Evidence map›Paper›PMID 32524365›Full record

ArticlePharmaceutical research2020

Chase Dosing of Lipid Formulations to Enhance Oral Bioavailability of Nilotinib in Rats.

Niklas J Koehl, René Holm, Martin Kuentz, Brendan T Griffin

Abstract read
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Article in Pharmaceutical research, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
1.0field-weighted citation impact, top 24% 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

5 citing papers in PubMed, 11 citations in OpenAlex.

  1. Article
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  4. Review
  5. Molecular pharmaceutics · 2021
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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

4 authors at 3 institutions in 4 countries.

Niklas J KoehlSchool of Pharmacy, University College Cork, Cork, Ireland.
René HolmDrug Product Development, Janssen Research and Development, Johnson & Johnson, Turnhoutseweg 30, 2340, Beerse, Belgium.
Martin KuentzUniversity of Applied Sciences and Arts Northwestern Switzerland, Institute of Pharma Technology, Muttenz, Switzerland.
Brendan T GriffinSchool of Pharmacy, University College Cork, Cork, Ireland. Brendan.Griffin@ucc.ie.
University College Cork · IEFHNW University of Applied Sciences and Arts · CHRoskilde University · DK

Funding

Horizon 2020 674909
6 · The paper itself

Abstract

purposeLipid-based formulations (LBF) have shown oral bioavailability enhancement of lipophilic drugs, but not necessarily in the case of hydrophobic drugs. This study explored the potential of lipid vehicles to improve the bioavailability of the hydrophobic drug nilotinib comparing a chase dosing approach and lipid suspensions.

methodsNilotinib in vivo bioavailability in rats was determined after administering an aqueous suspension chase dosed with blank olive oil, Captex 1000, Peceol or Capmul MCM, respectively. Absolute bioavailability was determined (relative to an intravenous formulation). Pharmacokinetic parameters were compared to lipid suspensions.

resultsCompared to the lipid suspensions, the chase dosed lipids showed a 2- to 7-fold higher bioavailability. Both long chain chase dosed excipients also significantly increased the bioavailability up to 2-fold compared to the aqueous suspension. Deconvolution of the pharmacokinetic data indicated that chase dosing of nilotinib resulted in prolonged absorption compared to the aqueous suspension.

conclusionChase dosed LBF enhanced the in vivo bioavailability of nilotinib. Long chain lipids showed superior performance compared to medium chain lipids. Chase dosing appeared to prolong the absorption phase of the drug. Therefore, chase dosing of LBF is favourable compared to lipid suspensions for 'brick dust' molecules such as nilotinib. Graphical Abstract The potential of bio-enabling lipid vehicles, administered via chase dosing and lipid suspensions, has been evaluated as an approach to enhance oral bioavailability of nilotinib.

Indexed as

AnimalsBiological AvailabilityChemistry, PharmaceuticalDiglyceridesDose-Response Relationship, DrugExcipientsHydrophobic and Hydrophilic InteractionsLipidsLiposomesMaleMonoglyceridesOleic AcidsOlive OilPyrimidinesRatsRats, Sprague-DawleyCapmul MCMDiglyceridesExcipientsLipidsLiposomesMonoglyceridesnilotinibOleic AcidsOlive OilPeceolPyrimidinesSorafenibSuspensionsWaterbrick dust moleculechase dosinglipid based formulationlipid suspensionpoorly water-soluble drugs

Identifiers

PMID32524365
OpenAlexW3032974176

What OpenQuestion holds

Textmetadata
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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.