Search results for " elimination half-life"

showing 2 items of 2 documents

Polyoxypregnanes as safe, potent, and specific ABCB1-inhibitory pro-drugs to overcome multidrug resistance in cancer chemotherapy in vitro and in vivo

2021

Multidrug resistance (MDR) mediated by ATP binding cassette subfamily B member 1 (ABCB1) is significantly hindering effective cancer chemotherapy. However, currently, no ABCB1-inhibitory drugs have been approved to treat MDR cancer clinically, mainly due to the inhibitor specificity, toxicity, and drug interactions. Here, we reported that three polyoxypregnanes (POPs) as the most abundant constituents of Marsdenia tenacissima (M. tenacissima) were novel ABCB1-modulatory pro-drugs, which underwent intestinal microbiota-mediated biotransformation in vivo to generate active metabolites. The metabolites at non-toxic concentrations restored chemosensitivity in ABCB1-overexpressing cancer cells v…

ABCC1 ATP binding cassette subfamily C member 1IC50 half maximal inhibitory concentrationMultidrug resistancePharmacologyNADPH reduced nicotinamide adenine dinucleotide phosphateF bioavailabilitychemistry.chemical_compoundPCR polymerase chain reaction0302 clinical medicineMDR multidrug resistanceECL electrochemiluminescencet1/2 elimination half-lifeLC–MS liquid chromatography coupled with mass spectrometryN.D. not detectedGeneral Pharmacology Toxicology and PharmaceuticsBBB blood–brain barriermedia_commonATF3 activating transcription factor 30303 health sciencesChemistryABC ATP-binding cassetteNMPA National Medical Products AdministrationPXR pregnane X receptorSDS-PAGE sodium dodecyl sulfate-polyacrylamide gel electrophoresisHBSS Hankʹs balanced salt solutionABCB1Combination chemotherapyProdrugMarsdenia tenacissimaCmax peak concentrationPaclitaxelGAPDH glyceraldehyde-3-phosphate dehydrogenase030220 oncology & carcinogenesisBHI brain heart infusionOriginal ArticleAUC0–∞ area under plasma concentration vs. time curveMRT mean residence timeDrugmedia_common.quotation_subjectRM1-950Vd volume of distributionABCB1 ATP binding cassette subfamily B member 1UIC-2 mouse monoclonal ABCB1 antibodyABCG2 ATP binding cassette subfamily G member 2Combination chemotherapyCYP cytochrome P450 isozymePI propidium iodideTEER transepithelial electrical resistance03 medical and health sciencesPBS phosphate buffer salineFBS fetal bovine serumDox doxorubicinIn vivoPOP polyoxypregnanemedicine030304 developmental biologyEVOM epithelial tissue voltohmmeterTmax time for peak concentrationCancerLBE lowest binding energyPE phycoerythrinmedicine.diseaseMultiple drug resistancePolyoxypregnanePapp apparent permeabilityN.A. not applicableCancer cellH&E hematoxylin and eosinMDR1a multidrug resistance protein 1aTherapeutics. PharmacologyqPCR quantitative PCRM. tenacissima Marsdenia tenacissimaCL clearanceSD standard derivationActa Pharmaceutica Sinica B
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In vitro evaluation of poloxamer in situ forming gels for bedaquiline fumarate salt and pharmacokinetics following intramuscular injection in rats

2019

Graphical abstract

In situPO Propylene oxideIV IntravenousP338 Poloxamer 338lcsh:RS1-441Pharmaceutical Sciencechemistry.chemical_compoundn Sample sizeSD Standard deviationIM Intramuscularchemistry.chemical_classificationC0 Analyte plasma concentration at time zeroDoE Design of experimentsUV UltravioletPharmacology. TherapyK2.EDTA Potassium ethylenediaminetetraacetic acidLC–MS/MS Liquid chromatography-tandem mass spectrometryH&E Hematoxylin and eosintmax Sampling time to reach the maximum observed analyte plasma concentrationIn situ forming gelsCMC Critical micellar concentrationCmax Maximum observed analyte plasma concentrationIntramuscular injectionDN Dose normalizedGPT Gel point temperaturePLGA Poly-(DL-lactic-co-glycolic acid)TFA Trifluoroacetic acidCAN AcetonitrileATP Adenosine 5′ triphosphateSalt (chemistry)Polyethylene glycolPoloxamerArticlelcsh:Pharmacy and materia medicaPharmacokineticsIn vivoUHPLC Ultra-high performance liquid chromatographyPharmacokineticsAUClast Area under the analyte concentration versus time curve from time zero to the time of the last measurable (non-below quantification level) concentrationEO Ethylene oxideNMP N-methyl-2-pyrrolidoneComputingMethodologies_COMPUTERGRAPHICSAUC∞ Area under the analyte concentration vs time curve from time zero to infinite timeP407 Poloxamer 407In vitro releasePoloxamerCMT Critical micellar temperatureGel erosionIn vitrot1/2 Apparent terminal elimination half-lifechemistryMDR-TB Multi-drug resistant tuberculosisAUC80h Area under the analyte concentration versus time curve from time zero to 80 htlast Sampling time until the last measurable (non-below quantification level) analyte plasma concentrationMRM Multiple reaction monitoringNuclear chemistrySustained releaseInternational Journal of Pharmaceutics: X
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