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Structure –biocompatibility and transfection activity relationships of cationic polyaspartamides with (dialkylamino)alkyl and alkyl or hydroxyalkyl side groups
Publication date: 30 January 2017 Source:International Journal of Pharmaceutics, Volume 517, Issues 1–2 Author(s): Diana Salakhieva, Vesta Shevchenko, Csaba Németh, Benjámin Gyarmati, András Szilágyi, Timur Abdullin A series of 14 cationic derivatives of poly(aspartic acid) i.e. cationic polyaspartamides with different (dialkylamino)alkyl and alkyl or hydroxyalkyl side groups was synthesized by nucleophilic addition on polysuccinimide. The resulting polyaspartamides have moderate amphiphilic properties. Relationships between the structure and ratio of side groups and in vitro properties o...
Source: International Journal of Pharmaceutics - December 22, 2016 Category: Drugs & Pharmacology Source Type: research

Astaxanthin conjugated polypyrrole nanoparticles as a multimodal agent for photo-based therapy and imaging
In conclusion, the fabricated PPy@BSA-Astx nanoparticles can be used as photoacoustic imaging based prognostic agents for photothermal or photodynamic treatment. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - December 22, 2016 Category: Drugs & Pharmacology Source Type: research

Albumin nanoparticles for glutathione-responsive release of cisplatin: New opportunities for medulloblastoma
Publication date: 30 January 2017 Source:International Journal of Pharmaceutics, Volume 517, Issues 1–2 Author(s): Giuseppina Catanzaro, Manuela Curcio, Giuseppe Cirillo, Umile Gianfranco Spizzirri, Zein Mersini Besharat, Luana Abballe, Alessandra Vacca, Francesca Iemma, Nevio Picci, Elisabetta Ferretti Redox-responsive nanoparticles were synthesized by desolvation of bovine serum albumin followed by disulfide-bond crosslinking with N, Nʹ-Bis (acryloyl) cystamine. Dynamic light scattering and transmission electron microscopy studies revealed spherical nanoparticles (mean diameter: 83nm, polydispersity index: 0.3) t...
Source: International Journal of Pharmaceutics - December 22, 2016 Category: Drugs & Pharmacology Source Type: research

Crystallization of probucol from solution and the glassy state
Publication date: 30 January 2017 Source:International Journal of Pharmaceutics, Volume 517, Issues 1–2 Author(s): Kohsaku Kawakami, Chie Ohba Crystallization of probucol (PBL) from both solution and glassy solid state was investigated. In the crystallization study from solution, six solvents and three methods, i.e., evaporation, addition of a poor solvent, and cooling on ice, were used to obtain various crystal forms. In addition to common two crystal forms (forms I and II), two further forms (forms III and cyclohexane-solvate) were found in this study, and their thermodynamic relationships were determined. Forms I...
Source: International Journal of Pharmaceutics - December 22, 2016 Category: Drugs & Pharmacology Source Type: research

Effects of excipients and curing process on the abuse deterrent properties of directly compressed tablets
In conclusion, addition of large amount of excipients, especially water soluble ones in Polyox™ based ADF tablets increase the risk of abuse by various routes of administration. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - December 22, 2016 Category: Drugs & Pharmacology Source Type: research

Activity of vancomycin release from bioinspired coatings of hydroxyapatite or TiO2 nanotubes
Publication date: 30 January 2017 Source:International Journal of Pharmaceutics, Volume 517, Issues 1–2 Author(s): Daniela Ionita, Daniela Bajenaru-Georgescu, Georgeta Totea, Anca Mazare, Patrik Schmuki, Ioana Demetrescu Herein we investigate the efficiency of various biomimetic coatings for localized drug delivery, using vancomycin as key therapeutic drug, which is a widely used antibiotic for the treatment of strong infections caused by positive Gram bacteria. We evaluate classical hydroxyapatite and biomimetic hydroxyapatite-collagen coatings obtained by electrochemical deposition as well as TiO2 nanotubes arrays...
Source: International Journal of Pharmaceutics - December 22, 2016 Category: Drugs & Pharmacology Source Type: research

