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European Journal of Pharmaceutics and Biopharmaceutics

Andreas Beyer, Holger Grohganz, Korbinian Löbmann, Thomas Rades, Claudia S Leopold
Co-amorphisation represents a promising approach to increase the physical stability and dissolution rate of amorphous active pharmaceutical ingredients (APIs) as an alternative to polymer glass solutions. For amorphous and co-amorphous systems, it is reported that the preparation method and the blend ratio play major roles with regard to the resulting physical stability. Therefore, in the present study, co-amorphous naproxen-indomethacin (NAP/IND) was prepared by melt-quenching at three different cooling rates and at ten different NAP/IND blend ratios...
October 13, 2016: European Journal of Pharmaceutics and Biopharmaceutics
A-S Boisgard, M Lamrayah, M Dzikowski, D Salmon, P Kirilov, C Primard, F Pirot, B Fromy, B Verrier
One of the main goals in the galenic development of innovative topical treatment options for inflammatory skin diseases such as psoriasis and atopic dermatitis is to selectively deliver the drug at the inflammation site. Recent studies have highlighted the beneficial use of polymeric nanoparticles for anti-inflammatory therapy and topical anti-inflammatory drug delivery due to their ability to form a drug reservoir retaining the drug locally at the site of action. Our approach consisted in designing innovative topical semi-solid formulations of poly(lactic acid) (PLA) nanoparticles as anti-inflammatory drug vehicles for local treatment of inflammatory skin diseases...
October 1, 2016: European Journal of Pharmaceutics and Biopharmaceutics
Abdolali Amiri, Phuong Uyen Le, Alexandre Moquin, Gayane Machkalyan, Kevin Petrecca, John W Gillard, Nathan Yoganathan, Dusica Maysinger
Carbonic anhydrase IX (CAIX) is a transmembrane enzyme upregulated in several types of tumors including glioblastoma multiforme (GBM). GBM is among the most aggressive tumors among gliomas. Temozolomide (TMZ) therapy combined with surgical or radiation approaches are standard treatments but not effective in long term. In this study we tested the treatment with acetazolamide (ATZ), an inhibitor of CAIX, alone or combined with TMZ. The experiments were performed in 2D and 3D cultures (spheroids) using glioblastoma U251N and human brain tumor stem cells (BTSC)...
October 1, 2016: European Journal of Pharmaceutics and Biopharmaceutics
Moran Golan, Valeria Feinshtein, Ayelet David
The key for successful gene silencing is to design a safe and efficient siRNA delivery system for the transfer of therapeutic nucleic acids into the target cells. Here, we describe the design of hydrophilic N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer displaying multiple copies of octaarginine (R8) and its use in promoting the effective delivery of small interfering RNA (siRNA) molecules intracellularly. Fluorescein-5-isothiocyanate (FITC)-labeled HPMA copolymer-bound R8 (P-R8-FITC) was synthesized with increasing R8 molar ratios (4 to 9...
October 1, 2016: European Journal of Pharmaceutics and Biopharmaceutics
Karl Sydow, Heike Nikolenko, Dorothea Lorenz, Rainer H Müller, Margitta Dathe
Lipopeptide-based micelles and liposomes were found to differ in cell recognition and uptake mode into blood brain barrier (BBB) endothelial cells. Here we analyze the role of size and surface charge of micelles and liposomes composed of different lipopeptide sequences with respect to uptake into human brain capillary (HBMEC) and aortic (HAoEC) endothelial cells. Comparable to the dipalmitoylated apolipoprotein E-derived P2A2, lipopeptides of cationic poly-arginine (P2Rn), poly-lysine (P2Kn) and an anionic glutamic-acid sequence (P2En) self assemble into micelles (12-14 nm in diameter) with high surface charge density, and bind to small (SUVs, about 24 nm in diameter) and large (LUV, about 100 nm in diameter) liposomes at variable lipid to peptide ratios...
October 1, 2016: European Journal of Pharmaceutics and Biopharmaceutics
Nazareth Eliana Ceschan, Verónica Bucalá, María Verónica Ramírez-Rigo, Hugh David Charles Smyth
The inhalatory route has emerged as an interesting non-invasive alternative for drug delivery. This allows both pulmonary (local) or systemic treatments (via alveolar absorption). Further advantages in terms of stability, dose and patient preference have often lead researchers to focus on dry powder inhaler delivery systems. Atenolol is an antihypertensive drug with low oral bioavailability and gastrointestinal side effects. Because atenolol possesses adequate permeation across human epithelial membranes, it has been proposed as a good candidate for inhalatory administration...
September 30, 2016: European Journal of Pharmaceutics and Biopharmaceutics
Ngo Bich Nga Nathalie Tran, Fanny Knorr, Wing Cheung Mak, Kwan Yee Cheung, Heike Richter, Martina Meinke, Jürgen Lademann, Alexa Patzelt
Hair follicle research is currently focused on the development of drug-loaded nanocarriers for the targeting of follicular structures in the treatment of skin and hair follicle-related disorders. In the present study, a dual-label nanocarrier system was implemented in which FITC-labeled BSA hydrogel nanocarriers loaded with the model drug and dye TRITC-dextran were applied topically to porcine ear skin. Follicular penetration and the distribution of both dyes corresponding to the nanocarriers and the model drug in the follicular ducts subsequent to administration to the skin were investigated using confocal laser scanning microscopy...
