Transport of levofloxacin in the OK kidney epithelial cell line: interaction with p-aminohippurate transport.

Abstract:

PURPOSE:To evaluate the mechanism of renal transport of quinolone antibacterial drugs, we examined the interaction of levofloxacin with p-aminohippurate (PAH) transport systems and the transport of levofloxacin in renal epithelial cells. METHODS:Transport of [14C]PAH or [14C]levofloxacin was measured using OK cell monolayers grown on microporous membrane filters. RESULTS:Transcellular transport from the basolateral to the apical side and cellular accumulation of [14C]PAH were inhibited by levofloxacin. Both the initial uptake of [14C]PAH from the basolateral side and the efflux to the apical side were inhibited by levofloxacin. The basolateral-to-apical transcellular transport of [14C]levofloxacin was greater than that in the opposite direction. [14C]Levofloxacin efflux to the apical side was greater than that to the basolateral side. Unlabeled levofloxacin and grepafloxacin inhibited the transcellular transport of [14C]levofloxacin, accompanied by an increase of cellular accumulation. However, neither PAH nor an anion transport inhibitor 4-4'-diisothiocyanostilbene-2,2'-disulfonic acid (DIDS) affected the basolateral-to-apical transport of [14C]levofloxacin nor its uptake from the basolateral side. CONCLUSIONS:These results indicated that levofloxacin inhibits PAH transport across both the basolateral and apical membranes of OK cells, but are not transported via the systems for PAH transport. The existence of a specific transport system for quinolones was indicated in OK cells.

journal_name

Pharm Res

journal_title

Pharmaceutical research

authors

Matsuo Y,Yano I,Habu Y,Katsura T,Hashimoto Y,Inui K

doi

10.1023/a:1011012822437

subject

Has Abstract

pub_date

2001-05-01 00:00:00

pages

573-8

issue

5

eissn

0724-8741

issn

1573-904X

journal_volume

18

pub_type

杂志文章
  • Differential molar heat capacities to test ideal solubility estimations.

    abstract:PURPOSE:Calculation of the ideal solubility of a crystalline solute in a liquid solvent requires knowledge of the difference in the molar heat capacity at constant pressure of the solid and the supercooled liquid forms of the solute, delta Cp. Since this parameter is not usually known, two assumptions have been used to...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1012148910975

    authors: Neau SH,Bhandarkar SV,Hellmuth EW

    更新日期:1997-05-01 00:00:00

  • Antiangiogenic effect of docetaxel and everolimus as individual and dual-drug-loaded micellar nanocarriers.

    abstract:PURPOSE:The in vitro inhibitory effect of Docetaxel (DTX) and Everolimus (EVR) alone and together in poly(ethylene glycol)-block-poly(D,L-lactic acid) (PEG-b-PLA) nanocarriers on angiogenic processes and acute toxicity in mice was evaluated. METHODS:PEG-b-PLA DTX and/or EVR nanocarriers were characterized for size, dr...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-013-1188-z

    authors: Mishra GP,Doddapaneni BS,Nguyen D,Alani AW

    更新日期:2014-03-01 00:00:00

  • Pharmaceutical evaluation of gas-filled microparticles as gene delivery system.

    abstract:PURPOSE:To produce and characterize a nonviral ultrasound-controlled release system of plasmid DNA (pDNA) encapsulated in gas-filled poly(D,L-lactide-co-glycolide) microparticles (PLGA-MPs). METHODS:Different cationic polymers were used to form pDNA/polymer complexes to enhance the stability of pDNA during micropartic...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1014430631844

    authors: Seemann S,Hauff P,Schultze-Mosgau M,Lehmann C,Reszka R

    更新日期:2002-03-01 00:00:00

  • Histone H1-mediated transfection: serum inhibition can be overcome by Ca2+ ions.

