European Journal of Pharmaceutics and BiopharmaceuticsThis 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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Imaging Tools for Pharmaceutical Development.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
PMID: 19919848 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutics and Biopharmaceutics)
Source: European Journal of Pharmaceutics and Biopharmaceutics - November 14, 2009 Category: Drugs & Pharmacology Authors: Gurny R, Mäder K Tags: Eur J Pharm Biopharm Source Type: journals

Relevant Shaking Stress Conditions For Antibody Preformulation Development.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In protein formulation development shaking stress is often employed to assess the physical stability of antibody formulations against aggregation. Since there are currently no guidelines describing suitable test conditions, very different shaking stress designs are used. These different designs may influence the resulting stability data. The aim of this study was to establish a shaking stress design within the protein range of 2-5mg/ml which can rapidly distinguish between antibody formulations of poor stability and those with potential for further development. Small scale shaking stress experiments were performed with...
Source: European Journal of Pharmaceutics and Biopharmaceutics - November 13, 2009 Category: Drugs & Pharmacology Authors: Eppler A, Weigandt M, Hanefeld A, Bunjes H Tags: Eur J Pharm Biopharm Source Type: journals

ATR-FTIR spectroscopy and spectroscopic imaging of solvent and permeant diffusion across model membranes.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The uptake and diffusion of solvents across polymer membranes is important in controlled drug delivery, effects on drug uptake into, for example, infusion bags and containers, as well as transport across protective clothing. Attenuated Total Reflectance Fourier Transform Infrared (ATR-FTIR) spectroscopy has been used to monitor the effects of different solvents on the diffusion of a model compound, 4-cyanophenol (CNP) across silicone membrane and on the equilibrium concentration of CNP obtained in the membrane following diffusion. ATR-FTIR spectroscopic imaging of membrane diffusion was used to gain an understanding of...
Source: European Journal of Pharmaceutics and Biopharmaceutics - November 11, 2009 Category: Drugs & Pharmacology Authors: McAuley WJ, Lad MD, Mader KT, Santos P, Tetteh J, Kazarian SG, Hadgraft J, Lane ME Tags: Eur J Pharm Biopharm Source Type: journals

Characterization of a polyurethane based controlled release system for local delivery of chlorhexidine diacetate.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In conclusion, the polyurethane based system developed in this study is potentially useful as a local delivery system for CDA and could be used not only in surgery but also in dental and clinical applications. PMID: 19909814 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutics and Biopharmaceutics)
Source: European Journal of Pharmaceutics and Biopharmaceutics - November 9, 2009 Category: Drugs & Pharmacology Authors: Huynh TT, Padois K, Sonvico F, Rossi A, Zani F, Pirot F, Doury J, Falson F Tags: Eur J Pharm Biopharm Source Type: journals

Cyclodextrin-based nanosponges encapsulating camptothecin: physico-chemical characterization, stability and cytotoxicity.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
This study aimed at formulating complexes of CAM with three types of beta-cyclodextrin NS obtained with different cross-linking ratio (viz. 1:2, 1:4 and 1:8 on molar basis with the crosslinker) to protect the lactone ring from hydrolysis and to prolong the release kinetics of CAM. Crystalline (F(1:2), F(1:4) and F(1:8)) and paracrystalline NS formulations were prepared. XRPS, DSC and FTIR studies confirmed the interactions of CAM with NS. XRPD showed that the crystallinity of CAM decreased after loading. CAM was loaded as much as 21%, 37% and 13% w/w in F(1:2), F(1:4) and F(1:8) respectively while the paracrystalline NS fo...
Source: European Journal of Pharmaceutics and Biopharmaceutics - November 6, 2009 Category: Drugs & Pharmacology Authors: Swaminathan S, Pastero L, Serpe L, Trotta F, Vavia P, Aquilano D, Trotta M, Zara G, Cavalli R Tags: Eur J Pharm Biopharm Source Type: journals

Curing of aqueous polymeric film coatings: importance of the coating level and type of plasticizer.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 better understand the effects of the curing conditions on the resulting drug release patterns from pellets coated with aqueous polymer dispersions. Diltiazem HCl was used as model drug, ethylcellulose as polymer, triethyl citrate (TEC), dibutyl sebacate (DBS), and distilled acetylated monoglycerides (Myvacet) as plasticizers. Interestingly, the effects of the curing conditions strongly depended on the coating level and type of plasticizer: In the case of TEC, the drug release rate monotonically decreased with increasing harshness of the curing conditions (time, temperature and relative humi...
Source: European Journal of Pharmaceutics and Biopharmaceutics - November 3, 2009 Category: Drugs & Pharmacology Authors: Yang QW, Flament MP, Siepmann F, Busignies V, Leclerc B, Herry C, Tchoreloff P, Siepmann J Tags: Eur J Pharm Biopharm Source Type: journals

Investigation into the intragranular structures of microcrystalline cellulose and pre-gelatinised starch.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The internal structures of commercial spheronised microcrystalline cellulose (s-MCC) and pre-gelatinised starch (PGS) granules were investigated, using a range of methods. Results from scanning electron microscopy (SEM), transmission electron microscopy (TEM) and atomic force microscopy (AFM) revealed hierarchical structures, with dimensions ranging from nanometres to a few micrometres, for both materials. Residual fragments of plant cell walls, consisting largely of crystalline fibrillar bundles, were indicated within s-MCC granules, while PGS granules appeared to consist of densely packed spherical features. The lack...
Source: European Journal of Pharmaceutics and Biopharmaceutics - October 31, 2009 Category: Drugs & Pharmacology Authors: Laity P, Cassidy A, Skepper J, Jones B, Cameron R Tags: Eur J Pharm Biopharm Source Type: journals

