A mechanism enhancing macromolecule transport through paracellular spaces induced by Poly-L-Arginine: Poly-L-Arginine induces the internalization of tight junction proteins via clathrin-mediated endocytosis.

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 evaluate the use of an in vitro intestinal permeability model to predict rat and human absorption as well as to evaluate the use of an internal standard to control for intra- and inter-rat variability. METHODS:In vivo peroral absorption and in vitro steady-state intestinal permeability coefficients were det...

journal_title：Pharmaceutical research

authors： Dowty ME,Dietsch CR

更新日期：1997-12-01 00:00:00

abstract：PURPOSE:A thermodynamic analysis of the binding to rat cortex adenosine A1 receptor of N6-substituted (full agonists) and N6-substituted-deoxyribose (partial agonists) adenosine derivatives was performed. The intrinsic activity of the compounds was evaluated by measurements of the inhibition of forskolin stimulated 3',...

journal_title：Pharmaceutical research

authors： Dalpiaz A,Scatturin A,Pavan B,Varani K,IJzerman AP,Andrea Borea P

更新日期：1999-07-01 00:00:00

abstract：PURPOSE:To determine the extent of lateral spread and stratum corneum (SC) penetration of caffeine (CAF), hydrocortisone (HC) and ibuprofen (IBU) using a novel concentric tape stripping technique. METHOD:Ethanolic solutions of CAF, HC or IBU were applied to the forearm of 8 volunteers. At various time points, 10 succe...

journal_title：Pharmaceutical research

authors： Gee CM,Nicolazzo JA,Watkinson AC,Finnin BC

更新日期：2012-08-01 00:00:00

abstract：PURPOSE:To assess the uridine diphosphate (UDP)-glucuronosyltransferase (UGT) isozymes involved in the glucuronidation of niflumic acid in human liver. METHODS:The glucuronidation activity of niflumic acid was determined in liver microsomes and recombinant UGT isozymes by incubation of niflumic acid with UDP-glucuroni...

journal_title：Pharmaceutical research

authors： Mano Y,Usui T,Kamimura H

更新日期：2006-07-01 00:00:00

abstract：PURPOSE:1. The assessment of the role of hair follicles and sweat glands in skin resistance and percutaneous iontophoretic flux of 9-desglycinamide, 8-arginine vasopressin (DGAVP) by comparing two skin species: human stratum corneum which contained hair follicles, sweat and sebaceous glands, and shed snake skin which l...

journal_title：Pharmaceutical research

authors： Craane-van Hinsberg WH,Verhoef JC,Bax LJ,Junginger HE,Boddé HE

更新日期：1995-10-01 00:00:00

abstract：:Five aliphatic 5'-esters of 5-iodo-2'deoxyuridine (IDU) were synthesized via an acid chloride alcoholysis reaction. The solubility in pH 7.4 phosphate buffer, lipophilicity as determined by partition experiments in octanol/pH 7.4 buffer, and cytotoxicity of these potential prodrugs were evaluated. The esters showed a ...

journal_title：Pharmaceutical research

authors： Narurkar MM,Mitra AK

更新日期：1988-11-01 00:00:00

abstract：PURPOSE:The aim of this work was to develop a quantitative, flow cytometric method for tracking the endolysosomal escape of a fluorescently labelled saporin toxin. METHODS:Flow cytometric measurements of fluorescent pulse width and height were used to track the endocytic uptake into Daudi cells of a fluorescently labe...

journal_title：Pharmaceutical research

authors： Wensley HJ,Johnston DA,Smith WS,Holmes SE,Flavell SU,Flavell DJ

更新日期：2019-12-23 00:00:00

abstract：PURPOSE:Chemically modified heparin-DOCA was prepared and found to have markedly lower anticoagulant activity than heparin. In the present study, we elucidated the antiangiogenic and antitumoral activities of heparin-DOCA derivative. METHODS:To evaluate the antiangiogenic and antitumoral effects of heparin-DOCA, capil...

journal_title：Pharmaceutical research

authors： Park K,Kim YS,Lee GY,Nam JO,Lee SK,Park RW,Kim SY,Kim IS,Byun Y

更新日期：2007-01-01 00:00:00

abstract：:A simple viscometric method was used to quantify mucin-polymer bioadhesive bond strength. Viscosities of 15% (w/v) porcine gastric mucin dispersions in 0.1 N HCl (pH 1) or 0.1 N acetate buffer (pH 5.5) were measured with a Brookfield viscometer in the absence (eta m) or presence (eta t) of selected neutral, anionic, a...

