ATV/r significantly enhanced cell uptake, retention and antiretroviral activities without altering cell viability. Enhanced retentions of folate-coated nanoART within recycling endosomes provided a stable subcellular drug depot. Importantly, up to a five-fold enhanced plasma and tissue drug levels followed folate-coated formulation injection in mice. Folate polymer encased ATV/r improves nanoART pharmacokinetics bringing the technology one step closer to human use.


This team of authors describes a novel method for macrophage folate receptor-targeted antiretroviral therapy. Atazanvir entry, retention, and antiretroviral activities were superior using the presented method, and so was its biodistribution, enabling a more efficient way to address human immunodeficiency virus infections, with a hoped for clinical application in the near future.

Copyright © 2013 Elsevier Inc. All rights reserved.


3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide; ATV; ATV/r; BSA; CHO; Chinese hamster ovary; FA; FOLR; Folate; Human immunodeficiency virus; LAMP; MDM; MTT; Macrophages; NanoART; PBS; PDI; PFA; Poloxamer 407; RME; RT; RTV; Targeted drug delivery; atazanavir; bovine serum albumin; folate receptor; folic acid; lysosomal associated membrane protein; monocyte-derived macrophages; nanoART; nanoformulated antiretroviral therapeutics; paraformaldehyde; phosphate buffered saline; polydispersity index; receptor-mediated endocytosis; reverse transcriptase; ritonavir; ritonavir-boosted atazanavir

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