Pharmacodynamics of cisplatin-loaded PLGA nanoparticles administered to tumor bearing mice.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Biodegradable poly (lactic-co-glycolic) acid (PLGA) nanoparticles incorporating cisplatin have been developed to evaluate its in vivo efficacy in tumor bearing mice In vitro study proved two mechanism of action for cisplatin depending on the dose and the rate at which this dose is delivered. In vivo study, 5 mg/kg of cisplatin-nanoparticles administered to mice, exhibited a tumor inhibition similar to free-cisplatin, although the area under cisplatin concentration-time curve between 0 and 21 days (AUC(0-21)) had lower value for the formulation than for drug solution (P<0.05). This result was associated with a higher...
Source: European Journal of Pharmaceutics and Biopharmaceutics - October 30, 2009 Category: Drugs & Pharmacology Authors: Moreno D, Zalba S, Navarro I, de Ilarduya CT, Garrido MJ Tags: Eur J Pharm Biopharm Source Type: journals

Inulin solid dispersion technology to improve the absorption of the BCS Class IV drug TMC240.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
TMC240 is a very poorly soluble and poorly permeating HIV protease inhibitor. In order to enhance its oral bioavailability, a fast dissolving inulin based solid dispersion tablet was developed. During the dissolution test in water (0.5 or 1.0% SLS), this tablet released at least 80% of TMC240 within 30 min, while the physical mixture tablet of the same composition released only 6% after 2 h. In a subsequent single-dose study in dogs (200 mg of TMC240), plasma concentrations of TMC240 remained below the lower limit of quantification (<1.00 ng/mL) in all animals (n=3 per tested formulation), except in one dog receivin...
Source: European Journal of Pharmaceutics and Biopharmaceutics - October 24, 2009 Category: Drugs & Pharmacology Authors: Visser MR, Baert L, van 't Klooster G, Schueller L, Geldof M, Vanwelkenhuysen I, De Kock H, De Meyer S, Frijlink HW, Rosier J, Hinrichs WL Tags: Eur J Pharm Biopharm Source Type: journals

Thermally sensitive gels based on chitosan derivatives for the treatment of oral mucositis.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The aim of the present work was the development of a thermally sensitive mucoadhesive gel based on chitosan derivatives for the treatment of oral mucositis. Trimethyl chitosan (TMC) and methylpyrrolidinone chitosan (MPC) were considered. They were mixed with glycerophosphate (GP) according to different polymer/GP molar ratios and characterized for gelation properties by means of rheological analysis in comparison with chitosan. The influence of molecular weight and substitution degree (SD) of TMC on gelation temperature and time was investigated. The mucoadhesive properties of the mixtures were also assessed using porc...
Source: European Journal of Pharmaceutics and Biopharmaceutics - October 22, 2009 Category: Drugs & Pharmacology Authors: Rossi S, Marciello M, Bonferoni MC, Ferrari F, Sandri G, Caramella C, Dacarro C, Grisoli P Tags: Eur J Pharm Biopharm Source Type: journals

Guidelines to cell engineering for monoclonal antibody production.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Monoclonal antibodies (mAbs) are currently used for many diagnostic and therapeutic applications. The high demand for these biopharmaceuticals has led to the development of large-scale manufacturing processes, with productivity improvements being mainly achieved by optimization of bioreactor systems. However, more recently, the early steps of production, previous to bioreactor culture, have been presented as alternative areas where productivity enhancements can be achieved. Thus, this review describes the progress made for the improvement of productivity in mammalian expression systems for the high-production of mAbs. ...
Source: European Journal of Pharmaceutics and Biopharmaceutics - October 21, 2009 Category: Drugs & Pharmacology Authors: Costa AR, Rodrigues ME, Henriques M, Azeredo J, Oliveira R Tags: Eur J Pharm Biopharm Source Type: journals

A quantitative evaluation of the molecular binding affinity between a monoclonal antibody conjugated to a nanoparticle and an antigen by surface plasmon resonance.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In conclusion, at the cellular level AMB8LK immunoNPs may carry drugs to desired overexpressing antigen cells with adequate affinity properties, potentially leading to improved drug therapy and reduced systemic adverse effects. PMID: 19835957 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutics and Biopharmaceutics)
Source: European Journal of Pharmaceutics and Biopharmaceutics - October 12, 2009 Category: Drugs & Pharmacology Authors: Debotton N, Zer H, Parnes M, Harush-Frenkel O, Kadouche J, Benita S Tags: Eur J Pharm Biopharm Source Type: journals

Non-invasive MRI detection of individual pellets in the human stomach.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
MRI is a powerful and non-invasive method to follow the fate of oral drug delivery systems in men. Until now, most MRI studies focused on monolithic dosage forms (tablets, capsules). Small sized multi-particulate drug delivery systems are very difficult to detect due to the poor differentiation between the delivery system and the food. A new approach was developed to overcome the described difficulties and to permit the selective imaging of small multi-particulate dosage forms within the stomach. We took advantage of the different sensitivity to susceptibility artefacts of T(2)-weighted spin echo- and T(2)-weighted gra...
Source: European Journal of Pharmaceutics and Biopharmaceutics - October 8, 2009 Category: Drugs & Pharmacology Authors: Knörgen M, Spielmann RP, Abdalla A, Metz H, Mäder K Tags: Eur J Pharm Biopharm Source Type: journals