Engineered sodium hyaluronate respirable dry powders for pulmonary drug delivery
This study aimed to overcome formulation and manufacturing impediments to engineer biocompatible spray-dried HYA powders for inhalation. Novel methodology was developed to produce HYA microparticles by spray drying. Different types of surfactant were included in the formulation to improve powder respirability, which was evaluated in vitro using cascade impactors. The individual formulation components and formulated products were evaluated for their biocompatibility with A549 respiratory epithelial cells. The inclusion of stearyl surfactants, 5% w/v, produced the most respirable HYA-powders; FPF 59.0–66.3%. A trend to...
Source: International Journal of Pharmaceutics - December 22, 2016 Category: Drugs & Pharmacology Source Type: research

Acrylated chitosan for mucoadhesive drug delivery systems
Publication date: 30 January 2017 Source:International Journal of Pharmaceutics, Volume 517, Issues 1–2 Author(s): Yulia Shitrit, Havazelet Bianco-Peled A new mucoadhesive polymer was synthesized by conjugating chitosan to poly(ethylene glycol)diacrylate (PEGDA) via the Michael type reaction. The product was characterized using NMR. Higher PEGDA grafting efficacy was observed with low molecular weight PEGDA (0.7kDa), compared to long 10kDa PEGDA. The acrylation percentage was calculated based on the reaction of ninhydrin with chitosan, and supported the qualitative NMR findings. The adhesive properties were studied ...
Source: International Journal of Pharmaceutics - December 22, 2016 Category: Drugs & Pharmacology Source Type: research

NaCl strongly modifies the physicochemical properties of aluminum hydroxide vaccine adjuvants
Publication date: 30 January 2017 Source:International Journal of Pharmaceutics, Volume 517, Issues 1–2 Author(s): Jean-François Art, Aurélien vander Straeten, Christine C. Dupont-Gillain The immunostimulation capacity of most vaccines is enhanced through antigen adsorption on aluminum hydroxide (AH) adjuvants. Varying the adsorption conditions, i.e. pH and ionic strength (I), changes the antigen adsorbed amount and therefore the ability of the vaccine to stimulate the immune system. Vaccine formulations are thus resulting from an empirical screening of the adsorption conditions. This work aims at stud...
Source: International Journal of Pharmaceutics - December 22, 2016 Category: Drugs & Pharmacology Source Type: research

Crystalline solid dispersion-a strategy to slowdown salt disproportionation in solid state formulations during storage and wet granulation
Publication date: 30 January 2017 Source:International Journal of Pharmaceutics, Volume 517, Issues 1–2 Author(s): Haichen Nie, Wei Xu, Lynne S. Taylor, Patrick J. Marsac, Stephen R. Byrn Salt disproportionation (a conversion from the ionized to the neutral state) in solid formulations is a potential concern during manufacturing or storage of products containing a salt of the active pharmaceutical ingredient (API) due to the negative ramifications on product performance. However, it is challenging to find an effective approach to prevent or mitigate this undesirable reaction in formulations. Hence, the overall objec...
Source: International Journal of Pharmaceutics - December 22, 2016 Category: Drugs & Pharmacology Source Type: research

Nasal drug delivery: Design of a novel mucoadhesive and in situ gelling polymer
Publication date: 30 January 2017 Source:International Journal of Pharmaceutics, Volume 517, Issues 1–2 Author(s): Claudia Menzel, Max Jelkmann, Flavia Laffleur, Andreas Bernkop-Schnürch The aim of the present study was to establish a novel polymeric excipient for liquid nasal dosage forms exhibiting viscosity increasing properties, improved mucoadhesion and stability towards oxidation in solution. In order to achieve this goal, 2-mercaptonicotinic acid was first coupled to l-cysteine by disulfide exchange reaction and after purification directly attached to the polymeric backbone of xanthan gum by carbodiimide...
Source: International Journal of Pharmaceutics - December 22, 2016 Category: Drugs & Pharmacology Source Type: research

