European Journal of Pharmaceutical Sciences (EUR J PHARM SCI )

Publisher: European Federation for Pharmaceutical Sciences, Elsevier


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.

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  • Website
    European Journal of Pharmaceutical Sciences website
  • Other titles
    European journal of pharmaceutical sciences (Online), Pharmaceutical sciences, EJPS
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    Document, Periodical, Internet resource
  • Document type
    Internet Resource, Computer File, Journal / Magazine / Newspaper

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    • NIH Authors articles will be submitted to PMC after 12 months
    • Authors who are required to deposit in subject repositories may also use Sponsorship Option
    • Pre-print can not be deposited for The Lancet
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Publications in this journal

  • [Show abstract] [Hide abstract]
    ABSTRACT: The pervasiveness of tribo-electric charge during pharmaceutical processing can lead to the exacerbation of a range of problems including segregation, content heterogeneity and particle surface adhesion. The excipients, hydroxypropyl methylcellulose (HPMC) and methylcellulose (MC), are often used in drug delivery systems and so it is important to understand the impact of associated factors on their charging and adhesion mechanisms, however, little work has been reported in this area. Such phenomena become more prominent when excipients are introduced to a powder mixture alongside the active pharmaceutical ingredient(s) (APIs) with inter- and intra-particulate interactions giving rise to electrification and surface adhesion of powder particles. The aim of this study was to understand the impact of material attributes (particle size, hydroxypropoxyl (Hpo) to methoxyl (Meo) ratio and molecular size) on the charging and adhesion characteristics of cellulose ethers. Furthermore, a poorly compactible and highly electrostatically charged drug, flurbiprofen, was used to develop binary powder mixtures having different polymer to drug ratios and the relationship between tribo-electric charging and surface adhesion was studied. Charge was induced on powder particles and measured using a custom built device based on a shaking concept, consisting of a Faraday cup connected to an electrometer. The diversity in physicochemical properties has shown a significant impact on the tribo-electric charging and adhesion behaviour of MC and HPMC. Moreover, the adhesion and electrostatic charge of the API was significantly reduced when MC and HPMC were incorporated and tribo-electric charging showed a linear relationship (R(2)= 0.81-0.98) with particle surface adhesion, however, other factors were also involved. It is anticipated that such a reduction in charge and particle surface adhesion would improve flow and compaction properties during processing.
    European Journal of Pharmaceutical Sciences 09/2014;
  • 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 01/2014; 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.
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    ABSTRACT: Drug absorption from the gastrointestinal (GI) tract is a highly complex process dependent upon numerous factors including the physicochemical properties of the drug, characteristics of the formulation and interplay with the underlying physiological properties of the GI tract. The ability to accurately predict oral drug absorption during drug product development is becoming more relevant given the current challenges facing the pharmaceutical industry. Physiologically-based pharmacokinetic (PBPK) modeling provides an approach that enables the plasma concentration-time profiles to be predicted from preclinical in vitro and in vivo data and can thus provide a valuable resource to support decisions at various stages of the drug development process. Whilst there have been quite a few successes with PBPK models identifying key issues in the development of new drugs in vivo, there are still many aspects that need to be addressed in order to maximize the utility of the PBPK models to predict drug absorption, including improving our understanding of conditions in the lower small intestine and colon, taking the influence of disease on GI physiology into account and further exploring the reasons behind population variability. Importantly, there is also a need to create more appropriate in vitro models for testing dosage form performance and to streamline data input from these into the PBPK models. As part of the Oral Biopharmaceutical Tools (OrBiTo) project, this review provides a summary of the current status of PBPK models available. The current challenges in PBPK set-ups for oral drug absorption including the composition of GI luminal contents, transit and hydrodynamics, permeability and intestinal wall metabolism are discussed in detail. Further, the challenges regarding the appropriate integration of results from in vitro models, such as consideration of appropriate integration/estimation of solubility and the complexity of the in vitro release and precipitation data, are also highlighted as important steps to advancing the application of PBPK models in drug development. It is expected that the "innovative" integration of in vitro data from more appropriate in vitro models and the enhancement of the GI physiology component of PBPK models, arising from the OrBiTo project, will lead to a significant enhancement in the ability of PBPK models to successfully predict oral drug absorption and advance their role in preclinical and clinical development, as well as for regulatory applications.
    European Journal of Pharmaceutical Sciences 09/2013;
  • [Show abstract] [Hide abstract]
    ABSTRACT: This study evaluates the potential application of micellar liquid chromatography (MLC) to predict skin permeation with a series of model compounds. MLC has previously been found to be useful in the prediction of partition coefficient values (logP) for pharmaceutical compounds, yet has not been incorporated in skin permeability models prior to this work. This article provides statistically supported data that this technique enhances the ability to predict the permeability of similar drugs through the skin (Kp). The replacement of a traditional physicochemical parameter, namely the octanol-water partition coefficient (logPow) with a chromatographically determined value (logPmw), results in a quantitative partition-permeability relationship that is robust to variation. MLC offers many benefits compared with the traditional techniques employed to obtain logP values.
    European Journal of Pharmaceutical Sciences 08/2013;
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    European Journal of Pharmaceutical Sciences 05/2013; 49(4):699-711.
  • [Show abstract] [Hide abstract]
    ABSTRACT: Several barriers need to be overcome to ensure successful gene transfection, including passing of the foreign gene through the plasma membrane, escape of this material from lysosomal degradation, and its translocation into the nucleus. We previously showed that the biosurfactant mannosylerythritol lipid-A (MEL-A) enhanced the efficiency of gene transfection mediated by cationic liposomes by facilitating rapid delivery of foreign genes into target cells through membrane fusion between liposomes and the plasma membrane. Moreover, using MEL-A-containing cationic liposomes, the foreign gene was efficiently delivered into the nucleus because it was released directly into the cytosol and thus escaped lysosomal degradation. Here we investigated the effect of pre-condensation of plasmid DNA by a cationic polymer, protamine, on gene transfection. We found that the efficiency of pre-condensed DNA transfection mediated by MEL-A-containing OH liposomes was >10 times higher than that of non-condensed DNA transfection. In contrast, the efficiency of pre-condensed DNA transfection mediated by OH liposomes was only 1.5 times higher than that of non-condensed DNA transfection. MEL-A did not influence plasmid DNA encapsulation by cationic liposomes, but it greatly accelerated the nuclear delivery of pre-condensed plasmid DNA. Our findings indicate that MEL-A and protamine synergistically accelerate the nuclear delivery of foreign gene and consequently promote gene transfection efficiency.
    European Journal of Pharmaceutical Sciences 02/2013;
  • European Journal of Pharmaceutical Sciences 01/2013;

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