Binding and uptake of wheat germ agglutinin-grafted PLGA-nanospheres by caco-2 monolayers.

abstract：PURPOSE:Lapatinib, a small molecule EGFR/HER2 inhibitor, partially inhibits the outgrowth of HER2+ brain metastases in preclinical models and in a subset of CNS lesions in clinical trials of HER2+ breast cancer. We investigated the ability of lapatinib to reach therapeutic concentrations in the CNS following (14)C-lapa...

journal_title：Pharmaceutical research

authors： Taskar KS,Rudraraju V,Mittapalli RK,Samala R,Thorsheim HR,Lockman J,Gril B,Hua E,Palmieri D,Polli JW,Castellino S,Rubin SD,Lockman PR,Steeg PS,Smith QR

更新日期：2012-03-01 00:00:00

abstract：PURPOSE:Due to protease inhibitor (PI) efflux transport by P-glycoprotein (P-gp), insufficient PI concentrations result in low ongoing HIV replication in the so-called virus sanctuaries (brain and testes). The aim of the present study was to evaluate indinavir-loaded nanocapsules (Ind-LNC) including Solutol HS15, an ex...

journal_title：Pharmaceutical research

authors： Pereira de Oliveira M,Garcion E,Venisse N,Benoit JP,Couet W,Olivier JC

更新日期：2005-11-01 00:00:00

abstract：PURPOSE:Monoamine oxidases (MAOs) are non-CYP enzymes that contribute to systemic elimination of therapeutic agents, and localized on mitochondrial membranes. The aim of the present study was to validate quantitative estimation of metabolic clearance of MAO substrate drugs using human liver microsomes (HLMs). METHODS:...

journal_title：Pharmaceutical research

authors： Masuo Y,Nagamori S,Hasegawa A,Hayashi K,Isozumi N,Nakamichi N,Kanai Y,Kato Y

更新日期：2017-06-01 00:00:00

abstract：PURPOSE:To evaluate different dissolution testing methods and subsequently develop a simple to perform but reproducible and discriminating dissolution technique for inhalative powders. METHODS:From a dry powder a fraction of aerosolized particles with an aerodynamic particle size below 5 μm was collected on regenerate...

journal_title：Pharmaceutical research

authors： May S,Jensen B,Wolkenhauer M,Schneider M,Lehr CM

更新日期：2012-08-01 00:00:00

abstract：PURPOSE:Anticancer chemotherapy usually involves the administration of several anticancer drugs that differ in their action mechanisms. Here, we aimed to test whether the combination of omacetaxine mepesuccinate (OMT) and doxorubicin (DOX) could show synergism, and whether the liposomal co-delivery of these two drugs c...

journal_title：Pharmaceutical research

authors： Shim G,Lee S,Choi J,Lee S,Kim CW,Oh YK

更新日期：2014-08-01 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:This study was carried out to examine the blood-brain barrier (BBB) transport of human basic fibroblast growth factor (bFGF) and investigate its mechanism. METHODS:The BBB transport of 125I-bFGF was measured by several in vivo methods including intravenous administration, in situ internal carotid artery perfus...

journal_title：Pharmaceutical research

authors： Deguchi Y,Naito T,Yuge T,Furukawa A,Yamada S,Pardridge WM,Kimura R

更新日期：2000-01-01 00:00:00

abstract：:A series of carboxyfluorescein (CF)-containing multilamellar vesicle (MLV) dispersions was prepared and extruded through polycarbonate membranes ranging in size from 0.2 to 5 microns. Vesicle dispersions were nebulized for 80 min using a Collison nebulizer, and the release of CF was monitored during nebulization. Solu...

journal_title：Pharmaceutical research

authors： Niven RW,Speer M,Schreier H

更新日期：1991-02-01 00:00:00

abstract：PURPOSE:At elevated temperatures, the rate of drug release and skin permeation from transdermal delivery systems (TDS) may be higher than at a normal skin temperature. The aim of this study was to compare the effect of heat on the transdermal delivery of two model drugs, nicotine and fentanyl, from matrix-type TDSs wit...

