FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2003143984> ?p ?o ?g. }

• W2003143984 endingPage "69" @default.
• W2003143984 startingPage "62" @default.
• W2003143984 abstract "The aim of the present study was to improve the inhibitory properties of poly(ethylene glycol) (PEG) as excipient in drug delivery systems by covalent attachment of thiol moieties. This was achieved by grafting PEG to polyethylenimine (PEI) and finally thiolation with γ-thiobutyrolatone. Furthermore, the potential of this novel thiolated PEG-g-PEI co-polymer on the transport of rhodamine-123 (Rho-123) as P-gp substrate across freshly excised rat intestinal mucosa was evaluated in Ussing-type chambers. Apparent permeability coefficients (Papp) were calculated and compared with values gained from experiments with the well-established P-gp inhibitors verapamil, reduced GSH, 6-mercatopurine and vitamin E-TPGS and the structurally similar compounds, myrj® 52 and brij® 35. The thiolated co-polymer displayed 145.07 ± 1.64 μmol/g of remaining primary amino groups, 84.30 ± 5.43 μmol/g of immobilized thiol groups and 12.74 ± 1.57 μmol/g of disulfide bonds. The approximate molecular mass of the thiolated co-polymer was 16,000 Da. The 1H-NMR spectrum of PEG-g-PEI co-polymer was characterized by the presence of signal groups of PEG, hexamethylene diisocyanate (HMDI) and PEI substructures. Studies with Caco-2 cells revealed that the thiolated co-polymer shows 6.69 ± 0.27% of cytotoxicity by LDH assay and 93.33 ± 0.07% of cell viability by MTT assay. The thiolated co-polymer in a concentration of 0.5% (w/v) displayed a more pronounced effect on the absorptive transport of Rho-123 (Papp = 15.2 ± 1.0 × 10−6 cm/s) in comparison to reduced GSH, 6-mercatopurine, vitamin E-TPGS, myrj® 52 and brij® 35. The thiolated co-polymer increased the transport of Rho-123 up to 3.3-fold in comparison to Rho-123 without any inhibitor used as control (Papp = 4.7 ± 0.1 × 10−6 cm/s). The thiolated co-polymer applied in a concentration of 0.1%, 0.25% and 0. 5% (w/v) did not only enhance the absorption but also decreased the secretory transport of Rho-123 resulting in efflux ratios (secretory Papp/absorptive Papp) of 1.0, 1.4 and 2.0, respectively. Because of these features the novel thiolated PEG-g-PEI co-polymer seems to exhibit promising properties as novel P-gp inhibitor." @default.
• W2003143984 created "2016-06-24" @default.
• W2003143984 creator A5031909295 @default.
• W2003143984 creator A5035632031 @default.
• W2003143984 creator A5042837610 @default.
• W2003143984 creator A5084211983 @default.
• W2003143984 date "2010-10-01" @default.
• W2003143984 modified "2023-10-12" @default.
• W2003143984 title "Design and in vitro evaluation of a novel polymeric P-glycoprotein (P-gp) inhibitor" @default.
• W2003143984 cites W110858387 @default.
• W2003143984 cites W141733981 @default.
• W2003143984 cites W1578745312 @default.
• W2003143984 cites W1963564206 @default.
• W2003143984 cites W1965973983 @default.
• W2003143984 cites W1992589600 @default.
• W2003143984 cites W2007580653 @default.
• W2003143984 cites W2014779616 @default.
• W2003143984 cites W2014809892 @default.
• W2003143984 cites W2016011381 @default.
• W2003143984 cites W2020718845 @default.
• W2003143984 cites W2030818672 @default.
• W2003143984 cites W2038039411 @default.
• W2003143984 cites W2041587333 @default.
• W2003143984 cites W2044213123 @default.
• W2003143984 cites W2051215695 @default.
• W2003143984 cites W2056698306 @default.
• W2003143984 cites W2058029995 @default.
• W2003143984 cites W2073909305 @default.
• W2003143984 cites W2093630016 @default.
• W2003143984 cites W2114918609 @default.
• W2003143984 cites W2121036187 @default.