    abstract:PURPOSE:One of the drawbacks of polycationic and cationic liposomal gene transfer is its sensitivity to serum. Gene therapy requires the transfectant-DNA complex to be resistant to serum as well as blood. Since Ca2+ has proved to be an efficient cofactor of polycationic gene transfer, we decided to investigate its effe...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1007581700996

    authors: Haberland A,Knaus T,Zaitsev SV,Buchberger B,Lun A,Haller H,Böttger M

    更新日期:2000-02-01 00:00:00

  • Nasal Administration of Cationic Nanoemulsions as Nucleic Acids Delivery Systems Aiming at Mucopolysaccharidosis Type I Gene Therapy.

    abstract:PURPOSE:This study demonstrates the nasal administration (NA) of nanoemulsions complexed with the plasmid encoding for IDUA protein (pIDUA) as an attempt to reach the brain aiming at MPS I gene therapy. METHODS:Formulations composed of DOPE, DOTAP, MCT (NE), and DSPE-PEG (NE-PEG) were prepared by high-pressure homogen...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-018-2503-5

    authors: Schuh RS,Bidone J,Poletto E,Pinheiro CV,Pasqualim G,de Carvalho TG,Farinon M,da Silva Diel D,Xavier RM,Baldo G,Matte U,Teixeira HF

    更新日期:2018-09-26 00:00:00

  • Paclitaxel-loaded poly(n-butylcyanoacrylate) nanoparticle delivery system to overcome multidrug resistance in ovarian cancer.

    abstract:PURPOSE:The aim of this study was to test the ability of paclitaxel-loaded poly(butylcyanoacrylate) (PBCA) nanoparticles to overcome multidrug resistance (MDR) in human ovarian resistant cells (A2780/T) and investigate its possible mechanism. METHODS:We prepared paclitaxel-loaded PBCA nanoparticles by interfacial poly...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-010-0346-9

    authors: Ren F,Chen R,Wang Y,Sun Y,Jiang Y,Li G

    更新日期:2011-04-01 00:00:00

  • Molecular structure and dynamics of cis(Z)-and trans(E)-flupenthixol and clopenthixol.

    abstract::The three-dimensional structures and molecular electrostatic potentials of the cis(Z) and trans(E)-isomers of flupenthixol and clopenthixol were examined by computer graphics and molecular mechanical and quantum mechanical calculations, and their internal molecular motions were studied by molecular dynamics simulation...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015842926345

    authors: Sylte I,Dahl SG

    更新日期:1991-04-01 00:00:00

  • Enhanced oral delivery of curcumin from N-trimethyl chitosan surface-modified solid lipid nanoparticles: pharmacokinetic and brain distribution evaluations.

    abstract:PURPOSE:Solid lipid nanoparticles (SLNs) have been proposed as a colloidal carrier system that could enhance the oral bioavailability of curcumin. However, a burst release of the loaded drug, which occurs in acidic environments, has been a main obstacle to the oral delivery of curcumin by using SLNs as a carrier system...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-014-1469-1

    authors: Ramalingam P,Ko YT

    更新日期:2015-02-01 00:00:00

  • Biodegradable poly(2-dimethylamino ethylamino)phosphazene for in vivo gene delivery to tumor cells. Effect of polymer molecular weight.

    abstract:PURPOSE:Previously, we have shown that complexes of plasmid DNA with the biodegradable polymer poly(2-dimethylamino ethylamino)phosphazene (p(DMAEA)-ppz) mediated tumor selective gene expression after intravenous administration in mice. In this study, we investigated the effect of p(DMAEA)-ppz molecular weight on both ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-007-9299-z

    authors: de Wolf HK,de Raad M,Snel C,van Steenbergen MJ,Fens MH,Storm G,Hennink WE

    更新日期:2007-08-01 00:00:00

  • Fuzzy modeling of skin permeability coefficients.

    abstract:PURPOSE:The purpose of this work was to determine whether a new modeling methodology using fuzzy logic c an predict skin permeability coefficients that are given compound descriptors that have been proven to affect percutaneous penetration. METHOD:Three fuzzy inference models were developed using subtractive clusterin...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1022273115847

    authors: Pannier AK,Brand RM,Jones DD

    更新日期:2003-02-01 00:00:00

  • The effect of engineered mannitol-lactose mixture on dry powder inhaler performance.

