European Journal of Pharmaceutical SciencesThis is an RSS file. You can use it to subscribe to this data in your favourite RSS reader, such as GoogleReader, or to display this data on your own website or blog. Subscribe to this data using MyMedWorm.Subscribe to this data using GoogleReader.Subscribe to this data using Bloglines.Subscribe to this data using MyYahoo.

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386 records returned

Transport of Chitosan-DNA nanoparticles in human intestinal M-cell model versus normal intestinal enterocytes.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Oral vaccination is one of the most promising applications of polymeric nanoparticles. Using two different in vitro cellular models to partially reproduce the characteristics of intestinal enterocytes and M-cells, this study demonstrates that nanoparticle transport through the M-cell co-culture model is 5 fold that of the intestinal epithelial monolayer, with at least 80% of the chitosan-DNA nanoparticles uptaken in the first 30minutes. Among the properties of nanoparticles studied, ligand decoration has the most dramatic effect on the transcytosis rate: transferrin modification enhances transport through both models b...
Source: European Journal of Pharmaceutical Sciences - November 11, 2009 Category: Drugs & Pharmacology Authors: Kadiyala I, Loo Y, Roy K, Rice J, Leong KW Tags: Eur J Pharm Sci Source Type: journals

New insights into the mode of action of ultradeformable vesicles using calcein as hydrophilic fluorescent marker.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In conclusion, our results argue against the model that deformable vesicles would carry hydrophilic drugs across the skin and act as a sustained release system in deep tissues. PMID: 19903526 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences)
Source: European Journal of Pharmaceutical Sciences - November 7, 2009 Category: Drugs & Pharmacology Authors: Bahia AP, Azevedo EG, Ferreira LA, Frézard F Tags: Eur J Pharm Sci Source Type: journals

Development of Swelling/Floating Gastroretentive Drug Delivery System Based on a Combination of Hydroxyethyl Cellulose and Sodium Carboxymethyl Cellulose for Losartan and its Clinical Relevance in Healthy Volunteers with CYP2C9 Polymorphism.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The aim of this study was to develop an optimal gastroretentive drug delivery system (GRDDS) for administering Losartan. Additionally, the influence of optimized GRDDS on the bioavailability of Losartan and the formation extent of active metabolite E3174 by CYP2C9 polymorphism was investigated. Swellable and floatable GRDDS tablets combining hydroxyethylcellulose (HEC), sodium carboxymethylcellulose (NaCMC), and sodium bicarbonate were prepared at various compression pressures for evaluating swelling characteristics and floating capacity. Then Losartan was incorporated into optimized formulations for in vitro and in vi...
Source: European Journal of Pharmaceutical Sciences - November 7, 2009 Category: Drugs & Pharmacology Authors: Chen RN, Ho HO, Yu CY, Sheu MT Tags: Eur J Pharm Sci Source Type: journals

The role of organic cation transporters (OCT) in the transfer of metformin in the dually perfused human placenta.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
CONCLUSIONS: A higher transfer rate of metformin was detected in fetal-to-maternal than maternal-to-fetal direction, but a similar difference was observed with antipyrine. Inhibition of OCTs did not have a significant effect on the placental transfer of metformin. Although the existence of other active transporting systems cannot be ruled out, the influence of OCT-dependent active transport system on the placental pharmacokinetics of metformin is unlikely significant. PMID: 19900541 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences)
Source: European Journal of Pharmaceutical Sciences - November 6, 2009 Category: Drugs & Pharmacology Authors: Tertti K, Ekblad U, Heikkinen T, Rahi M, Rönnemaa T, Laine K Tags: Eur J Pharm Sci Source Type: journals

5-hydroxy-L-tryptophan alters gaboxadol pharmacokinetics in rats: Involvement of PAT1 and rOat1 in gaboxadol absorption and elimination.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In conclusion, gaboxadol acts as a substrate for hPAT1 and is a substrate of rOat1. In rats, 5-HTP decreased the initial absorption rate and increased AUC of gaboxadol. 5-HTP thus had a significant impact on the pharmacokinetic profile of gaboxadol. PMID: 19900542 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences)
Source: European Journal of Pharmaceutical Sciences - November 6, 2009 Category: Drugs & Pharmacology Authors: Larsen M, Holm R, Jensen KG, Sveigaard C, Brodin B, Nielsen CU Tags: Eur J Pharm Sci Source Type: journals

Comparative study on determination of antioxidant and membrane activities of propofol and its related compounds.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Certain anesthetics have been suggested to protect against the pathological states associated with oxidative stress. We compared the antioxidant and membrane activities of propofol (2,6-diisopropylphenol) and its related compounds to address the structure-activity relationship especially in a lipid membrane phase. They were studied for the effects on 1,1-diphenyl-2-picrylhydrazyl radicals, nitro blue tetrazolium reduction by superoxide anions and membrane lipid peroxidation by peroxynitrite, and also for the induced changes in membrane fluidity of liposomes. 2-Isopropylphenols scavenged free radicals with the potency b...
Source: European Journal of Pharmaceutical Sciences - November 5, 2009 Category: Drugs & Pharmacology Authors: Tsuchiya H, Ueno T, Tanaka T, Matsuura N, Mizogami M Tags: Eur J Pharm Sci Source Type: journals

Microsphere-based Drug Releasing Scaffolds for Inducing Osteogenesis of Human Mesenchymal Stem Cells in vitro.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In conclusion, by promoting osteogenic development of hMSCs in vitro, this newly designed controlled release system opens a new door to bone reparation and regeneration. PMID: 19895885 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences)
Source: European Journal of Pharmaceutical Sciences - November 3, 2009 Category: Drugs & Pharmacology Authors: Shi X, Wang Y, Varshney RR, Ren L, Gong Y, Wang DA Tags: Eur J Pharm Sci Source Type: journals

