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European Journal of Pharmaceutics and Biopharmaceutics

A Schittny, H Ogawa, J Huwyler, M Puchkov
Hot-melt extrusion allows for the continuous production of amorphous solid dispersions, which are used to enhance bioavailability of poorly soluble drugs in pharmaceutical drug delivery. To facilitate formulation and extrusion process development, we propose a mathematical model describing the formation of amorphous solid dispersions in the context of this process. The model is based on the calculation of two key process values: 1) time to dissolution of solid drug particles in molten polymer during extrusion and 2) mean residence of material in the extruder...
September 18, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Shwe Phyu Hlaing, Jihyun Kim, Juho Lee, Nurhasni Hasan, Jiafu Cao, Muhammad Naeem, Eun Hee Lee, Jae Ho Shin, Yunjin Jung, Bok-Leul Lee, Byung Hak Jhun, Jin-Wook Yoo
Methicillin-resistant Staphylococcus aureus (MRSA)-infected wounds have become a significant clinical issue worldwide. Recently, nitric oxide (NO) has emerged as a potent antibacterial agent against MRSA infections and a wound-healing enhancer. Nevertheless, clinical applications of NO have been largely restricted by its gaseous state and short half-life. In this study, our aim was to develop S-nitrosoglutathione (GSNO, an endogenous NO donor)-loaded poly(lactic-co-glycolic acid) [PLGA] microparticles (GSNO-MPs) that release NO over a prolonged period, to accelerate the healing of MRSA-infected wounds with less frequent dosing...
September 14, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Maria B C de Matos, Nataliia Beztsinna, Christoph Heyder, Marcel H A M Fens, Enrico Mastrobattista, Raymond M Schiffelers, Gero Leneweit, Robbert J Kok
Lysolipid-containing thermosensitive liposomes (LTSL) are clinically-relevant drug nanocarriers which have been used to deliver small molecule cytostatics to tumors in combination with local hyperthermia (42 °C) to trigger local drug release. The objective of this study was to investigate the feasibility of LTSL for encapsulation and triggered release of macromolecular drugs such as plant-derived cytotoxins. As therapeutic protein we used Mistletoe lectin-1 (ML1) - a ribosome-inactivating protein with potent cytotoxic activity in tumor cells...
September 14, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Abhay Jain, Harsh S Shah, Paul R Johnson, Ajit S Narang, Ken R Morris, Rahul V Haware
Anisotropic features with other crystallographic properties like d-spacing, and attachment energy (Eatt ) can predict material performance during the secondary pharmaceutical processing. A newly developed state-of-the-art compression cell lodged in a powder X-ray diffractometer was used to measure anisotropic Young's moduli (YM) of flufenamic acid (FFA) polymorphs in this study. Methodology is based on the generation of a single crystal deformation in this cell, which reflects as a change in the d-spacing in the PXRD pattern...
September 10, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Jacqueline Horn, Eleonora Tolardo, Davide Fissore, Wolfgang Friess
Bulking agents as mannitol (Man) and glycine (Gly) require high bulking agent to stabilizer ratios to ensure their crystallization during the freeze-drying process. The aim of this study was to investigate several amino acids (AA) as potential alternative bulking agents in low AA to sucrose (Suc) ratios. A fast freeze-drying process was performed above the collapse temperature (Tc) of the amorphous phase challenging the crystalline AA scaffold. Lyophilizates and liquid formulations were characterized by differential scanning calorimetry...
September 7, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Isabell Speer, Denise Steiner, Yasmin Thabet, Jörg Breitkreutz, Arno Kwade
Orodispersible films (ODFs) provide high application comfort due to rapid disintegration in the oral cavity. They increasingly found the approval of pharmaceutical research and development and were added to the European Pharmacopeia in 2012. The European Pharmacopeia explicitly demands disintegration testing for ODFs, but does not refer to a suitable method. The aim of this study was to collect and evaluate existing disintegration methods regarding their suitability to investigate different ODF formulations...
September 7, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Lee B Sims, Hunter A Miller, Michael E Halwes, Jill M Steinbach-Rankins, Hermann B Frieboes
The secreted mucus layer in the vaginal epithelium presents a formidable barrier to the transport of active agents for the prevention and treatment of female reproductive tract (FRT) infections. Nanoparticle-mediated drug delivery has been proposed to help facilitate the transport and release of active agents through the cervicovaginal mucus (CVM) and underlying mucosa. However, both nanoparticles (NPs) and free active agents face a variety of challenges, often requiring the administration of high localized doses to circumvent leakage and poor penetration to targeted intravaginal tissue compartments...
