European Journal of Pharmaceutical Sciences (EUR J PHARM SCI )

Publisher: European Federation for Pharmaceutical Sciences, Elsevier

Description

The European Journal of Pharmaceutical Sciences is the official journal of the European Federation for Pharmaceutical Sciences (EUFEPS). The journal publishes research reports, review articles and scientific commentaries on all aspects of the pharmaceutical sciences with strong emphasis on originality and scientific quality. The Editors welcome articles in this multidisciplinary field, ranging from drug discovery, over drug delivery to drug development. More specifically, the Journal publishes reports in medicinal chemistry, pharmacology, drug absorption and metabolism, pharmacokinetics and pharmacodynamics, pharmaceutical and biomedical analysis, drug delivery including gene delivery, drug targeting, pharmaceutical technology, pharmaceutical biotechnology and clinical drug evaluation. Scientific commentaries and review articles are generally by invitation only or by consent of the Editors. Proceedings of scientific meetings may be published as special issues or supplements to the Journal. Manuscripts submitted to the Journal are only accepted on the understanding that (a) they are subject to editorial review (generally by two independent referees); (b) they have not been, and will not be, published in whole or in part in any other journal; (c) the recommendations of the Declarations of Helsinki and Tokyo, for humans, and the European Community guidelines as accepted principles for the use of experimental animals have been adhered to.

  • Impact factor
    2.99
    Show impact factor history
     
    Impact factor
  • 5-year impact
    3.42
  • Cited half-life
    6.60
  • Immediacy index
    0.58
  • Eigenfactor
    0.01
  • Article influence
    0.87
  • Website
    European Journal of Pharmaceutical Sciences website
  • Other titles
    European journal of pharmaceutical sciences (Online), Pharmaceutical sciences, EJPS
  • ISSN
    0928-0987
  • OCLC
    38945661
  • Material type
    Document, Periodical, Internet resource
  • Document type
    Internet Resource, Computer File, Journal / Magazine / Newspaper

Publisher details

Elsevier

  • Pre-print
    • Author can archive a pre-print version
  • Post-print
    • Author can archive a post-print version
  • Conditions
    • Pre-print allowed on any website or open access repository
    • Voluntary deposit by author of authors post-print allowed on authors' personal website, arXiv.org or institutions open scholarly website including Institutional Repository, without embargo, where there is not a policy or mandate
    • Deposit due to Funding Body, Institutional and Governmental policy or mandate only allowed where separate agreement between repository and the publisher exists.
    • Permitted deposit due to Funding Body, Institutional and Governmental policy or mandate, may be required to comply with embargo periods of 12 months to 48 months .
    • Set statement to accompany deposit
    • Published source must be acknowledged
    • Must link to journal home page or articles' DOI
    • Publisher's version/PDF cannot be used
    • Articles in some journals can be made Open Access on payment of additional charge
    • NIH Authors articles will be submitted to PubMed Central after 12 months
    • Publisher last contacted on 18/10/2013
  • Classification
    ​ green

