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European Journal of Pharmaceutics and Biopharmaceutics

Esther S Bochmann, Elgin E Üstüner, Andreas Gryczke, Karl G Wagner
The feasibility of predicting melt rheology by using the glass transition temperature (Tg) of a desired amorphous solid dispersion (ASD) for hot-melt extrusion (HME) and other melt based processes is presented. Three groups of three different active pharmaceutical ingredients (APIs) or plasticizer/copovidone mixtures, with identical glass transition in rheological testing, were used. Their rheological behavior as a function of temperature and frequency were analyzed by means of small amplitude oscillatory shear (SAOS) on an oscillatory rheometer...
May 19, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Katrin Göke, Thomas Lorenz, Alexandros Repanas, Frederic Schneider, Denise Steiner, Knut Baumann, Heike Bunjes, Andreas Dietzel, Jan H Finke, Birgit Glasmacher, Arno Kwade
Low aqueous solubility of active pharmaceutical ingredients presents a serious challenge in the development process of new drug products. This article provides an overview on some of the current approaches for the formulation of poorly water-soluble drugs with a special focus on strategies pursued at the Center of Pharmaceutical Engineering of the TU Braunschweig. These comprise formulation in lipid-based colloidal drug delivery systems and experimental as well as computational approaches towards the efficient identification of the most suitable carrier systems...
May 19, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Katrin Göke, Heike Bunjes
Passive drug loading can be used to effectively identify suitable colloidal lipid carrier systems for poorly water-soluble drugs. This method comprises incubation of preformed carrier systems with drug powder and subsequent determination of the resulting drug load of the carrier particles. Until now, the passive loading mechanism is unknown, which complicates reliable routine use. In this work, the influence of drug characteristics on the course of passive loading was investigated systematically varying drug surface area and drug solubility...
May 18, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Giulia Di Prima, Silvia Saladino, Flavia Bongiovì, Giorgia Adamo, Giulio Ghersi, Giovanna Pitarresi, Gaetano Giammona
In this work a new copolymer of inulin (INU) derivatized with ethylendiamine (EDA) and retinoic acid (RA), named INU-EDA-RA, was synthetized, characterized and employed to produce micelles as carriers for topical administration of corticosteroids for the potential treatment of diseases of posterior eye segment. Spectroscopic analysis confirmed a molar derivatization degree of 11.30 and 4.30 % in EDA and RA, respectively. INU-EDA-RA micelles are capable of strong mucoadhesive interactions which result time-independent and stable over time but concentration depending...
May 13, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Lucas A Rigo, Cristiane S Carvalho-Wodarz, Adriana R Pohlmann, Silvia S Guterres, Nicole Schneider-Daum, Claus-Michael Lehr, Ruy C R Beck
The anti-inflammatory effect of polymeric deflazacort nanocapsules (NC-DFZ) was investigated, and possible improvement of epithelial barrier function using filter grown monolayers of A549 and Calu-3 using as models was assessed. NC prepared from poly(ε-caprolactone) (PCL) had a mean size around 200 nm, slightly negative zeta potential (∼ - 8 mV), and low polydispersity index (< 0.10). Encapsulation of DFZ had an efficiency of 85%. No cytotoxic effects were observed at particle concentration of 9.85 x 10(11) NC/ml, which was therefore chosen to evaluate the effect of NC-DFZ at 1% (w/v) of PCL and 0...
May 13, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Moritz Beck-Broichsitter, Nina Oesterheld
The size of airborne particles determines their deposition pattern within the lungs and therefore, the efficacy of inhalation therapy. The present study analyzed factors affecting liquid atomization performed by vibrating-membrane technology. First, the process of vibrating-membrane nebulization (eFlow(®)rapid and Aeroneb(®) Pro) was challenged with numerous inorganic salts and active pharmaceutical ingredients. All investigated samples caused a sigmoidal decrease in aerosol droplet size upon an increase in concentration...
May 9, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Manisha Kumari, L Ray, M P Purohit, S Patnaik, A B Pant, Y Shukla, P Kumar, K C Gupta
The anticancer properties of selenium (Se) and curcumin nanoparticles in solo formulations as well as in combination with other therapeutic agents have been proved time and again. Exploiting this facet of the two, we clubbed their tumoricidal characteristics and designed curcumin loaded Se nanoparticles (Se-CurNPs) to achieve an enhanced therapeutic effect. We evaluated their therapeutic effects on different cancer cell lines and Ehrlich's ascites carcinoma mouse model. In vitro results showed that Se-CurNPs were most effective on colorectal carcinoma cells (HCT116) compared to the other cancer cell lines used and possessed pleiotropic anticancer effects...