Influence Of Reaction Medium During Synthesis Of Gantrez((R))An119 Nanoparticles For Oral Vaccination.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Two synthesis methods of poly(methyl vinyl ether-co-maleic anhydride) (Gantrez((R))AN119) nanoparticles (NP) (used for oral vaccination) were compared. Wheat germ agglutinin (WGA) was used as ligand to enhance the bioadhesive properties of NP and beta-galactosidase as antigen. The first method encapsulated beta-galactosidase in NP by co-precipitation in an acetone/water mixture containing 44% acetone. In the second method, antigen addition occurred in 100% acetone. To improve stability, NP were crosslinked with 1,3-diaminopropane. The stability of WGA-conjugated NP with encapsulated antigen diminished at lower pH and w...
Source: European Journal of Pharmaceutics and Biopharmaceutics - October 7, 2009 Category: Drugs & Pharmacology Authors: Katrien V, Vesna M, Eric C, Dieter D, Joke L, Els A, Chris V, Jean-Paul R Tags: Eur J Pharm Biopharm Source Type: journals

Fusion Production of Solid Dispersions Containing a Heat Sensitive Active Ingredient by Hot Melt Extrusion and KinetiSol((R)) Dispersing.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
This study clearly demonstrated the importance of carrier selection to facilitate lower temperature processing, as well as the effect of residence time on product potency. Furthermore, KinetiSol((R)) Dispersing provided significant advantages over hot melt extrusion due to the reduced residence times and lower required processing temperatures. This allowed for the production of solid dispersions with enhanced product potency. PMID: 19818402 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutics and Biopharmaceutics)
Source: European Journal of Pharmaceutics and Biopharmaceutics - October 5, 2009 Category: Drugs & Pharmacology Authors: Dinunzio JC, Brough C, Hughey JR, Miller DA, Williams RO, McGinity JW Tags: Eur J Pharm Biopharm Source Type: journals

Methodology for phase selection of a weak basic drug candidate, utilizing kinetic solubility profiles in biorelevant media.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
We aimed to develop a phase selection methodology for a weak basic active pharmaceutical ingredient (API) that would require less than 10 mg of the API and monitor the real time kinetic solubility of the API in two biorelevant media. Three sets of kinetic solubility measurements were conducted for free form I and the disulfate salt of an API (compound A) in order to determine the better API phase for further development of the compound. Tests consisted of solid API dissolution in both simulated gastric fluid (SGF) and fasted-state intestinal fluid (FaSSIF), and precipitation kinetics by injection of liquid state API in...
Source: European Journal of Pharmaceutics and Biopharmaceutics - October 4, 2009 Category: Drugs & Pharmacology Authors: Furukawa S, Zhao C, Ohki Y Tags: Eur J Pharm Biopharm Source Type: journals

Artificial neural networks in the optimization of a nimodipine controlled release tablet formulation.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Artificial neural networks (ANNs) were employed in the optimization of a nimodipine zero-order release matrix tablet formulation and their efficiency was compared to that of multiple linear regression (MLR) on an external validation set. The amounts of PEG-4000, PVP K30, HPMC K100 and HPMC E50LV were used as independent variables following a statistical experimental design, and three dissolution parameters (time at which the 90% of the drug was dissolved, t(90%), percentage of nimodipine released in 2 and 8 hours, Y(2h), and Y(8h), respectively) were chosen as response variables. It was found that a feed-forward back-p...
Source: European Journal of Pharmaceutics and Biopharmaceutics - October 4, 2009 Category: Drugs & Pharmacology Authors: Barmpalexis P, Kanaze FI, Kachrimanis K, Georgarakis E Tags: Eur J Pharm Biopharm Source Type: journals

Flowability characterisation of drug-excipient blends using a novel powder avalanching method.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In conclusion, the novel avalanche testing instrument provided complementary information to conventional flowability methodologies and a thorough assessment of pharmaceutical blends is needed to avoid CFCs in view of a robust formulation development and hence with respect to building quality into the design of the solid dosage forms. PMID: 19796683 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutics and Biopharmaceutics)
Source: European Journal of Pharmaceutics and Biopharmaceutics - September 27, 2009 Category: Drugs & Pharmacology Authors: Nalluri VR, Kuentz M Tags: Eur J Pharm Biopharm Source Type: journals

Properties of Melt Extruded Enteric Matrix Pellets.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The objective of this study was to investigate the properties of enteric matrix pellets that were prepared by hot-melt extrusion in a one-step, continuous process. Five polymers (Eudragit(R) L100-55, L100 and S100, Aqoat(R) grades LF and HF) were investigated as possible matrix formers, and pellets prepared with Eudragit(R) S100 demonstrated superior gastric protection and acceptable processibility. Extruded pellets containing Eudragit(R) S100 and up to 40% theophylline released less than 10% drug over 2 hours in acid, however, the processibility and yields were compromised by the high amounts of the non-melting drug mater...
Source: European Journal of Pharmaceutics and Biopharmaceutics - September 22, 2009 Category: Drugs & Pharmacology Authors: Schilling SU, Shah NH, Malick AW, McGinity JW Tags: Eur J Pharm Biopharm Source Type: journals

Characterization of the copolymer poly(ethyleneglycol-g-vinylalcohol) as a potential carrier in the formulation of solid dispersions.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In order to fully exploit the graft copolymer poly(ethyleneglycol-g-vinylalcohol) (EG/VA) in the formulation of solid dispersions a characterization of its phase behavior before, during and after spray-drying and hot-melt extrusion is performed. Solid state characterization was performed using MDSC and XRPD. The effect of heating/cooling rate on the degree of crystallinity was studied using HPer DSC and ultra-fast chip calorimetry. EG/VA consists of two semi-crystalline fractions, one corresponding to the polyethyleneglycol (PEG) fraction (T(g)=-57 degrees C, T(m)=15 degrees C) and one corresponding to the polyvinylalc...
Source: European Journal of Pharmaceutics and Biopharmaceutics - September 22, 2009 Category: Drugs & Pharmacology Authors: Sandra G, Pieterjan K, A MJ, Van Humbeeck J, Vincent M, Thijs P, Evgeny Z, Christoph S, Van den Mooter G Tags: Eur J Pharm Biopharm Source Type: journals

