ArticleJournal of controlled release : official journal of the Controlled Release Society2019
Creation of a long-acting rilpivirine prodrug nanoformulation.
Article in Journal of controlled release : official journal of the Controlled Release Society, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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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.
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Who cites it
15 citing papers in PubMed.
- Effect of Alkyl Chain Length on Physicochemical and Pharmacokinetic Performance of Aripiprazole Fatty Acid Prodrugs for Long-Acting Injectable Suspensions.Pharmaceutics · 2026Article
- Recent Advances in Antiviral Drug Delivery Strategies.AAPS PharmSciTech · 2025Review
- Novel pH-Responsive Structural Rearrangement of Myristic Acid-Conjugated Quetiapine Nanosuspension for Enhanced Long-Acting Delivery Performance.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2024Article
- Prodrug approaches for the development of a long-acting drug delivery systems.Advanced drug delivery reviews · 2023Review
- Roles of Fatty Acid Chain Length and Enzyme-Oriented Drug Controlled Release from pH-Triggering Self-Assembled Fatty Acid Conjugated Quetiapine Nanosuspensions.International journal of nanomedicine · 2023Article
- Real-Life Therapeutic Concentration Monitoring of Long-Acting Cabotegravir and Rilpivirine: Preliminary Results of an Ongoing Prospective Observational Study in Switzerland.Pharmaceutics · 2022Article
- Transformation of dolutegravir into an ultra-long-acting parenteral prodrug formulation.Nature communications · 2022Article
- Long-acting antiretrovirals: a new era for the management and prevention of HIV infection.The Journal of antimicrobial chemotherapy · 2022Review
- Virus-Mimicking Polymer Nanoparticles Targeting CD169ACS applied materials & interfaces · 2022Article
- Transformation of tenofovir into stable ProTide nanocrystals with long-acting pharmacokinetic profiles.Nature communications · 2021Article
- Europium sulfide nanoprobes predict antiretroviral drug delivery into HIV-1 cell and tissue reservoirs.Nanotheranostics · 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
- A year-long extended release nanoformulated cabotegravir prodrug.Nature materials · 2020Article
- Rilpivirine-associated aggregation-induced emission enables cell-based nanoparticle tracking.Biomaterials · 2020Article
- Rod-shape theranostic nanoparticles facilitate antiretroviral drug biodistribution and activity in human immunodeficiency virus susceptible cells and tissues.Theranostics · 2020Article
Corrections and comments
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Authors and funding
16 authors.
Funding
Abstract
Antiretroviral therapy requires lifelong daily dosing to attain viral suppression, restore immune function, and improve quality of life. As a treatment alternative, long-acting (LA) antiretrovirals can sustain therapeutic drug concentrations in blood for prolonged time periods. The success of recent clinical trials for LA parenteral cabotegravir and rilpivirine highlight the emergence of these new therapeutic options. Further optimization can improve dosing frequency, lower injection volumes, and facilitate drug-tissue distributions. To this end, we report the synthesis of a library of RPV prodrugs designed to sustain drug plasma concentrations and improved tissue biodistribution. The lead prodrug M3RPV was nanoformulated into the stable LA injectable NM3RPV. NM3RPV treatment led to RPV plasma concentrations above the protein-adjusted 90% inhibitory concentration for 25 weeks with substantial tissue depots after a single intramuscular injection in BALB/cJ mice. NM3RPV elicited 13- and 26-fold increases in the RPV apparent half-life and mean residence time compared to native drug formulation. Taken together, proof-of-concept is provided that nanoformulated RPV prodrugs can extend the apparent drug half-life and improve tissue biodistribution. These results warrant further development for human use.
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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.