Different Efflux Transporter Affinity and Metabolism of 99mTc-2-Methoxyisobutylisonitrile and 99mTc-Tetrofosmin for Multidrug Resistance Monitoring in Cancer.

abstract：:The delivery of therapeutic nucleic acids to neurons has the potential to treat neurological disease and spinal cord injury. While select viral vectors have shown promise as gene carriers to neurons, their potential as therapeutic agents is limited by their toxicity and immunogenicity, their broad tropism, and the cos...

journal_title：Pharmaceutical research

authors： Bergen JM,Park IK,Horner PJ,Pun SH

更新日期：2008-05-01 00:00:00

abstract：PURPOSE:Tissue partitioning is an important component of drug distribution and half-life. Protein binding and lipid partitioning together determine drug distribution. METHODS:Two structure-based models to predict partitioning into microsomal membranes are presented. An orientation-based model was developed using a mem...

journal_title：Pharmaceutical research

authors： Nagar S,Korzekwa K

更新日期：2017-03-01 00:00:00

abstract：PURPOSE:SN-38, a potent chemotherapeutic drug, has not been used clinically because of its severe side effects and poor solubility. In this work, we aimed to evaluate the effect of dose and multiple injections of SN-38-loaded polymeric depots on antitumor efficacy and toxicity in vivo. METHODS:Preparation and characte...

journal_title：Pharmaceutical research

authors： Manaspon C,Nasongkla N,Chaimongkolnukul K,Nittayacharn P,Vejjasilpa K,Kengkoom K,Boongird A,Hongeng S

更新日期：2016-12-01 00:00:00

abstract：:A method is described for the assay of phenobarbital N-glucosylation using UDP-D-[6-3H]glucose. The radioactive phenobarbital N-glucoside conjugates [(5R)-PBG, (5S)-PBG] formed during the incubations were resolved from each other and from uncharacterized radioactive products by semipreparative HPLC. The product ratio ...

journal_title：Pharmaceutical research

authors： Soine WH,Safi H,Westkaemper RB

更新日期：1992-05-01 00:00:00

abstract：PURPOSE:To design and synthesize fatty acid-RGD peptide amphiphiles with ADA linker for their potential delivery of hydrophobic drugs like paclitaxel targeted to α(v)β(3) integrin overexpressing tumors. METHODS:Four amphiphiles - C16 or C18 fatty acid-RGD peptide and ADA linker were designed and synthesized. CMC, size...

journal_title：Pharmaceutical research

authors： Javali NM,Raj A,Saraf P,Li X,Jasti B

更新日期：2012-12-01 00:00:00

abstract：PURPOSE:Previously, a respirable powder (RP) formulation of pirfenidone (PFD) was developed for reducing phototoxic risk; however, PFD-RP demonstrated unacceptable in vitro inhalation performance. The present study aimed to develop a new RP system of PFD with favorable inhalation properties by spray-drying method. MET...

journal_title：Pharmaceutical research

authors： Seto Y,Suzuki G,Leung SS,Chan HK,Onoue S

更新日期：2016-06-01 00:00:00

abstract：PURPOSE:To determine whether a Protected Graft Copolymer (PGC) containing fatty acid can be used as a stabilizing excipient for GLP-1 and whether PGC/GLP-1 given once a week can be an effective treatment for diabetes. METHODS:To create a PGC excipient, polylysine was grafted with methoxypolyethyleneglycol and fatty ac...

journal_title：Pharmaceutical research

authors： Castillo GM,Reichstetter S,Bolotin EM

更新日期：2012-01-01 00:00:00

abstract：:A new transdermal therapeutic system (TTS) for nitroglycerin is presented that controls release of the active substance by means of desorption and diffusion. The drug release, in the dosage range examined under sink conditions, is independent of electrolytes and pH of the aqueous acceptor medium, but it does depend on...

journal_title：Pharmaceutical research

authors： Wolff M,Cordes G,Luckow V

更新日期：1985-01-01 00:00:00

abstract：PURPOSE:The purpose of this research was to evaluate the effect of ultrasound on mass transport across fetal membrane for direct fetal drug delivery and sensing of the amniotic fluid in a noninvasive manner. METHODS:Post-delivery human fetal membranes (chorioamnion) were used for in vitro experiments, in which the eff...

journal_title：Pharmaceutical research

authors： Wolloch L,Azagury A,Goldbart R,Traitel T,Groisman G,Hallak M,Kost J

更新日期：2015-02-01 00:00:00

abstract：:Various derivatives of the C-terminal amide group in N-protected amino acid and peptide amides were synthesized to assess their suitability as prodrug forms with the aim of protecting the amide or peptide bond against cleavage by alpha-chymotrypsin. Whereas N-acetylation, N-hydroxymethylation, and N-phthalidylation di...

