Synthesis, physicochemical properties, and cytotoxicity of a series of 5'-ester prodrugs of 5-iodo-2'-deoxyuridine.

abstract：PURPOSE:To evaluate the effect of re-directing the uptake mechanism of polyplexes containing oligodeoxynucleotide (ODN) decoys to nuclear factor kappa B (NF-kappaB) from absorptive-mediated to receptor-mediated endocytosis. MATERIALS AND METHODS:Complexes of ODNs and a co-polymer of biotin-polyethylenglycol and polyet...

journal_title：Pharmaceutical research

authors： Bhattacharya R,Osburg B,Fischer D,Bickel U

更新日期：2008-03-01 00:00:00

abstract：PURPOSE:To study the influence of cytotoxicity of macromolecules, VEGF gene expression, and vascular permeability on the enhanced permeability and retention (EPR) effect. METHODS:Mice bearing xenografts of A2780 multidrug resistant human ovarian carcinoma were treated by free doxorubicin (DOX) and N-(2-hydroxypropyl)m...

journal_title：Pharmaceutical research

authors： Minko T,Kopeckova P,Pozharov V,Jensen KD,Kopecek J

更新日期：2000-05-01 00:00:00

abstract：PURPOSE:Reverse micellar solutions of diclofenac sodium were encapsulated in soft gelatine capsules. On contact with aqueous media they exhibited an application induced transformation (AIT) into a semisolid system of liquid crystals (SSLC) which slows down drug release. The aim of the present paper was to study in vitr...

journal_title：Pharmaceutical research

authors： Schneeweis A,Müller-Goymann CC

更新日期：1997-12-01 00:00:00

abstract：PURPOSE:An in vitro dynamic pharmacokinetic (PK) cell culture system was developed to more precisely simulate physiologic nanoparticle/drug exposure. METHODS:A dynamic PK cell culture system was developed to more closely reflect physiologic nanoparticle/drug concentrations that are changing with time. Macrophages were...

journal_title：Pharmaceutical research

authors： Kutscher HL,Morse GD,Prasad PN,Reynolds JL

更新日期：2019-02-01 00:00:00

abstract：PURPOSE:To examine the effect of particle size and morphology on aerosol dispersion using jet-milled and spray-dried mannitol particles in narrow size distributions within the respirable range. METHODS:Particle size and morphology were examined by laser diffraction and scanning electron microscopy, respectively. Aeros...

journal_title：Pharmaceutical research

authors： Louey MD,Van Oort M,Hickey AJ

更新日期：2004-07-01 00:00:00

abstract：PURPOSE:The long-term stability and nasal absorption characteristics of a basic nasal formulation of azetirelin, a thyrotropin-releasing hormone analog and its absorption enhancement by incorporation of acylcarnitines in the formulation were investigated. METHODS:The long-term stability of basic nasal azetirelin formu...

journal_title：Pharmaceutical research

authors： Kagatani S,Inaba N,Fukui M,Sonobe T

更新日期：1998-01-01 00:00:00

abstract：PURPOSE:Although flomoxef (FMOX) has attracted substantial attention as an antibiotic against extended-spectrum beta-lactamase-producing Escherichia coli (ESBL-producing E. coli), the pharmacokinetics/pharmacodynamics (PK/PD) characteristics of FMOX against ESBL-producing E. coli is unclear. The aim of this study was t...

journal_title：Pharmaceutical research

authors： Tashiro S,Hayashi M,Takemura W,Igarashi Y,Liu X,Mizukami Y,Kojima N,Enoki Y,Taguchi K,Yokoyama Y,Nakamura T,Matsumoto K

更新日期：2021-01-06 00:00:00

abstract：PURPOSE:Many genetic disorders, including chondrodysplasias, and acquired disorders impair growth plate function, resulting in short and sometimes malformed bones. There are multiple endocrine and paracrine factors that promote chondrogenesis at the growth plate, which could potentially be used to treat these disorders...

journal_title：Pharmaceutical research

authors： Cheung CS,Zhu Z,Lui JC,Dimitrov D,Baron J

更新日期：2015-07-01 00:00:00

abstract：PURPOSE:The purpose of this study was to evaluate an effect of the proteolytic enzyme papain on permeation of low molecular weight heparin (LMWH) in vitro and in vivo. MATERIALS AND METHODS:In vitro permeation studies were performed using rat small intestine as permeation barrier. In order to determine the ratio of pa...