Experimental observations and dissipative particle dynamic simulations on microstructures of pH-sensitive polymer containing amorphous solid dispersions
In this study, lacidipine-Eudragit_E_100 solid dispersions with 20% drug loading were prepared using the solvent evaporation. Dissolution tested showed that ASD had a significantly high rate, which was dependent on the pH of the medium. Based on time-dependent measurement of supersaturation and particle size, inhibition of crystal growth by Eudragit_E_100 differed at pH 1.2 and 6.8 to a great extent. Dissipative particle dynamic (DPD) simulation revealed that at pH 1.2, the swollen microstructures of the particles were associated with rapid drug release. At pH 6.8, a compacted microstructure of small amorphous particle-agg...
Source: International Journal of Pharmaceutics - December 22, 2016 Category: Drugs & Pharmacology Source Type: research

Ex vivo encapsulation of dexamethasone sodium phosphate into human autologous erythrocytes using fully automated biomedical equipment
Publication date: 30 January 2017 Source:International Journal of Pharmaceutics, Volume 517, Issues 1–2 Author(s): Giovanni Mambrini, Marco Mandolini, Luigia Rossi, Francesca Pierigè, Giovanni Capogrossi, Patricia Salvati, Sonja Serafini, Luca Benatti, Mauro Magnani Erythrocyte-based drug delivery systems are emerging as potential new solutions for the release of drugs into the bloodstream. The aim of the present work was to assess the performance of a fully automated process (EDS) for the ex-vivo encapsulation of the pro-drug dexamethasone sodium phosphate (DSP) into autologous erythrocytes in compliance wit...
Source: International Journal of Pharmaceutics - December 22, 2016 Category: Drugs & Pharmacology Source Type: research

Effects of different combinations of nanocrystallization technologies on avanafil nanoparticles: in vitro, in vivo and stability evaluation
Publication date: 30 January 2017 Source:International Journal of Pharmaceutics, Volume 517, Issues 1–2 Author(s): Kareem AbuBakr Soliman, Howida Kamal Ibrahim, Mahmoud Mohammed Ghorab The study investigated the effects of different combined top-down and bottom-up nanocrystallization technologies on particle size and solid state of avanafil nanoparticles. Combined antisolvent precipitation-ultrasonication (sonoprecipitation) technique was adopted to prepare 18 formulas according to 32.21 factorial design using 3 stabilizers; Tween 80, polyvinyl alcohol (PVA) and Pluronic F68 at different concentrations with differen...
Source: International Journal of Pharmaceutics - December 21, 2016 Category: Drugs & Pharmacology Source Type: research

Effective targeting of gemcitabine to pancreatic cancer through PEG-cored Flt-1 antibody-conjugated dendrimers
In conclusion, dendrimer-based targeted delivery of chemotherapeutics may serve as a promising approach for the treatment of malignancies such as pancreatic cancer that do not benefit from conventional chemotherapy. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - December 21, 2016 Category: Drugs & Pharmacology Source Type: research

Transdermal therapeutic systems for memantine delivery. Comparison of passive and iontophoretic transport
Publication date: 30 January 2017 Source:International Journal of Pharmaceutics, Volume 517, Issues 1–2 Author(s): S. del Río-Sancho, C.E. Serna-Jiménez, M. Sebastián-Morelló, M.A. Calatayud-Pascual, C. Balaguer-Fernández, A. Femenía-Font, Y.N. Kalia, V. Merino, A. López-Castellano Memantine is a non-competitive N-methyl-d-aspartate (NMDA) receptor antagonist used in the treatment of moderate to severe dementia including the symptoms of Alzheimer’s disease (AD). It is administered orally but compliance, swallowing problems and the routine use of multiple medicat...
Source: International Journal of Pharmaceutics - December 10, 2016 Category: Drugs & Pharmacology Source Type: research