journal_title：Pharmaceutical research

authors： Kahns AH,Bundgaard H

更新日期：1991-12-01 00:00:00

abstract：PURPOSE:The heparin-paclitaxel conjugates using amino acid as linker (HD2), with low anticoagulant activity, the similar anticancer activity as paclitaxel, offer great potential for further investigation. METHODS:Two types of heparin-paclitaxel conjugates (HD) have been developed, in which O-acetylated heparin as carr...

journal_title：Pharmaceutical research

authors： Wang Y,Xin D,Liu K,Xiang J

更新日期：2009-04-01 00:00:00

abstract：PURPOSE:The aim of the study is to determine whether a biodegradable elastomeric device that uses an osmotic pressure delivery mechanism can release different therapeutic proteins at a nearly constant rate in nanomolar concentrations with high bioactivity, given the same formulation conditions. Vascular endothelial gro...

journal_title：Pharmaceutical research

authors： Gu F,Neufeld R,Amsden B

更新日期：2006-04-01 00:00:00

abstract：:Intranasal route continues to be one of the main focuses of drug delivery research. Although it is generally perceived that the nasal route could avoid the first-pass metabolism in liver and gastrointestinal tract, the role of metabolic conversions in systemic and brain-targeted deliveries of the parent compounds and ...

journal_title：Pharmaceutical research

authors： Wong YC,Zuo Z

更新日期：2010-07-01 00:00:00

abstract：PURPOSE:Modulating sialylation of therapeutic glycoproteins may be used to influence their clearance and systemic exposure. We studied the effect of low and high sialylated IL4-10 fusion protein (IL4-10 FP) on in vitro and in vivo bioactivity and evaluated the effect of differential sialylation on pharmacokinetic param...

journal_title：Pharmaceutical research

authors： Steen-Louws C,Boross P,Prado J,Meeldijk J,Langenhorst JB,Huitema ADR,den Hartog MT,Boon L,Lafeber FPJG,Hack CE,Eijkelkamp N,Popov-Celeketic J

更新日期：2019-12-26 00:00:00

abstract：PURPOSE:To examine whether the glass transition temperature (Tg) of freeze-dried formulations containing polymer excipients can be accurately predicted by molecular dynamics simulation using software currently available on the market. Molecular dynamics simulations were carried out for isomaltodecaose, a fragment of de...

journal_title：Pharmaceutical research

authors： Yoshioka S,Aso Y,Kojima S

更新日期：2003-06-01 00:00:00

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

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

更新日期：2002-03-01 00:00:00

abstract：PURPOSE:LY3015014 is a humanized immunoglobulin G4 (IgG4) monoclonal antibody that binds to the catalytic domain of PCSK9 and reduce low-density lipoprotein cholesterol (LDL-C) in patients with hypercholesterolemia that is poorly controlled by maximally tolerated statin therapy. The objective of this pharmacokinetic/ph...

journal_title：Pharmaceutical research

authors： Shen T,James DE,Krueger KA

更新日期：2017-01-01 00:00:00

abstract：:Lecithin-stabilized triglyceride emulsions are subject to hydrolysis by pancreatic lipase. The time profiles of these reactions are characterized by a lag-phase and a zero-order phase. Lag phases are more pronounced with long-chain triglycerides. Ca2+ is effective in reducing the lag-phase and activating lipase. Kinet...

journal_title：Pharmaceutical research

authors： Alvarez FJ,Stella VJ

更新日期：1989-06-01 00:00:00

abstract：PURPOSE:The sensitivity and effectiveness of indirect metrics proposed for the assessment of comparative absorption rates in bioequivalence studies [Cmax, Tmax, partial AUC (AUCp), feathered slope (SLf), intercept metric (I)] were originally tested by assuming first-order absorption. The present study re-evaluates thei...

journal_title：Pharmaceutical research

authors： Ring A,Tothfalusi L,Endrenyi L,Weiss M

更新日期：2000-05-01 00:00:00

abstract：PURPOSE:Bioavailability of orally administered drugs is much influenced by the behavior, performance and fate of the dosage form within the gastrointestinal (GI) tract. Therefore, MRI in vivo methods that allow for the simultaneous visualization of solid oral dosage forms and anatomical structures of the GI tract have ...

journal_title：Pharmaceutical research

authors： Christmann V,Rosenberg J,Seega J,Lehr CM

更新日期：1997-08-01 00:00:00

abstract：PURPOSE:Anticancer chemotherapy usually involves the administration of several anticancer drugs that differ in their action mechanisms. Here, we aimed to test whether the combination of omacetaxine mepesuccinate (OMT) and doxorubicin (DOX) could show synergism, and whether the liposomal co-delivery of these two drugs c...

