Iontophoresis-facilitated delivery of prednisolone through throat skin to the trachea after topical application of its succinate salt.

Abstract:

PURPOSE:The possibility of direct delivery of steroids through the skin to the trachea and the effect of iontophoresis on delivery efficacy were evaluated after the application of an ionic steroidal prodrug, prednisolone sodium succinate (PS-Na), to the throat skin. METHODS:Fluorescein sodium salt (FL-Na) and PS-Na were applied as model compounds at a concentration of 1% in pH 7.4 phosphate-buffered saline to the throat skin of hairless rats, and constant current-cathodal iontophoresis (0.4 mA/cm(2)) was performed for 8 or 10 h. RESULTS:In vitro permeation experiment involving cathodal iontophoresis through excised hairless rat abdominal skin revealed 30- and 10-times higher levels of skin permeation of PS and its active drug, prednisolone (P), than those induced without iontophoresis. In vivo iontophoresis treatment of the rat's throat skin produced 2.6-, 1.6- and 12-times higher FL, PS and P concentrations, respectively, in the trachea than those observed without iontophoresis. CONCLUSION:The present results suggest the usefulness of topical application of the ionic steroidal prodrugs onto throat skin followed by iontophoresis treatment for directly delivering the steroid to the trachea.

journal_name

Pharm Res

journal_title

Pharmaceutical research

authors

Ishii H,Suzuki T,Todo H,Kamimura M,Sugibayashi K

doi

10.1007/s11095-010-0337-x

subject

Has Abstract

pub_date

2011-04-01 00:00:00

pages

839-47

issue

4

eissn

0724-8741

issn

1573-904X

journal_volume

28

pub_type

杂志文章
  • Phagocytosis of nanoparticles by human immunodeficiency virus (HIV)-infected macrophages: a possibility for antiviral drug targeting.

    abstract::Human monocytes/macrophages (MO/MAC) were isolated from peripheral blood and cultivated on hydrophobic Teflon membranes. This culture system is suitable for HIV infection of MO/MAC in vitro. After transfer into 24-well plates the mature macrophages (infected or uninfected) were used for measurements of phagocytosis. T...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015852732512

    authors: Schäfer V,von Briesen H,Andreesen R,Steffan AM,Royer C,Tröster S,Kreuter J,Rübsamen-Waigmann H

    更新日期:1992-04-01 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

  • Impact of Buffer, Protein Concentration and Sucrose Addition on the Aggregation and Particle Formation during Freezing and Thawing.

    abstract:PURPOSE:This study addresses the effect of freezing and thawing on a therapeutic monoclonal antibody (mAb) solution and the corresponding buffer formulation. Particle formation, crystallization behaviour, morphology changes and cryo-concentration effects were studied after varying the freezing and thawing rates, buffer...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-018-2378-5

    authors: Hauptmann A,Podgoršek K,Kuzman D,Srčič S,Hoelzl G,Loerting T

    更新日期:2018-03-19 00:00:00

  • Esterase-like activity of serum albumin: characterization of its structural chemistry using p-nitrophenyl esters as substrates.

    abstract:PURPOSE:To elucidate the catalytic mechanism of the esterase-like activity of serum albumin (SA), the reactivity of SA from six species was investigated using p-nitrophenyl esters as model substrates. METHODS:The effect of pH and the energetic and thermodynamic profiles of SA were determined for all species for p-nitr...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/b:pham.0000016241.84630.06

    authors: Sakurai Y,Ma SF,Watanabe H,Yamaotsu N,Hirono S,Kurono Y,Kragh-Hansen U,Otagiri M

    更新日期:2004-02-01 00:00:00

  • Site- and stereospecific ocular drug delivery by sequential enzymatic bioactivation.

    abstract::Intraocular enzymes convert the ketoxime analogues of some beta-adrenergic blockers via a sequential bioactivation process involving hydrolysis to the corresponding ketones followed by reduction to the aryloxyaminoalcohols, which then exert known and predictable physiological and pharmacological effects only at the si...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015863521513

    authors: Bodor N,Prokai L

    更新日期:1990-07-01 00:00:00

  • Acylation of exenatide by glycolic acid and its anti-diabetic activities in db/db mice.