May 9, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Manuela Curcio, Luis Diaz-Gomez, Giuseppe Cirillo, Angel Concheiro, Francesca Iemma, Carmen Alvarez-Lorenzo
pH/redox dual-responsive nanogels (DEX-SS) were prepared by precipitation polymerization of methacrylated dextran (DEXMA), 2-aminoethylmethacrylate (AEMA) and N,N'-bis(acryloyl)cystamine (BAC), and then loaded with methotrexate (MTX). Nanogels were spherical and exhibited homogeneous size distribution (460 nm, PDI < 0.30) as observed using dynamic light scattering (DLS) and scanning electron microscopy (SEM). DEX-SS were sensitive to the variations of pH and redox environment. Nanogels incubated in buffer pH 5...
May 3, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Eva M Vicente-Perez, Eneko Larrañeta, Maelíosa T C McCrudden, Adrien Kissenpfennig, Shauna Hegarty, Helen O McCarthy, Ryan F Donnelly
We address, for the first time, the impact of skin insertion on multiple occasions of polymeric microneedle arrays in an animal model in vivo. Dissolving microneedle arrays prepared from aqueous blends of 20% w/w Gantrez(®) S-97 BF and 40% w/w poly(vinyl pyrrolidone) 58 kDa and hydrogel-forming microneedle arrays prepared from aqueous blends of and poly(ethyleneglycol) 10 kDa were repeatedly applied to the skin of hairless mice in vivo. Skin appearance and skin barrier function, as illustrated by measurement of transepidermal water loss, were not measurably altered during the entire study period...
May 3, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Hanady Ajine Bibi, René Holm, Annette Bauer-Brandl
The simultaneous processes of lipid digestion and absorption together determine the oral bioavailability of drugs incorporated into lipid based drug delivery systems (LBDDS). A number of slightly different protocols for in vitro lipolysis are widely accepted; however, the permeation process has so far not been included into the models due to the harsh conditions of lipid digestion compromising permeation barriers. The present study for the first time combines biomimetic permeation and lipolysis of LBDDS. The focus of the current work was on the functional stability of the barrier - Permeapad(®) during lipid digestion...
May 3, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Nazende Günday Türeli, Afra Torge, Jenny Juntke, Bianca C Schwarz, Nicole Schneider-Daum, Akif Emre Türeli, Claus-Michael Lehr, Marc Schneider
Current pulmonary treatments against Pseudomonasaeruginosa infections in cystic fibrosis (CF) lung suffer from deactivation of the drug and immobilization in thick and viscous biofilm/mucus blend, along with the general antibiotic resistance. Administration of nanoparticles (NPs) with high antibiotic load capable of penetrating the tight mesh of biofilm/mucus can be an advent to overcome the treatment bottlenecks. Biodegradable and biocompatible polymer nanoparticles efficiently loaded with ciprofloxacin complex offer a solution for emerging treatment strategies...
May 2, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Aharon Azagury, Eliz Amar-Lewis, Reut Appel, Mordechai Hallak, Joseph Kost
Chemical penetration enhancers (CPEs) have long been used for mass transport enhancement across membranes. Many CPEs are used in a solution or gel and could be a solvent. The use of CPEs is mainly limited due to their toxicity/irritation levels. This study presents the evaluation of encapsulated CPEs in nano-sized polymeric particles on the chorioamnion (CA) membrane mass transport. CPEs' mass encapsulated in nanoparticles was decreased by 10,000-fold. Interestingly, this approach resulted in a 6-fold increase in mass transport across the CA...
April 29, 2017: European Journal of Pharmaceutics and Biopharmaceutics
A T Larsen, R Holm, A Müllertz
In this study, the potential of co-administering an aqueous suspension with a placebo lipid vehicle, i.e. chase dosing, was investigated in rats relative to the aqueous suspension alone or a solution of the drug in the lipid vehicle. The lipid investigated in the present study was Labrafil M2125CS and three evaluated poorly soluble model compounds, danazol, cinnarizine and halofantrine. For cinnarizine and danazol the oral bioavailability in rats after chase dosing or dosing the compound dissolved in Labrafil M21515CS was similar and significantly higher than for the aqueous suspension...
April 29, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Evren H Gokce, Sakine Tuncay Tanrıverdi, Ipek Eroglu, Nicolas Tsapis, Goksel Gokce, Isıl Tekmen, Elias Fattal, Ozgen Ozer
An alternative formulation for the treatment of diabetic foot wounds that heal slowly is a requirement in pharmaceutical field. The aim of this study was to develop a dermal matrix consisting of skin proteins and lipids with an antioxidant that will enhance healing and balance the oxidative stress in the diabetic wound area due to the high levels of glucose. Thus a novel three dimensional collagen-laminin porous dermal matrix was developed by lyophilization. Resveratrol-loaded hyaluronic acid and dipalmitoylphosphatidylcholine microparticles were combined with this dermal matrix...
