Evidence map›Paper›PMID 21671137›Full record

ArticlePharmaceutical research2011

Potential of amino acid/dipeptide monoester prodrugs of floxuridine in facilitating enhanced delivery of active drug to interior sites of tumors: a two-tier monolayer in vitro study.

Yasuhiro Tsume, John M Hilfinger, Gordon L Amidon

Abstract read
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In one paragraph

Article in Pharmaceutical research, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
0.9field-weighted citation impact, top 27% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

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.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

7 citing papers in PubMed, 19 citations in OpenAlex.

  1. Transporter-Mediated Drug Delivery.Molecules (Basel, Switzerland) · 2023
    Review
  2. Amino Acids in the Development of Prodrugs.Molecules (Basel, Switzerland) · 2018
    Review
  3. Article
  4. Modern prodrug design for targeted oral drug delivery.Molecules (Basel, Switzerland) · 2014
    Article
  5. The development of orally administrable gemcitabine prodrugs with D-enantiomer amino acids: enhanced membrane permeability and enzymatic stability.European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V · 2014
    Article
  6. Article
  7. Selection of suitable prodrug candidates for in vivo studies via in vitro studies; the correlation of prodrug stability in between cell culture homogenates and human tissue homogenates.Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques · 2012
    Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

3 authors at 2 institutions in 1 country.

Yasuhiro TsumeDepartment of Pharmaceutical Science, University of Michigan, Ann Arbor, Michigan 48109, USA.
John M Hilfinger
Gordon L Amidon
University of Michigan–Ann Arbor · USTherapeutics Systems Research Laboratories (United States) · US

Funding

USE OF MUCCOSAL CELL CARRIERS/EYZYMES IN ORAL ABSORPTIONR01GM037188 · NIGMS · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI AMIDON, GORDON L · 1986 to 2013
$4.4M
NIGMS NIH HHS 2R01GM037188
6 · The paper itself

Abstract

purposeTo evaluate the advantages of amino acid/dipeptide monoester prodrugs for cancer treatments by assessing the uptake and cytotoxic effects of floxuridine prodrugs in a secondary cancer cell monolayer following permeation across a primary cancer cell monolayer.

methodsThe first Capan-2 monolayer was grown on membrane transwell inserts; the second monolayer was grown at the bottom of a plate. The permeation of floxuridine and its prodrugs across the first monolayer and the uptake and cell proliferation assay on secondary layer were sequentially determined.

resultsAll floxuridine prodrugs exhibited greater permeation across the first Capan-2 monolayer than the parent drug. The correlation between uptake and growth inhibition in the second monolayer with intact prodrug permeating the first monolayer suggests that permeability and enzymatic stability are essential for sustained action of prodrugs in deeper layers of tumors. The correlation of uptake and growth inhibition were vastly superior for dipeptide prodrugs to those obtained with mono amino acid prodrugs.

conclusionsAlthough a tentative general overall correlation between intact prodrug and uptake or cytotoxic action was obtained, it appears that a mixture of floxuridine prodrugs with varying beneficial characteristics may be more effective in treating tumors.

Indexed as

Amino AcidsCell Line, TumorCell ProliferationDelayed-Action PreparationsDipeptidesDrug Delivery SystemsDrug StabilityEnzyme StabilityFloxuridineHumansNeoplasmsPermeabilityProdrugsAmino AcidsDelayed-Action PreparationsDipeptidesFloxuridineProdrugs

Identifiers

PMID21671137
OpenAlexW1970304612

What OpenQuestion holds

Textmetadata
Read underepoch 390

Registered trials

None linked

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.