Scratch Resistance of Plasticized Hydroxypropyl Methylcellulose (HPMC) Films Intended for Tablet Coatings.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Scratch resistance (SR) of externally plasticized hydroxypropyl methylcellulose (HPMC) films intended for tablet film coatings was studied. Special attention was paid to effects of short-term aging and ultraviolet (UV) treatment on the SR properties of these films. Controlled scratching of the films was performed with a Lloyd LRX materials tester featuring a spherical steel tip. Scratch surface profiles were measured by scanning white light interferometry (SWLI). The influence of using an external plasticizer on the SR was studied by comparing scratch dimensions in non-plasticized films to samples plasticized either wi...
Source: European Journal of Pharmaceutics and Biopharmaceutics - September 20, 2009 Category: Drugs & Pharmacology Authors: Hanhijärvi K, Majava T, Kassamakov I, Heinämäki J, Aaltonen J, Haapalainen J, Hæggström E, Yliruusi J Tags: Eur J Pharm Biopharm Source Type: journals

Size dependent release of fluorescent macromolecules and nanoparticles from radically cross-linked hydrogels.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In this study we examined the suitability of poly(ethylene glycol) [PEG] based hydrogels as release systems for nanometer-sized drugs or drug carriers, like nanoparticles, using the radically cross-linkable oligo(poly(ethylene glycol)fumarate) [OPF] together with two cross-linking agents. Different fluorescent nanoparticulate probes with respect to size and physical structure were incorporated in the cross-linked hydrogels and the obtained release profiles were correlated with the physical properties and the chemical structure of the gels, indicating a strong dependence of the release on the chosen PEG prepolymers. The pre...
Source: European Journal of Pharmaceutics and Biopharmaceutics - September 13, 2009 Category: Drugs & Pharmacology Authors: Henke M, Brandl F, Goepferich AM, Tessmar JK Tags: Eur J Pharm Biopharm Source Type: journals

Utilising Atomic Force Microscopy for the Characterisation of Nanoscale Drug Delivery Systems.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The introduction of Atomic Force Microscopy (AFM) techniques has revolutionised our ability to characterise colloidal objects. AFM allows the visualisation of samples with sub-nanometre resolution in three dimensions in atmospheric or submerged conditions. Nanomedical research is increasingly focused on the design, characterisation and delivery of nano-sized drug carriers such as nanoparticles, liposomes, and polyplexes and this review aims to highlight the scope and advantages of AFM in this area. A significant amount of work has been carried out in Drug Delivery System (DDS) research in recent years using a large var...
Source: European Journal of Pharmaceutics and Biopharmaceutics - September 11, 2009 Category: Drugs & Pharmacology Authors: Sitterberg J, Ozcetin A, Ehrhardt C, Bakowsky U Tags: Eur J Pharm Biopharm Source Type: journals

Nano-sized water-in-oil-in-water emulsion enhances intestinal absorption of calcein, a high solubility and low permeability compound.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Our goal was to develop safe and stable multilayer emulsions capable of enhancing intestinal absorption of biopharmaceutics classification system (BCS) class III drugs. First, w/o emulsions were prepared using calcein as a model BCS class III compound and condensed ricinoleic acid tetraglycerin ester as a hydrophobic emulsifier. Then water-in-oil-in-water (w/o/w) emulsions were prepared with shirasu porous glass (SPG) membranes. Particle size analyses and calcein leakage from oil droplets in w/o/w emulsions led us to select stearic acid hexaglycerin esters (HS-11) and Gelucire 44/14 as hydrophilic emulsifiers. Analyses...
Source: European Journal of Pharmaceutics and Biopharmaceutics - September 11, 2009 Category: Drugs & Pharmacology Authors: Koga K, Takarada N, Takada K Tags: Eur J Pharm Biopharm Source Type: journals

Recent advances in confocal microscopy for studying drug delivery to the eye: concepts and pharmaceutical applications.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Since its seminal introduction 50 years ago, confocal microscopy has been applied in numerous fields in life sciences. This review presents the different key elements of confocal microscopes, in particular scanning techniques, light sources and especially laser sources are presented in this review. Furthermore an overview of the different image processing systems coupled with confocal microscopy is provided. The chapter closes with the applications of confocal microscopy in drug delivery to the eye. PMID: 19755157 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutics and Biopharmaceutics)
Source: European Journal of Pharmaceutics and Biopharmaceutics - September 11, 2009 Category: Drugs & Pharmacology Authors: Furrer P, Gurny R Tags: Eur J Pharm Biopharm Source Type: journals

Drug delivery to the brain using surfactant-coated poly(lactide-co-glycolide) nanoparticles: Influence of the formulation parameters.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Poly(lactide-co-glycolide) (PLGA) nanoparticles coated with poloxamer 188 (Pluronic((R)) F68) or polysorbate 80 (Tween((R)) 80) enable an efficient brain delivery of the drugs after intravenous injection. This ability was evidenced by two different pharmacological test systems employing as model drugs the anti-tumour antibiotic doxorubicin and the agonist of opioid receptors loperamide, which being P-gp substrates can cross the blood-brain barrier (BBB) only in pharmacologically insignificant amounts: Binding of doxorubicin to the surfactant-coated PLGA nanoparticles, however, enabled a high anti-tumour effect against ...
Source: European Journal of Pharmaceutics and Biopharmaceutics - September 11, 2009 Category: Drugs & Pharmacology Authors: Gelperina S, Maksimenko O, Khalansky A, Vanchugova L, Shipulo E, Abbasova K, Berdiev R, Wohlfart S, Chepurnova N, Kreuter J Tags: Eur J Pharm Biopharm Source Type: journals