• W2003143984 cites W2151067374 @default.
• W2003143984 doi "https://doi.org/10.1016/j.jconrel.2010.06.023" @default.
• W2003143984 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/20603165" @default.
• W2003143984 hasPublicationYear "2010" @default.
• W2003143984 type Work @default.
• W2003143984 sameAs 2003143984 @default.
• W2003143984 citedByCount "38" @default.
• W2003143984 countsByYear W20031439842012 @default.
• W2003143984 countsByYear W20031439842013 @default.
• W2003143984 countsByYear W20031439842014 @default.
• W2003143984 countsByYear W20031439842015 @default.
• W2003143984 countsByYear W20031439842016 @default.
• W2003143984 countsByYear W20031439842017 @default.
• W2003143984 countsByYear W20031439842018 @default.
• W2003143984 countsByYear W20031439842019 @default.
• W2003143984 countsByYear W20031439842020 @default.
• W2003143984 countsByYear W20031439842021 @default.
• W2003143984 countsByYear W20031439842022 @default.
• W2003143984 countsByYear W20031439842023 @default.
• W2003143984 crossrefType "journal-article" @default.
• W2003143984 hasAuthorship W2003143984A5031909295 @default.
• W2003143984 hasAuthorship W2003143984A5035632031 @default.
• W2003143984 hasAuthorship W2003143984A5042837610 @default.
• W2003143984 hasAuthorship W2003143984A5084211983 @default.
• W2003143984 hasConcept C10138342 @default.
• W2003143984 hasConcept C104317684 @default.
• W2003143984 hasConcept C12554922 @default.
• W2003143984 hasConcept C13245373 @default.
• W2003143984 hasConcept C13965031 @default.
• W2003143984 hasConcept C162324750 @default.
• W2003143984 hasConcept C178790620 @default.
• W2003143984 hasConcept C185592680 @default.
• W2003143984 hasConcept C188027245 @default.
• W2003143984 hasConcept C202751555 @default.
• W2003143984 hasConcept C2775925850 @default.
• W2003143984 hasConcept C2777516009 @default.
• W2003143984 hasConcept C2779820397 @default.
• W2003143984 hasConcept C2780020223 @default.
• W2003143984 hasConcept C2780783641 @default.
• W2003143984 hasConcept C43617362 @default.
• W2003143984 hasConcept C521977710 @default.
• W2003143984 hasConcept C53227056 @default.
• W2003143984 hasConcept C54009773 @default.
• W2003143984 hasConcept C54400483 @default.
• W2003143984 hasConcept C55493867 @default.
• W2003143984 hasConcept C71240020 @default.
• W2003143984 hasConcept C86803240 @default.
• W2003143984 hasConceptScore W2003143984C10138342 @default.
• W2003143984 hasConceptScore W2003143984C104317684 @default.
• W2003143984 hasConceptScore W2003143984C12554922 @default.
• W2003143984 hasConceptScore W2003143984C13245373 @default.
• W2003143984 hasConceptScore W2003143984C13965031 @default.
• W2003143984 hasConceptScore W2003143984C162324750 @default.
• W2003143984 hasConceptScore W2003143984C178790620 @default.
• W2003143984 hasConceptScore W2003143984C185592680 @default.
• W2003143984 hasConceptScore W2003143984C188027245 @default.
• W2003143984 hasConceptScore W2003143984C202751555 @default.
• W2003143984 hasConceptScore W2003143984C2775925850 @default.
• W2003143984 hasConceptScore W2003143984C2777516009 @default.
• W2003143984 hasConceptScore W2003143984C2779820397 @default.
• W2003143984 hasConceptScore W2003143984C2780020223 @default.
• W2003143984 hasConceptScore W2003143984C2780783641 @default.
• W2003143984 hasConceptScore W2003143984C43617362 @default.
• W2003143984 hasConceptScore W2003143984C521977710 @default.
• W2003143984 hasConceptScore W2003143984C53227056 @default.
• W2003143984 hasConceptScore W2003143984C54009773 @default.
• W2003143984 hasConceptScore W2003143984C54400483 @default.

• next