    abstract:PURPOSE:To co-crystallise mannitol and lactose with a view to obtaining crystals with more favourable morphological features than either lactose or mannitol alone, suitable for use as carriers in formulations for dry powder inhalers (DPIs) using simultaneous engineering of lactose-mannitol mixtures. METHODS:Mannitol a...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-012-0743-3

    authors: Kaialy W,Larhrib H,Martin GP,Nokhodchi A

    更新日期:2012-08-01 00:00:00

  • Site specific rectal drug administration in man with an osmotic system: influence on "first-pass" elimination of lidocaine.

    abstract::Lidocaine was administered to healthy volunteers at different sites in the rectum. Unchanged drug and monoethylglycinexylidide (MEGX) concentrations were measured in plasma with a newly developed gas chromatographic method. Lidocaine was given rectally by means of an osmotic system (Osmet(®)) which delivered 25 mg/h a...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/A:1016380104424

    authors: de Leede LG,de Boer AG,Feijen CD,Breimer DD

    更新日期:1984-05-01 00:00:00

  • Development of a sensitive activity assay for high-volume evaluation of human renin inhibitory peptides in rat serum: results with U-71,038.

    abstract::A sensitive activity assay for high volume evaluation of human renin inhibitory peptides (RIPs) in rat sera (range 2-80 ng/ml) was developed based on the low affinity of RIPs to rat renin and their high affinity to human renin. The utility of this activity assay was tested by measuring concentrations of a human RIP, U...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015883709275

    authors: Ruwart MJ,Sharma SK,Harris DW,Lakings DB,Rush BD,Wilkinson KF,Cornette JC,Evans DB,Friis JM,Cook KJ

    更新日期:1990-04-01 00:00:00

  • LXR alpha transactivates mouse organic solute transporter alpha and beta via IR-1 elements shared with FXR.

    abstract:PURPOSE:Recently identified organic solute transporter (Ost) alpha and beta are located on the basolateral membrane of enterocytes and may be responsible for the intestinal absorption of many substrates including bile acids. In the present study, the mechanism governing the transcriptional regulation of their expressio...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-006-9163-6

    authors: Okuwaki M,Takada T,Iwayanagi Y,Koh S,Kariya Y,Fujii H,Suzuki H

    更新日期:2007-02-01 00:00:00

  • Hollow fibers as an oral sustained-release delivery system using propranolol hydrochloride.

    abstract::Fibers were spun by the downward configuration of the wet spinning technique. This configuration is capable of encapsulating nonspherical and/or coarse particles. We examined encapsulation of propranolol hydrochloride and the ability of the fibers to act as a sustained-release delivery system for propranolol hydrochlo...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015982521706

    authors: Hussain MA,DiLuccio RC,Shefter E,Hurwitz AR

    更新日期:1989-12-01 00:00:00

  • Proofs of the structure of lipid coated nanoparticles (SMBV) used as drug carriers.

    abstract:PURPOSE:Supramolecular Biovectors (SMBV) consist of cross-linked cationic nanoparticles surrounded by a lipid membrane. The purpose was to study the structure of the lipid membrane and to characterise its interaction with the nanoparticles in order to differentiate SMBV from other polymer/lipid associations. METHODS:T...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1007504124603

    authors: De Miguel I,Imbertie L,Rieumajou V,Major M,Kravtzoff R,Betbeder D

    更新日期:2000-07-01 00:00:00

  • Stereoselective metabolism of bupropion by cytochrome P4502B6 (CYP2B6) and human liver microsomes.

    abstract:PURPOSE:Hydroxylation of the antidepressant and smoking deterrent drug bupropion is a clinically important bioactivation and elimination pathway. Bupropion hydroxylation is catalyzed selectively by cytochrome P4502B6 (CYP2B6). CYP2B6-catalyzed bupropion hydroxylation has been used as an in vitro and in vivo phenotypic ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-008-9535-1

    authors: Coles R,Kharasch ED

    更新日期:2008-06-01 00:00:00

  • Effect of vehicles on the maximum transepidermal flux of similar size phenolic compounds.

