Effect of some penetration enhancers on epithelial membrane lipid domains: evidence from fluorescence spectroscopy studies.

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：PURPOSE:Fractal kinetics was used for the analysis of the carrier-mediated transport for drugs across the intestinal epithelial cells. METHODS:The transport was examined under various agitation rates using a monolayer of Caco-2 cells and rabbit ileum sheets. RESULTS:The passive transport of antipyrine across Caco-2 c...

journal_title：Pharmaceutical research

authors： Ogihara T,Tamai I,Tsuji A

更新日期：1998-04-01 00:00:00

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

authors： Sylte I,Dahl SG

更新日期：1991-04-01 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

authors： Rümenapp C,Gleich B,Haase A

更新日期：2012-05-01 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：BACKGROUND:With the recent approval of the first small interfering RNA (siRNA) therapeutic formulated as nanoparticles, there is increased incentive for establishing the factors of importance for the design of stable solid dosage forms of such complex nanomedicines. METHODS:The aims of this study were: (i) to identify...

journal_title：Pharmaceutical research

authors： Dormenval C,Lokras A,Cano-Garcia G,Wadhwa A,Thanki K,Rose F,Thakur A,Franzyk H,Foged C

更新日期：2019-08-02 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

authors： Hazra A,Pyszczynski NA,DuBois DC,Almon RR,Jusko WJ

更新日期：2008-04-01 00:00:00

abstract：PURPOSE:The purpose of this work was to investigate the mechanisms of cocrystal formation during cogrinding and storage of solid reactants, and to establish the effects of water by cogrinding with hydrated form of reactants and varying RH conditions during storage. METHODS:The hydrogen bonded 1:1 carbamazepine-sacchar...

journal_title：Pharmaceutical research

authors： Jayasankar A,Somwangthanaroj A,Shao ZJ,Rodríguez-Hornedo N

更新日期：2006-10-01 00:00:00

abstract：PURPOSE:Using monolayers of human pancreatic adenocarcinoma cells (Panc-1) that express multidrug resistance-associated protein (MRP), the present work investigates the effects of Pluronic block copolymers on the functional activity of MRP. METHODS:The studies examined the accumulation and efflux of the MRP selective ...

journal_title：Pharmaceutical research

authors： Miller DW,Batrakova EV,Kabanov AV

更新日期：1999-03-01 00:00:00

abstract：PURPOSE:The aim of the study is to investigate the effect of polymer blending on entrapment and release of ganciclovir (GCV) from poly(D,L-lactide-co-glycolide) (PLGA) microspheres using a set of empirical equations. METHODS:Two grades of PLGA, PLGA 7525 [D,L-lactide:glycolide(75:25), MW 90,000-126,000 Da] and Resomer...

journal_title：Pharmaceutical research

authors： Duvvuri S,Gaurav Janoria K,Mitra AK

更新日期：2006-01-01 00:00:00

abstract：PURPOSE:Vancomycin (VCM) concentration is often out of therapeutic range (10-20 μg/ml) in patients receiving continuous renal replacement therapy (CRRT). The purposes of this study were to develop a practical VCM population pharmacokinetic (PPK) model and to evaluate the potential of Bayesian prediction-based therapeut...

journal_title：Pharmaceutical research

authors： Oda K,Jono H,Kamohara H,Nishi K,Tanoue N,Saito H

更新日期：2020-05-28 00:00:00

abstract：PURPOSE:To assess the role of intestinal CYP2D6 in oral first-pass drug clearance by comparing the enzyme content and catalytic activity of a prototype CYP2D6 substrate, metoprolol, between microsomes prepared from human intestinal mucosa and from human livers. METHODS:Microsomes were prepared from a panel of 31 human...

journal_title：Pharmaceutical research

authors： Madani S,Paine MF,Lewis L,Thummel KE,Shen DD

更新日期：1999-08-01 00:00:00

abstract：PURPOSE:There is evidence that cholesterol affects the ATPase and transport functions of P-glycoprotein (P-gp). To study the influence of cholesterol on P-gp in a well defined lipid environment, we reconstituted P-gp in egg phosphatidylcholine (PhC) and PhC/cholesterol proteoliposomes with negligible residual amounts o...

journal_title：Pharmaceutical research

authors： Bucher K,Belli S,Wunderli-Allenspach H,Krämer SD

更新日期：2007-11-01 00:00:00

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

authors： Li H,Yan G,Kern SE,Lim CS

更新日期：2003-10-01 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

authors： Oriz ME,Núñez-Vergara LJ,Squella JA

更新日期：2003-02-01 00:00:00

abstract：PURPOSE:To investigate the relationship between mean dissolution time (MDT) and dose/solubility ratio (q) using the diffusion layer model. METHODS:Using the classic Noyes-Whitney equation and considering a finite dose, we derived an expression for MDT as a function of q under various conditions. q was expressed as a d...

journal_title：Pharmaceutical research

authors： Rinaki E,Dokoumetzidis A,Macheras P

更新日期：2003-03-01 00:00:00

abstract：PURPOSE:Highly lipophilic basic drugs, the antiestrogens AE 1 (log P = 5.82) and AE 2 (log P = 7.8) shall be delivered transdermally. METHODS:Transdermal permeation of drugs, enhancers, and solvents from various fluid formulations were characterized by in-vitro permeation studies through excised skin of hairless mice....