September 6, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Osama Saher, Cristina S J Rocha, Eman M Zaghloul, Oscar Wiklander, Susanna Zamolo, Marc Heitz, Kariem Ezzat, Dhanu Gupta, Jean-Louis Reymond, Rula Zain, Florian Hollfelder, Tamis Darbre, Karin E Lundin, Samir El Andaloussi, C I Edvard Smith
Despite the advances in gene therapy and in oligonucleotide (ON) chemistry, efficient cellular delivery remains an obstacle. Most current transfection reagents suffer from low efficacy or high cytotoxicity. In this report, we describe the synergism between lipid and dendrimer delivery vectors to enhance the transfection efficiency, while avoiding high toxicity. We screened a library of 20 peptide dendrimers representing three different generations and evaluated their capability to deliver a single-stranded splice-switching ON after formulating with lipids (DOTMA/DOPE)...
September 4, 2018: European Journal of Pharmaceutics and Biopharmaceutics
X Unamuno, E Imbuluzqueta, F Salles, P Horcajada, M J Blanco-Prieto
Due to their high porosity and versatile composition and structure, nanoscaled Metal-Organic Frameworks (nanoMOFs) have been recently proposed as novel drug delivery systems, and have been demonstrated to have important capacities and potential for controlled release of different active ingredients. Gentamicin (GM; a broad spectrum aminoglycoside antibiotic indicated in bacterial septicemia therapy) has great therapeutic interest, but the associated bioavailability and toxicity drawbacks accompanying high doses and repeated administration of this free drug make its encapsulation inside new nanocarriers necessary...
September 1, 2018: European Journal of Pharmaceutics and Biopharmaceutics
D Dahlgren, C Roos, A Lundqvist, C Tannergren, M Sjöblom, E Sjögren, H Lennernäs
The relevance of the rat single-pass intestinal perfusion model for investigating in vivo time-dependent effects of absorption-modifying excipients (AMEs) is not fully established. Therefore, the dynamic effect and recovery of the intestinal mucosa was evaluated based on the lumen-to-blood flux (Jabs ) of six model compounds, and the blood-to-lumen clearance of 51 Cr-EDTA (CLCr ), during and after 15- and 60-min mucosal exposure of the AMEs, sodium dodecyl sulfate (SDS) and chitosan, in separate experiments...
September 1, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Katarzyna Jelonek, Joanna Jaworska, Małgorzata Pastusiak, Michał Sobota, Jakub Włodarczyk, Paulina Karpeta, Bożena Kaczmarczyk, Janusz Kasperczyk, Piotr Dobrzyński
Despite extensive development of bioresorbable drug-eluting vascular scaffolds it is still challenging to achieve controlled drug delivery. The lack of capacity for adjusting the drug dose and inadequate release behavior are one of the main reasons of the side effects. However, so far, mainly biodegradable drug-eluting coatings of metallic stents have been studied in regard to explain drug release mechanisms. The objective of this study was to develop degradable polymer coatings applicable to bioresorbable polymer-based scaffolds...
September 1, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Serena Bertoni, Beatrice Albertini, Luisa Stella Dolci, Nadia Passerini
Oral local delivery of therapeutic biologics is generally limited due to the multiple obstacles of the gastrointestinal (GI) tract, mainly represented by acidic stomach pH and digestive enzymes. In the present study, spray congealing was used to prepare solid lipid microparticles (SLMs) loaded with β-galactosidase (lactase), an enzyme used for the treatment of lactose intolerance, to achieve a local drug delivery to the small intestine. Lactase was characterized in terms of activity at different pH, kinetic parameters and proteolytic degradation by digestive enzymes...
August 31, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Didier Clenet, Tatiana Vinit, Damien Soulet, Claire Maillet, Françoise Guinet-Morlot, Aure Saulnier
Vaccine thermostability is key to successful global immunization programs as it may have a significant impact on the continuous cold-chain maintenance logistics, as well as affect vaccine potency. Modern biological and biophysical techniques were combined to in-depth characterize the thermostability of a formulated rabies virus (RABV) in terms of antigenic and genomic titer, virus particle count and aggregation state. Tunable resistive pulse sensing (TRPS) and nanoparticle tracking analysis (NTA) were used to count virus particles while simultaneously determining their size distribution...
