Evidence map›Paper›PMID 19283769›Full record

ArticleJournal of pharmaceutical sciences2009

Investigation of the micellar effect of pluronic P85 on P-glycoprotein inhibition: cell accumulation and equilibrium dialysis studies.

Naveed Shaik, Nagdeep Giri, William F Elmquist

Open access · greenAbstract read
In one paragraph

Article in Journal of pharmaceutical sciences, 2009. 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
1.2field-weighted citation impact, top 21% 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, 29 citations in OpenAlex.

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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 1 institution in 1 country.

Naveed ShaikDepartment of Pharmaceutics, College of Pharmacy, University of Minnesota, 308 Harvard St. SE, Minneapolis, Minnesota 55455, USA.
Nagdeep Giri
William F Elmquist
University of Minnesota · US

Funding

Improving the CNS Delivery of Anti-retroviral CompoundsR01NS042549 · NINDS · UNIVERSITY OF MINNESOTA TWIN CITIES · PI ELMQUIST, WILLIAM · 2002 to 2007
$1.4M
NINDS NIH HHS NS42549NINDS NIH HHS R01 NS042549
6 · The paper itself

Abstract

The objective of this study was: (1) to characterize the P-gp inhibitory effect of different concentrations of Pluronic P85 on anti-HIV-1 drug cellular accumulation, and (2) to investigate the relationship between cellular accumulation and free fraction of drug. Cellular accumulation studies in MDCKII-WT and MDCKII-MDR1 cell monolayers showed a biphasic dose response characterized by decline in accumulation at Pluronic concentrations greater than the CMC. This phenomenon was independent of the inhibition of P-gp efflux by Pluronic. Cell-free equilibrium dialysis was used to determine the effect of Pluronic P85 on drug free fraction and the affinity of Pluronic micelles for drug was modeled. Nelfinavir and saquinavir associated extensively with micelles and equilibrium free fractions were low at P85 concentrations above the CMC, with association constants being in the order nelfinavir > saquinavir >>> abacavir. Abacavir, a P-gp substrate, showed no association with micelles yet showed a biphasic response in cellular accumulation. These data suggest that, above the CMC, inhibition of P-gp is not affected but rather factors such as micellar trapping could contribute to decreased accumulation. Therefore, the in vitro evaluation of the effect of Pluronic formulations on active transport should take into account both the physicochemical properties of drug and the composition of Pluronic.

Indexed as

AbacavirAcridinesAnimalsATP Binding Cassette Transporter, Subfamily B, Member 1Biological Transport, ActiveCell-Free SystemCell LineCellsDialysisDideoxynucleosidesDiphenylhexatrieneDogsDose-Response Relationship, DrugDrug Resistance, MultipleFluorescent DyesHIV-1AbacavirAcridinesATP Binding Cassette Transporter, Subfamily B, Member 1DideoxynucleosidesDiphenylhexatrieneElacridarFluorescent DyesMannitolMicellesNelfinavirPoloxamerProtease InhibitorsSaquinavirSurface-Active AgentsTetrahydroisoquinolines

Identifiers

PMID19283769
PMCPMC2755653
OpenAlexW2076910870

What OpenQuestion holds

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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.