    abstract:PURPOSE:In principle, maximum transepidermal fluxes of solutes should be similar for different vehicles, except when the solute or vehicle modifies the skin. Here we estimated maximum flux, stratum corneum solubility, diffusivity and permeability coefficient for a range of similarly sized phenolic compounds with varyin...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-012-0846-x

    authors: Zhang Q,Li P,Liu D,Roberts MS

    更新日期:2013-01-01 00:00:00

  • In Vivo Stability of Therapeutic Proteins.

    abstract::Significant efforts are made to characterize molecular liabilities and degradation of the drug substance (DS) and drug product (DP) during various product life-cycle stages. The in vivo fate of a therapeutic protein is usually only considered in terms of pharmacokinetics (PKs) and pharmacodynamics (PDs). However, the ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章,评审

    doi:10.1007/s11095-019-2689-1

    authors: Schuster J,Koulov A,Mahler HC,Detampel P,Huwyler J,Singh S,Mathaes R

    更新日期:2020-01-03 00:00:00

  • High-performance liquid chromatographic (HPLC) assay using fluorescence detection for the simultaneous determination of gallopamil and norgallopamil in human plasma.

    abstract::Gallopamil is a calcium-channel antagonist with reported activity in experimental animals three to five times higher than that of verapamil. An automated high-performance liquid chromatographic (HPLC) method with fluorescence detection is described for the simultaneous determination of gallopamil and its metabolite no...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1016401405119

    authors: McLean AM,Babcock-Atkinson E,Rein K,Ruggirello DA,Gonzalez MA,Noonan PK

    更新日期:1987-08-01 00:00:00

  • Pharmacokinetic analysis and antiepileptic activity of tetra-methylcyclopropane analogues of valpromide.

    abstract:PURPOSE:The described structure pharmacokinetic pharmacodynamic relationships (SPPR) study explored the utilization of tetramethylcyclopropane analogues of valpromide (VPD), or tetramethylcyclopropane carboxamide derivatives of valproic acid (VPA) as new antiepileptics. METHODS:The study was carried out by investigati...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1016055517724

    authors: Bialer M,Hadad S,Kadry B,Abdul-Hai A,Haj-Yehia A,Sterling J,Herzig Y,Yagen B

    更新日期:1996-02-01 00:00:00

  • Induction of heme oxygenase-1 (HO-1) and NAD[P]H: quinone oxidoreductase 1 (NQO1) by a phenolic antioxidant, butylated hydroxyanisole (BHA) and its metabolite, tert-butylhydroquinone (tBHQ) in primary-cultured human and rat hepatocytes.

    abstract:PURPOSE:This study was aimed to investigate the effects of a phenolic antioxidant, butylated hydroxyanisole (BHA) and its metabolite, tert-butylhydroquinone (tBHQ) on the induction of HO-1, NQO1 and Nrf2 proteins and their regulatory mechanisms in primary-cultured hepatocytes. METHODS:After exposure of BHA and tBHQ to...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-006-9094-2

    authors: Keum YS,Han YH,Liew C,Kim JH,Xu C,Yuan X,Shakarjian MP,Chong S,Kong AN

    更新日期:2006-11-01 00:00:00

  • Amplification of butyrylcholinesterase and acetylcholinesterase genes in normal and tumor tissues: putative relationship to organophosphorous poisoning.

    abstract::Cholinesterases are ubiquitous carboxylesterase type B enzymes capable of hydrolyzing the neurotransmitter acetylcholine which are transiently expressed in multiple germline, embryonic, and tumor cells. The acute poisoning effects of various organophosphorous compounds are generally attributed to their irreversible co...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章,评审

    doi:10.1023/a:1015867021628

    authors: Soreq H,Zakut H

    更新日期:1990-01-01 00:00:00

  • Accelerated blood clearance phenomenon upon repeated injection of PEG-modified PLA-nanoparticles.