journal_title：Pharmaceutical research

authors： Hassan EE,Gallo JM

更新日期：1990-05-01 00:00:00

abstract：PURPOSE:The aim of this study was to investigate the depth-dependent intradermal immunogenicity of inactivated polio vaccine (IPV) delivered by depth-controlled microinjections via hollow microneedles (HMN) and to investigate antibody response enhancing effects of IPV immunization adjuvanted with CpG oligodeoxynucleoti...

journal_title：Pharmaceutical research

authors： Schipper P,van der Maaden K,Romeijn S,Oomens C,Kersten G,Jiskoot W,Bouwstra J

更新日期：2016-09-01 00:00:00

abstract：PURPOSE:Permeation studies, with near infrared (NIR) light and anti-aggregation antibody formulation, were used to investigate the in vitro permeation of bevacizumab, ranibizumab and aflibercept through human sclera. METHODS:A vertical, spherical Franz cell diffusion apparatus was used for this scleral tissue permeati...

journal_title：Pharmaceutical research

authors： Giannos SA,Kraft ER,Zhao ZY,Merkley KH,Cai J

更新日期：2018-03-29 00:00:00

abstract：:Short-lived gamma emitting radioisotopes can be incorporated into polylactide/glycolide polymeric microspheres with various specific activities for possible use in understanding the in-vivo deposition, distribution and clearance of microparticulate drug carrier systems. The incorporated radiolabel is stable with negli...

journal_title：Pharmaceutical research

authors： Thanoo BC,Doll WJ,Mehta RC,Digenis GA,DeLuca PP

更新日期：1995-12-01 00:00:00

abstract：:The dermal route is an attractive route for vaccine delivery due to the easy skin accessibility and a dense network of immune cells in the skin. The development of microneedles is crucial to take advantage of the skin immunization and simultaneously to overcome problems related to vaccination by conventional needles (...

journal_title：Pharmaceutical research

authors： Leone M,Mönkäre J,Bouwstra JA,Kersten G

更新日期：2017-11-01 00:00:00

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

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

更新日期：2013-01-01 00:00:00

abstract：PURPOSE:To group microcrystalline celluloses (MCCs) using a combination of artificial neural network (ANN) and data clustering. METHODS:Radial basis function (RBF) network was used to model the torque measurements of the various MCCs. Output from the RBF network was used to group the MCCs using a data clustering techn...

journal_title：Pharmaceutical research

authors： Soh JL,Chen F,Liew CV,Shi D,Heng PW

更新日期：2004-12-01 00:00:00

abstract：PURPOSE:To investigate the effects of small aliphatic pendent groups conjugated through an acid-sensitive linker to the core of brushed block copolymer micelles on particle properties. METHODS:The brushed block copolymers were synthesized by conjugating five types of 2-alkanone (2-butanone, 2-hexanone, 2-octanone, 2-d...

journal_title：Pharmaceutical research

authors： Lee HJ,Bae Y

更新日期：2013-08-01 00:00:00

abstract：PURPOSE:The objective of this work was to assess, in vitro, the passage of P-glycoprotein dependent drugs across brain capillary endothelial cells, when these drugs are associated with a reversing agent. METHODS:An in vitro model of the blood-brain barrier consisting of a coculture of brain capillary endothelial cells...

journal_title：Pharmaceutical research

authors： Fenart L,Buée-Scherrer V,Descamps L,Duhem C,Poullain MG,Cecchelli R,Dehouck MP

更新日期：1998-07-01 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：PURPOSE:Stable transformants expressing human multidrug resistance 1 (MDR1), monkey MDR1, canine MDR1, rat MDR1a, rat MDR1b, mouse mdr1a, and mouse mdr1b in LLC-PK1 were established to investigate species differences in P-glycoprotein (P-gp, ABCB1) mediated efflux activity. METHODS:The seven cDNAs of MDR1 from five an...

journal_title：Pharmaceutical research

authors： Takeuchi T,Yoshitomi S,Higuchi T,Ikemoto K,Niwa S,Ebihara T,Katoh M,Yokoi T,Asahi S

更新日期：2006-07-01 00:00:00

abstract：OBJECTIVE:Amorphous pharmaceuticals, a viable approach to enhancing bioavailability, must be stable against crystallization. An amorphous drug can be stabilized by dispersing it in a polymer matrix. To implement this approach, it is desirable to know the drug's solubility in the chosen polymer, which defines the maxima...