Simple and scalable method for peptide inhalable powder production.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The aim of the work was to produce capreomycin dry powder and capreomycin loaded PLGA microparticles intended for tuberculosis inhalation therapy, using simple and scalable methods. Capreomycin physico-chemical characteristics have been modified by hydrophobic ion pairing with sodium oleate. The powder suspension was processed by high pressure homogenization and spray-dried. Spray-drying was also used to prepare capreomycin oleate (CO) loaded PLGA microparticles. CO powder was suspended in the organic phase containing PLGA and the suspension was spray-dried. Particle dimensions were determined using photon correlation ...
Source: European Journal of Pharmaceutical Sciences - October 29, 2009 Category: Drugs & Pharmacology Authors: Schoubben A, Blasi P, Giovagnoli S, Ricci M, Rossi C Tags: Eur J Pharm Sci Source Type: journals

Effect of Hydroxyl Substitution of Flavone on Angiogenesis and Free Radical Scavenging Activities: A Structure Activity Relationship Studies Using Computational Tools.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Angiogenesis is a key process needed for the growth and survival of solid tumors. Anti-angiogenesis may arrest the tumor growth and keep check on cancer metastasis. Developing antiangiogenic agents has remained a significant hope in the mainstream of anticancer research. The free radical implications in the initiation of cancers are well established. In the present studies, simple flavone and flavones with hydroxyl substitution in 'A' and 'C' ring at 3, 5, 6, and 7 were studied for antiangiogenic activities using Chorioallantoic Membrane (CAM) model and kinetics of DPPH (2, 2-diphenyl-1-picryl hydrazine) and superoxide...
Source: European Journal of Pharmaceutical Sciences - October 26, 2009 Category: Drugs & Pharmacology Authors: Rajesh G, Harshala S, Dhananjay G, Jadhav A, Vikram G Tags: Eur J Pharm Sci Source Type: journals

A new approach to characterise pharmaceutical aerosols: measurement of aerosol from a single dose aqueous inhaler with an optical particle counter.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
An in-line sampling system with dilution units for aqueous droplet aerosols from single dose inhalers (Berodual Respimat((R)), Boehringer Ingelheim Pharma GmbH & Co. KG, Germany) for an optical particle counter is described. The device has been designed to interface with a white light aerosol spectrometer (welas((R)) digital 2100, Palas((R)) GmbH, Germany) that allows the time-resolved measurement of highly concentrated aerosols. Performance of the sampling system with regard to the measured particle size distribution (PSD) is compared to Next Generation Impactor (NGI) and to laser diffraction measurements (Sympate...
Source: European Journal of Pharmaceutical Sciences - October 26, 2009 Category: Drugs & Pharmacology Authors: Kuhli M, Weiss M, Steckel H Tags: Eur J Pharm Sci Source Type: journals

Pharmacology of EAPB0203, a novel imidazo[1,2-a]quinoxaline derivative with anti-tumoral activity on melanoma.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In spite of the development of new anticancer drugs by the pharmaceutical industry, melanoma and T lymphomas are diseases for which medical advances remain limited. Thus, there was an urgent need of new therapeutics with an original mechanism of action. Since several years, our group develops quinoxalinic compounds. In this paper, the first preclinical results concerning one lead compound, EAPB0203, are presented. This compound exhibits in vitro cytotoxic activity on A375 and M4Be human melanoma cell lines superior to that of imiquimod and fotemustine. A liquid chromatography-mass spectrometry method was first validate...
Source: European Journal of Pharmaceutical Sciences - October 22, 2009 Category: Drugs & Pharmacology Authors: Khier S, Deleuze-Masquefa C, Moarbess G, Gattacceca F, Margout D, Solassol I, Cooper JF, Pinguet F, Bonnet PA, Bressolle FM Tags: Eur J Pharm Sci Source Type: journals

Computational Discovery of Novel Trypanosomicidal Drug-like Chemicals by Using Bond-based Non-stochastic and Stochastic Quadratic Maps and Linear Discriminant Analysis.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Herein we present results of a Quantitative Structure-Activity Relationship (QSAR) studies to classify and design, in a rational way, new antitrypanosomal compounds by using non-stochastic and stochastic bond-based quadratic indices. A data set of 440 organic chemicals, 143 with antitrypanosomal activity and 297 having other clinical uses, is used to develop QSAR models based on Linear Discriminant Analysis (LDA). Non-stochastic model correctly classifies more than 93% and 95% of chemicals in both training and external prediction groups, respectively. On the other hand, the stochastic model shows an accuracy of about t...
Source: European Journal of Pharmaceutical Sciences - October 22, 2009 Category: Drugs & Pharmacology Authors: Castillo-Garit JA, Vega MC, Rolon M, Marrero-Ponce Y, Kouznetsov VV, Torres DF, Gómez-Barrio A, Bello AA, Montero A, Torrens F, Pérez-Giménez F Tags: Eur J Pharm Sci Source Type: journals

Ex vivo permeability experiments in excised rat intestinal tissue and in vitro solubility measurements in aspirated human intestinal fluids support age-dependent oral drug absorption.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In conclusion, age-dependent permeability of intestinal tissue (rather than age-dependent luminal drug solubility) may contribute to altered intestinal drug absorption in older patients compared to young adults. PMID: 19837159 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences)
Source: European Journal of Pharmaceutical Sciences - October 14, 2009 Category: Drugs & Pharmacology Authors: Annaert P, Brouwers J, Bijnens A, Lammert F, Tack J, Augustijns P Tags: Eur J Pharm Sci Source Type: journals

