Evidence map›Paper›PMID 21671133›Full record

ArticlePharmaceutical research2011

Enhanced topical and transdermal delivery of antineoplastic and antiviral acyclic nucleoside phosphonate cPr-PMEDAP.

Kateřina Vávrová, Petra Kovaříková, Barbora Skolová, Martina Líbalová, Jaroslav Roh, Robert Cáp, Antonín Holý, Alexandr Hrabálek

Abstract read
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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 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
0.8field-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

1 citing paper in PubMed, 9 citations in OpenAlex.

  1. 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

8 authors at 3 institutions in 1 country.

Kateřina VávrováCentre for New Antivirals and Antineoplastics Faculty of Pharmacy in Hradec Králové, Charles University in Prague, Hradec Králové, Czech Republic. katerina.vavrova@faf.cuni.cz
Petra Kovaříková
Barbora Skolová
Martina Líbalová
Jaroslav Roh
Robert Cáp
Antonín Holý
Alexandr Hrabálek
Charles University · CZUniversity Hospital Hradec Králové · CZCzech Academy of Sciences, Institute of Organic Chemistry and Biochemistry · CZ

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

purposeAcyclic nucleoside phosphonates possess unique antiviral and antineoplastic activities; however, their polar phosphonate moiety is associated with low ability to cross biological membranes. We explored the potential of transdermal and topical delivery of 2,6-diaminopurine derivative cPr-PMEDAP.

methodsIn vitro diffusion of cPr-PMEDAP was investigated using formulations at different pH and concentration and with permeation enhancer through porcine and human skin.

resultsAbility of 0.1-5% cPr-PMEDAP to cross human skin barrier was very low with flux values ~40 ng/cm(2)/h, the majority of compound found in the stratum corneum. The highest permeation rates were found at pH 6; increased donor concentration had no influence. The permeation enhancer dodecyl 6-dimethylaminohexanoate (DDAK, 1%) increased flux of cPr-PMEDAP (up to 61 times) and its concentration in nucleated epidermis (up to ~0.5 mg of cPr-PMEDAP/g of the tissue). No deamination of cPr-PMEDAP into PMEG occurred during permeation studies, but N-dealkylation into PMEDAP mediated by skin microflora was observed.

conclusionsTransdermal or topical application of cPr-PMEDAP enabled by the permeation enhancer DDAK may provide an attractive alternative route of administration of this potent antitumor and antiviral compound.

Indexed as

AdenineAdministration, CutaneousAnimalsAntineoplastic AgentsAntiviral AgentsCaproatesDimethylaminesDodecanolHumansHydrogen-Ion ConcentrationMethylaminesOrganophosphonatesPermeabilitySkinSwineAdenineAntineoplastic AgentsAntiviral AgentsCaproatesDimethylaminesDodecanoldodecyl 6-(dimethylamino)hexanoateMethylaminesN(6)-cyclopropyl-9-(2-phosphonylmethoxyethyl)-2,6-diaminopurineOrganophosphonates

Identifiers

PMID21671133
OpenAlexW1986873793

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.