Surface Functionalized Polymethacrylic acid Based Hydrogel Microparticles for Oral Drug Delivery.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
AIM: of the present work was to develop novel thiol functionalized hydrogel microparticles based on Poly(methacrylic acid)-Chitosan-Poly(ethylene glycol) (PCP) for oral drug delivery applications. PCP microparticles were prepared by a modified ionic gelation process in aqueous medium. Thiol modification of surface carboxylic acid groups of PCP particles was carried out by coupling L-cysteine with a water-soluble carbodiimide. Ellman's method was adopted to quantify the sulphydryl groups and dynamic light scattering technique was used to measure the average particle size. Cytotoxicity of the modified particles was evalu...
Source: European Journal of Pharmaceutics and Biopharmaceutics - September 4, 2009 Category: Drugs & Pharmacology Authors: Sajeesh S, Bouchemal K, Sharma CP, Vauthier C Tags: Eur J Pharm Biopharm Source Type: journals

Preparation of a fast dissolving oral thin film containing dexamethasone: a possible application to antiemesis during cancer chemotherapy.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
We prepared fast dissolving oral thin film that contains dexamethasone and base materials, including microcrystalline cellulose, polyethylene glycol, hydroxypropylmethyl cellulose, polysorbate 80 and low-substituted hydroxypropyl cellulose. This preparation showed excellent uniformity and stability, when stored at 40 degrees C and 75% in humidity for up to 24 weeks. The film was disintegrated within 15 second after immersion into distilled water. The dissolution test showed that approximately 90% of dexamethasone was dissolved within 5 min. Subsequently, pharmacokinetic properties of dexamethasone were compared in rats...
Source: European Journal of Pharmaceutics and Biopharmaceutics - September 3, 2009 Category: Drugs & Pharmacology Authors: Shimoda H, Taniguchi K, Nishimura M, Matsuura K, Tsukioka T, Yamashita H, Inagaki N, Hirano K, Yamamoto M, Kinosada Y, Itoh Y Tags: Eur J Pharm Biopharm Source Type: journals

A pilot study evaluating the safety of vaginal administration of a multi-particulate pellet formulation.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
CONCLUSION: No major differences could be observed between the groups, whereby all changes in pH and microflora could be ascribed to withdrawal bleeding, indicating that gelatin capsules, starch pellets and lyophilized powder are acceptable carrier materials for the vaginal delivery of probiotic strains. PMID: 19733660 [PubMed - as supplied by publisher] (Source: European Journal of Pharmaceutics and Biopharmaceutics)
Source: European Journal of Pharmaceutics and Biopharmaceutics - September 2, 2009 Category: Drugs & Pharmacology Authors: Santiago GL, Poelvoorde N, De Corte S, Claeys G, Trog M, De Backer E, Saerens B, Vervaet C, De Boeck F, Van Bortel L, Remon JP, Temmerman M, Vaneechoutte M, Verhelst R Tags: Eur J Pharm Biopharm Source Type: journals

RPMI 2650 epithelial model and three-dimensional reconstructed human nasal mucosa as in vitro models for nasal permeation studies.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 human nasal epithelial cell line RPMI 2650 regarding its usefulness as in vitro model for drug permeation studies. Particularly, the influence of the air-liquid interface in culture and coculture with human nasal fibroblasts (HNF) on the differentiation and permeation barrier properties of the cell layer was examined. In addition to a non-contact-coculture, we developed a three-dimensional construct of the human nasal mucosa composed of a collagen matrix with embedded HNF, covered by a RPMI 2650 epithelial cell layer. Microscopic examination as well as measurement of the...
Source: European Journal of Pharmaceutics and Biopharmaceutics - September 2, 2009 Category: Drugs & Pharmacology Authors: Wengst A, Reichl S Tags: Eur J Pharm Biopharm Source Type: journals

Application of Electron Paramagnetic Resonance (EPR) - Spectroscopy and Imaging in drug delivery research - chances and challenges.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Electron paramagnetic resonance (EPR) spectroscopy is a powerful technique to study chemical species with unpaired electrons. Since its discovery in 1944 it has been widely used in a number of research fields such as physics, chemistry, biology and material and food science. This review is focused on its application in drug delivery research. EPR permits the direct measurement of microviscosity and micropolarity inside drug delivery systems (DDS), the detection of microacidity, phase transitions and the characterisation of colloidal drug carriers. Additional information about the spatial distribution can be obtained by...
Source: European Journal of Pharmaceutics and Biopharmaceutics - August 28, 2009 Category: Drugs & Pharmacology Authors: Kempe S, Metz H, Mäder K Tags: Eur J Pharm Biopharm Source Type: journals

Preparation and evaluation of tacrolimus-loaded nanoparticles for lymphatic delivery.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In an effort to improve lymphatic targeting efficiency and reduce the toxicity of tacrolimus, the emulsification-diffusion method was used to load the drug into nanoparticles (NP). Poly (lactide-co-glycolide) (PLGA) and PLGA surface-modified with poly (ethylene glycol) (PEG) were used as polymers. Mean particle size and drug encapsulation efficiency of PLGA were 218 +/- 51 nm and 60.0 +/- 1.2% and for PEG-PLGA NP were 220 +/- 33 nm and 60.3 +/- 2.0%. NP were characterized by thermal analyzer and X-ray diffractometry (XRD), and their shapes were observed by scanning electron microscopy (SEM) and transmission electron mi...
Source: European Journal of Pharmaceutics and Biopharmaceutics - August 20, 2009 Category: Drugs & Pharmacology Authors: Shin SB, Cho HY, Kim DD, Choi HG, Lee YB Tags: Eur J Pharm Biopharm Source Type: journals