Thermosensitive nanofibers loaded with ciprofloxacin as antibacterial wound dressing materials
Publication date: 30 January 2017 Source:International Journal of Pharmaceutics, Volume 517, Issues 1–2 Author(s): Heyu Li, Gareth R. Williams, Junzi Wu, Yao Lv, Xiaozhu Sun, Huanling Wu, Li-Min Zhu To obtain wound dressings which could be removed easily without secondary injuries, we prepared thermoresponsive electrospun fiber mats containing poly(di(ethylene glycol) methyl ether methacrylate) (PDEGMA). Blend fibers of PDEGMA and poly(l-lactic acid-co-ε-caprolactone) (P(LLA-CL) were fabricated via electrospinning, and analogous fibers containing the antibiotic ciprofloxacin (CIF) were also prepared. Smooth ...
Source: International Journal of Pharmaceutics - December 9, 2016 Category: Drugs & Pharmacology Source Type: research

Strategy for assessment of the colloidal and biological stability of H1N1 influenza A viruses
Publication date: 30 January 2017 Source:International Journal of Pharmaceutics, Volume 517, Issues 1–2 Author(s): Frank Hämmerling, Oliver Lorenz-Cristea, Pascal Baumann, Jürgen Hubbuch Current influenza vaccines are mostly formulated as liquids which requires a continuous cold chain to maintain the stability of the antigen. For development of vaccines with an increased stability at ambient temperatures, manifold parameters and their influences on the colloidal stability and activity of the antigen have to be understood. This work presents a strategy to examine both, the colloidal stability and the remain...
Source: International Journal of Pharmaceutics - December 9, 2016 Category: Drugs & Pharmacology Source Type: research

Identification of different shapes, colors and sizes of standard oral dosage forms in diabetes type 2 patients —A pilot study
Publication date: 30 January 2017 Source:International Journal of Pharmaceutics, Volume 517, Issues 1–2 Author(s): Sven Stegemann, Regina Riedl, Harald Sourij The clear identification of drug products by the patients is essential for a safe and effective medication management. In order to understand the impact of shape, size and color on medication identification a study was performed in subjects with type 2 diabetes mellitus (T2D). Ten model drugs differentiated by shape, size and color were evaluated using a mixed method of medication schedule preparation by the participants followed by a semi-structured interview...
Source: International Journal of Pharmaceutics - December 8, 2016 Category: Drugs & Pharmacology Source Type: research

Learning from patients: Identifying design features of medicines that cause medication use problems
Publication date: 30 January 2017 Source:International Journal of Pharmaceutics, Volume 517, Issues 1–2 Author(s): Kim Notenboom, Hubert GM Leufkens, Herman Vromans, Marcel L Bouvy Usability is a key factor in ensuring safe and efficacious use of medicines. However, several studies showed that people experience a variety of problems using their medicines. The purpose of this study was to identify design features of oral medicines that cause use problems among older patients in daily practice. A qualitative study with semi-structured interviews on the experiences of older people with the use of their medicines was pe...
Source: International Journal of Pharmaceutics - December 8, 2016 Category: Drugs & Pharmacology Source Type: research

Elucidation and visualization of solid-state transformation and mixing in a pharmaceutical mini hot melt extrusion process using in-line Raman spectroscopy
Publication date: 30 January 2017 Source:International Journal of Pharmaceutics, Volume 517, Issues 1–2 Author(s): Jeroen Van Renterghem, Ashish Kumar, Chris Vervaet, Jean Paul Remon, Ingmar Nopens, Yvan Vander Heyden, Thomas De Beer Mixing of raw materials (drug+polymer) in the investigated mini pharma melt extruder is achieved by using co-rotating conical twin screws and an internal recirculation channel. In-line Raman spectroscopy was implemented in the barrels, allowing monitoring of the melt during processing. The aim of this study was twofold: to investigate (I) the influence of key process parameters (screw s...
Source: International Journal of Pharmaceutics - December 8, 2016 Category: Drugs & Pharmacology Source Type: research

