ArticleInternational journal of pharmaceutics2010
Synthesis and in vitro evaluation of potential sustained release prodrugs via targeting ASBT.
Article in International journal of pharmaceutics, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed, 28 citations in OpenAlex.
- Structural insight into sodium-dependent bile acid transport by members of the SLC10 family.Structure (London, England : 1993) · 2026Article
- Improvement of Antialveolar echinococcosis efficacy of novel Albendazole-Bile acids Derivatives with Enhanced Oral Bioavailability.PLoS neglected tropical diseases · 2023Article
- Tyrosine Phosphorylation Regulates Plasma Membrane Expression and Stability of the Human Bile Acid Transporter ASBT (Molecular pharmaceutics · 2019Article
- Human bile acid transporter ASBT (SLC10A2) forms functional non-covalent homodimers and higher order oligomers.Biochimica et biophysica acta. Biomembranes · 2018Article
- Advanced Prodrug Strategies in Nucleoside and Non-Nucleoside Antiviral Agents: A Review of the Recent Five Years.Molecules (Basel, Switzerland) · 2017Review
- Modern prodrug design for targeted oral drug delivery.Molecules (Basel, Switzerland) · 2014Article
- Structural requirements of bile acid transporters: C-3 and C-7 modifications of steroidal hydroxyl groups.European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences · 2012Article
- The solute carrier family 10 (SLC10): beyond bile acid transport.Molecular aspects of medicineReview
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
The objective was to synthesize prodrugs of niacin and ketoprofen that target the human apical sodium-dependent bile acid transporter (ASBT) and potentially allow for prolonged drug release. Each drug was conjugated to the naturally occurring bile acid chenodeoxycholic acid (CDCA) using lysine as a linker. Their inhibitory binding and transport properties were evaluated in stably transfected ASBT-MDCK monolayers, and the kinetic parameters K(i), K(t), normJ(max), and P(p) were characterized. Enzymatic stability of the conjugates was evaluated in Caco-2 and liver homogenate. Both conjugates were potent inhibitors of ASBT. For the niacin prodrug, substrate kinetic parameter K(t) was 8.22microM and normJ(max) was 0.0917. In 4h, 69.4% and 26.9% of niacin was released from 1microM and 5microM of the conjugate in Caco-2 homogenate, respectively. For the ketoprofen prodrug, K(t) was 50.8microM and normJ(max) was 1.58. In 4h, 5.94% and 3.73% of ketoprofen was released from 1microM and 5microM of the conjugate in Caco-2 homogenate, and 24.5% and 12.2% of ketoprofen was released in liver homogenate, respectively. In vitro results showed that these bile acid conjugates are potential prolonged release prodrugs with binding affinity for ASBT.
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