ArticleInternational journal of pharmaceutics2014
Synthesis and in vitro evaluation of bile acid prodrugs of floxuridine to target the liver.
Article in International journal of pharmaceutics, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed, 28 citations in OpenAlex.
- Development of novel liver-targeting glucocorticoid prodrugs.Medicine in drug discovery · 2024Article
- Transporter-Mediated Drug Delivery.Molecules (Basel, Switzerland) · 2023Review
- Oligonucleotides Carrying Nucleoside Antimetabolites as Potential Prodrugs.Current medicinal chemistry · 2023Review
- Advanced prodrug strategies in nucleoside analogues targeting the treatment of gastrointestinal malignancies.Frontiers in cell and developmental biology · 2023Review
- Roles and action mechanisms of bile acid-induced gastric intestinal metaplasia: a review.Cell death discovery · 2022Review
- Evaluation of Floxuridine Oligonucleotide Conjugates Carrying Potential Enhancers of Cellular Uptake.International journal of molecular sciences · 2021Article
- Enhanced Liver Targeting of Camptothecin via Conjugation with Deoxycholic Acid.Molecules (Basel, Switzerland) · 2019Article
- Mechanism of hepatic targeting via oral administration of DSPE-PEG-cholic acid-modified nanoliposomes.International journal of nanomedicine · 2017Article
- Repurposing FDA-approved drugs as therapeutics to treat Rift Valley fever virus infection.Frontiers in microbiology · 2015Article
Corrections and comments
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
Floxuridine is often used to treat metastatic liver disease and is given as an infusion directly into the hepatic artery to increase the amount of intact drug that reaches the liver. The objective of this work was to design and synthesize prodrugs of floxuridine through conjugation to chenodeoxycholic acid (CDCA) to target the liver via the bile acid liver uptake transporter Na(+)/taurocholate cotransporting polypeptide (NTCP, SLC10A1). Two isomeric prodrugs of floxuridine were synthesized: floxuridine 3'glutamic acid-CDCA and floxuridine 5'-glutamic acid-CDCA. Both were potent inhibitors and substrates of NTCP. Floxuridine 3'glutamic acid-CDCA showed Ki=6.86±1.37 μM, Km=10.7±2.1 μM, and passive permeability=0.663(±0.121)×10(-7) cm/s while floxuridine 5'-glutamic acid-CDCA showed Ki=0.397±0.038 μM, Km=40.4±15.2 μM, and passive permeability=1.72(±0.18)×10(-7) cm/s. Floxuridine itself had a higher passively permeability of 7.54(±0.45)×10(-7) cm/s in the same cell line, indicating that both prodrugs have the potential for lower non-specific effects than the drug alone. Prodrugs were stable in rat plasma (t=3 h), but quickly released in rat liver s9 fraction, suggesting future in vivo evaluation.
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Registered trials
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