Evaluation of the cytotoxicity, genotoxicity and mucus permeation capacity of several surface modified poly(anhydride) nanoparticles designed for oral drug delivery
Publication date: 30 January 2017 Source:International Journal of Pharmaceutics, Volume 517, Issues 1–2 Author(s): T Iglesias, A López de Cerain, JM Irache, N Martín-Arbella, M Wilcox, J Pearson, A Azqueta The main concerns with drugs designed for oral administration are their inactivation or degradation in the harsh conditions of the gastrointestinal tract, their poor solubility through the gastrointestinal mucus gel layer, the poor intestinal epithelium permeability that limits their absorption, and their toxicity. In this context, poly(anhydride) nanoparticles are capable of protecting the drug from...
Source: International Journal of Pharmaceutics - December 7, 2016 Category: Drugs & Pharmacology Source Type: research

In vitro inhibition of Clostridium difficile by commercial probiotics: A microcalorimetric study
Publication date: 30 January 2017 Source:International Journal of Pharmaceutics, Volume 517, Issues 1–2 Author(s): Mansa Fredua-Agyeman, Paul Stapleton, Abdul W. Basit, Anthony E. Beezer, Simon Gaisford The aim of the study was to investigate the influence of some commercial probiotics on the growth of Clostridium difficile using isothermal microcalorimetry, a technique which can monitor the real time growth of bacteria. Commercial probiotic strains and products, Lactobacillus acidophilus LA-5®, Bifidobacterium lactis BB-12®, Probio 7® and Symprove™ were co-cultured with C. difficile in Brain Heart...
Source: International Journal of Pharmaceutics - December 7, 2016 Category: Drugs & Pharmacology Source Type: research

The use of partially hydrolysed polyvinyl alcohol for the production of high drug-loaded sustained release pellets via extrusion-spheronisation and coating: In vitro and in vivo evaluation
Publication date: 30 January 2017 Source:International Journal of Pharmaceutics, Volume 517, Issues 1–2 Author(s): G. Verstraete, W. De Jaeghere, J. Vercruysse, W. Grymonpré, V. Vanhoorne, F. Stauffer, T. De Beer, A. Bezuijen, J.P. Remon, C. Vervaet Partially hydrolysed polyvinyl alcohol (PVA) was evaluated as a pelletisation aid for the production of pellets with a high acetaminophen and metformin hydrochloride concentration (>70%, w/w). Mixtures with varying drug concentration and PVA/microcrystalline cellulose (MCC) ratios were processed via extrusion-spheronisation, either after addition of PVA as ...
Source: International Journal of Pharmaceutics - December 7, 2016 Category: Drugs & Pharmacology Source Type: research

Layer-by-layer nanoparticle platform for cancer active targeting
Publication date: 30 January 2017 Source:International Journal of Pharmaceutics, Volume 517, Issues 1–2 Author(s): Min Sung Suh, Jie Shen, Liisa T. Kuhn, Diane J. Burgess Nanoparticles as drug delivery carriers have been investigated over the last few decades, particularly for cancer treatment. The rationale in developing such nanoparticles is to maximize drug efficacy while minimizing toxic side effects. This can be most effectively achieved through target specific drug delivery. A novel biocompatible nanoparticle platform prepared using the core-shell self-assembly technique is reported. The core consists of calci...
Source: International Journal of Pharmaceutics - December 5, 2016 Category: Drugs & Pharmacology Source Type: research