journal_title：Pharmaceutical research

authors： Grabovac V,Schmitz T,Föger F,Bernkop-Schnürch A

更新日期：2007-05-01 00:00:00

abstract：PURPOSE:To develop an enzymatically-controlled pulsatile drug release system based on an impermeable capsule body, which contains the drug and is closed by an erodible pectin/pectinase-plug. METHODS:The plug was prepared by direct compression of pectin and pectinase in different ratios. In addition to the disintegrati...

journal_title：Pharmaceutical research

authors： Krögel I,Bodmeier R

更新日期：1999-09-01 00:00:00

abstract：:At an ever increasing pace, synthetic biomaterials are being developed with specific functionalities for tissue engineering applications. These biomaterials possess properties including biocompatibility, mechanical strength, and degradation as well as functionalities such as specific cell adhesion and directed cell mi...

journal_title：Pharmaceutical research

authors： Falco EE,Patel M,Fisher JP

更新日期：2008-10-01 00:00:00

abstract：PURPOSE:To advance fundamental biological and translational research with the bacterium Neisseria gonorrhoeae through the prediction of novel small molecule growth inhibitors via naïve Bayesian modeling methodology. METHODS:Inspection and curation of data from the publicly available ChEMBL web site for small molecule ...

journal_title：Pharmaceutical research

authors： Pereira JC,Daher SS,Zorn KM,Sherwood M,Russo R,Perryman AL,Wang X,Freundlich MJ,Ekins S,Freundlich JS

更新日期：2020-07-13 00:00:00

abstract：PURPOSE:To study the role of unsaturated fatty acid ester substituents in the autoxidation of polysorbate 80 using quantitative kinetics. METHODS:Oxidation kinetics were monitored at 40 degrees C in aqueous solution by tracking head space oxygen consumption using a fiber optic oxygen sensor with phase shift fluorescen...

journal_title：Pharmaceutical research

authors： Yao J,Dokuru DK,Noestheden M,Park SS,Kerwin BA,Jona J,Ostovic D,Reid DL

更新日期：2009-10-01 00:00:00

abstract：PURPOSE:To develop an efficient tumor vasculature-targeted polymeric micelle delivery system for combretastatin A4 (CA4), a novel antivascular agent. METHODS:CA4-loaded micelles were prepared from poly (ethylene glycol)-b-poly (d, l-lactide) copolymers. RGD peptides that target integrins alphavbeta3 and alphavbeta5, m...

journal_title：Pharmaceutical research

authors： Wang Y,Yang T,Wang X,Wang J,Zhang X,Zhang Q

更新日期：2010-09-01 00:00:00

abstract：PURPOSE:The aim of the study is to suppress the progress of estrogen-dependent breast cancer by inhibiting the membrane transporter, which mediates the internalization of estrone-3-sulfate as estrogen precursor in the cancer cells. METHODS:The uptake of estrone-3-sulfate by estrogen-dependent breast cancer MCF-7 cells...

journal_title：Pharmaceutical research

authors： Nozawa T,Suzuki M,Yabuuchi H,Irokawa M,Tsuji A,Tamai I

更新日期：2005-10-01 00:00:00

abstract：PURPOSE:To evaluate the effects of several buffers and excipients on the stability of glucagon during freeze-drying and storage as dried powder formulations. METHODS:The chemical and physical stability of glucagon in freeze-dried solid formulations was evaluated by a variety of techniques including mass spectrometry (...

journal_title：Pharmaceutical research

authors： Fang WJ,Qi W,Kinzell J,Prestrelski S,Carpenter JF

更新日期：2012-12-01 00:00:00

abstract：PURPOSE:To investigate in vitro if P-glycoprotein (P-gp) transport can differentiate between antibiotic drugs exhibiting increased active renal clearance (CL(r)) in cystic fibrosis (CF) patients (i.e., dicloxacillin, trimethoprim) and drugs that do not exhibit this phenomenon (i.e.. cefsulodin, sulfamethoxazole). METH...

journal_title：Pharmaceutical research

authors： Susanto M,Benet LZ

更新日期：2002-04-01 00:00:00

abstract：:The interdependent relationship between pharmacology and toxicology is fundamental to the concepts of efficacy and safety of both drugs and xenobiotics. The traditional concept of establishing efficacious and tolerated doses to define a 'therapeutic window' appears simplistic in the context of an exponentially increas...

journal_title：Pharmaceutical research

authors： Sayes CM,Staats H,Hickey AJ

更新日期：2014-09-01 00:00:00

abstract：PURPOSE:The aim of the present study was to design a new mucosal drug delivery system composed of liposomes dispersed within a bioadhesive hydrogel containing methyl-beta-cyclodextrin (Me(beta)CD) for controlled drug release. METHODS:A hydrophilic model molecule, inulin, was encapsulated within positively charged and ...

