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 The leading web portal for pharmacy resources, news, education and careers October 22, 2017
Pharmacy Choice - Pharmaceutical News - Findings on Pharmaceutical Research Detailed by Investigators at University of Maryland (Synthesis and in vitro evaluation of bile acid prodrugs of... - October 22, 2017

Pharmacy News Article

 1/9/15 - Findings on Pharmaceutical Research Detailed by Investigators at University of Maryland (Synthesis and in vitro evaluation of bile acid prodrugs of...

Findings on Pharmaceutical Research Detailed by Investigators at University of Maryland (Synthesis and in vitro evaluation of bile acid prodrugs of floxuridine to target the liver)

By a News Reporter-Staff News Editor at Drug Week Fresh data on Drugs and Therapies are presented in a new report. According to news reporting out of Baltimore, Maryland, by NewsRx editors, research stated, "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)."

Our news journalists obtained a quote from the research from the University of Maryland, "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 K-i = 6.86 +/- 1.37 mu M, K-m = 10.7 +/- 2.1 mu M, and passive permeability = 0.663 (+/- 0.121) x 10(-7) cm/s while floxuridine 5'-glutamic acid-CDCA showed K-i = 0.397 +/- 0.038 mu M, K-m = 40.4 +/- 15.2 mu M, and passive permeability = 1.72 (+/- 0.18) x 10(-7) cm/s. Floxuridine itself had a higher passively permeability of 7.54 (+/- 0.45) x 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."

According to the news editors, the research concluded: "Prodrugs were stable in rat plasma (t = 3 h), but quickly released in rat liver s9 fraction, suggesting future in vivo evaluation."

For more information on this research see: Synthesis and in vitro evaluation of bile acid prodrugs of floxuridine to target the liver. International Journal of Pharmaceutics, 2014;475(1-2):597-604. International Journal of Pharmaceutics can be contacted at: Elsevier Science Bv, PO Box 211, 1000 Ae Amsterdam, Netherlands. (Elsevier - www.elsevier.com; International Journal of Pharmaceutics - www.elsevier.com/wps/product/cws-home/505513)

Our news journalists report that additional information may be obtained by contacting D. Vivian, University of Maryland, Sch Pharm, Baltimore, MD 21201, United States (see also Drugs and Therapies).

Keywords for this news article include: Maryland, Baltimore, United States, Drugs and Therapies, North and Central America

Our reports deliver fact-based news of research and discoveries from around the world. Copyright 2015, NewsRx LLC



(c) 2015 NewsRx LLC

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