Correlating gastric emptying of amphotericin B and paracetamol solid lipid nanoparticles with changes in particle surface chemistry
In this study, we examine the stability of amphotericin B (AmB) and paracetamol (PAR) SLNs in simulated GI fluids during gastric emptying. On contact with the simulated fluids, the particles increased in size due to ingress of the dissolution media into the particles. Simulated gastric emptying revealed that the formulations had mean sizes <350nm and neutral surface charges, both of which are optimal for intestinal absorption of SLNs. There was ingress of the fluids into the SLNs, followed by diffusion of the dissolved drug, whose rate depended on the solubility of the loaded-drug in the particular medium. Ti...
Source: International Journal of Pharmaceutics - December 5, 2016 Category: Drugs & Pharmacology Source Type: research

Fabrication of liposomal doxorubicin exhibiting ultrasensitivity against phospholipase A2 for efficient pulmonary drug delivery to lung cancers
We report that a hybrid liposome composed of phospholipid (DPPC) and PEGylated block-copolymer (Poloxamer 188) can rapidly release an encapsulated hydrophilic drug in the presence of PLA2. DPPC/P188 liposomes released approximately 80% of the encapsulated calcein (a fluorescence marker) within 10min in the presence of 120 mU of PLA2 at 37°C in vitro, whereas several other liposomal compositions used for inhalation therapy did not. DPPC/P188 liposomes were stable in the absence of PLA2 at 37°C after 60min incubation and drug release by PLA2 was dependent on the amount of P188 incorporated into the DPPC liposomes. Dr...
Source: International Journal of Pharmaceutics - December 5, 2016 Category: Drugs & Pharmacology Source Type: research

Fabrication of self-assembled chitosan-dispersed LDL nanoparticles for drug delivery with a one-step green method
Publication date: 30 January 2017 Source:International Journal of Pharmaceutics, Volume 517, Issues 1–2 Author(s): Jing Tian, Shasha Xu, Hongbing Deng, Xinxing Song, Xiujuan Li, Jiajia Chen, Feng Cao, Bin Li Self-assembled nanoparticles (NPs) composed of chitosan (CS) and low density lipoprotein (LDL) of hen eggs were prepared by a one-step green synthesis of mixing CS solution and LDL suspension. The formulated CS-LDL NPs were then applied to encapsulate doxorubicin hydrochloride (DOX) with the encapsulation efficiency of 51.7%. The average particle size and ζ-potential of DOX-loaded CS-LDL NPs (CS-LDL-DOX NPs...
Source: International Journal of Pharmaceutics - December 5, 2016 Category: Drugs & Pharmacology Source Type: research

Effect of the oral administration of nanoencapsulated quercetin on a mouse model of Alzheimer ’s disease
Publication date: 30 January 2017 Source:International Journal of Pharmaceutics, Volume 517, Issues 1–2 Author(s): Lina Clara Gayoso e Ibiapina Moreno, Elena Puerta, José Eduardo Suárez-Santiago, Nereide Stela Santos-Magalhães, Maria J. Ramirez, Juan M. Irache Quercetin has been identified as a promising compound with a neuroprotective potential against age-related neurodegenerative diseases such as Alzheimer's disease (AD). Nevertheless, the clinical application of quercetin is hampered by its low oral bioavailability. The aim of this work was to evaluate the capability of nanoencapsulated quer...
Source: International Journal of Pharmaceutics - December 5, 2016 Category: Drugs & Pharmacology Source Type: research

Predicting optimal wet granulation parameters for extrusion-spheronisation of pharmaceutical pellets using a mixer torque rheometer
Publication date: 30 January 2017 Source:International Journal of Pharmaceutics, Volume 517, Issues 1–2 Author(s): Manuel Kuhs, John Moore, Gayathri Kollamaram, Gavin Walker, Denise Croker Mixer torque rheometry (MTR) was evaluated as a pre-production (pre-formulation and optimization) tool for predicting ideal liquid-to-solid ratios (L/S) for extrusion-spheronisation of a wide range of APIs using 10g formulations. APIs of low, medium and high solubility were formulated at low and high loadings (15 and 40% w/w, respectively) with PVP as binder (5%) and MCC as the major excipient. L/S corresponding to the maximum tor...
Source: International Journal of Pharmaceutics - December 5, 2016 Category: Drugs & Pharmacology Source Type: research

