Abstract：
PURPOSE:To identify and quantify, in vitro and in vivo (in humans), the charge-carrying species during transdermal iontophoresis of lidocaine hydrochloride as a function of the concentration of drug relative to that of sodium chloride in the anodal solution. METHODS:In vitro experiments in standard diffusion cells quantified lidocaine delivery and the outward migration of chloride across the skin. Electrotransport of Na+ was inferred by difference, allowing transport numbers of the three main charge-carrying species to be deduced. In vivo, outward electrotransport of Cl- was measured and compared to the corresponding in vitro results. RESULTS:The transport number of lidocaine increased linearly with increasing mole fraction and reached 0.15-0.20 at X(L) = 1.0. In the absence of Na+, most of the charge was carried by Cl- (>80%) despite the skin retaining its net negative charge and cation permselectivity. In vivo data correlated very well with in vitro results. CONCLUSIONS:The mole faction of drug (relative to competing ions of like polarity) is the crucial determinant of the extent to which it can carry charge across the skin during iontophoresis. The outward electromigration of Cl-, in the sense opposite to drug delivery, may offer a useful means by which to optimize iontophoretic efficiency in the absence of competing cations in the anode formulation.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Marro D,Kalia YN,Delgado-Charro MB,Guy RHdoi
10.1023/a:1013370529366subject
Has Abstractpub_date
2001-12-01 00:00:00pages
1709-13issue
12eissn
0724-8741issn
1573-904Xjournal_volume
18pub_type
杂志文章abstract：PURPOSE:To create poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs), where a drug-encapsulating NP core is covered with polyethylene glycol (PEG) in a normal condition but exposes a cell-interactive TAT-modified surface in an environment rich in matrix metalloproteinases (MMPs). METHODS:PLGA NPs were modified w...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1039-y
更新日期：2013-08-01 00:00:00
abstract：PURPOSE:To monitor the biodistribution of IgG1 aggregates upon subcutaneous (SC) and intravenous (IV) administration in mice and measure their propensity to stimulate an early immune response. METHODS:A human mAb (IgG1) was fluorescently labeled, aggregated by agitation stress and injected in SKH1 mice through SC and ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1154-9
更新日期：2014-01-01 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
pub_type： 杂志文章
doi：10.1023/a:1011913723928
更新日期：1998-07-01 00:00:00
abstract：:Pediatric brain tumors are most common cancers in childhood and among the leading causes of death in children. Chemotherapy has been used as adjuvant (i.e. after) or neoadjuvant (i.e. before) therapy to surgery and radiotherapy for the management of pediatric brain tumors for more than four decades and gained more att...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1007/s11095-013-1196-z
更新日期：2014-03-01 00:00:00
abstract：:We studied the effects of two verapamil analogs, anipamil and ronipamil, in traumatic shock. Noble-Collip drum trauma produced a shock state characterized by an eight-fold increase in plasma cathepsin D activity, a 13-fold increase in the rate of plasma myocardial depressant factor (MDF) accumulation, and a survival t...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/A:1016363316777
更新日期：1985-05-01 00:00:00
abstract：:High molecular weight drugs in general, and peptides in particular, are usually delivered by parenteral route because they are poorly absorbed or degraded in the gastrointestinal tract. To optimize therapy, it is desirable to search for nonparenteral routes of administration and to deliver the drug in a controlled-rel...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018948924992
更新日期：1993-06-01 00:00:00
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
更新日期：2013-01-01 00:00:00
abstract：PURPOSE:The addition of high amounts of calcium remains a pharmaceutical concern due to its precipitation with phosphate in total parenteral nutrient (TPN) admixtures, compromising also the stability of the lipid emulsion. MATERIALS AND METHODS:Calcium-phosphate solubility was compared when using binary PN solutions v...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-008-9671-7
更新日期：2008-11-01 00:00:00
abstract：:A fluorescence measurement system and methods of data analysis were developed to measure rapid kinetics of transdermal transport in vitro. Three variations on the technique were demonstrated, where the receptor compartment concentration was determined by: 1) fluorescence measurements of aliquots removed at discrete ti...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016254013374
更新日期：1995-04-01 00:00:00
abstract：:Aucubin, a promising hepatoprotecting iridoid glucoside, was given intravenously (iv), orally (po), intraperitoneally (ip), and hepatoportally (pv) to rats. A linear pharmacokinetic behavior was obtained after iv administation of 400-400 mg/kg of aucubin. The half-life of aucubin in the postdistributive phase (t1/2, b...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015821527621
更新日期：1991-08-01 00:00:00
abstract：PURPOSE:To evaluate the reaction of a large series of pharmacologically significant 1,4-dihydropyridine (1,4-DHP) compounds with superoxide (O2.-) in dimethylsulfoxide using differential pulse voltammetry and controlled potential electrolysis. METHODS:Differential pulse voltammetry was used to track the consumption of...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1022291624933
更新日期：2003-02-01 00:00:00
abstract：:A two-step analytic procedure to determine the rate and extent of metabolite production following administration of the parent compound is described. The procedure provides the rate and extent of metabolite production as a function of time by application of the general model independent approach of deconvolution. The ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015951426191
更新日期：1988-06-01 00:00:00
abstract：PURPOSE:The work aims at investigating the correlation of water sorption potential with different measures of molecular mobility in an annealed amorphous model compound (trehalose). METHODS:Amorphous trehalose, prepared by freeze-drying, was annealed at 100°C (17°C < T (g)) for up to 120 h. Global mo...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-012-0910-6
更新日期：2013-03-01 00:00:00