journal_title：Pharmaceutical research

authors： Funke AP,Schiller R,Motzkus HW,Günther C,Müller RH,Lipp R

更新日期：2002-05-01 00:00:00

abstract：:This review describes the design and current development of leukotriene biosynthesis inhibitors as potential antiinflammatory agents. Knowledge of the enzymatic mechanism of 5-lipoxygenase led to specific inhibitors of this enzyme which catalyzes a key step in the leukotriene pathway. Competitive inhibitors include ir...

journal_title：Pharmaceutical research

authors： Cashman JR

更新日期：1985-11-01 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:Present study assessed the influence of gallate esterification on the anti-cancer activity of procyanidin B2 (B2) in androgen-dependent human prostate carcinoma LNCaP cells employing B2-3,3'-di-O-gallate (B2-G(2)), two mono-gallate esters B2-3-O-gallate (B2-3G) and B2-3'-O-gallate (B2-3'G) and the parent compou...

journal_title：Pharmaceutical research

authors： Chou SC,Kaur M,Thompson JA,Agarwal R,Agarwal C

更新日期：2010-04-01 00:00:00

abstract：:The pulmonary deposition and pharmacokinetics of human growth hormone (hGH), administered by aerosol and instillate, in formulations containing 99mTc-DTPA (for gamma scintigraphic imaging) have been studied in five male New Zealand White rabbits. Gamma scintigraphy indicated that the peripheral:central deposition tend...

journal_title：Pharmaceutical research

authors： Colthorpe P,Farr SJ,Smith IJ,Wyatt D,Taylor G

更新日期：1995-03-01 00:00:00

abstract：PURPOSE:Phase II metabolism involves the conjugation of a polar moiety, such as sulfate or glucuronic acid, to a (relatively) nonpolar xenobiotic. Although it might be expected that such conjugates may exhibit amphiphilic character (e.g., surface activity and potential to form micelles), no detailed study of the micell...

journal_title：Pharmaceutical research

authors： Shackleford DM,Prankerd RJ,Scanlon MJ,Charman WN

更新日期：2003-03-01 00:00:00

abstract：PURPOSE:To characterize the uptake mechanism of zidovudine (AZT), a nucleoside reverse transcriptase inhibitor, in syncytiotrophoblast cells using the TR-TBT 18d-1 cell line previously established by our group. MATERIALS AND METHODS:The effects of several transporter inhibitors on the initial and steady-state apical u...

journal_title：Pharmaceutical research

authors： Sai Y,Nishimura T,Shimpo S,Chishu T,Sato K,Kose N,Terasaki T,Mukai C,Kitagaki S,Miyakoshi N,Kang YS,Nakashima E

更新日期：2008-07-01 00:00:00

abstract：PURPOSE:Understanding the critical factors governing the crystallization tendency of organic compounds is vital when assessing the feasibility of an amorphous formulation to improve oral bioavailability. The objective of this study was to investigate potential links between viscosity and crystallization tendency for or...

journal_title：Pharmaceutical research

authors： Baird JA,Santiago-Quinonez D,Rinaldi C,Taylor LS

更新日期：2012-01-01 00:00:00

abstract：:Emulsions (o/w) were prepared from solid-state emulsions comprised of various matrix materials and oils and the resultant particle size properties determined. Results suggest that for those matrices that can form solid-state emulsions, the droplet size decreased as a function of time, as previously observed. The final...

journal_title：Pharmaceutical research

authors： Shively ML

更新日期：1993-08-01 00:00:00

abstract：PURPOSE:The blood-brain barrier (BBB) essentially restricts therapeutic drugs from entering into the brain. This study tests the hypothesis that brain endothelial cell derived exosomes can deliver anticancer drug across the BBB for the treatment of brain cancer in a zebrafish (Danio rerio) model. MATERIALS AND METHODS...

journal_title：Pharmaceutical research

authors： Yang T,Martin P,Fogarty B,Brown A,Schurman K,Phipps R,Yin VP,Lockman P,Bai S

更新日期：2015-06-01 00:00:00

abstract：PURPOSE:We compared cationic, polyamine-coated microparticles (MPs) and anionic, protein-coated MPs with respect to their phagocytosis and phagosomal fate in dendritic cells (DCs) and macrophages (Mphi). METHODS:Polystyrene MPs were surface modified by covalent coupling with fluorescein isothiocyanate-labeled polyamin...

journal_title：Pharmaceutical research

authors： Thiele L,Merkle HP,Walter E

更新日期：2003-02-01 00:00:00

abstract：PURPOSE:We reported that suramin produced chemosensitization at nontoxic doses. This benefit was lost at the approximately 10-fold higher, maximally tolerated doses (MTD). The aim of the current study was to identify in patients the chemosensitizing suramin dose that delivers 10-50 microM plasma concentrations over 48 ...

journal_title：Pharmaceutical research

authors： Chen D,Song SH,Wientjes MG,Yeh TK,Zhao L,Villalona-Calero M,Otterson GA,Jensen R,Grever M,Murgo AJ,Au JL

更新日期：2006-06-01 00:00:00

abstract：PURPOSE:The main goal of this research was to assess the mechanical properties of APIs' polymorphic forms at the single-crystal level (piroxicam, famotidine, nifedipine, olanzapine) in order to predict their bulk deformational attributes, which are critical for some pharmaceutical technology processes. METHODS:The mec...

journal_title：Pharmaceutical research

authors： Egart M,Janković B,Lah N,Ilić I,Srčič S

更新日期：2015-02-01 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