April 28, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Tamás Bozó, András Wacha, Judith Mihály, Attila Bóta, Miklós S Z Kellermayer
Cochleates, calcium-stabilized membrane rolls of nanoscale diameter, promise a unique and efficient way of delivering lipid-soluble drugs, proteins or nucleic acids into biological systems because they protect the encapsulated material against enzymatic or chemical degradation. Self-aggregation, which typically arises during production and storage is a major obstacle that has so far precluded the development of an efficient cochleate-based drug-delivery system. Here we show that citric acid, added transiently in a narrow concentration range, effectively disperses cochleate aggregates, stabilizes the disperse state for long-term storage and preserves the canonical ultrastructure and topological characteristics of cochleate nanoparticles...
April 28, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Vito Coviello, Stefania Sartini, Luca Quattrini, Cecilia Baraldi, Maria Cristina Gamberini, Concettina La Motta
Nano-sized colloidal carriers represent innovative drug delivery systems, as they allow a targeted and prolonged release of poorly water-soluble drugs, improving their bioavailability and modifying their pharmacokinetic parameters. In this work we describe cyclodextrin-based nanosponges, obtained through polimerization of β-cyclodextrin with diphenyl carbonate as the cross-linking agent, loaded with a novel multi-effective heterocyclic compound, DB103, able to regulate key cellular events involved in the remodelling of vessels wall...
April 26, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Vida Rahmani, Rand Elshereef, Heather Sheardown
Alginate and cationically modified alginate microparticles were prepared with the goal of developing hydrogel microparticles that offer controlled release of protein drugs mainly by modification of the absolute charge of the hydrogel network. Protein loading and release studies were carried out using model proteins with different net charges (i.e. low, high, and neutral isoelectric points) covering a broad range of molecular weights. The Projection to Latent Structures (PLS) method was used for qualitatively and quantitatively describing the relationships between the properties of proteins such as net charge and molecular weight, polymer properties including degree of substitution and microparticle size, and the release kinetics (kt(n))...
April 26, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Ajit S Narang, Anand Balakrishnan, John Morrison, Jinjiang Li, Jennifer Wang, Huidong Gu, Katrina Taylor, Kenneth Santone, Jon Ehrmann, Sophie Beyer, Xujin Lu, Rod Ketner, Jennifer Pizzano, Tami Orcutt, Eric Shields, Heidi Dulac, Sharon Aborn, Margaret Batchelder, Kimberley Lentz
Variability in oral absorption in pre-clinical species makes human dose projection challenging. In this study, we investigated the mechanistic basis of variability in oral absorption of a model hydrophobic compound with pH-dependent solubility, BMS-955829, after oral dosing in rats, dogs, and cynomolgus monkeys. The contribution of regional absorption to pharmacokinetic variability was assessed in ported monkeys by direct drug intraduodenal and intraileal administration. The effect of BMS-955829 on gastric emptying and intestinal motility was investigated by radiography after co-administration of barium...
April 25, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Claudio Palazzo, Giuseppe Trapani, Gilles Ponchel, Adriana Trapani, Christine Vauthier
The aim of the present work was to evaluate the mucoadhesive properties of poly(isobutyl cyanoacrylate) (PIBCA) nanoparticles (NPs) coated with Low Molecular Weight (LMW) chitosan (CS)- and glycol chitosan (GCS)-based thiomers as well as with the corresponding LMW unmodified polysaccharides. For this purpose, all the CS- and GCS-based thiomers were prepared under simple and mild conditions starting from the LMW unmodified polymers CS and GCS. The resulting NPs were of spherical shape with diameters ranging from 400 to 600 nm and 187 to 309 nm, for CS- and GCS-based NPs, respectively...
April 25, 2017: European Journal of Pharmaceutics and Biopharmaceutics
Jesse Popov, Roger Gilabert-Oriol, Marcel B Bally
Therapeutic monoclonal antibodies hold great promise in the treatment of cancer and other diseases, but their unclear mechanism of action makes it difficult to identify features that will increase their efficacy. One such feature may be antibody valence, since enhanced therapeutic efficacies have been observed using multivalent, as opposed to bivalent, antibodies. For example, multivalent antibody-lipid nanoparticles (Ab-LNPs) containing rituximab (Rtx) or trastuzumab show significantly increased therapeutic activity compared to equivalent doses of the bivalent antibodies...
April 24, 2017: European Journal of Pharmaceutics and Biopharmaceutics
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