September 29, 2016: European Journal of Pharmaceutics and Biopharmaceutics
Jari Rubbens, Joachim Brouwers, Jan Tack, Patrick Augustijns
This study investigated the impact of relevant gastrointestinal conditions on the intraluminal dissolution, supersaturation and precipitation behavior of the weakly basic drug indinavir. The influence of (i) concomitant PPI intake and (ii) the nutritional state on the gastrointestinal behavior of indinavir was assessed in order to identify the underlying mechanisms responsible for previously reported interactions. Five healthy volunteers were recruited into a cross-over study containing the following arms: fasted state, fed state and fasted state with concomitant proton pump inhibitor (PPI) use...
September 28, 2016: European Journal of Pharmaceutics and Biopharmaceutics
Ožbej Zupančič, Julia Anita Grießinger, Julia Rohrer, Irene Pereira de Sousa, Lukas Danninger, Alexandra Partenhauser, Nadine Flavia Elli Sündermann Laffleur, Andreas Bernkop-Schnürch
AIM: It was the aim of this study to develop SEDDS for oral enoxaparin administration and evaluate it in vitro and in vivo. METHODS: The emulsifying properties of SEDDS composed of long chain lipids (LC-SEDDS), medium chain lipids (MC-SEDDS), short chain lipids (SC-SEDDS) and no lipids (NL-SEDDS) were evaluated. Thereafter, enoxaparin was incorporated via hydrophobic ion pairing in the chosen SEDDS, which were evaluated regarding their mucus permeating properties, stability towards pancreatic lipase, drug release profile and cytotoxicity...
September 28, 2016: European Journal of Pharmaceutics and Biopharmaceutics
Diego Romano Perinelli, Marco Cespi, Luca Casettari, Driton Vllasaliu, Michela Cangiotti, Maria Francesca Ottaviani, Gianfabio Giorgioni, Giulia Bonacucina, Giovanni Filippo Palmieri
Toxicity is one of the main concern limiting the use of surfactants. Many efforts have been devoted to the development of new amphiphilic molecules characterized by a lower toxicological profile and environmental impact. N-acyl amino acids are a class of anionic surfactants that can find applications in different technological fields as an alternative to sulphate-based surfactants (e.g., sodium dodecyl sulphate). The understanding of the relationship between chemical structure and toxicological profile is fundamental for the disclosure of the full potential of these amphiphiles...
September 28, 2016: European Journal of Pharmaceutics and Biopharmaceutics
Anatoli Bogdan, Mario J Molina, Heikki Tenhu
Although freeze-induced phase separation and the ice/FCS (freeze-concentration solution) morphology of aqueous solutions play an important role in fields ranging from life sciences and biotechnology to geophysics and high-altitude ice clouds, their understanding is far from complete. Herein, using differential scanning calorimetry (DSC) and optical cryo-microscope (OC-M), we have studied the freezing and glass transition behavior and the ice/FCS morphology of emulsified 10 - 60 wt % CA (citric acid) solutions in the temperature region of ∼308 and 153 K...
September 20, 2016: European Journal of Pharmaceutics and Biopharmaceutics
T S Anirudhan, Anoop S Nair, J Parvathy
An extended wear therapeutic contact lens (TCL) for the sustained delivery of timolol maleate (TML) was fabricated based on molecular imprinting technique. The designed TCL comprised of a TML imprinted copolymer of carboxymethyl chitosan-g-hydroxy ethyl methacrylate-g-polyacrylamide (CmCS-g-HEMA-g-pAAm) embedded onto a poly HEMA matrix (pHEMA). Successful reloading of TML onto the lens was monitored using a simple and novel UV-Visible spectrophotometric method which showed an excellent reloading capacity of 6...
September 20, 2016: European Journal of Pharmaceutics and Biopharmaceutics
K Wlodarski, L Tajber, W Sawicki
The aim of this research was to develop immediate release tablets comprising solid dispersion (IRSDTs) of tadalafil (Td) in a vinylpyrrolidone and vinyl acetate block copolymer (PVP-VA), characterized by improved dissolution profiles. The solid dispersion of Td in PVP-VA (Td/PVP-VA) in a weight ratio of 1:1 (w/w) was prepared using two different processes i.e. spray drying and ball milling. While the former process has been well established in the formulation of IRSDTs the latter has not been exploited in these systems yet...
September 19, 2016: European Journal of Pharmaceutics and Biopharmaceutics
Paulina Jakubiak, Franz Schuler, Rubén Alvarez-Sánchez
Thorough understanding and control of the different crystal forms of a drug product is a key for fine chemistry and materials science; it ultimately determines the product's physicochemical properties and performance. In this work, we extend the application of a mechanistic dissolution-precipitation model to solvent-mediated solid form transformations. To address the relevance of the model, various kinetic solvent-mediated polymorphic transition studies were retrieved from the literature. Our model succeeds in accurately describing the experimental data, shedding light on the molecular steps driving the polymorphic conversion...