Characterization and in vitro activities of cell-free antigens from Histoplasma capsulatum-loaded biodegradable microspheres.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In the last decades, the incidence of histoplasmosis, a pulmonary fungal disease caused by Histoplasma capsulatum, has increased worldwide. In this context, vaccines for the prevention of this infection or therapies are necessary. Cell-free antigens (CFAgs) from H. capsulatum when administered for murine immunization purposes are able to confer protection and control of the infection, since they activate cellular immunity. However, the most of vaccination procedures need several antigens administrations and immunoadjuvants, which are not approved for use in humans. The aim of this study was to develop and characterize ...
Source: European Journal of Pharmaceutical Sciences - October 11, 2009 Category: Drugs & Pharmacology Authors: Dos Santos DF, Nicolete R, Souza PR, Bitencourt CD, Junior RR, Bonato VL, Silva CL, Faccioli LH Tags: Eur J Pharm Sci Source Type: journals

Hepatitis C Virus NS3 Protease Inhibitors: Large, Flexible Molecules of Peptide Origin Shows Satisfactory Permeability Across Caco-2 Cells.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The purpose of this study was to investigate the intestinal absorption of tripeptide-based compounds intended for treatment of Hepatitis C Virus (HCV) infection. The intestinal permeability of eleven HCV NS3 protease inhibitors (Mw 687-841, ClogD(pH7.4) 1.2-7.3 and 10-13 hydrogen bond donors/acceptors) were measured using Caco-2 cells. Each compound was investigated in the apical to basolateral (a-b) and basolateral to apical (b-a) direction at pH 7.4. For compounds displaying efflux the experiment was repeated in the presence of 1muM GF120918 to investigate possible involvement of P-glycoprotein (Pgp; ABCB1). All comp...
Source: European Journal of Pharmaceutical Sciences - October 11, 2009 Category: Drugs & Pharmacology Authors: Bergström CA, Bolin S, Artursson P, Rönn R, Sandström A Tags: Eur J Pharm Sci Source Type: journals

Blood Brain Barrier Permeability and Therapeutic Time Window of Ginkgolide B in Ischemia - Reperfusion Injury.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In conclusion, Ginkgolide B could pass through BBB, especially after ischemia - reperfusion injury of brain, and might be therapeutically effective for ischemia / reperfusion injury of human brain. PMID: 19833202 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences)
Source: European Journal of Pharmaceutical Sciences - October 11, 2009 Category: Drugs & Pharmacology Authors: Fang W, Deng Y, Li Y, Shang E, Fang F, Lv P, Bai L, Qi Y, Yan F, Mao L Tags: Eur J Pharm Sci Source Type: journals

Lipid membrane interactions of indacaterol and salmeterol: do they influence their pharmacology properties?Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
This study compares the lipid membrane interactions of indacaterol, an ultra long acting beta-2 agonist that is given once a day, to salmeterol, a twice a day beta-2 agonist, in order to elucidate the potential mechanisms leading to their different pharmacology properties. Salmeterol but not indacaterol perturbed dimyristoyl-phosphatidylcholine membranes. While the liposome partitioning of the two compounds was similar, independent of the lipid composition, the membrane affinity of indacaterol was two-fold greater than that of salmeterol when rafts, i.e. detergent-insoluble membrane domains, were used as the partition phas...
Source: European Journal of Pharmaceutical Sciences - October 7, 2009 Category: Drugs & Pharmacology Authors: Lombardi D, Cuenoud B, Krämer SD Tags: Eur J Pharm Sci Source Type: journals

Effects of the flavonol quercetin on the bioavailability of simvastatin in pigs.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The influence of the dietary flavonol quercetin on the pharmacokinetics of the HMG-CoA reductase inhibitor simvastatin was investigated in pigs. Simvastatin (0.25mg/kg body weight) was orally administered to 6 pigs either without or with quercetin (10mg/kg). In addition, simvastatin was administered to 3 pigs that had received a diet supplemented with the flavonol over a period of 1 week. Daily quercetin intake was 10mg/kg in these animals. Co ingestion of quercetin with the statin did not alter area under the concentration time curve (AUC(0-->infinity)), time to achieve maximum plasma concentration (t(max)) or half...
Source: European Journal of Pharmaceutical Sciences - October 1, 2009 Category: Drugs & Pharmacology Authors: Cermak R, Wein S, Wolffram S, Langguth P Tags: Eur J Pharm Sci Source Type: journals

The Influence of Drug-Drug Interaction and Patients' Characteristics on Valproic Acid's Clearance in Adults with Epilepsy using Nonlinear Mixed Effects Modeling.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
This study confirms the interaction of VPA with TPR, which is presumably dependent on VPA dose. PMID: 19804822 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences)
Source: European Journal of Pharmaceutical Sciences - October 1, 2009 Category: Drugs & Pharmacology Authors: Vučićević K, Miljković B, Pokrajac M, Prostran M, Martinović Z, Grabnar I Tags: Eur J Pharm Sci Source Type: journals

Pharmacokinetic evaluation and modeling of formulated levodopa intranasal delivery systems.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In conclusion, the L-dopa nasal delivery system could be used as a good rescue therapy for PD patients who experience symptom fluctuation with oral L-dopa administration. PMID: 19804823 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences)
Source: European Journal of Pharmaceutical Sciences - October 1, 2009 Category: Drugs & Pharmacology Authors: Kim TK, Kang W, Chun IK, Oh SY, Lee YH, Gwak HS Tags: Eur J Pharm Sci Source Type: journals

Three isostructural solvates of finasteride and their solid-state characterization.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Three crystalline hemi-hydrate, channel solvates (classified as solvates from here on) of finasteride (N-(1,1-di-methylethyl)-3-oxo-4-aza-5alpha-androst-1-ene-17beta-carboxamide) have been obtained and fully characterized. The acetone, methyl ethyl ketone (MEK), and toluene solvates of finasteride, described herein, were found to be isostructural and belong as additional members to a family of previously reported finasteride solvates. Vacuum drying at 85 degrees C for one day produced the metastable, anhydrous Form II of finasteride from all three solvated materials. PMID: 19804824 [PubMed - as supplied by publishe...
Source: European Journal of Pharmaceutical Sciences - October 1, 2009 Category: Drugs & Pharmacology Authors: Schultheiss N, Smit JP, Hanko JA Tags: Eur J Pharm Sci Source Type: journals