Publications in this journal

  • [Show abstract] [Hide abstract]
    ABSTRACT: Various polymer drug conjugates (13–16) such as primaquine and dihydroartemisinin conjugated 2-propoxy substituted polyphosphazenes (13), primaquine and dihydroartemisinin conjugated 4-acetamidophenoxy substituted polyphosphazenes (14), primaquine and dihydroartemisinin conjugated 4-formyl substituted polyphosphazenes (15) and primaquine and dihydroartemisinin conjugated 4-aminoethylbenzoate substituted polyphosphazenes (16) were synthesized using substituted polyphosphazenes as polymer and primaquine and dihydroartemisinin as combination antimalarial pharmacophores and formulated to nanoparticles to achieve novel controlled combined drug delivery approach for radical cure of malaria. The polymeric backbone was suitably substituted to impart different physicochemical properties. The polymer-drug conjugates were characterized by IR, 1HNMR, 31PNMRand their molecular weights were determined by Gel Permeation Chromatography. The thermal properties of the conjugates (13–16) were studied by DSC and TGA. The conjugates (13–16) were then formulated to nanoparticles formulations to increase their uptake by hepatocytes and to achieve targeted drug delivery. The nanoparticle formulations were characterized by Zeta Sizer and their morphology were studied by TEM (Transmission Electron Microscopy) imaging. The nanoparticles formulations exhibited biphasic in vitro drug release profile, the initial burst release followed by a sustained release owing to the non-fickian diffusion during first step release and fickian diffusion during second step release. In vivo antimalarial efficacy was tested using Plasmodium berghei (NK65 resistant strain) infected swiss albino mice at different doses. The combination therapy exhibited promising antimalarial efficacy at lower doses in comparison to the standard drug combination. Further, this combination therapy provided protection over 35 days without any recrudescence, thus proving to be effective against resistant malaria. The study provides an alternative combination regimen found to be effective in the treatment of resistant malaria.
    European Journal of Pharmaceutical Sciences 01/2015; 66:123-137.
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    ABSTRACT: A mathematical model was developed to predict the amount of drug delivered into the skin via the dissolution of a microneedle (MN). This approach differs markedly from previous research which focused on similar phenomena but failed to include a biological membrane. Dimensionless governing equations were derived to help predict the needle height and fate of the active ingredient in the skin layer after application of the device. Simulation studies with fentanyl revealed that the drug concentration was proportional to its mass fraction in the MN. The effect of the pitch on skin permeation was mildly nonlinear. A larger amount of fentanyl was delivered from microneedle arrays with smaller pitch size. The dissolution process was independent of changes in the elimination rate constant. An optimization algorithm was applied to show how to recover this parameter from needle height – time data.
    European Journal of Pharmaceutical Sciences 12/2014;
  • [Show abstract] [Hide abstract]
    ABSTRACT: Various polymer drug conjugates (13-16) such as primaquine and dihydroartemisinin conjugated 2-propoxy substituted polyphosphazenes (13), primaquine and dihydroartemisinin conjugated 4-acetamidophenoxy substituted polyphosphazenes (14), primaquine and dihydroartemisinin conjugated 4-formyl substituted polyphosphazenes (15) and primaquine and dihydroartemisinin conjugated 4-aminoethylbenzoate substituted polyphosphazenes (16) were synthesized using substituted polyphosphazenes as polymer and primaquine and dihydroartemisinin as combination antimalarial pharmacophores and formulated to nanoparticles to achieve novel controlled combined drug delivery approach for radical cure of malaria. The polymeric backbone was suitably substituted to impart different physicochemical properties. The polymer-drug conjugates were characterized by IR, 1H-NMR, 31P-NMR and their molecular weights were determined by Gel Permeation Chromatography. The thermal properties of the conjugates (13-16) were studied by DSC and TGA. The conjugates (13-16) were then formulated to nanoparticles formulations to increase their uptake by hepatocytes and to achieve targeted drug delivery. The nanoparticle formulations were characterized by Zeta Sizer and their morphology were studied by TEM (Transmission Electron Microscopy) imaging. The nanoparticles formulations exhibited biphasic in vitro drug release profile, the initial burst release followed by a sustained release owing to the non-fickian diffusion during first step release and fickian diffusion during second step release. In vivo antimalarial efficacy was tested using P. berghei (NK65 resistant strain) infected swiss albino mice at different doses. The combination therapy exhibited promising antimalarial efficacy at lower doses in comparison to the standard drug combination. Further, this combination therapy provided protection over 35 days without any recrudescence, thus proving to be effective against resistant malaria. The study provides an alternative combination regimen found to be effective in the treatment of resistant malaria.
    European Journal of Pharmaceutical Sciences 10/2014;