    abstract:PURPOSE:To prepare acylated exenatide analogues and investigate their biological properties for guiding the development of PLGA formulations of exenatide. METHODS:The acylated exenatide analogues were prepared by reaction with glycolic acid (GA), one constitutional unit of PLGA, and characterized by HPLC-MS/MS and Cir...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-014-1298-2

    authors: Liang R,Li X,Zhang R,Shi Y,Wang A,Chen D,Sun K,Liu W,Li Y

    更新日期:2014-08-01 00:00:00

  • Chemical degradation kinetics of recombinant hirudin (HV1) in aqueous solution: effect of pH.

    abstract:PURPOSE:To gain information on the chemical stability pattern and the kinetics of the degradation of recombinant hirudin variant HV1 (rHir), a thrombin-specific inhibitor protein of 65 amino acids, in aqueous solution as a function of pH. METHODS:Stability of rHir was monitored at 50 degrees C in the framework of a cl...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1011918108849

    authors: Gietz U,Alder R,Langguth P,Arvinte T,Merkle HP

    更新日期:1998-09-01 00:00:00

  • A comparison of peptidase activities and peptide metabolism in cultured mouse keratinocytes and neonatal mouse epidermis.

    abstract::One of the barriers to transdermal delivery of peptides is the metabolic activity of the epidermis. To define this metabolic activity, aminopeptidase activity and Leu-enkephalin metabolism were measured in the epidermis obtained from neonatal mouse skin and in cultured mouse keratinocytes. Aminopeptidase activity was ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015882323677

    authors: Shah PK,Borchardt RT

    更新日期:1991-01-01 00:00:00

  • 16HBE14o- human bronchial epithelial cell layers express P-glycoprotein, lung resistance-related protein, and caveolin-1.

    abstract:PURPOSE:To study the expression of P-glycoprotein (P-gp), lung resistance-related protein (LRP), and caveolin-1 (cav-1) in the human bronchial epithelial cell line 16HBE14o-. METHODS:The presence of P-gp, LRP, and cav-1 in 16HBE14o- cell layers was evaluated using immunocytochemical staining and visualization with con...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1023230328687

    authors: Ehrhardt C,Kneuer C,Laue M,Schaefer UF,Kim KJ,Lehr CM

    更新日期:2003-04-01 00:00:00

  • Cancer chemoprevention by natural products: how far have we come?

    abstract::Since ancient times, natural products, herbs and spices have been used for preventing several diseases, including cancer. The term chemoprevention was coined in the late 1970s and referred to the prevention of cancer by selective use of phytochemicals or their analogs. The field utilizes experimental carcinogenesis mo...

    journal_title:Pharmaceutical research

    pub_type: 历史文章,杂志文章,评审

    doi:10.1007/s11095-010-0085-y

    authors: Mehta RG,Murillo G,Naithani R,Peng X

    更新日期:2010-06-01 00:00:00

  • Novel microneedle patches for active insulin delivery are efficient in maintaining glycaemic control: an initial comparison with subcutaneous administration.

    abstract:PURPOSE:Good glycaemic control is essential to minimize the risk for diabetes-induced complications. Also, compliance is likely to be higher if the procedure is simple and painless. This study was designed to validate painless intradermal delivery via a patch-like microneedle array. MATERIALS AND METHODS:Diabetes was ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-007-9256-x

    authors: Nordquist L,Roxhed N,Griss P,Stemme G

    更新日期:2007-07-01 00:00:00

  • Effects of solute characteristics and concentration on a lyotropic liquid crystal: solute-induced phase change.

    abstract::We investigated the effects of increased concentrations of the solutes, salicylic acid, benzoic acid, and o-, m-, and p-methoxy benzoic acids, on the anisotropic properties of a liquid crystal solvent. The lamellar liquid crystal was composed of 37% polyoxyethylene (20) isohexadecyl ether in aqueous buffer of pH 1. Ph...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1018920118631

    authors: Ibrahim HG,Sallam ES,Takieddin M,Habboub M

    更新日期:1993-05-01 00:00:00

  • Enhanced accumulation of sialyl Lewis X-carboxymethylpullulan conjugate in acute inflammatory lesion.

    abstract:PURPOSE:E-selectin is a cell adhesion molecule that is specifically expressed in the inflammatory vascular endothelium in response to cytokines such as IL-1 beta and TNF-alpha, and interacts with specific ligands containing sialyl Lewis X (Neu5Ac alpha 2-3Gal beta 1-4(Fuc alpha 1-3)GlcNAc-, SLex). In order to investiga...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1018849029727

    authors: Horie K,Sakagami M,Kuramochi K,Hanasaki K,Hamana H,Ito T

    更新日期:1999-02-01 00:00:00

  • Biliary excretion of glycyrrhizin in rats: kinetic basis for multiplicity in bile canalicular transport of organic anions.