Thromboxane A(2) receptor-mediated epidermal growth factor receptor transactivation: involvement of PKC-delta and PKC-varepsilon in the shedding of epidermal growth factor receptor ligands.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
We examined thromboxane A(2) receptor (TP)-mediated transactivation of epidermal growth factor receptor (EGFR) through the shedding of EGFR ligands. A TP agonist U46619 caused the phosphorylation of EGFR in 1321N1 human astrocytoma cells, which was inhibited by an EGFR selective inhibitor AG1478 and by a disintegrin and metalloproteinase (ADAM) inhibitor TAPI-2, indicating TP stimulation caused the EGFR transactivation through the EGFR ligand shedding. Since 1321N1 cells expressed heparin binding-EGF (HB-EGF) mRNA, the mechanism of TP-mediated EGFR transactivation was examined in HEK293 cells expressing alkaline phosphatas...
Source: European Journal of Pharmaceutical Sciences - October 1, 2009 Category: Drugs & Pharmacology Authors: Uchiyama K, Saito M, Sasaki M, Obara Y, Higashiyama S, Nakahata N Tags: Eur J Pharm Sci Source Type: journals

Dynamics of Target-Mediated Drug Disposition.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
We present a mathematical analysis of the basic model underlying target-mediated drug disposition (TMDD) in which a ligand is supplied through an initial bolus or through a constant rate infusion and forms a complex with a receptor (target), which is supplied and removed continuously. Ligand and complex may be eliminated according to first-order processes. We assume that the total receptor pool (free and bound) is constant in time and we give a geometrical description of the evolution of the concentrations of ligand, receptor and receptor-ligand complex which offers a transparent way to compare the full model with simpler ...
Source: European Journal of Pharmaceutical Sciences - September 24, 2009 Category: Drugs & Pharmacology Authors: Peletier LA, Gabrielsson J Tags: Eur J Pharm Sci Source Type: journals

Formulate-ability of ten compounds with different physicochemical profile in SMEDDS.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In order to gain a better understanding of the reasons of successful self-microemulsifying drug delivery systems (SMEDDS) formulation, ten poorly water-soluble drugs, exhibiting different physicochemical properties, were selected. The solubility of the compounds was determined in various oils (long and medium chain) and surfactants (HLB > 12 and HLB < 10). The best performing excipients were selected for SMEDDS formulation. The droplet size and zeta potential of SMEDDS were measured in the absence and the presence of drug. Media, time and the presence of drug showed little or no influence on droplet size of most ...
Source: European Journal of Pharmaceutical Sciences - September 22, 2009 Category: Drugs & Pharmacology Authors: Thi TD, Van Speybroeck M, Barillaro V, Martens J, Annaert P, Augustijns P, Van Humbeeck J, Vermant J, Van den Mooter G Tags: Eur J Pharm Sci Source Type: journals

Solid state characterization of the anti-HIV drug TMC114: interconversion of amorphous TMC114, TMC114 ethanolate and hydrate.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The interconversion of the ethanolate, hydrate and amorphous form of TMC114 ((3-[(4-amino-benzenesulfonyl)-isobutyl-amino]-1-benzyl-2-hydroxypropyl)-carbamic acid hexahydrofuro-[2,3-b]furan-3-yl ester) in open conditions was characterized. TMC114 hydrate and ethanolate form isostructural channel solvates. The crystal structure of TMC114 was obtained from single crystal X-ray diffraction, confirming that it is a channel solvate. Ethanol and water can exchange with one another. TMC114 ethanolate converts into TMC114 hydrate at moderate or high relative humidity (RH) at 25 degrees C, and it converts back into the ethanola...
Source: European Journal of Pharmaceutical Sciences - September 22, 2009 Category: Drugs & Pharmacology Authors: Van Gyseghem E, Stokbroekx S, Armas HN, Dickens J, Vanstockem M, Baert L, Rosier J, Schueller L, Van den Mooter G Tags: Eur J Pharm Sci Source Type: journals

Enantioselective retention of beta-blocking agents on Human Serum Albumin and alpha(1)-Acid Glycoprotein HPLC columns: relationships with different scales of lipophilicity.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The enantioselective retention of thirteen -blockers on HPLC stationary phases supporting human serum albumin (HSA) or alpha(1)-acid glycoprotein (AGP) was investigated. Eight beta-blockers were enantiomerically resolved on the AGP column whereas only four beta-blockers were resolved on the HSA column. Moreover, interactions between beta-blockers and AGP were much stronger than those with HSA. Retention values on both HSA and AGP for less retained enantiomers related well with various lipophilicity parameters, with the best relationships found with log(w)(IAM) values obtained on HPLC stationary phases supporting phosph...
Source: European Journal of Pharmaceutical Sciences - September 20, 2009 Category: Drugs & Pharmacology Authors: Francesco B, Carmen C, Lucia G, Rotonda L, Immacolata M Tags: Eur J Pharm Sci Source Type: journals