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    ABSTRACT: Antiepileptic drugs (AEDs)-induced adverse consequences on bone are now well recognized. Despite this, there is limited data on the effect of anti-osteoporotic therapies on AEDs-induced bone loss. We hypothesize that estrogen deprivation following phenytoin (PHT) and sodium valproate (SVP) therapy could lead to adverse bony effects. Both PHT and SVP inhibit human aromatase enzyme and stimulate microsomal catabolism of oestrogens. Estrogen deficiency states are known to reduce the deposition of transforming growth factor-β (TGF-β3), a bone matrix protein, having anti-osteoclastic property. Thus, an attempt was made to investigate the effect of raloxifene, a selective oestrogen receptor modulator, in comparison with calcium and vitamin D3 (CVD) supplementation, on PHT and SVP-induced alterations in bone in mice and to unravel the role of estradiol and TGF-β3 in mediation of bony effects by either AEDs or raloxifene. Further, the effect of raloxifene on seizures and on the antiepileptic efficacy of PHT and SVP was investigated. Swiss strains of female mice were treated with PHT (35 mg/kg, p.o.) and SVP (300 mg/kg, p.o.) for 120 days to induce bone loss as evidenced by reduced bone mineral density (BMD) and altered bone turnover markers (BTMs) in lumbar bones (alkaline phosphatase, tartarate resistant acid phosphatase, hydroxyproline) and urine (calcium). The bone loss was accompanied by reduced serum estradiol levels and bone TGF-β3 content. Preventive and curative treatment with raloxifene ameliorated bony alterations and was more effective than CVD. It also significantly restored estradiol and TGF-β3 levels. Deprived estrogen levels (that in turn reduced lumbar TGF-β3 content) following PHT and SVP, thus, might represent one of the various mechanisms of AEDs-induced bone loss. Raloxifene preserved the bony changes without interfering with antiepileptic efficacy of these drugs, and hence raloxifene could be a potential therapeutic option in the management of PHT and SVP-induced bone disease if clinically approved.
    European Journal of Pharmaceutical Sciences 10/2014; 62:219–226.
  • Source
    European Journal of Pharmaceutical Sciences 10/2014; 63:243.
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    ABSTRACT: Valproic acid is an anti-convulscant drug that is widely used in the treatment of different types of epilepsy and since its introduction the clinical use has increased rapidly both as a sole agent and in combination therapies. The mechanism of action has been linked to blockade of voltage-dependent sodium channels and potentiation of GABAergic transmission. The most widely used route of administration of valproic acid is oral, although it can also be given intravenously and rectally and its pharmacokinetics has been studied extensively. The aim of this work was to develop a physiologically based pharmacokinetic model for plasma and tissue/organ prediction in children and adults following intravenous and oral dosing of valproic acid. The plasma/tissue concentration profile will be used for clinical trial simulation in Dravet syndrome, a rare form of epilepsy in children where the combination of valproic acid, stiripentol and clobazam has shown remarkable results. A physiologically based pharmacokinetic model was developed with compartments for gut lumen, enterocyte, gut tissue, systemic blood, kidney, liver, brain, spleen, muscle and rest of body. System and drug specific parameters for the model were obtained from the literature from in vitro and in vivo experiments. The model was initially developed for adults and scaled to children using age-dependent changes in anatomical and physiological parameters and ontogeny functions for enzyme maturation assuming the same elimination pathways in adults and children. The results from the model validation showed satisfactory prediction of plasma concentration both in terms of mean prediction and variability in children and adults following intravenous and oral dosing especially after single doses. The model also adequately predicts clearance in children. Due to limited distribution of valproic acid into tissues, the concentration in plasma is about 8-9 times higher than tissues/organs. The model could help to improve clinical outcome in the treatment of Dravet syndrome through dose optimisation.
    European Journal of Pharmaceutical Sciences 10/2014; 63:45–52.
  • European Journal of Pharmaceutical Sciences 06/2014;
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    ABSTRACT: Assessment of oral drug bioavailability is an important parameter for new chemical entities (NCEs) in drug development cycle. After evaluating the pharmacological response of these new molecules, the following critical stage is to investigate their in vitro permeability. Despite the great success achieved by prodrugs, covalent linking the drug molecule with a hydrophobic moiety might result in a new entity that might be toxic or ineffective. Therefore, an alternative that would improve the drug uptake without affecting the efficacy of the drug molecule would be advantageous. The aim of the current study is to investigate the effect of ion-pairing on the permeability profile of a model drug: indomethacin (IND) to understand the mechanism behind the permeability improvement across Caco-2 monolayers. Arginine and lysine formed ion-pairs with IND at various molar ratios 1:1, 1:2, 1:4 and 1:8 as reflected by the double reciprocal graphs. The partitioning capacities of the IND were evaluated using octanol/water partitioning studies and the apparent permeabilities (Papp) were measured across Caco-2 monolayers for the different formulations. Partitioning studies reflected the high hydrophobicity of IND (Log P= 3) which dropped upon increasing the concentrations of arginine/lysine in the ion pairs. Nevertheless, the prepared ion pairs improved IND permeability especially after 60 minutes of the start of the experiment. Coupling partitioning and permeability results suggest a decrease in the passive transcellular uptake due to the drop in IND partition capacities and a possible involvement of active carriers. Future work will investigate which transport gene might be involved in the absorption of the ion paired formulations using molecular biology technologies.
    European Journal of Pharmaceutical Sciences 05/2014;
