ArticleAntimicrobial agents and chemotherapy2013
Preclinical pharmacokinetics and tissue distribution of long-acting nanoformulated antiretroviral therapy.
Article in Antimicrobial agents and chemotherapy, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 48 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
48 citing papers in PubMed, 73 citations in OpenAlex.
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- A scalable ultra-long-acting tenofovir phosphonate prodrug sustains HBV suppression.Science advances · 2025Article
- Recent Advances in Antiviral Drug Delivery Strategies.AAPS PharmSciTech · 2025Review
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- Improvement in Bioavailability and Pharmacokinetic Characteristics of Efavirenz with Booster Dose of Ritonavir in PEGylated PAMAM G4 Dendrimers.AAPS PharmSciTech · 2022Article
- Correlating Mass Spectrometry Imaging and Liquid Chromatography-Tandem Mass Spectrometry for Tissue-Based Pharmacokinetic Studies.Metabolites · 2022Article
- Atazanavir versus lopinavir on Covid-19 infection: A retrospective protease inhibitors comparative study 2020.Caspian journal of internal medicine · 2022Article
- Intramuscular and subcutaneous administration of antiretroviral drugs, compared with oral, enhances delivery to lymphoid tissues in BALB/c mice.The Journal of antimicrobial chemotherapy · 2021Article
- Comparison of the Efficacy and Safety of Atazanavir/Ritonavir Plus Hydroxychloroquine with Lopinavir/Ritonavir Plus Hydroxychloroquine in Patients with Moderate COVID-19, A Randomized, Double-blind Clinical Trial.Iranian journal of pharmaceutical research : IJPR · 2021Article
- Nanosystems Applied to HIV Infection: Prevention and Treatments.International journal of molecular sciences · 2020Review
- Head-to-head comparative pharmacokinetic and biodistribution (PK/BD) study of two dexamethasone prodrug nanomedicines on lupus-prone NZB/WF1 mice.Nanomedicine : nanotechnology, biology, and medicine · 2020Article
- Atazanavir, Alone or in Combination with Ritonavir, Inhibits SARS-CoV-2 Replication and Proinflammatory Cytokine Production.Antimicrobial agents and chemotherapy · 2020Article
- The Synergistic Effect of an ATP-Competitive Inhibitor of mTOR and Metformin on Pancreatic Tumor Growth.Current developments in nutrition · 2020Article
- Synthesis of a long acting nanoformulated emtricitabine ProTide.Biomaterials · 2019Article
- Assessing the lymphoid tissue bioavailability of antiretrovirals in human primary lymphoid endothelial cells and in mice.The Journal of antimicrobial chemotherapy · 2019Article
- The Promise of Long-Acting Antiretroviral Therapies: From Need to Manufacture.Trends in microbiology · 2019Review
- Recent developments of nanotherapeutics for targeted and long-acting, combination HIV chemotherapy.European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V · 2019Review
- Injectable long-acting human immunodeficiency virus antiretroviral prodrugs with improved pharmacokinetic profiles.International journal of pharmaceutics · 2018Article
- Three HIV Drugs, Atazanavir, Ritonavir, and Tenofovir, Coformulated in Drug-Combination Nanoparticles Exhibit Long-Acting and Lymphocyte-Targeting Properties in Nonhuman Primates.Journal of pharmaceutical sciences · 2018Article
Corrections and comments
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Authors and funding
13 authors at 2 institutions in 1 country.
Funding
Abstract
Long-acting injectable nanoformulated antiretroviral therapy (nanoART) was developed with the explicit goal of improving medicine compliance and for drug targeting of viral tissue reservoirs. Prior nanoART studies completed in humanized virus-infected mice demonstrated sustained antiretroviral responses. However, the pharmacokinetics (PK) and tissue distribution of nanoART were not characterized. To this end, the PK and tissue distribution of nanoformulated atazanavir (ATV) and ritonavir (RTV) injected subcutaneously or intramuscularly in mice and monkeys were evaluated. Fourteen days after injection, ATV and RTV levels were up to 13-, 41-, and 4,500-fold higher than those resulting from native-drug administration in plasma, tissues, and at the site of injection, respectively. At nanoART doses of 10, 50, 100, and 250 mg/kg of body weight, relationships of more- and less-than-proportional increases in plasma and tissue levels with dose increases were demonstrated with ATV and RTV. Multiple-dose regimens showed serum and tissue concentrations up to 270-fold higher than native-drug concentrations throughout 8 weeks of study. Importantly, nanoART was localized in nonlysosomal compartments in tissue macrophages, creating intracellular depot sites. Reflective data were obtained in representative rhesus macaque studies. We conclude that nanoART demonstrates blood and tissue antiretroviral drug levels that are enhanced compared to those of native drugs. The sustained and enhanced PK profile of nanoART is, at least in part, the result of the sustained release of ATV and RTV from tissue macrophases and at the site of injection.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.