Molecular mobility in liquid and glassy states of Telmisartan (TEL) studied by Broadband Dielectric Spectroscopy.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The molecular relaxation in liquid and glassy states of Telmisartan (TEL) has been studied by Broadband Dielectric Spectroscopy (BDS) covering wide temperature and frequency range. Multiple relaxation processes were observed. Besides the primary alpha-relaxation, two secondary relaxations beta and gamma (labelled in order of decreasing time scale) have been reported. Well-separated beta-process observed above and below glass transition temperature T(g), has activation energy E(beta)=81.8kJ/mol and was identified as intermolecular Johari-Goldstein (JG) process. The gamma-relaxation visible in dielectric loss spectra at ...
Source: European Journal of Pharmaceutical Sciences - September 15, 2009 Category: Drugs & Pharmacology Authors: Adrjanowicz K, Wojnarowska Z, Wlodarczyk P, Kaminski K, Paluch M, Mazgalski J Tags: Eur J Pharm Sci Source Type: journals

Combined hydroxypropyl-beta-cyclodextrin and poly(anhydride) nanoparticles improves the oral permeability of paclitaxel.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The aim of this work was to study the effect of the combination between 2-hydroxypropyl-beta-cyclodextrin (HPCD) and bioadhesive nanoparticles on the encapsulation and intestinal permeability of paclitaxel (PTX). In this context, a solid inclusion complex between PTX and HPCD was prepared by the evaporation method. Then, the complex was incorporated in poly(anhydride) nanoparticles by a solvent displacement method. The resulting nanoparticles, PTX-HPCD NP, displayed a size of about 300nm and a drug loading of about 170mug/mg (500-fold higher than in the absence of HPCD). The effect of these nanoparticles on the permeab...
Source: European Journal of Pharmaceutical Sciences - September 14, 2009 Category: Drugs & Pharmacology Authors: Agüeros M, Ruiz-Gatón L, Vauthier C, Bouchemal K, Espuelas S, Ponchel G, Irache JM Tags: Eur J Pharm Sci Source Type: journals

Pharmacokinetic-pharmacodynamic modeling of the effect of propofol on alpha(1)-adrenoceptor-mediated positive inotropy in rat heart.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Since it is unclear whether and how propofol affects the alpha(1)-mediated inotropic response, we used a pharmacokinetic-pharmacodynamic modeling approach in isolated rat hearts to analyze the effect of propofol on receptor binding and signal transduction. In Langendorff rat hearts perfused with buffer containing 12.3muM phenylephrine, 1.27nmol doses of [(3)H]-prazosin were infused (over 1min), in the absence and presence of propofol (28muM). Simultaneous analysis of prazosin outflow concentration and inotropic response (left ventricular developed pressure) using an agonist-antagonist interaction model allowed to estim...
Source: European Journal of Pharmaceutical Sciences - September 14, 2009 Category: Drugs & Pharmacology Authors: Weiss M, Hassna R, Sermsappasuk P, Bednarek T Tags: Eur J Pharm Sci Source Type: journals

Triple verses Glimepiride plus Metformin therapy on Cardiovascular Risk Biomarkers and Diabetic-Cardiomyopathy in Insulin Resistance Type 2 Diabetes Mellitus Rats.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In conclusion, Triple oral hypoglycaemic therapy improves glycemic control, insulin sensitivity, retards diabetic cardiomyopathy and does not increased body weight; decrease more detrimental inflammatory markers, increase interlukin-10 and adiponectin in neonatal streptozotocin induced IRtype2DM Wistar Albino Rats. Triple therapy showed a synergistic effect and was promising in insulin resistance, better in additional cardiovascular risk reduction and those nonresponders to metformin add on glimepiride therapy. PMID: 19765654 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutical Sciences)
Source: European Journal of Pharmaceutical Sciences - September 14, 2009 Category: Drugs & Pharmacology Authors: Sharma AK, Srinivasan BP Tags: Eur J Pharm Sci Source Type: journals

Comparison of the dissolution and pharmacokinetic profiles of two galenical formulations of the endothelin receptor antagonist macitentan.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Macitentan (ACT-064992) is an orally active endothelin receptor antagonist. We first compared the in vitro dissolution characteristics of uncoated and film-coated tablets with hard gelatin capsules containing 10mg ACT-064992. Subsequently, we compared the oral pharmacokinetics of ACT-064992 and its active metabolite ACT-132577 of the coated tablet and the gelatin capsule formulation in 11 male volunteers. The dissolution profile showed a rapid disintegration of all formulations with >90% dissolution of ACT-064992 within 45minutes. The pharmacokinetics of ACT-064992 and its metabolite ACT-132577 were comparable for t...
Source: European Journal of Pharmaceutical Sciences - September 14, 2009 Category: Drugs & Pharmacology Authors: Kummer O, Haschke M, Hammann F, Bodmer M, Bruderer S, Regnault Y, Dingemanse J, Krähenbühl S Tags: Eur J Pharm Sci Source Type: journals

Pharmacokinetics of ipriflavone and its two metabolites, M1 and M5, after the intravenous and oral administration of ipriflavone to rat model of diabetes mellitus induced by streptozotocin.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Ipriflavone was reported to be primarily metabolized via hepatic cytochrome P450 (CYP) 1A1/2 and 2C11 in male Sprague-Dawley rats. The protein expression and/or mRNA levels of hepatic CYP1A subfamily and 2C11 was reported to be increased and decreased, respectively, in diabetic rats induced by streptozotocin (DMIS rats). Thus, the pharmacokinetic parameters of ipriflavone and its two metabolites, M1 and M5, were compared after the i.v. (20mg/kg) and p.o. (200mg/kg) administration of ipriflavone to control and DMIS rats. After both i.v. and p.o. administration of ipriflavone to DMIS rats, the AUCs of ipriflavone were si...
Source: European Journal of Pharmaceutical Sciences - September 13, 2009 Category: Drugs & Pharmacology Authors: Lee DY, Chung HJ, Choi YH, Lee U, Kim SH, Lee I, Lee MG Tags: Eur J Pharm Sci Source Type: journals

