ArticleInternational journal of nanomedicine2019
Synthesis and characterization of a long-acting emtricitabine prodrug nanoformulation.
Article in International journal of nanomedicine, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 21 citations in OpenAlex.
- Exploring prodrug approaches for Alzheimer's treatment: an overview.Neurodegenerative disease management · 2026Review
- Recent Advances in Antiviral Drug Delivery Strategies.AAPS PharmSciTech · 2025Review
- Polymer Delivery Systems for Long-Acting Antiretroviral Drugs.Pharmaceutics · 2024Review
- Polymer-prodrug conjugates as candidates for degradable, long-acting implants, releasing the water-soluble nucleoside reverse-transcriptase inhibitor emtricitabine.Journal of materials chemistry. B · 2023Article
- Chronic Hepatitis B Infection: New Approaches towards Cure.Biomolecules · 2023Review
- The best backbone for HIV prevention, treatment, and elimination: Emtricitabine+tenofovir.Antiviral therapy · 2022Review
- Prodrug Therapies for Infectious and Neurodegenerative Diseases.Pharmaceutics · 2022Review
- Synthesis and antiviral activity of fatty acyl conjugates of remdesivir against severe acute respiratory syndrome coronavirus 2 and Ebola virus.European journal of medicinal chemistry · 2021Article
- Solubility Data, Solubility Parameters and Thermodynamic Behavior of an Antiviral Drug Emtricitabine in Different Pure Solvents: Molecular Understanding of Solubility and Dissolution.Molecules (Basel, Switzerland) · 2021Article
- Long-acting approaches for delivery of antiretroviral drugs for prevention and treatment of HIV: a review of recent research.Expert opinion on drug delivery · 2020Review
- Solubility, Hansen Solubility Parameters and Thermodynamic Behavior of Emtricitabine in Various (Polyethylene Glycol-400 + Water) Mixtures: Computational Modeling and Thermodynamics.Molecules (Basel, Switzerland) · 2020Article
- Synthesis and Characterization of Long-Acting Darunavir Prodrugs.Molecular pharmaceutics · 2020Article
Corrections and comments
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Authors and funding
11 authors at 3 institutions in 2 countries.
Funding
Abstract
purposeA palmitoylated prodrug of emtricitabine (FTC) was synthesized to extend the drug's half-life, antiretroviral activities and biodistribution.
methodsA modified FTC prodrug (MFTC) was synthesized by palmitoyl chloride esterification. MFTC's chemical structure was evaluated by nuclear magnetic resonance. The created hydrophobic prodrug nanocrystals were encased into a poloxamer surfactant and the pharmacokinetics (PK), biodistribution and antiretroviral activities of the nanoformulation (NMFTC) were assessed. The conversion of MFTC to FTC triphosphates was evaluated.
resultsMFTC coated with poloxamer formed stable nanocrystals (NMFTC). NMFTC demonstrated an average particle size, polydispersity index and zeta potential of 350 nm, 0.24 and -20 mV, respectively. Drug encapsulation efficiency was 90%. NMFTC was readily taken up by human monocyte-derived macrophages yielding readily detected intracellular FTC triphosphates and an extended PK profile.
conclusionNMFTC shows improved antiretroviral activities over native FTC. This is coordinate with its extended apparent half-life. The work represents an incremental advance in the development of a long-acting FTC formulation.
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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.