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    ABSTRACT: The purpose of this study was to systematically design pure antibiotic drug dry powder inhalers (DPIs) for targeted antibiotic pulmonary delivery in the treatment of pulmonary infections and comprehensively correlate the physicochemical properties in the solid-state and spray-drying conditions effects on aerosol dispersion performance as dry powder inhalers (DPIs). The two rationally chosen model antibiotic drugs, tobramycin (TOB) and azithromycin (AZI), represent two different antibiotic drug classes of aminoglycosides and macrolides, respectively. The particle size distributions were narrow, unimodal, and in the microparticulate/nanoparticulate size range. The SD particles possessed relatively spherical particle morphology, smooth surface morphology, low residual water content, and the absence of long-range molecular order. The emitted dose (ED%), fine particle fraction (FPF%) and respirable fraction (RF%) were all excellent. The MMAD values were in the inhalable range (< 10μm) with smaller MMAD values for SD AZI powders in contrast to SD TOB powders. Positive linear correlations were observed between the aerosol dispersion performance parameter of FPF with increasing spray-drying pump rates and also with the difference between thermal parameters expressed as Tg-To (i.e. the difference between the glass transition temperature and outlet temperature) for SD AZI powders. The aerosol dispersion performance for SD TOB appeared to be influenced by its high water vapor sorption behavior (hygroscopicity) and the ratio of pump rate/To. Aerosol dispersion performance of SD powders were distinct for both antibiotic drug aerosol systems and also between different pump rates for each system.
    European Journal of Pharmaceutical Sciences 02/2014; 15:191-205.
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    ABSTRACT: Development of a bio-composite using synergistic combination is a promising strategy to address various pathological manifestations of acute and chronic wounds. In the present work, we have combined three materials viz., mupirocin as an antimicrobial drug, sol–gel processed silica microsphere as drug carrier for sustained delivery of drug and collagen, an established wound healer as scaffold. The mupirocin-loaded silica microspheres (Mu-SM) and Mu-SM loaded collagen scaffold were characterized for surface morphology, entrapment efficiency and distribution homogeneity, in vitro drug release, water uptake capacity, cell proliferation and antibacterial activity. In vivo wound healing efficacy of the bio-composite was experimented using full thickness excision wound model in Wistar albino rats. The Mu-SM incorporated collagen scaffold showed good in vitro characteristics in terms of better water uptake, sustained drug availability and antimicrobial activity. The wound closure analysis revealed that the complete epithelialisation was observed at 14.2 ± 0.44 days for Mu-SM loaded collagen, whereas this was 17.4 ± 0.44 days and 20.6 ± 0.54 days for collagen and control groups, respectively. Consequently, the synergistic strategy of combining mupirocin-loaded silica microspheres and collagen as a Mu-SM loaded collagen dressing material would be an ideal biomaterial for the treatment of surface wounds, burns and foot ulcers.
    European Journal of Pharmaceutical Sciences 02/2014; 52:26–33.
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    ABSTRACT: Purpose: The aim of this study is to develop a specific, sensitive, simple, and rapid HPLC method with UV detection to study pharmacokinetics of tirofiban in serum of rats alone or in the presence of heparin as simultaneous therapy. Material and Methods: Thirty six Wistar rats were used randomly assigned in two groups: control group (n = 18), and group with experimentally induced venous thrombosis by ligature of the femoral vein (n = 18). Tirofiban hydrochloride was dissolved in sterile saline. The i.v. bolus doses (0,6 mg/kg; 0,8 mg/kg; 1 mg/kg) were injected using tail vein. Blood samples were taken in the presence of heparin starting 15 minutes after injection and continuously during one hour in the interval of 15 minutes. Tirofiban concentration was analysed immediately. Blood samples were centrifuged 5 min at 3500 rpm min-1. The serum was treated carefully and methanol was added for precipitation of proteins in ratio serum: methanol = 1:3. The tubes were centrifuged again for 5 min at 3500 rpm min-1 and supernatant was injected into the HPLC column. HPLC separation was carried out at ambient temperature, using reversed-phase LiChrospher® 100 RP-18 column (4.0 mm × 250 mm, 5 μm particle size). The chromatographic separation was performed by isocratic mode with of 0,1 M KH2PO4 (ph=5.0, adjusted with 1.0 N sodium hydroxide solution) and acetonitrile in the ratio of 80:20 % v/v as mobile phase with a flow rate of 1.0 ml min-1 The UV was performed at 274 nm in the injection volume of 50 µl. Tirofiban concentration was also determined in spiked human and rat serum samples. Results: The response was linear over the range of 0.03 – 0.18 mg mL-1 in mobile phase and serum samples. The limit of detection (LOD) for tirofiban was 1.84, 13,8 and 14.6 μg mL-1 in methanol, spiked rat serum and spiked human serum, respectively. Plasma concentration-time profile obtained from the experimental group was significantly different from plasma concentration-time profile obtained from the control group. Conclusions: The described method can be readily applied, without any interference from endogenous substances, to study pharmacokinetics of tirofiban in serum given alone or in the presence of heparin as simultaneous therapy and for therapeutic monitoring of levels of tirofiban in serum samples. Literature Reference Oertel R, Köhler A, Koster A, Kirch W., Determination of Tirofiban in human serum by liquid chromatography-tandem mass spectrometry, J Chromatogr B Analyt Technol Biomed Life Sci. 2004 Jun 5;805(1):181-5. Sharlene M. Day, Jennifer L. Reeve, Daniel D. Myers, William P. Fay., Murine thrombosis models. Thromb Haemost 2004; 92: 486–94.
    European Journal of Pharmaceutical Sciences 09/2013; 50(Supplement 1):117.