Multiple approaches to pharmaceutical polymorphism investigation - a case study.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Polymorph screening of Compound A, an investigational drug, revealed two anhydrous polymorphs (Forms I and II) and two monohydrates (Forms III and IV) of this pharmaceutical solid. The physiochemical properties of the four forms were characterized by thermal analysis, hot-stage microscopy, equilibrium solubility and intrinsic dissolution rate measurements, and X-ray powder diffraction. Inter-conversion relationship of the four forms was fully elucidated. Thermodynamic stability relationship was inferred from melting data for Form I and Form II and evaluated by van't Hoff plot for Form III and Form IV. Form I and Form I...
Source: European Journal of Pharmaceutical Sciences - September 9, 2009 Category: Drugs & Pharmacology Authors: Li H, Kiang YH, Jona J Tags: Eur J Pharm Sci Source Type: journals

Inhibition of nucleoside transport and synergistic potentiation of methotrexate cytotoxicity by cimicifugoside, a triterpenoid from Cimicifuga simplex.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Cimicifugoside, a triterpenoid isolated from Cimicifuga simplex, which has been used as a traditional Chinese medicine due to its anti-inflammatory, analgesic or anti-pyretic action, was examined for inhibition of nucleoside transport and synergistic potentiation of methotrexate cytotoxicity. Cimicifugoside inhibited uptake of uridine, thymidine and adenosine in human leukemia U937 cells with the low nanomolar IC(50) values, but did not affect that of uracil, leucine or 2-deoxyglucose at </=100nM. Cimicifugoside analogs differentially inhibited uridine uptake in the order cimicifugoside > cimicifugenin (aglycon o...
Source: European Journal of Pharmaceutical Sciences - September 9, 2009 Category: Drugs & Pharmacology Authors: Yawata A, Matsuhashi Y, Kato H, Uemura K, Kusano G, Ito J, Chikuma T, Hojo H Tags: Eur J Pharm Sci Source Type: journals

Simultaneous monitoring of drug and solvent diffusion across a model membrane using ATR-FTIR spectroscopy.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy has been used to simultaneously follow the diffusion of model drugs and solvent across polydimethylsiloxane (silicone) membrane. Three model drugs, cyanophenol (CNP), methyl nicotinate (MN) and butyl paraben (BP) were selected to cover a range of lipophilicities. Isostearyl isostearate (ISIS) was chosen as the solvent because its large molecular weight should facilitate observation of whether the drug molecules are able to diffuse through the membrane independently of the solvent. The diffusion of the three drugs and the solvent was success...
Source: European Journal of Pharmaceutical Sciences - September 7, 2009 Category: Drugs & Pharmacology Authors: McAuley WJ, Mader KT, Tetteh J, Lane ME, Hadgraft J Tags: Eur J Pharm Sci Source Type: journals

Evaluation of intestinal absorption enhancement and local mucosal toxicity of two promoters. I. Studies in isolated rat and human colonic mucosae.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The effects of two absorption promoters, (sodium caprate (C(10)) and melittin), on intestinal permeability and viability were measured in intact rat and human colonic epithelia mounted in Ussing chambers. Apical-side addition of C(10) (10mM) and melittin (10-50muM) rapidly reduced the transepithelial electrical resistance (TEER) and increased the apparent permeability coefficient (Papp) of [(14)C]-mannitol and FITC-dextran-4 kDa (FD4) across colonic mucosae from both species. Effects of C(10) on flux were greater than those of melittin at the concentrations selected. C(10) irreversibly decreased TEER, but the effects o...
Source: European Journal of Pharmaceutical Sciences - September 4, 2009 Category: Drugs & Pharmacology Authors: Maher S, Kennelly R, Bzik VA, Baird AW, Wang X, Winter D, Brayden DJ Tags: Eur J Pharm Sci Source Type: journals

Paclitaxel and immune system.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Chemotherapy remains the mainstay of treatment for both early stage as well as metastatic tumors. Paclitaxel (PTX), a novel anticancer drug, is a prominent taxane which is active against a broad range of tumors that are generally considered to be refractory to conventional chemotherapy, with benefits gained in terms of overall survival and disease-free survival. PTX is initially characterized as a mitotic inhibitor, and its anti-neoplastic effect is derived from binding to tubulin and excessive microtubule stabilization. Interestingly, drugs traditionally used for tumor cytoreduction, can exert both positive and negati...
Source: European Journal of Pharmaceutical Sciences - September 2, 2009 Category: Drugs & Pharmacology Authors: Javeed A, Ashraf M, Ghafoor A, Mukhtar MM Tags: Eur J Pharm Sci Source Type: journals

TMC-MCC (N-trimethyl Chitosan- Mono-N-carboxymethyl Chitosan) Nanocomplexes for Mucosal Delivery of Vaccines.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In this study, for the first time, TMC/MCC complex nanoparticles as a delivery system and as an adjuvant were developed and evaluated to obtain systemic and mucosal immune responses against nasally administered tetanus toxoid (TT). Nanoparticles were developed by complexation between the oppositely charged chitosan derivatives, N-trimethyl chitosan (TMC, polycationic) and mono-N-carboxymethyl chitosan (MCC, polyampholytic) without using any crosslinker for mucosal vaccination. The cellular viability was found to be higher with TMC/MCC complex compared to that of MCC and TMC alone. Size, zeta-potential and morphology of the...
Source: European Journal of Pharmaceutical Sciences - September 2, 2009 Category: Drugs & Pharmacology Authors: Sayın B, Somavarapu S, Li XW, Sesardic D, Senel S, Alpar OH Tags: Eur J Pharm Sci Source Type: journals