Evaluation of highly branched cyclic dextrin in inhalable particles of combined antibiotics for the pulmonary delivery of anti-tuberculosis drugs
Publication date: 30 January 2017 Source:International Journal of Pharmaceutics, Volume 517, Issues 1–2 Author(s): Kazunori Kadota, Arisa Senda, Hideaki Tagishi, John Oluwasogo Ayorinde, Yuichi Tozuka This work aims to identify a suitable formulation for the pulmonary delivery of combinations of inhalational drugs using highly branched cyclic dextrin (HBCD) macromolecules. We compared the effectiveness between powders prepared from HBCD with those prepared from five alternative excipients (lactose, maltose, sucrose, β-cyclodextrin and methyl β-cyclodextrin) in the pulmonary delivery of a single-dosage form...
Source: International Journal of Pharmaceutics - December 5, 2016 Category: Drugs & Pharmacology Source Type: research

Spray-dried nanocrystals for a highly hydrophobic drug: Increased drug loading, enhanced redispersity, and improved oral bioavailability
In conclusion, we developed a method to solidify aqueous nanocrystals with increased drug loading, good redispersity and improved bioavailability for high hydrophobic drugs. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - November 30, 2016 Category: Drugs & Pharmacology Source Type: research

Improved sustained release of antigen from immunostimulatory DNA hydrogel by electrostatic interaction with chitosan
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Yumiko Ishii-Mizuno, Yuka Umeki, Yoshinori Onuki, Hiroshi Watanabe, Yuki Takahashi, Yoshinobu Takakura, Makiya Nishikawa Immunostimulatory DNA hydrogel (sDNA hydrogel) containing unmethylated cytosine-phosphate-guanine (CpG) sequences has been demonstrated to be a useful antigen delivery system, which can effectively induce an antigen-specific immune response through stimulation of the innate immune system. However, relatively rapid release of antigens from the sDNA hydrogel limits its potential. To enh...
Source: International Journal of Pharmaceutics - November 30, 2016 Category: Drugs & Pharmacology Source Type: research

A novel approach for dry powder coating of pellets with Ethylcellulose. Part I: Evaluation of film formulation and process set up
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Beatrice Albertini, Serena Bertoni, Cecilia Melegari, Luisa Stella Dolci, Nadia Passerini An innovative dry powder coating technology was developed in a high-shear granulator using ethylcellulose (E10) as polymer. Several solid plasticizers were investigated with the aim of decreasing the polymer Tg at least to the highest possible working temperature (80°C). DSC analysis of physical mixtures of E10 and plasticizers evidenced that lauric acid (LA) was the most effective plasticizer. In order to reac...
Source: International Journal of Pharmaceutics - November 30, 2016 Category: Drugs & Pharmacology Source Type: research

Preparation, characterization and in vivo pharmacokinetic study of PVP-modified oleanolic acid liposomes
Publication date: 30 January 2017 Source:International Journal of Pharmaceutics, Volume 517, Issues 1–2 Author(s): Yan Liu, Xiao Luo, Xiaochao Xu, Nannan Gao, Xiaohong Liu The primary purpose of the present study was to design and optimize a liposomal formulation of the poorly water-soluble drug oleanolic acid (OA) to improve its oral bioavailability, and prolong the duration of therapeutic drug level. Liposomes containing a soybean lecithin and cholesterol lipid bilayer, a protective hydrophilic polyvinylpyrrolidone-K30 (PVP-K30) coating, and a protective bile salt, sodium deoxycholate, were prepared by a thin-film...
Source: International Journal of Pharmaceutics - November 30, 2016 Category: Drugs & Pharmacology Source Type: research