    abstract:PURPOSE:We recently developed prostaglandin E(1) (PGE(1))-encapsulated nanoparticles, prepared with a poly(lactide) homopolymer (PLA, Mw = 17,500) and monomethoxy poly(ethyleneglycol)-PLA block copolymer (PEG-PLA) (NP-L20). In this study, we tested whether the accelerated blood clearance (ABC) phenomenon is observed wi...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-009-9943-x

    authors: Ishihara T,Takeda M,Sakamoto H,Kimoto A,Kobayashi C,Takasaki N,Yuki K,Tanaka K,Takenaga M,Igarashi R,Maeda T,Yamakawa N,Okamoto Y,Otsuka M,Ishida T,Kiwada H,Mizushima Y,Mizushima T

    更新日期:2009-10-01 00:00:00

  • Characterization of therapeutic monoclonal antibodies reveals differences between in vitro and in vivo time-course studies.

    abstract:PURPOSE:To examine and determine the sites and the kinetics of IgG1 mAb modifications from both in vitro (rat plasma and PBS) and in vivo (rat model) time-course studies. METHODS:A comprehensive set of protein characterization methods, including RPLC/MS, LC-MS/MS, iCIEF, capSEC, and CE-SDS were performed in this repor...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-012-0860-z

    authors: Yin S,Pastuskovas CV,Khawli LA,Stults JT

    更新日期:2013-01-01 00:00:00

  • Compression behavior of orthorhombic paracetamol.

    abstract:PURPOSE:Orthorhombic crystals of paracetamol exhibit good technological properties during compression. The purpose of this study was to investigate the compression behavior of this substance and to compare it to that of monoclinic paracetamol. From the crystal structure, it could be hypothesized that sliding planes are...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1011954800246

    authors: Joiris E,Di Martino P,Berneron C,Guyot-Hermann AM,Guyot JC

    更新日期:1998-07-01 00:00:00

  • Supercooled smectic nanoparticles: a potential novel carrier system for poorly water soluble drugs.

    abstract:PURPOSE:The possibility of preparing nanoparticles in the supercooled thermotropic liquid crystalline state from cholesterol esters with saturated acyl chains as well as the incorporation of model drugs into the dispersions was investigated using cholesteryl myristate (CM) as a model cholesterol ester. METHODS:Nanopar...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/b:pham.0000045237.46019.6e

    authors: Kuntsche J,Westesen K,Drechsler M,Koch MH,Bunjes H

    更新日期:2004-10-01 00:00:00

  • Immunopotentiator-Loaded Polymeric Microparticles as Robust Adjuvant to Improve Vaccine Efficacy.

    abstract:PURPOSE:Adjuvants are required to ensure the efficacy of subunit vaccines. Incorporating molecular immunopotentiators within particles could overcome drawbacks of molecular adjuvants (such as solubility and toxicity), and improve adjuvanticity of particles, achieving stronger adjuvant activity. Aim of this study is to ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-015-1666-6

    authors: Zhang W,Wang L,Yang T,Liu Y,Chen X,Liu Q,Jia J,Ma G

    更新日期:2015-09-01 00:00:00

  • Assessment of blood-brain barrier permeability using the in situ mouse brain perfusion technique.

    abstract:PURPOSE:To assess the blood-brain barrier (BBB) permeability of 12 clinically-used drugs in mdr1a(+/+) and mdr1a(-/-) mice, and investigate the influence of lipophilicity, nonspecific brain tissue binding, and P-gp-mediated efflux on the rate of brain uptake. METHODS:The BBB partition coefficient (PS) was determined u...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-009-9876-4

    authors: Zhao R,Kalvass JC,Pollack GM

    更新日期:2009-07-01 00:00:00

  • Enhanced Anti-Tumor Efficacy of Lipid-Modified Platinum Derivatives in Combination with Survivin Silencing siRNA in Resistant Non-Small Cell Lung Cancer.

    abstract:PURPOSE:Cisplatin, is recognized as a first line therapeutic for the treatment of non-small cell lung cancer (NSCLC). Cisplatin resistance is identified as the most detrimental complication during treatment and has been associated with upregulation of several genes, such as the anti-apoptotic gene survivin. In this stu...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-016-2016-z

    authors: Mattheolabakis G,Ling D,Ahmad G,Amiji M

    更新日期:2016-12-01 00:00:00