journal_title：Pharmaceutical research

authors： Shin SH,Ghosh P,Newman B,Hammell DC,Raney SG,Hassan HE,Stinchcomb AL

更新日期：2017-09-01 00:00:00

abstract：PURPOSE:The stability of lipid emulsions (LE) containing various cosurfactants (oleic acid, cholesterol, Tween 80, or HCO-60) was evaluated using the maximum total interaction energy, Vtmax and the energy barrier for coalescence, W. METHODS:The Vtmax and W were calculated from the zeta potential and the rate of increa...

journal_title：Pharmaceutical research

authors： Yamaguchi T,Nishizaki K,Itai S,Hayashi H,Ohshima H

更新日期：1995-09-01 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:S-(4-Nitrobenzyl)-6-thioinosine (NBMPR) is routinely used at concentrations of 0.10 μM and 0.10 mM to specifically inhibit transport of nucleosides mediated by equilibrative nucleoside transporters 1 (ENT1) and 2 (ENT2), respectively. We recently showed that NBMPR (0.10 mM) might also inhibit placental active e...

journal_title：Pharmaceutical research

authors： Karbanova S,Sorf A,Jiraskova L,Lalinska A,Ptackova Z,Staud F,Cerveny L

更新日期：2020-02-21 00:00:00

abstract：PURPOSE:To explore whether miR-19 is involved in the regulation of multidrug resistance (MDR), one of the main causes of breast cancer mortality, and modulates sensitivity of tumor cells to chemotherapeutic agents. METHODS:We analyzed miRNA expression levels in three MDR cell lines in comparison with their parent cell...

journal_title：Pharmaceutical research

authors： Liang Z,Li Y,Huang K,Wagar N,Shim H

更新日期：2011-12-01 00:00:00

abstract：PURPOSE:To evaluate the impact of intestinal first-pass metabolism (Fg) by cytochrome P4503A (CYP3A) and uridine 5'-diphosphate-glucuronosyltransferases (UGT) on in vivo oral absorption of their substrate drugs. METHODS:CYP3A and UGT substrates were orally administered to portal-vein cannulated (PV) rats to evaluate t...

journal_title：Pharmaceutical research

authors： Matsuda Y,Konno Y,Hashimoto T,Nagai M,Taguchi T,Satsukawa M,Yamashita S

更新日期：2015-02-01 00:00:00

abstract：PURPOSE:Propofol is a widely used anesthetic agent with highly desirable fast "on" and "off" effects. It is currently formulated as lipid emulsions, which are known to support microbial growth. In this study, a novel, lipid-free nanodispersion formulation of propofol was characterized. METHODS:The formulation was eval...

journal_title：Pharmaceutical research

authors： Chen H,Zhang Z,Almarsson O,Marier JF,Berkovitz D,Gardner CR

更新日期：2005-03-01 00:00:00

abstract：PURPOSE:To examine the theoretical/practical utility of the liver-to-blood partition coefficient (Kpuu) for predicting drug-drug interactions (DDIs), and compare the Kpuu-approach to the extended clearance concept AUCR-approach. METHODS:The Kpuu relationship was derived from first principles. Theoretical simulations i...

journal_title：Pharmaceutical research

authors： Sodhi JK,Liu S,Benet LZ

更新日期：2020-03-25 00:00:00

abstract：:Azo polymers based upon 2-hydroxyethyl methacrylate, methyl methacrylate, and methacrylic acid, and containing N,N'-bis [(methacryloyloxyethyl)oxy(carbonylamino)]azobenzene as azo aromatic agent were evaluated in vivo as coating for colon-specific drug delivery. The gastrointestinal absorption of theophylline from cap...

journal_title：Pharmaceutical research

authors： Van den Mooter G,Samyn C,Kinget R

更新日期：1995-02-01 00:00:00

abstract：:Cyclosporine (CsA) is commercially available for oral administration as a solution in olive oil with alcohol and an emulsifier. To improve its variable absorption and low patient acceptability, several oral formulations were prepared and tested in vitro and in vivo in dogs. A tablet formulation prepared by direct comp...

journal_title：Pharmaceutical research

authors： Abdallah HY,Mayersohn M

更新日期：1991-04-01 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：:A new method of analysis for the antihypertensive drug, hydralazine, is introduced. The assay involves the addition of p-nitrobenzaldehyde to blood samples containing hydralazine, to form a stable Schiff's base, hydralazine p-nitrobenzaldehyde hydrazone. The derivative is extracted from the blood into hexane and the s...