September 17, 2016: European Journal of Pharmaceutics and Biopharmaceutics
Katarina Bukara, Laurent Schueller, Jan Rosier, Mark A Martens, Tinne Daems, Loes Verheyden, Siemon Eelen, Michiel Van Speybroeck, Cristian Libanati, Johan A Martens, Guy Van Den Mooter, Françoise Frérart, Koen Jolling, Marjan De Gieter, Branko Bugarski, Filip Kiekens
Formulating poorly water soluble drugs using ordered mesoporous silica materials is an emerging approach to tackle solubility-related bioavailability problems. The current study was conducted to assess the bioavailability-enhancing potential of ordered mesoporous silica in man. In this open-label, randomized, two-way cross-over study, 12 overnight fasted healthy volunteers received a single dose of fenofibrate formulated with ordered mesoporous silica or a marketed product based on micronized fenofibrate. Plasma concentrations of fenofibric acid, the pharmacologically active metabolite of fenofibrate, were monitored up to 96h post-dose...
September 17, 2016: European Journal of Pharmaceutics and Biopharmaceutics
Felix Schneider, Michael Grimm, Mirko Koziolek, Christiane Modeß, Anne Dokter, Tarek Roustom, Werner Siegmund, Werner Weitschies
In the present study temperature, pH and pressure profiles of nine healthy human volunteers were investigated after ingestion of the SmartPill® under conditions simulating the fasted state treatment in bioavailability and bioequivalence studies. In a previously published study the same subjects received the SmartPill® under fed conditions as recommended by the FDA. Since large non-digestible objects are mainly emptied during phase III of the interdigestive migrating motor complex, the gastric residence time of the SmartPill® was found to be clearly shorter under fasting conditions...
September 14, 2016: European Journal of Pharmaceutics and Biopharmaceutics
Amey S Puranik, Ludovic P Pao, Vanessa M White, Nicholas A Peppas
pH-responsive, polyanionic nanoscale hydrogels were developed for the oral delivery of hydrophobic therapeutics, such as common chemotherapeutic agents. Nanoscale hydrogels were designed to overcome physicochemical and biological barriers associated with oral delivery of hydrophobic therapeutics such as low solubility and poor permeability due to P-glycoprotein related drug efflux. Synthesis of these nanoscale materials was achieved by a robust photoemulsion polymerization method. By varying hydrophobic monomer components, four formulations were synthesized and screened for optimal physicochemical properties and in vitro biocompatibility...
September 12, 2016: European Journal of Pharmaceutics and Biopharmaceutics
Omer Salman Qureshi, Alam Zeb, Muhammad Akram, Myung-Sic Kim, Jong-Ho Kang, Hoo-Seong Kim, Arshad Majid, Inbo Han, Sun-Young Chang, Ok-Nam Bae, Jin-Ki Kim
The aim of this study was to enhance the anti-inflammatory effects of carbon monoxide (CO) via sustained release of CO from carbon monoxide-releasing molecule-2-loaded lipid nanoparticles (CORM-2-NPs). CORM-2-NPs were prepared by hot high pressure homogenization method using trilaurin as a solid lipid core and Tween 20/Span 20/Myrj S40 as surfactants mixture. The physicochemical properties of CORM-2-NPs were characterized and CO release from CORM-2-NPs was assessed by myoglobin assay. In vitro anti-inflammatory effects were evaluated by nitric oxide assay in lipopolysaccharide-stimulated RAW 264...
September 12, 2016: European Journal of Pharmaceutics and Biopharmaceutics
Anne Paavola, Christopher M Bernards, Per H Rosenberg
In order to avoid the risks of side-effects of epidural local anesthetics and opioids, the use of nonsteroidal anti-inflammatory drugs (NSAIDs) epidurally would be an interesting option of analgesic therapy. The fairly short duration of action of spinally administered NSAIDs, e.g., ibuprofen, may be prolonged by using controlled release poloxamer gel formulation. Using a microdialysis technique we studied the epidural and intrathecal pharmacokinetics of ibuprofen after its epidural administration as a poloxamer 407 formulation or a solution formulation...
September 8, 2016: European Journal of Pharmaceutics and Biopharmaceutics
Kesinee Netsomboon, Alexandra Partenhauser, Julia Rohrer, Nadine Elli Sündermann, Felix Prüfert, Wongsakorn Suchaoin, Flavia Laffleur, Andreas Bernkop-Schnürch
The purpose of this study was to synthesize preactivated thiomers with different degree of preactivation and to evaluate their potential as novel excipient for nasal apomorphine administration. The thiomer (PAA-cys) was synthesized by addition of thiol groups on poly(acrylic acid) with various molecular mass including 100, 250 and 450 kDa followed by immobilization of 2-mercaptonicotinic acid (2MNA) to thiol groups by disulfide bond formation resulting in PAA-cys-2MNA. These thiomers (PAA100-cys, PAA250-cys and PAA450-cys) were in the next step preactivated by 56...
September 8, 2016: European Journal of Pharmaceutics and Biopharmaceutics
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