    abstract:PURPOSE:To examine the presence of multiplicity for the biliary excretion of xenobiotic conjugates, we studied the disposition of glycyrrhizin (GR), which has glucuronide within its molecular structure and has the ability to inhibit the biliary excretion of liquiritigenin (LG) glucuronides. METHODS:GR was administered...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1016033124819

    authors: Shimamura H,Suzuki H,Tagaya O,Horie T,Sugiyama Y

    更新日期:1996-12-01 00:00:00

  • Transfer of lipophilic markers from PLGA and polystyrene nanoparticles to caco-2 monolayers mimics particle uptake.

    abstract:PURPOSE:The objective of this study was to evaluate nanoparticle uptake by the Caco-2 monolayer model in vitro. Special emphasis was placed on the localization and the quantification of the uptake of fluorescently labeled polystyrene and poly(lactic-co-glycolic acid) (PLGA) nanoparticles. METHODS:Intracellular fluores...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015393710253

    authors: Pietzonka P,Rothen-Rutishauser B,Langguth P,Wunderli-Allenspach H,Walter E,Merkle HP

    更新日期:2002-05-01 00:00:00

  • The role of polysorbate 80 and HPβCD at the air-water interface of IgG solutions.

    abstract:PURPOSE:To test the hypothesis of surface displacement as the underlying mechanism for IgG stabilization by polysorbates and HPβCD against surface-induced aggregation. METHODS:Adsorption/desorption-kinetics of IgG-polysorbate 80/-HPβCD were monitored. Maximum bubble pressure method was used for processes within second...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-012-0854-x

    authors: Serno T,Härtl E,Besheer A,Miller R,Winter G

    更新日期:2013-01-01 00:00:00

  • Evaluation of amorphous ursodeoxycholic acid by thermal methods.

    abstract:PURPOSE:The purpose of this study was to characterize the amorphous state of ursodeoxycholic acid (UDCA) samples by using isothermal microcalorimetry, X-ray diffraction, infrared (IR) spectroscopy and solid state carbon 13 nuclear magnetic resonance (13C-NMR) spectroscopy, and to demonstrate the application of the ther...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1012114825513

    authors: Yonemochi E,Ueno Y,Ohmae T,Oguchi T,Nakajima S,Yamamoto K

    更新日期:1997-06-01 00:00:00

  • Messenger RNA expression of transporter and ion channel genes in undifferentiated and differentiated Caco-2 cells compared to human intestines.

    abstract:PURPOSE:The purpose of this work was to study the influence of cell differentiation on the mRNA expression of transporters and channels in Caco-2 cells and to assess Caco-2 cells as a model for carrier-mediated drug transport in the intestines. METHOD:Gene mRNA expression was measured using a custom-designed microarra...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1022282221530

    authors: Anderle P,Rakhmanova V,Woodford K,Zerangue N,Sadée W

    更新日期:2003-01-01 00:00:00

  • The relationship of pKa and acute skin irritation in man.

    abstract::The relationship between pKa and skin irritation in man is studied for a homologous series of benzoic acid derivatives, which permeate through human skin at comparable rates (15-88 micrograms/cm2/hr). Skin irritation and pKa are correlated for pKa less than or equal to 4. Laser Doppler velocimetric assessment of skin ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015931105660

    authors: Berner B,Wilson DR,Guy RH,Mazzenga GC,Clarke FH,Maibach HI

    更新日期:1988-10-01 00:00:00

  • Expedited Tablet Formulation Development of a Highly Soluble Carbamazepine Cocrystal Enabled by Precipitation Inhibition in Diffusion Layer.

    abstract:PURPOSE:To address the problem of precipitation of a poorly soluble drug during dissolution of highly soluble cocrystals by preparing granules intimately mixed with a water-soluble polymer. METHODS:Effectiveness of polymers as precipitation inhibitors during the dissolution of carbamazepine-nicotinamide (CBZ-NCT) cocr...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-019-2622-7

    authors: Yamashita H,Sun CC

    更新日期:2019-04-23 00:00:00

  • Pulsatile drug release from an insoluble capsule body controlled by an erodible plug.