Multivariate analysis of relationships between material properties, process parameters and tablet tensile strength for alpha-lactose monohydrates.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The present work describes an approach to quantify relationships between the material properties of various alpha-lactose monohydrate grades (alphaLM), process parameters (punch velocity, lubricant fraction), and the tablet tensile strength (TS). Milled, sieved, agglomerated and spray-dried alphaLMs were studied. Each material was tableted (11mm flat punches, constant true volume of 0.2833 cm(3)) on a compaction simulator at a pressure of 104.4+/-0.1 MPa. The force-displacement data was analyzed by applying a combination of compression descriptors (derived from Kawakita and Heckel equations, work-related parameters). T...
Source: European Journal of Pharmaceutics and Biopharmaceutics - August 17, 2009 Category: Drugs & Pharmacology Authors: Haware RV, Tho I, Bauer-Brandl A Tags: Eur J Pharm Biopharm Source Type: journals

Sculptured drug-eluting stent for the on-site delivery of tacrolimus.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
This work aimed to evaluate the flexibility of a novel pyrolytic carbon coated drug-eluting stent platform which presents the peculiarity of deep sculptures realized on the stent's outer surface (reservoirs). Tacrolimus (TCR) or TCR/excipient mixtures were loaded into the reservoirs and their permanence into stent's reservoirs was verified by an in vitro short time release test in human blood. Moreover, the impact of the excipients on the TCR physical state and surface morphology of the reservoirs and the release kinetics were studied. The reservoirs resulted homogeneously filled. Upon exposure to blood, no loss of mat...
Source: European Journal of Pharmaceutics and Biopharmaceutics - August 13, 2009 Category: Drugs & Pharmacology Authors: Minghetti P, Cilurzo F, Selmin F, Casiraghi A, Grignani A, Montanari L Tags: Eur J Pharm Biopharm Source Type: journals

Influence of Degree of Substitution of HES-HEMA on the Release of Incorporated Drug Models from Corresponding Hydrogels.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Hydrogel microparticles were produced by a radical polymerisation of hydroxyethyl methacrylate-hydroxyethyl starch (HES-HEMA) in an all aqueous two phase system (ATPS). The microspheres show a monomodal size distribution and have the ability to entrap high amounts of water. The release of proteins or other testing substances from the HES-HEMA hydrogels can be controlled by the choice of the network density of the hydrogel by varying the degree of substitution (DS), the size of the entrapped substance, and by conditions enhancing the degradation of the hydrogel network. PMID: 19683570 [PubMed - as supplied by publis...
Source: European Journal of Pharmaceutics and Biopharmaceutics - August 12, 2009 Category: Drugs & Pharmacology Authors: Schwoerer AD, Harling S, Scheibe K, Menzel H, Daniels R Tags: Eur J Pharm Biopharm Source Type: journals

Effects of Liquisolid Formulations on Dissolution of Naproxen.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
This study was designed to evaluate the effects of different formulation variables, i.e. type of non-volatile liquid vehicles and drug concentrations, on drug dissolution rates. The liquisolid tablets were formulated with three different liquid vehicles, namely Cremophor((R)) EL (polyoxyl 35 castor oil), Synperonic((R)) PE/L61 (poloxamer 181, polyoxyethylene-polyoxypropylene copolymer) and poly ethylene glycol 400 (PEG400) at two drug concentrations, 20%w/w and 40%w/w. Avicel((R)) PH102 was used as a carrier material, Cab-o-sil((R)) M-5 as a coating material and maize starch as a disintegrant. The empirical method as intro...
Source: European Journal of Pharmaceutics and Biopharmaceutics - August 9, 2009 Category: Drugs & Pharmacology Authors: Tiong N, Elkordy AA Tags: Eur J Pharm Biopharm Source Type: journals

Effects of penetration enhancers on Shuangwu Traumatic Formula: in vitro percutaneous absorption and in vivo pharmacodynamic evaluation of an herb medicine.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The purposes of this study were to improve the transdermal permeation of the Shangwu Traumatic Formula by chemical penetration enhancers and to investigate the pharmacodynamic changes of the formula caused by incorporated enhancers. The effects of different enhancers on the transdermal absorption of piperine, the representative component of formula, were investigated by in vitro permeation studies. The tests showed an increasing enhancement effect in the following order: Azone/N-methylpyrrolidone (NMP)>Oleic acid>Azone/Peppermint oil>Azone/Oleic acid> Azone/Propylene glycol>Azone >Peppermint oil>NM...
Source: European Journal of Pharmaceutics and Biopharmaceutics - August 7, 2009 Category: Drugs & Pharmacology Authors: Gu S, Gao J, Hou X, Ding B, Zhang W, Gao S, Ding X Tags: Eur J Pharm Biopharm Source Type: journals

Topical delivery of 5-aminolevulinic acid-encapsulated ethosomes in a hyperproliferative skin animal model using the CLSM technique to evaluate the penetration behavior.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Psoriasis, an inflammatory skin disease, exhibits recurring itching, soreness, and cracked and bleeding skin. Currently, the topical delivery of 5-aminolevulinic acid-photodynamic therapy (ALA-PDT) is an optional treatment for psoriasis which provides long-term therapeutic effects, is non-toxic, and enjoys better compliance by patients. However, the precursor of ALA is hydrophilic, and thus its ability to penetrate the skin is limited. Also, little research has provided a platform to investigate the penetration behavior in disordered skin. We employed a highly potent ethosomal carrier (phosphatidylethanolamine; PE) to ...
Source: European Journal of Pharmaceutics and Biopharmaceutics - August 2, 2009 Category: Drugs & Pharmacology Authors: Fang YP, Huang YB, Wu PC, Tsai YH Tags: Eur J Pharm Biopharm Source Type: journals