August 14, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Philippe Berben, Jef Stappaerts, Matthias J A Vink, Elena Domínguez-Vega, Govert W Somsen, Joachim Brouwers, Patrick Augustijns
In a previously performed small-scale clinical study, healthy volunteers were asked to ingest an oral solution of itraconazole (Sporanox® ) containing 40% 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) (i) with or (ii) without a standardized volume of water (240 mL) after which gastrointestinal and blood samples were collected. Although omitting water during the administration of Sporanox® resulted in noticeably higher duodenal concentrations of itraconazole, systemic exposure was almost unaffected. It is assumed that this discrepancy can be explained by differences in the extent of entrapment of itraconazole in the duodenum caused by differential complexation depending on the concentration of cyclodextrins...
June 27, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Maciej Gajda, Karol P Nartowski, Janusz Pluta, Bożena Karolewicz
Solid-state synthesis of pharmaceutical cocrystals is of contemporary interest as it offers an efficient way to modify the physicochemical properties of Active Pharmaceutical Ingredient (API) including its melting point, solubility, compressibility or physical stability, without compromising its structural integrity and bioactivity. Therefore, research of novel and emerging techniques for solvent-free, continuous and scalable methods for cocrystal formation is of paramount importance for further industrial development...
October 2018: European Journal of Pharmaceutics and Biopharmaceutics
Laurent Salade, Nathalie Wauthoz, Marjorie Vermeersch, Karim Amighi, Jonathan Goole
No abstract text is available yet for this article.
October 2018: European Journal of Pharmaceutics and Biopharmaceutics
Seungki Lee, Jung A Kwon, Keon Hee Park, Chang Min Jin, Ji Bong Joo, Inhee Choi
Mesoporous silica nanoparticles (MSNs) have drawn attention as efficient nanocarriers for drug delivery systems owing to their unique physiochemical properties. However, systemically controlling the kinetics of drug release from the nanocarriers and in situ monitoring of the drug release are still challenging. Here, we report surface-capped MSNs used for controlled drug release and demonstrate label-free in situ Raman monitoring of released drugs based on the molecule-specific spectral fingerprints. By capping the surface of MSNs with amine moieties, gold nanoparticles, and albumin, we achieved high loading efficiencies (up to 97%) of doxorubicin and precisely controlled drug release stimulated by changing pH value...
October 2018: European Journal of Pharmaceutics and Biopharmaceutics
S Melzig, J H Finke, C Schilde, A Kwade
Antisolvent precipitation of poorly water-soluble drugs is a promising formulation technique to synthesize amorphous nanoparticles. The dissolution behavior of these nanoparticles is improved because of the high specific surface area and the amorphous state, leading to an enhanced bioavailability of the drug molecules. Nevertheless, stabilization of precipitated drug nanoparticles against agglomeration and recrystallization, which constitutes a key issue for further processing steps, has turned out to be a major challenge...
October 2018: European Journal of Pharmaceutics and Biopharmaceutics
Rafael de Oliveira Pedro, Stefan Hoffmann, Susana Pereira, Francisco M Goycoolea, Carla C Schmitt, Miguel G Neumann
Novel drug delivery strategies are needed to meet the complex challenges associated to cancer therapy. Biocompatible pH-sensitive drug delivery nanocarriers based on amphiphilic co-polymers seem to be promising for cancer treatment. In the present study, a drug delivery system was produced by encapsulating quercetin into novel pH-sensitive self-assembled amphiphilic chitosan nanoparticles. Up to 83% of quercetin was entrapped by the nanoparticles. The particle diameter, as measured by dynamic light scattering (DLS), ranged from ∼235 to ∼312 nm for the blank and ∼490 to ∼502 nm for the loaded carriers...
October 2018: European Journal of Pharmaceutics and Biopharmaceutics
Kira Nultsch, Oliver Germershaus
Engineering of drug delivery systems has evolved in recent decades from comparably simple designs that merely controlled drug release to complex, often multistage systems that respond to multiple biological or environmental stimuli. Matrix metalloproteases (MMPs) are a family of proteolytic enzymes that are involved in numerous physiologic and pathophysiologic processes, including cancer. Therefore, these enzymes represent highly relevant targets for the development of novel bioresponsive drug delivery systems...
October 2018: European Journal of Pharmaceutics and Biopharmaceutics
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