journal_title：Pharmaceutical research

authors： Tao J,Sun Y,Zhang GG,Yu L

更新日期：2009-04-01 00:00:00

abstract：PURPOSE:To investigate the underlying cause for the observed differences in self-associating and viscoelastic behavior between two monoclonal antibodies, MAb1, and MAb2. METHODS:Several mutants were designed by swapping charged residues in MAb1 with those present in MAb2 at their respective positions and vice versa. R...

journal_title：Pharmaceutical research

authors： Yadav S,Sreedhara A,Kanai S,Liu J,Lien S,Lowman H,Kalonia DS,Shire SJ

更新日期：2011-07-01 00:00:00

abstract：PURPOSE:To analyze the mechanics of some pharmaceutical agglomerates during uniaxial confined compression by using compression parameters derived from the Heckel, Kawakita and Adams equations, and to study the influence of these compression parameters on the tablet-forming ability of agglomerates. METHODS:Force and di...

journal_title：Pharmaceutical research

authors： Nicklasson F,Alderborn G

更新日期：2000-08-01 00:00:00

abstract：:The fluxes of nitroglycerine (NG) through human abdominal epidermis from different individuals were measured in vitro at 32°C. The mean NG flux for the entire group was 16.9 µg/cm(2) × hr, with a standard deviation of 47.7%. There are no significant differences in the means and the variances of NG fluxes between males...

journal_title：Pharmaceutical research

authors： Langguth P,Spahn H,Mutschler E

更新日期：1986-02-01 00:00:00

abstract：:This paper describes an investigation of the use of poly(lactic/glycolic acid) polymers for long-term delivery of high molecular weight, water-soluble proteins. Poly(lactic/glycolic acid) (PLGA) microspheres, containing (fluorescein isothiocyanate)-labeled bovine serum albumin and (fluorescein isothiocyanate)-labeled ...

journal_title：Pharmaceutical research

authors： Cohen S,Yoshioka T,Lucarelli M,Hwang LH,Langer R

更新日期：1991-06-01 00:00:00

abstract：PURPOSE:This work investigated the effect of relative humidity (RH) on bipolar electrostatic charge profiles of dry powder inhaler aerosols using the Bipolar Charge Analyzer (BOLAR). METHODS:Two commercial products, Pulmicort® (400 μg, budesonide) and Bricanyl® (500 μg, terbutaline sulfate) Turbuhaler®, were used as m...

journal_title：Pharmaceutical research

authors： Yu J,Wong J,Ukkonen A,Kannosto J,Chan HK

更新日期：2017-08-01 00:00:00

abstract：:Semitelechelic poly[N-(2-hydroxypropyl)methacrylamide]s (ST-PHPMA) containing one amino end-group and differing in molecular weight were synthesized by radical polymerization in the presence of 2-aminoethanethiol (AET) as chain transfer agent. These polymers were covalently attached via amide bonds to the surface of n...

journal_title：Pharmaceutical research

authors： Kamei S,Kopecek J

更新日期：1995-05-01 00:00:00

abstract：PURPOSE:To provide the physicochemical properties of vitrified trehalose for predicting its recrystallization. METHODS:Thin films of vitrified trehalose solutions were prepared at room temperature and exposed to various humid and temperature atmospheres. The in-situ amount of retained water in the vacuum-dried trehalo...

journal_title：Pharmaceutical research

authors： Shirakashi R,Takano K

更新日期：2018-05-10 00:00:00

abstract：PURPOSE:To elucidate the apical and basolateral components of the total unstirred water layer in regular permeability experiment. METHODS:A novel stirring apparatus was constructed to remove the basolateral unstirred water layer. Caco-2 cells were used as the permeability barrier both in Transwell-type and side-by-sid...

journal_title：Pharmaceutical research

authors： Korjamo T,Heikkinen AT,Waltari P,Mönkkönen J

更新日期：2008-07-01 00:00:00

abstract：PURPOSE:Empirical formulae relate the mean size of primary droplets from jet and ultrasonic nebulizers to a fluid's physicochemical properties. Although the size selective "filtering" effects of baffling and evaporation may modify the secondary aerosol produced, this research sought to evaluate whether viscosity and su...

journal_title：Pharmaceutical research

authors： McCallion ON,Taylor KM,Thomas M,Taylor AJ

更新日期：1995-11-01 00:00:00