abstract：PURPOSE:This study focuses on the formulation optimization, in vitro and in vivo performance of differently sized nano-crystalline liquid suspensions and spray-dried powders of a poorly soluble BCS class II compound i.e. Danazol. METHODS:A DoE approach was utilized to optimize stabilizer concentration and formulate da...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-014-1567-0
更新日期：2015-05-01 00:00:00
abstract：PURPOSE:Typical methods to study pMDI sprays employ particle sizing or visible light diagnostics, which suffer in regions of high spray density. X-ray techniques can be applied to pharmaceutical sprays to obtain information unattainable by conventional particle sizing and light-based techniques. METHODS:We present a t...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-016-1869-5
更新日期：2016-05-01 00:00:00
abstract：PURPOSE:Since glomerular filtration rate (GFR) is responsible for the elimination of a large number of water-soluble drugs, the aim of this study was to develop a semi-physiological function for GFR maturation from neonates to adults. METHODS:In the pharmacokinetic analysis (NONMEM VI) based on data of gentamicin, tob...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-014-1361-z
更新日期：2014-10-01 00:00:00
abstract：PURPOSE:The in-situ particle size of delavirdine mesylate in dry mix and tablets was determined. METHODS:Optical microscopy and fluorescence microscopy combined with image analysis were used for qualitative and quantitative measurements. RESULTS:Using optical microscopy, it was demonstrated qualitatively that fragmen...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018875130152
更新日期：1999-04-01 00:00:00
abstract：:Esmolol hydrochloride degrades in aqueous solutions by the hydrolysis of a labile aliphatic carboxyester group. The products are methanol and ASL-8123. The resulting aliphatic carboxylic acid moiety (ASL-8123) has a pK of 4.80, which is within 1 pH unit of the pH of the formulation. ASL-8123 therefore acts as a "secon...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015973425708
更新日期：1988-08-01 00:00:00
abstract：:Magnetic nanoparticles are useful as contrast agents for magnetic resonance imaging (MRI). Paramagnetic contrast agents have been used for a long time, but more recently superparamagnetic iron oxide nanoparticles (SPIOs) have been discovered to influence MRI contrast as well. In contrast to paramagnetic contrast agent...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1007/s11095-012-0711-y
更新日期：2012-05-01 00:00:00
abstract：:Monte Carlo simulation technique used to evaluate the effect of the arrangement of concentrations on the efficiency of estimation of population pharmacokinetic parameters in the preclinical setting is described. Although the simulations were restricted to the one compartment model with intravenous bolus input, they pr...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016267811074
更新日期：1995-05-01 00:00:00
abstract：PURPOSE:This study examines methylprednisolone (MPL) effects on the dynamics of hepatic low-density lipoprotein receptor (LDLR) mRNA and plasma lipids associated with increased risks for atherosclerosis. MATERIALS AND METHODS:Normal male Wistar rats were given 50 mg/kg MPL intramuscularly (IM) and sacrificed at variou...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-007-9371-8
更新日期：2008-04-01 00:00:00
abstract：OBJECTIVE:The objective of this work was to determine plasma protein adsorption and macrophage phagocytosis of biodegradable polyanhydride, polylactic acid and polylactic-co-glycolic acid microspheres prepared by both spray-drying and solvent evaporation techniques. METHODS:Microspheres were characterized by scanning ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1011935222652
更新日期：1998-02-01 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
pub_type： 杂志文章
doi：10.1007/s11095-016-2085-z
更新日期：2017-03-01 00:00:00
abstract：PURPOSE:β-Hydroxy-β-methylbutyrate (HMB), a nutritional supplement, elicits anabolic activity in muscle. Here we investigated the mechanism of HMB uptake in muscle cells. METHODS:Murine muscle cells (C2C12) and human mammary epithelial cells (MCF7) were used for uptake. As HMB is a monocarboxylate, focus was on monoca...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-019-2626-3
更新日期：2019-04-17 00:00:00
abstract：PURPOSE:The current study was designed to develop thiolated-graphene quantum dots (SH-GQDs) as a theranostic nanocarrier and evaluate its potential for the optimal scavenging of reactive oxygen species (ROS) in macrophages. METHODS:SH-GQDs were prepared by hydrothermal pyrolysis of carbon source (citric acid) in the p...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-016-2000-7
更新日期：2016-11-01 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
pub_type： 杂志文章
doi：10.1007/s11095-006-0250-5
更新日期：2006-07-01 00:00:00
abstract：:For the last 50 years we have known of a broad-spectrum agent tilorone dihydrochloride (Tilorone). This is a small-molecule orally bioavailable drug that was originally discovered in the USA and is currently used clinically as an antiviral in Russia and the Ukraine. Over the years there have been numerous clinical and...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-020-02799-8
更新日期：2020-03-25 00:00:00
abstract：PURPOSE:Relatively large (>5 microm) and porous (mass density <0.4 g/cm3) particles present advantages for the delivery of drugs to the lungs, e.g., excellent aerosolization properties. The aim of this study was, first, to formulate such particles with excipients that are either FDA-approved for inhalation or endogenou...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018910200420
更新日期：1999-11-01 00:00:00
abstract：PURPOSE:Induction of cell-mediated immune (CMI) responses is crucial for vaccine-mediated protection against difficult vaccine targets, e.g., Chlamydia trachomatis (Ct). Adjuvants are included in subunit vaccines to potentiate immune responses, but many marketed adjuvants stimulate predominantly humoral immune response...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-017-2180-9
更新日期：2017-08-01 00:00:00
abstract：PURPOSE:The objective of this study was to compare two different nebulizers: Eflow rapid® and Pari LC star® by scintigraphy and PK modeling to simulate epithelial lining fluid concentrations from measured plasma concentrations, after nebulization of CMS in baboons. METHODS:Three baboons received CMS by IV infusion and...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-015-1716-0
更新日期：2015-10-01 00:00:00