Role of MicroRNA-214 in Ginsenoside-Rg1-induced Angiogenesis.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
MicroRNAs (miRNAs) are small non-coding RNAs that act as post-transcriptional gene modulators. Ginsenoside-Rg1, one of the active components of ginseng, has been confirmed as an angiogenesis inducer. Using miRNA microarray analysis, a total of 17 (including miR-214) and 5 miRNAs were found to be down- or up-regulated by Rg1 in human umbilical vein endothelial cells (HUVEC), respectively. Since miR-214 is closely related to endothelial nitric oxide synthase (eNOS) and hence angiogenesis; its expression was further validated by qRT-PCR. We also investigated the role of miR-214 on eNOS expression and in tubulogenesis and ...
Source: European Journal of Pharmaceutical Sciences - September 2, 2009 Category: Drugs & Pharmacology Authors: Chan LS, Yue PY, Mak NK, Wong RN Tags: Eur J Pharm Sci Source Type: journals

Surface energy changes and their relationship with the dispersibility of salmeterol xinafoate powders for inhalation after storage at high RH.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
This study investigated the relationship between surface energy of micronized lactose, coarse lactose and salmeterol xinafoate and dispersibility from a mixture after storage at 75% RH. Surface energies, dispersibility, morphology, and presence of amorphous domains were determined by Inverse Gas Chromatography, Twin Stage Impinger, Scanning Electron Microscope and Dynamic Vapour Sorption, respectively. The fine particle fraction of mixture decreased significantly in four weeks (P<0.05), reaching a static level in three months. Amorphous content was not detected in the micronized lactose, coarse lactose and salmeterol xi...
Source: European Journal of Pharmaceutical Sciences - August 31, 2009 Category: Drugs & Pharmacology Authors: Das S, Larson I, Young P, Stewart P Tags: Eur J Pharm Sci Source Type: journals

Stabilized Polymeric Micelles by Electrostatic Interactions for Drug Delivery System.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Methoxy poly(ethylene glycol)-block-oligo(L-aspartic acid)-block-poly(varepsilon-caprolactone) with four aspartic acid groups was synthesized with a molecular weight and M(w)/M(n) of 8,930 and 1.22. Polymeric micelles were formed by dialysis and stabilized by electrostatic interactions between the carboxylic acid groups and calcium cations. The critical micelle concentration of mPEG-Asp-PCL was determined to be 0.078mg/mL. At 0.02mg/mL, the dissociation of micelles without ionic stabilization formed an opaque, phase-separated solution, while the stabilized micelles under the same conditions showed structural stability ...
Source: European Journal of Pharmaceutical Sciences - August 31, 2009 Category: Drugs & Pharmacology Authors: Cha EJ, Kim JE, Ahn CH Tags: Eur J Pharm Sci Source Type: journals

Inhibition of Bovine Viral Diarrhea Virus In vitro by Xanthohumol: Comparisons with Ribavirin and Interferon-alpha and Implications for the Development of Anti-Hepatitis C Virus Agents.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In this study, the ability of XN to inhibit bovine viral diarrhea virus (BVDV), a surrogate model of hepatitis C virus (HCV), was investigated. The antiviral activity of XN was compared with that of ribavirin (RBV) and interferon (IFN)-alpha. The results showed that XN could inhibit BVDV induced cytopathic effects (CPE). At 1000 TCID(50) and 100 TCID(50), the values of 50% effective concentration (EC(50)) were 3.24+/-0.02mg/l and 2.77+/-0.19mg/l, respectively, and the therapeutic indices were >7.72 and >9.03, respectively. XN inhibited BVDV E2 expression and viral RNA levels in a dose-dependent manner. At 6.25mg/l, X...
Source: European Journal of Pharmaceutical Sciences - August 27, 2009 Category: Drugs & Pharmacology Authors: Zhang N, Liu Z, Han Q, Chen J, Lou S, Qiu J, Zhang G Tags: Eur J Pharm Sci Source Type: journals

Advantages Of Neurofuzzy Logic Against Conventional Experimental Design And Statistical Analysis In Studying And Developing Direct Compression Formulations.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
This study has investigated the utility and potential advantages of an artificial intelligence technology- neurofuzzy logic- as a modeling tool to study direct compression formulations. The modeling performance was compare with traditional statistical analysis. From results it can be stated that the normalized error obtained from neurofuzzy logic was lower. Compared to the multiple regression analysis neurofuzzy logic showed higher accuracy in prediction for the five outputs studied. Rule sets generated by neurofuzzy logic are completely in agreement with the findings based on statistical analysis and advantageously genera...
Source: European Journal of Pharmaceutical Sciences - August 25, 2009 Category: Drugs & Pharmacology Authors: Landín M, Rowe RC, York P Tags: Eur J Pharm Sci Source Type: journals

Increasing the selectivity of amikacin in rat peritoneal macrophages using carrier erythrocytes.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The selectivity of amikacin in macrophages in vitro and its biodistribution in peritoneal macrophages and other tissues were studied in rats using carrier erythrocytes. Amikacin-loaded erythrocytes were prepared using a hypotonic dialysis method. The in vitro uptake of amikacin by peritoneal macrophages was studied using cell monolayers. The in vivo uptake by macrophages and the tissue distribution of amikacin were studied in two groups of rats that received either amikacin in saline solution, or amikacin-loaded erythrocytes. Pharmacokinetic analyses were performed using model-independent methods. The administration of...
Source: European Journal of Pharmaceutical Sciences - August 23, 2009 Category: Drugs & Pharmacology Authors: Briones E, Colino CI, Lanao MJ Tags: Eur J Pharm Sci Source Type: journals