journal_title：Pharmaceutical research

authors： Shim G,Lee S,Choi J,Lee S,Kim CW,Oh YK

更新日期：2014-08-01 00:00:00

abstract：:Gene delivery systems are designed to control the location of administered therapeutic genes within a patient's body. Successful in vivo gene transfer may require (i) the condensation of plasmid and its protection from nuclease degradation, (ii) cellular interaction and internalization of condensed plasmid, (iii) esca...

journal_title：Pharmaceutical research

authors： Mahato RI,Rolland A,Tomlinson E

更新日期：1997-07-01 00:00:00

abstract：PURPOSE:Indomethacin is well known to be metabolized via O-demethylation and N-deacylation. In this paper we found an enzyme involved in the hydrolysis of amide-linkage of indomethacin and partially characterized it as well as its substrate specificity. METHODS:An indomethacin hydrolyzing enzyme was purified to homoge...

journal_title：Pharmaceutical research

authors： Terashima K,Takai S,Usami Y,Adachi T,Sugiyama T,Katagiri Y,Hirano K

更新日期：1996-09-01 00:00:00

abstract：PURPOSE:Evidence suggests that uremic toxins such as hippurate (HA), indoleacetate (IA), indoxyl sulfate (IS), and 3-carboxy-4-methyl-5-propyl-2-furanpropionate (CMPF) promote the progression of renal failure by damaging tubular cells via rat organic anion transporter 1 (rOat1) and rOat3 on the basolateral membrane of ...

journal_title：Pharmaceutical research

authors： Deguchi T,Kouno Y,Terasaki T,Takadate A,Otagiri M

更新日期：2005-04-01 00:00:00

abstract：PURPOSE:The discovery of nano drug delivery system has rendered a great hope for improving cancer therapy. However, there are some inevitable obstacles that constrain its development, such as the physical and biological barriers, the toxicity of carrier materials and the physiological toxicity of drugs. Here, we report...

journal_title：Pharmaceutical research

authors： Zhang Z,Yu M,An T,Yang J,Zou M,Zhai Y,Sun W,Cheng G

更新日期：2019-12-10 00:00:00

abstract：PURPOSE:The objective of this study was to determine the influence of the peptide bond with emphasis on the carbonyl group on the interaction with and transport by the intestinal small-peptide carrier. Therefore enalapril, a known substrate for the small-peptide carrier, has been modified to an analogue with a reduced ...

journal_title：Pharmaceutical research

authors： Schoenmakers RG,Stehouwer MC,Tukker JJ

更新日期：1999-01-01 00:00:00

abstract：PURPOSE:Knowledge about the uptake mechanism and subsequent intracellular routing of non-viral gene delivery systems is important for the development of more efficient carriers. In this study we compared two established cationic polymers pDMAEMA and PEI with regard to their transfection efficiency and mechanism of cell...

journal_title：Pharmaceutical research

authors： van der Aa MA,Huth US,Häfele SY,Schubert R,Oosting RS,Mastrobattista E,Hennink WE,Peschka-Süss R,Koning GA,Crommelin DJ

更新日期：2007-08-01 00:00:00

abstract：PURPOSE:This work describes a method for functionalisation of nanoparticle surfaces with hydrophilic "nano-shields" and the application of advanced surface characterisation to determine PEG amount and accumulation at the outmost 10 nm surface that is the predominant factor in determining protein and cellular interactio...

journal_title：Pharmaceutical research

authors： Ebbesen MF,Whitehead B,Ballarin-Gonzalez B,Kingshott P,Howard KA

更新日期：2013-07-01 00:00:00

abstract：PURPOSE:To investigate the effect of benzofusion on NO donor properties and related biological activities of the furoxan system. The biological properties considered were the ability to increase the cytosolic levels of cGMP in C6 cells and vasodilation. METHODS:NO donor properties were investigated either in the prese...

journal_title：Pharmaceutical research

authors： Medana C,Di Stilo A,Visentin S,Fruttero R,Gasco A,Ghigo D,Bosia A

更新日期：1999-06-01 00:00:00

abstract：PURPOSE:To investigate the suitability of three antimicrobial peptides (AMPs) as cell-penetrating antimicrobial peptides. METHODS:Cellular uptake of three AMPs (PK-12-KKP, SA-3 and TPk) and a cell-penetrating peptide (penetratin), all 5(6)-carboxytetramethylrhodamine-labeled, were tested in HeLa WT cells and analyzed ...

journal_title：Pharmaceutical research

authors： Bahnsen JS,Franzyk H,Sayers EJ,Jones AT,Nielsen HM

更新日期：2015-05-01 00:00:00