journal_title：Pharmaceutical research

authors： Boulmedarat L,Piel G,Bochot A,Lesieur S,Delattre L,Fattal E

更新日期：2005-06-01 00:00:00

abstract：PURPOSE:Since the molecular mechanism of the cell cycle was established, various theoretical models of this process have been developed. A recent study revealed significant variability in cell cycle duration between mother and daughter cells, but this observation has not been incorporated into the theoretical models. ...

journal_title：Pharmaceutical research

authors： Bae H,Go YH,Kwon T,Sung BJ,Cha HJ

更新日期：2019-02-22 00:00:00

abstract：PURPOSE:In vitro and in vivo permeation studies were conducted to evaluate the characteristic of percutaneous administration of high hydrophilic drug L-carnitine (LC) by Functional MicroArray (FMA) painless intradermal delivery system. METHODS:In vitro study was designed to assess the effects of various skins, donor c...

journal_title：Pharmaceutical research

authors： Zhang S,Qin G,Wu Y,Gao Y,Qiu Y,Li F,Xu B

更新日期：2011-01-01 00:00:00

abstract：PURPOSE:Nanocrystalline drug-polymer dispersions are of significant interest in pharmaceutical delivery. The purpose of this work is to demonstrate the applicability of methods based on two-dimensional (2D) and multinuclear solid-state NMR (SSNMR) to a novel nanocrystalline pharmaceutical dispersion of ebselen with pol...

journal_title：Pharmaceutical research

authors： Vogt FG,Williams GR

更新日期：2012-07-01 00:00:00

abstract：:The transient dynamic swelling and dissolution behavior during the release of a growth hormone releasing peptide, [D-Trp2-D-Phe5]GHRP, from erodible, non-cross-linked poly(methyl methacrylate-co-methacrylic acid) (PMMA/MAA) beads has been investigated at pH 7.4 as a function of buffer concentration. Although the swell...

journal_title：Pharmaceutical research

authors： Lee PI

更新日期：1993-07-01 00:00:00

abstract：:The transepithelial transport of arginine vasopressin (AVP) across cultured rat alveolar epithelial cell monolayers was studied. At 0.1 nM donor [125I]AVP, the radiolabel flux measured in the apical-to-basolateral (AB) direction was about 10 times greater than that in the reverse (BA) direction. HPLC analyses of the b...

journal_title：Pharmaceutical research

authors： Yamahara H,Morimoto K,Lee VH,Kim KJ

更新日期：1994-11-01 00:00:00

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

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

更新日期：1987-08-01 00:00:00

abstract：PURPOSE:We have already demonstrated that the HMG-CoA reductase inhibitor, pravastatin is actively taken up by isolated rat hepatocytes via a multispecific anion transporter (Yamazaki et al., Am. J. Physiol. 264, G36-44, (1993)). We further attempted the quantitative evaluation of this uptake in different experimental ...

journal_title：Pharmaceutical research

authors： Ishigami M,Tokui T,Komai T,Tsukahara K,Yamazaki M,Sugiyama Y

更新日期：1995-11-01 00:00:00

abstract：:The intrasubject and intersubject variabilities for CGS 16617, an angiotensin converting enzyme inhibitor, were evaluated in an open-label, repeat single-dose bioavailability trial. Eight healthy male volunteers each received a 20-mg oral dose of CGS 16617 as an aqueous solution on four separate occasions. Components ...

journal_title：Pharmaceutical research

authors： Kochak GM,Smith RA,Choi RL,John V,Tipnis V,Honc F,deSilva JK,Weidler DJ

更新日期：1989-04-01 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：:Defined size fractions of polyethyleneglycol powder (MW = 10,000) were mixed with defined size fractions of alpha-lactose monohydrate in order to study the effect of compaction as a function of the weight ratios of the two excipients. For a precise control of the compression cycle, tablets were compressed on a Univers...

journal_title：Pharmaceutical research

authors： Blattner D,Kolb M,Leuenberger H

更新日期：1990-02-01 00:00:00

abstract：:The relative effectiveness of two beta-cyclodextrin derivatives, i.e., dimethyl-beta-cyclodextrin (DM beta CD) and hydroxypropyl-beta-cyclodextrin (HP beta CD), in enhancing enteral absorption of insulin was evaluated in the lower jejunal/upper ileal segments of the rat by means of an in situ closed loop method. The i...

journal_title：Pharmaceutical research

authors： Shao Z,Li Y,Chermak T,Mitra AK

更新日期：1994-08-01 00:00:00