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Nanomedicine (Lond). 2014 Jul;9(9):1341-52. doi: 10.2217/nnm.13.92. Epub 2013 Aug 1.

Small magnetite antiretroviral therapeutic nanoparticle probes for MRI of drug biodistribution.

Author information

1
Department of Pharmaceutical Sciences, University of Nebraska Medical Center, Omaha, NE 68198-5830, USA.

Abstract

AIM:

Drug toxicities, compliance and penetrance into viral reservoirs have diminished the efficacy of long-term antiretroviral therapy (ART) for treatment of HIV infection. Cell-targeted nanoformulated ART was developed to improve disease outcomes. However, rapid noninvasive determination of drug biodistribution is unrealized. To this end, small magnetite ART (SMART) nanoparticles can provide assessments of ART biodistribution by MRI.

MATERIALS & METHODS:

Poly(lactic-co-glycolic acid), 1,2-distearoyl-sn-glycero-3-phosphocholine- and 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-(methoxy-PEG 2000)-encased particles were synthesized with atazanavir (ATV) and magnetite. Uptake and retention of ATV and magnetite administered at 3:1 ratios (weight/weight) were determined in human monocyte-derived macrophages and mice.

RESULTS:

SMART particles were taken up and retained in macrophages. In mice, following parenteral SMART injection, magnetite and drug biodistribution paralleled one another with MRI signal intensity greatest in the liver and spleen at 24 h. Significantly, ATV and magnetite levels correlated.

CONCLUSION:

SMART can permit rapid assessment of drug tissue concentrations in viral reservoirs.

KEYWORDS:

HIV; macrophage; monocyte; nanomedicine; nanoparticles; small magnetite antiretroviral therapy

PMID:
23905578
PMCID:
PMC3909560
DOI:
10.2217/nnm.13.92
[Indexed for MEDLINE]
Free PMC Article

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