Characterisation of the conjugate of the (6-maleimidocaproyl)hydrazone derivative of doxorubicin with lactosaminated human albumin by (13)C NMR spectroscopy.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In order to improve the efficacy of doxorubicin (DOXO) in the treatment of hepatocellular carcinomas, the drug was conjugated with lactosaminated human albumin (L-HSA), a hepatotropic drug carrier. Conjugation was performed using the (6-maleimidocaproyl)hydrazone derivative of the drug (DOXO-EMCH). The maleimide group of DOXO-EMCH reacts with the aminoacidic residues of the carrier forming stable bonds, whereas the hydrazone bond is rapidly hydrolysed in the acidic endosomal and lysosomal compartments of the cells allowing the intracellular release of DOXO. To identify the amino acids of L-HSA involved in the bond with...
Source: European Journal of Pharmaceutical Sciences - August 16, 2009 Category: Drugs & Pharmacology Authors: Boga C, Fiume L, Baglioni M, Bertucci C, Farina C, Kratz F, Manerba M, Naldi M, Di Stefano G Tags: Eur J Pharm Sci Source Type: journals

Itraconazole/TPGS/Aerosil((R))200 solid dispersions Characterization, physical stability and in-vivo performance.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Solid dispersions were successfully prepared by co-spray-drying of TPGS-stabilized itraconazole nanosuspensions with Aerosil((R))200, followed by heat treatment of the powders. The itraconazole/ Aerosil((R))200 weight ratios amounted to 50/50, 30/70, 40/60 and 20/80. The itraconazole content of the powders was close to the expected value, with relative errors between 0.3 and 7.8%. XRPD, SSNMR and DSC evaluation on the powders revealed the formation of amorphous itraconazole and the absence of glassy itraconazole. Dissolution of the powders was enhanced compared to crystalline and glassy itraconazole (a 2-dimensional st...
Source: European Journal of Pharmaceutical Sciences - August 13, 2009 Category: Drugs & Pharmacology Authors: Van Eerdenbrugh B, Van Speybroeck M, Mols R, Houthoofd K, Martens JA, Froyen L, Van Humbeeck J, Augustijns P, Van Den Mooter G Tags: Eur J Pharm Sci Source Type: journals

Estimation of the percolation thresholds in ternary lobenzarit disodium-dextran-HPMC hydrophilic matrices tablets: Effects of initial porosity.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The aim of this work is to estimate the excipient percolation threshold for a new combined matrix native dextran (DT), serie B110-1-2 (Mw 2x10(6)): HPMC K4M CR: lobenzarit disodium (LBD) system and demonstrate the advantages of this ternary system with respect to previously reported binary dextran:LBD and HPMC:LBD tablets. The formulations studied were prepared with different amount of excipient (DT:HPMC, 4:1wt/wt for all tablets and relative polymer/drug particle size of 4.17) in the range of 10-70% wt/wt. Dissolution studies were carried out using the paddle method (100 r.p.m) and one face water uptake measurements w...
Source: European Journal of Pharmaceutical Sciences - August 6, 2009 Category: Drugs & Pharmacology Authors: Gil EC, Colarte AI, Bataille B, Brouillet F, Caraballo I Tags: Eur J Pharm Sci Source Type: journals

Evaluation of intestinal absorption and mucosal toxicity using two promoters. II. Rat instillation and perfusion studies.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
We compared the effectiveness of two absorption promoters, sodium caprate (C(10)) and melittin, in increasing the bioavailability (F) of poorly absorbed paracellular flux markers across the intestinal mucosae of rats in situ, together with examination of their effects on morphology. C(10) (100mM) and melittin (50muM) significantly increased absorption of FITC-dextran-4 kDa (FD4) following jejunal and colonic instillations. F of FD4 following jejunal instillations with C(10) was increased from 0.07% to 2.3%, while it was increased from 0.07% to 0.53% in the presence of melittin. F of FD4 following colonic instillations ...
Source: European Journal of Pharmaceutical Sciences - August 3, 2009 Category: Drugs & Pharmacology Authors: Maher S, Wang X, Bzik V, McClean S, Brayden DJ Tags: Eur J Pharm Sci Source Type: journals

Supercooled smectic nanoparticles: Influence of the matrix composition and in vitro cytotoxicity.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Cholesteryl nonanoate (CN), myristate (CM), palmitate (CP) and oleate (CO) alone or in combination were evaluated as matrix lipids for the preparation of supercooled smectic nanoparticles with a high stability against recrystallization during storage. The phase behavior of the cholesterol esters in the bulk was studied by polarizing light microscopy, differential scanning calorimetry (DSC) and small angle X-ray scattering (SAXS). Colloidal dispersions with pure and mixed cholesterol ester matrices were prepared by high-pressure melt homogenization and characterized by photon correlation spectroscopy, laser diffraction ...
Source: European Journal of Pharmaceutical Sciences - August 3, 2009 Category: Drugs & Pharmacology Authors: Kuntsche J, Koch MH, Fahr A, Bunjes H Tags: Eur J Pharm Sci Source Type: journals

Involvement of PI3K-Akt-Bad pathway in apoptosis induced by 2,6-di-O-methyl-beta-cyclodextrin, not 2,6-di-O-methyl-alpha-cyclodextrin, through cholesterol depletion from lipid rafts on plasma membranes in cells.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Cyclodextrins (CyDs), which are widely used to increase the solubility of drug in pharmaceutical fields, are known to induce hemolysis and cytotoxicity at high concentrations. However, it is still not unclear whether cell death induced by CyDs is apoptosis or not. Therefore, in the present study, we investigated the effects of various kinds of CyDs on apoptosis in the cells such as NR8383 cells, A549 cells and Jurkat cells. Of various CyDs, methylated CyDs inducted cell death under the present experimental conditions, but hydroxypropylated CyDs and sufobutyl ether-beta-CyD (SBE7-beta-CyD) did not. Of methylated CyDs, 2...
Source: European Journal of Pharmaceutical Sciences - August 3, 2009 Category: Drugs & Pharmacology Authors: Motoyama K, Kameyama K, Onodera R, Araki N, Hirayama F, Uekama K, Arima H Tags: Eur J Pharm Sci Source Type: journals