The enhancement of interstitial transport of a doxorubicin-lactosaminated albumin conjugate by imatinib: in rat hepatocellular carcinoma it is not preferentially higher than that in liver and bone marrow.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The enhancement of interstitial transport of a doxorubicin-lactosaminated albumin conjugate by imatinib: in rat hepatocellular carcinoma it is not preferentially higher than that in liver and bone marrow. Eur J Pharm Biopharm. 2009 Aug;72(3):630-1 Authors: Fiume L, Baglioni M, Busi C, Manerba M, Di Stefano G The finding that imatinib enhances the drug transport from bloodstream to neoplastic cells suggested a possible role of this drug as an adjuvant to the chemotherapeutics given in the treatment of solid malignancies.The present experiments aimed to verify whether imatinib can selectively increase the penetra...
Source: European Journal of Pharmaceutics and Biopharmaceutics - July 3, 2009 Category: Drugs & Pharmacology Authors: Fiume L, Baglioni M, Busi C, Manerba M, Di Stefano G Tags: Eur J Pharm Biopharm Source Type: journals

Comparison of two in vitro models for the analysis of follicular penetration and its prevention by barrier emulsions.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Comparison of two in vitro models for the analysis of follicular penetration and its prevention by barrier emulsions. Eur J Pharm Biopharm. 2009 Aug;72(3):600-4 Authors: Lademann J, Patzelt A, Richter H, Schanzer S, Sterry W, Filbry A, Bohnsack K, Rippke F, Meinke M The penetration of topically applied substances in and through the human skin is of special interest for the development and optimization of topically applied drugs and cosmetic products. In the present study, the efficacy of barrier emulsions in the prevention of the penetration of pollen allergens into the hair follicles was investigated. Because ...
Source: European Journal of Pharmaceutics and Biopharmaceutics - July 3, 2009 Category: Drugs & Pharmacology Authors: Lademann J, Patzelt A, Richter H, Schanzer S, Sterry W, Filbry A, Bohnsack K, Rippke F, Meinke M Tags: Eur J Pharm Biopharm Source Type: journals

A fluorescence-based in vitro assay for drug interactions with breast cancer resistance protein (BCRP, ABCG2).Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
CONCLUSIONS: The mitoxantrone-based assay can be used as a rapid FACS screening system to assess drug interactions with BCRP at the blood-brain barrier and therefore represents a useful tool in drug profiling. PMID: 19572416 [PubMed - in process] (Source: European Journal of Pharmaceutics and Biopharmaceutics)
Source: European Journal of Pharmaceutics and Biopharmaceutics - July 3, 2009 Category: Drugs & Pharmacology Authors: Mahringer A, Delzer J, Fricker G Tags: Eur J Pharm Biopharm Source Type: journals

Magnetic resonance imaging and x-ray microtomography studies of a gel-forming tablet formulation.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The capabilities of two methods for investigating tablet swelling are investigated, based on a study of a model gel-forming system. Results from magnetic resonance imaging (MRI) were compared with a novel application of X-ray microtomography (XmuT) to track the movements of embedded glass microsphere tracers as the model tablets swelled. MRI provided information concerning the movement of hydration fronts into the tablets and the composition of the swollen gel layer, which formed at the tablet surface and progressively thickened with time. Conversely, XmuT revealed significant axial expansion within the tablet core, at...
Source: European Journal of Pharmaceutics and Biopharmaceutics - June 25, 2009 Category: Drugs & Pharmacology Authors: Laity PR, Mantle MD, Gladden LF, Cameron RE Tags: Eur J Pharm Biopharm Source Type: journals

Improvement of cyclosporine A bioavailability by incorporating ethyl docosahexaenoate in the microemulsion as an oil excipient.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The aims of this study were to determine the effect of ethyl docosahexaenoate (DHA-EE) on cyclosporine A (CsA) bioavailability, while also examining the effect of DHA-EE on CsA when DHA-EE was incorporated into a microemulsion formulation as an oil ingredient. The oral co-administration of DHA-EE and CsA increased the blood CsA concentration in a dose-dependent manner, and the AUC and C(max) both increased by about 2-fold with 100 mg/kg DHA-EE. The microemulsion formulation of CsA consisted of Tween-20, ethanol, water and DHA-EE (53.3/6.5/35.9/3.3% w/w) (namely DHA-ME) was transparent and stable with an average particl...
Source: European Journal of Pharmaceutics and Biopharmaceutics - June 24, 2009 Category: Drugs & Pharmacology Authors: Hirunpanich V, Sato H Tags: Eur J Pharm Biopharm Source Type: journals

Lipid nanocapsules: ready-to-use nanovectors for the aerosol delivery of paclitaxel.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Aerosol drug delivery permits the development of dose-intensification strategies in severe, malignant lung diseases. The aim of the study was to demonstrate that the encapsulation of paclitaxel in lipid nanocapsules (LNC), a novel drug nanocarrier for lipophilic components, allows one to provide pulmonary drug delivery of paclitaxel by nebulisation thereby allowing preclinical and clinical studies. LNC dispersions are made into aerosols with commercial nebulisers. The structure, drug payload and cytotoxicity of nebulised LNCs were compared to fresh LNCs. The results demonstrated that LNC dispersions could be made into ...
Source: European Journal of Pharmaceutics and Biopharmaceutics - June 24, 2009 Category: Drugs & Pharmacology Authors: Hureaux J, Lagarce F, Gagnadoux F, Vecellio L, Clavreul A, Roger E, Kempf M, Racineux JL, Diot P, Benoit JP, Urban T Tags: Eur J Pharm Biopharm Source Type: journals

