Evidence map›Paper›PMID 27456759›Full record

ArticleNanomedicine (London, England)2016

Development and characterization of a long-acting nanoformulated abacavir prodrug.

Dhirender Singh, JoEllyn McMillan, James Hilaire, Nagsen Gautam, Diana Palandri, Yazen Alnouti, Howard E Gendelman, Benson Edagwa

Open access · hybridAbstract read
In one paragraph

Article in Nanomedicine (London, England), 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 33 papers.

0numbers the graph read from it
0cells of the map it votes in
33citing papers in PubMed
4.7field-weighted citation impact, top 5% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

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.

2 · The registry

The trial behind it

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.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

33 citing papers in PubMed, 49 citations in OpenAlex.

  1. Review
  2. Review
  3. Review
  4. CRISPR editing of CCR5 and HIV-1 facilitates viral elimination in antiretroviral drug-suppressed virus-infected humanized mice.Proceedings of the National Academy of Sciences of the United States of America · 2023
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  7. Pharmacology of HIV Cure: Site of Action.Clinical pharmacology and therapeutics · 2021
    Review
  8. Article
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  10. Article
  11. Article
  12. Article
  13. Article
  14. Article
  15. Creation of a long-acting rilpivirine prodrug nanoformulation.Journal of controlled release : official journal of the Controlled Release Society · 2019
    Article
  16. Article
  17. Review
  18. 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 · 2019
    Review
  19. HIV and the Macrophage: From Cell Reservoirs to Drug Delivery to Viral Eradication.Journal of neuroimmune pharmacology : the official journal of the Society on NeuroImmune Pharmacology · 2019
    Review
  20. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

8 authors at 1 institution in 1 country.

Dhirender SinghDepartment of Pharmaceutical Sciences, University of Nebraska Medical Center, Omaha, NE, USA.
JoEllyn McMillanDepartment of Pharmacology & Experimental Neuroscience, University of Nebraska Medical Center, Omaha, NE, USA.
James HilaireDepartment of Pharmacology & Experimental Neuroscience, University of Nebraska Medical Center, Omaha, NE, USA.
Nagsen GautamDepartment of Pharmaceutical Sciences, University of Nebraska Medical Center, Omaha, NE, USA.
Diana PalandriDepartment of Pharmacology & Experimental Neuroscience, University of Nebraska Medical Center, Omaha, NE, USA.
Yazen AlnoutiDepartment of Pharmaceutical Sciences, University of Nebraska Medical Center, Omaha, NE, USA.
Howard E GendelmanDepartment of Pharmaceutical Sciences, University of Nebraska Medical Center, Omaha, NE, USA.
Benson EdagwaDepartment of Pharmacology & Experimental Neuroscience, University of Nebraska Medical Center, Omaha, NE, USA.
University of Nebraska Medical Center · US

Funding

Therapeutics Core (Page 286)P30MH062261 · NIMH · UNIVERSITY OF NEBRASKA MEDICAL CENTER · PI GENDELMAN, HOWARD E · 2000 to 2021
$37.7M
Targeted Neuro Protection of HIV-1 Associated Neurologic DiseaseP01MH064570 · NIMH · UNIVERSITY OF ROCHESTER · PI GELBARD, HARRIS A · 2001 to 2014
$19.4M
Pharmacokinetics and Drug-Drug InteractionsP01DA028555 · NIDA · UNIVERSITY OF NEBRASKA MEDICAL CENTER · PI ALNOUTI, YAZEN · 2010 to 2019
$16.8M
Neuroprotective Immunity and HIV DementiaR01NS034239 · NINDS · UNIVERSITY OF NEBRASKA MEDICAL CENTER · PI Howard E Gendelman, R Lee Mosley · 1995 to 2026
$12.3M
Proteomics CoreP01NS043985 · NINDS · UNIVERSITY OF NEBRASKA MEDICAL CENTER · PI ZHENG, JIALIN CHARLES · 2003 to 2012
$11.8M
Role of EAAT2 and AEG-1 in Astrocyte Dysfunction and NeurodegenerationP01NS031492 · NINDS · ST. LUKE'S-ROOSEVELT INST FOR HLTH SCIS · PI GELBARD, HARRIS A · 1993 to 2007
$10.9M
Nanomedicine and NeuroAIDSR01NS036126 · NINDS · UNIVERSITY OF NEBRASKA MEDICAL CENTER · PI GENDELMAN, HOWARD E · 1997 to 2017
$5.7M
Nebraska Center for VirologyP30GM103509 · NIGMS · UNIVERSITY OF NEBRASKA LINCOLN · PI WOOD, CHARLES · 2012 to 2014
$3.3M
SMART HANDR01AG043540 · NIA · UNIVERSITY OF NEBRASKA MEDICAL CENTER · PI GENDELMAN, HOWARD E, POLUEKTOVA, LARISA Y · 2013 to 2017
$3.1M
NIA NIH HHS R01 AG043540NIDA NIH HHS P01 DA028555NIGMS NIH HHS P30 GM103509NIMH NIH HHS P01 MH064570NIMH NIH HHS P30 MH062261NINDS NIH HHS P01 NS031492NINDS NIH HHS P01 NS043985NINDS NIH HHS R01 NS034239NINDS NIH HHS R01 NS036126
6 · The paper itself

Abstract

aimA myristoylated abacavir (ABC) prodrug was synthesized to extend drug half-life and bioavailability.

methodsMyristoylated ABC (MABC) was made by esterifying myristic acid to the drug's 5-hydroxy-cyclopentene group. Chemical composition, antiretroviral activity, cell uptake and retention and cellular trafficking of free MABC and poloxamer nanoformulations of MABC were assessed by proton nuclear magnetic resonance and tested in human monocyte-derived macrophages. Pharmacokinetics of ABC and nanoformulated MABC were evaluated after intramuscular injection into mice.

resultsMABC antiretroviral activity in monocyte-derived macrophages was comparable to native drug. Encasement of MABC into poloxamer nanoparticles extended drug bioavailability for 2 weeks.

conclusionMABC synthesis and encasement in polymeric nanoformulations improved intracellular drug accumulation and demonstrate translational potential as part of a long-acting antiretroviral regimen.

Indexed as

AbacavirAnimalsAnti-HIV AgentsCell LineDelayed-Action PreparationsDideoxynucleosidesDrug LiberationHalf-LifeHIV-1HIV InfectionsHumansHydrophobic and Hydrophilic InteractionsInjections, IntramuscularMacrophagesMaleMiceAbacavirAnti-HIV AgentsDelayed-Action PreparationsDideoxynucleosidesPoloxamerProdrugsRitonavirabacavir prodrugantiretroviral therapymonocyte-macrophagesnanoformulated antiretroviralspharmacokinetics

Identifiers

PMID27456759
PMCPMC4996153
OpenAlexW2491169609

What OpenQuestion holds

Textmetadata
Read underepoch 390

Registered trials

None linked

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.