    abstract:PURPOSE:The objective of this study was to develop and evaluate a pulsatile drug delivery system based on an impermeable capsule body filled with drug and an erodible plug placed in the opening of the capsule body. METHODS:The erodible plugs were either prepared by direct compression followed by placing the tablets in...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1011940718534

    authors: Krögel I,Bodmeier R

    更新日期:1998-03-01 00:00:00

  • Estimation of the relative contribution of the transcellular and paracellular pathway to the transport of passively absorbed drugs in the Caco-2 cell culture model.

    abstract:PURPOSE:The objective of this investigation was to determine, using the Caco-2 cell culture model, the extent to which the paracellular and transcellular routes contributed to the transport of passively absorbed drugs. An effort was also made to determine the controlling factors in this process. METHODS:We selected a ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1012111008617

    authors: Pade V,Stavchansky S

    更新日期:1997-09-01 00:00:00

  • Direct observation of single particle electrostatic charging by atomic force microscopy.

    abstract:PURPOSE:To show that atomic force microscopy (AFM) can be used to directly study the electrostatic charging and dissipation of single pharmaceutical particles. MATERIALS AND METHODS:Particles of lactose attached to AFM cantilevers were charged on a glass surface at a relative humidity (RH) of 0.1%. By recording force-...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-006-9230-z

    authors: Bunker MJ,Davies MC,James MB,Roberts CJ

    更新日期:2007-06-01 00:00:00

  • Evaluation of Intranasal Vaccine Delivery Using Anatomical Replicas of Infant Nasal Airways.

    abstract:PURPOSE:Nasal delivery is a favorable route for vaccination against most respiratory infections, as antigen deposited in the nasal turbinate and Waldeyer's ring areas induce mucosal and systemic immune responses. However, little is known about the nasal distribution of the vaccines, specifically for infants. METHODS:A...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-020-02976-9

    authors: Wilkins JV Jr,Golshahi L,Rahman N,Li L

    更新日期:2021-01-15 00:00:00

  • Formulating weakly basic HCl salts: relative ability of common excipients to induce disproportionation and the unique deleterious effects of magnesium stearate.

    abstract:PURPOSE:Nine common excipients were examined to determine their ability to cause disproportionation of the HCl salt of a a weakly basic compound. The goal was to determine which excipients were problematic and correlate the results to known properties such as surface pH, slurry pH, or molecular structure. Such a correl...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-013-1002-y

    authors: John CT,Xu W,Lupton LK,Harmon PA

    更新日期:2013-06-01 00:00:00

  • Kinetic analysis of covalent binding between N-acetyl-L-cysteine and albumin through the formation of mixed disulfides in human and rat serum in vitro.

    abstract:PURPOSE:Covalent binding between N-acetyl-L-cysteine (NAC) and albumin was evaluated kinetically by conducting in vitro experiments. METHOD:After 14C-NAC was incubated with human or rat serum, the solution was analyzed by anion-exchange HPLC. The albumin-bound 14C-NAC was quantified by measuring the radioactivity in t...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1020749211745

    authors: Harada D,Naito S,Otagiri M

    更新日期:2002-11-01 00:00:00

  • Enhanced Follicular Delivery of Finasteride to Human Scalp Skin Using Heat and Chemical Penetration Enhancers.

    abstract:PURPOSE:The aim of this work was to evaluate whether improved topical delivery of finasteride, focussed to the hair follicles of human scalp skin could be achieved with application of short durations of heat and use of specific chemical penetration enhancers. METHODS:Franz cell experiments with human scalp skin were p...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-020-02822-y

    authors: Farah HA,Brown MB,McAuley WJ

    更新日期:2020-05-31 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

  • Correlation among agonist dose, rate of import, and transcriptional activity of liganded progesterone receptor B isoform in living cells.

    abstract:PURPOSE:To determine the correlation among progesterone dose, rate of import of progesterone-occupied progesterone receptor (PR) complexes into the nucleus of cells, and transcriptional activity of progesterone-PR complexes. METHODS:Live cell imaging and time-lapse microscopy of green fluorescent protein-tagged PR wer...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1026127015761

    authors: Li H,Yan G,Kern SE,Lim CS

    更新日期:2003-10-01 00:00:00

  • Establishment and characterization of the transformants stably-expressing MDR1 derived from various animal species in LLC-PK1.

    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

    pub_type: 杂志文章

    doi:10.1007/s11095-006-0285-7

    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