Modeling Drug Release From Hot-Melt Extruded Mini-Matrices With Constant And Non-Constant Diffusivities.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Different types of ethylcellulose-based mini-matrices were prepared by hot-melt extrusion and thoroughly characterized in vitro. Metoprolol tartrate was used as model drug and various amounts and types of polyethylene glycol (PEG)/polyethylene oxide (PEO) were added as release rate modifiers. Based on the experimental results, appropriate mathematical theories were identified/developed allowing for a better understanding of the underlying drug release mechanisms. For instance, it could be shown that at high initial PEG/PEO contents and/or intermediate initial PEG/PEO contents of low molecular weight, drug diffusion wit...
Source: European Journal of Pharmaceutics and Biopharmaceutics - June 19, 2009 Category: Drugs & Pharmacology Authors: Verhoeven E, Siepmann F, Beer TR, Loo DV, Mooter GV, Remon JP, Siepmann J, Vervaet C Tags: Eur J Pharm Biopharm Source Type: journals

Intra-articular drug delivery systems for the treatment of rheumatic diseases: a review of the factors influencing their performance.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Osteoarthritis and rheumatoid arthritis are rheumatic diseases for which a curative treatment does not currently exist. Their management is directed towards pain relief, achieved with different classes of drugs, among which non-steroidal and steroidal anti-inflammatory substances are the most frequently used. Nevertheless, the oral or systemic administration of such drugs is hindered by numerous side effects, which could be overcome by their intra-articular (i-a.) administration as dosage forms, capable of gradually releasing the active substance. The present review article summarises the research done in the field of ...
Source: European Journal of Pharmaceutics and Biopharmaceutics - June 18, 2009 Category: Drugs & Pharmacology Authors: Butoescu N, Jordan O, Doelker E Tags: Eur J Pharm Biopharm Source Type: journals

Noninvasive in vivo evaluation of in situ forming PLGA implants by benchtop magnetic resonance imaging (BT-MRI) and EPR spectroscopy.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In the present study we used benchtop magnetic resonance imaging (BT-MRI) for non-invasive and continuous in vivo studies of in situ forming poly(lactide-co-glycolide) (PLGA) implants without the use of contrast agents. Polyethylene glycol (PEG) 400 was used as an alternative solvent to the clinically used NMP. In addition to BT-MRI, we applied electron paramagnetic resonance (EPR) spectroscopy to characterize implant formation and drug delivery processes in vitro and in vivo. We were able to follow key processes of implant formation by EPR and MRI. Because EPR spectra are sensitive to polarity and mobility, we were ab...
Source: European Journal of Pharmaceutics and Biopharmaceutics - June 18, 2009 Category: Drugs & Pharmacology Authors: Kempe S, Metz H, Pereira PG, Mäder K Tags: Eur J Pharm Biopharm Source Type: journals

Effect of gliclazide immobilization into layered double hydroxide on drug release.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
This paper deals with a new hydrotalcite-like compound used as a matrix to improve dissolution rate of the poorly water soluble drug gliclazide, and to administer at the same time micro- and oligo-elements useful to improve insulin performance. Gliclazide is a second-generation sulfonylurea compound used in the treatment of type II diabetes mellitus. As a consequence of the poor water solubility, its absorption is limited. Thus, a new hydrotalcite-like compound containing Zinc and Cromium, micronutrients directly involved in the physiology of insulin and in the carbohydrate, lipid and protein metabolism, was synthesize...
Source: European Journal of Pharmaceutics and Biopharmaceutics - June 15, 2009 Category: Drugs & Pharmacology Authors: Ambrogi V, Perioli L, Ciarnelli V, Nocchetti M, Rossi C Tags: Eur J Pharm Biopharm Source Type: journals

Improvements of cellular stress response on resveratrol in liposomes.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Resveratrol (RSV) has proven potential in prophylaxis and treatment of various disorders mediated by free radicals and oxidative stress. RSV solubility, stability, and cytotoxicity must be regulated for satisfactory bioavailability. Here RSV was loaded into liposomes, characterized by PCS and TEM and evaluated on HEK293 cell line by metabolic activity assay, electron paramagnetic resonance and fluorescence microscopy. RSV at 10 muM induced changes in cell metabolic activity and significantly improved antioxidative capacity. At 100 muM it showed concentration dependent cytotoxicity. Oligolamellar liposomes with mean dia...
Source: European Journal of Pharmaceutics and Biopharmaceutics - June 11, 2009 Category: Drugs & Pharmacology Authors: Kristl J, Teskač K, Caddeo C, Abramović Z, Sentjurc M Tags: Eur J Pharm Biopharm Source Type: journals

In vivo evaluation of the vaginal distribution and retention of a multi-particulate pellet formulation.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Non-disintegrating microcrystalline cellulose pellets (MCC) and disintegrating starch-based pellets were evaluated as new vaginal drug delivery forms and compared with a powder formulation. Pellets and powder were packed in a HPMC or hard gelatine capsule and vaginally administered to 5 series of 5 healthy volunteers. Distribution and retention of the multi-particulate formulation was monitored by colposcopy and swabbing. Capsule disintegration in the vagina was slow. MCC pellets clustered around the fornix 3 h after administration and after 24 h only a few pellets were detected in the vaginal cavity. In contrast, star...
Source: European Journal of Pharmaceutics and Biopharmaceutics - June 10, 2009 Category: Drugs & Pharmacology Authors: Poelvoorde N, Verstraelen H, Verhelst R, Saerens B, Backer ED, Santiago GL, Vervaet C, Vaneechoutte M, Boeck FD, Bortel LV, Temmerman M, Remon JP Tags: Eur J Pharm Biopharm Source Type: journals