journal_title：Pharmaceutical research

authors： Semple HA,Tam YK,Tin S,Coutts RT

更新日期：1988-06-01 00:00:00

abstract：:Previous work from this laboratory showed site-dependent variations in the apparent permeability of insulin as measured using the everted rat gut sac technique, with the greatest permeability in the distal jejunum and the lowest in the duodenum (5). To quantify better the rate and extent of insulin absorption from the...

journal_title：Pharmaceutical research

authors： Schilling RJ,Mitra AK

更新日期：1992-08-01 00:00:00

abstract：PURPOSE:The aim was to design and thoroughly characterize monodisperse Fe3O4@SiO2-Ag nanoparticles with strong antibacterial properties, which makes them a candidate for targeting bacterial infections. METHODS:The monodisperse Fe3O4 nanoparticles were prepared by oleic acid-stabilized thermal decomposition of Fe(III) ...

journal_title：Pharmaceutical research

authors： Shatan AB,Venclíková K,Zasońska BA,Patsula V,Pop-Georgievski O,Petrovský E,Horák D

更新日期：2019-08-14 00:00:00

abstract：PURPOSE:We evaluated the effect of luminal bacterial metabolism on intestinal absorption of azetirelin in rats. In vitro characteristics of bacterial metabolism of azetirelin were also investigated with the goal of overcoming the low stability of the peptidic drug against luminal microorganisms. METHODS:Plasma azetire...

journal_title：Pharmaceutical research

authors： Sasaki I,Tamura T,Shibakawa T,Fujita T,Murakami M,Yamamoto A,Muranishi S

更新日期：1997-08-01 00:00:00

abstract：PURPOSE:The aim of this study was to develop a labile sphingosine-based liposome for intramuscular gene delivery. METHODS:Sphingosine-based liposomes were formulated in a range of solutions with phosphatidylcholine, then were associated to DNA. The physico-chemical characteristics of the sphingosine/EPC liposomes and ...

journal_title：Pharmaceutical research

authors： Baraldo K,Leforestier N,Bureau M,Mignet N,Scherman D

更新日期：2002-08-01 00:00:00

abstract：PURPOSE:To study the physical and release properties of different molecular weight (MW) pH- and temperature-responsive statistical terpolymers and beads of N-isopropylacrylamide (NIPAAm), butylmethacrylate (BMA) and acrylic acid (AA). METHODS:Random terpolymers of varying MW were synthesized with NIPAAm/BMA/AA of feed...

journal_title：Pharmaceutical research

authors： Ramkissoon-Ganorkar C,Gutowska A,Liu F,Baudys M,Kim SW

更新日期：1999-06-01 00:00:00

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 qua...

journal_title：Pharmaceutical research

authors： Marro D,Kalia YN,Delgado-Charro MB,Guy RH

更新日期：2001-12-01 00:00:00

abstract：PURPOSE:Synthetic hydrogels fabricated from photopolymerization are attractive for tissue engineering for their controlled macroscopic properties, the ability to incorporate biological functionalities, and cell encapsulation. The goal of the present study was to exploit the attractive features of synthetic hydrogels to...

journal_title：Pharmaceutical research

authors： Bryant SJ,Nicodemus GD,Villanueva I

更新日期：2008-10-01 00:00:00

abstract：PURPOSE:The aim of this study was to identify new surfactants with low skin irritant properties for use in pharmaceutical and cosmetic formulations, employing cell culture as an alternative method to in vivo testing. In addition, we sought to establish whether potential cytotoxic properties were related to the size of ...

journal_title：Pharmaceutical research

authors： Sanchez L,Mitjans M,Infante MR,Vinardell MP

更新日期：2004-09-01 00:00:00

abstract：PURPOSE:Some therapeutic peptides exhibit amyloidogenic properties that cause insolubility and cytotoxicity against neuronal cells in vitro. Here, we characterize the conformational change in monomeric therapeutic peptide to its fibrillar aggregate in order to prevent amyloidogenic formation during clinical application...

journal_title：Pharmaceutical research

authors： Onoue S,Ohshima K,Debari K,Koh K,Shioda S,Iwasa S,Kashimoto K,Yajima T

更新日期：2004-07-01 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