Solid lipid nanoparticles for sustained pulmonary delivery of Yuxingcao essential oil: Preparation, characterization and in vivo evaluation
The objective of this study was to prepare solid lipid nanoparticles (SLNs) for sustained pulmonary delivery of Yuxingcao essential oil (YEO). Three YEO loaded SLNs (SLN-200, SLN-400 and SLN-800) with different particle size were prepared and separated following a high-shear homogenization technique using Compritol 888 ATO as lipid and polyvinyl alcohol as an emulsifier. The particle size, zeta potential, drug encapsulation efficiency and drug loading of the SLNs were determined to be between 171 and 812nm, −17.1 and −19.3mV, between 76.6 and 90.2% and between 2.34 and 3.12%, respectively whereas the in vitro r...
Source: International Journal of Pharmaceutics - November 29, 2016 Category: Drugs & Pharmacology Source Type: research

Calcium phosphate nanoparticles functionalized with alendronate-conjugated polyethylene glycol (PEG) for the treatment of bone metastasis
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Weijing Chu, Yanjuan Huang, Chanzhen Yang, Yunhui Liao, Xuefei Zhang, Mina Yan, Shengmiao Cui, Chunshun Zhao Because of the peculiarity of the bone microstructure, the uptake of chemotherapeutics often happens at non-targeted sites, which induces side effects. In order to solve this problem, we designed a bone-targeting drug delivery system that can release drug exclusively in the nidus of the bone. Alendronate (ALN), which has a high ability to target to hydroxyapatite, was used to fabricate double ALN...
Source: International Journal of Pharmaceutics - November 29, 2016 Category: Drugs & Pharmacology Source Type: research

Pharmaceutical technology can turn a traditional drug, dexamethasone into a first-line ocular medicine. A global perspective and future trends
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Javier Rodríguez Villanueva, Laura Rodríguez Villanueva, Manuel Guzmán Navarro Dexamethasone is one of the most prescribed glucocorticoids. It is effective and safe in the treatment of a wide variety of ocular conditions, including anterior and posterior segment inflammation. However, its half-life in the vitreous humor is very short, which means that it typically requires frequent administrations, thus reducing patient adherence and causing therapeutic failure. Innovative dexametha...
Source: International Journal of Pharmaceutics - November 28, 2016 Category: Drugs & Pharmacology Source Type: research

Surfactant effect on the physicochemical characteristics of cationic solid lipid nanoparticles
In this study, three different cationic lipids (dioctadecyl dimethyl ammonium bromide, cetyltrimethyl ammonium bromide, cetylpyridinium chloride) and Brij 76 as nonionic surfactant were employed to formulate Precirol ATO 5 based cSLN using pEGFP-LUC as model plasmid. The physicochemical properties of cSLN were influenced by both type and amount of surfactants. Thermal analyses of bulk cSLN showed endothermic peaks significantly different from the ones of the single pure components, hinting a complete entanglement of the lipid matrix with the surfactants and justifying the different behavior of the cSLN in the ability to in...
Source: International Journal of Pharmaceutics - November 27, 2016 Category: Drugs & Pharmacology Source Type: research

pH-Sensitive PEGylated liposomes for delivery of an acidic dinitrobenzamide mustard prodrug: Pathways of internalization, cellular trafficking and cytotoxicity to cancer cells
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Mimi M. Yang, William R. Wilson, Zimei Wu This paper aims to develop and evaluate a pH-sensitive PEGylated liposomal (pPSL) system for tumor-targeted intracellular delivery of SN25860, a weakly acidic, poorly water-soluble dinitrobenzamide mustard prodrug which is activated by the E. coli nitroreductase nfB. pPSL and non pH-sensitive liposomes (nPSL), as reference, were formulated by thin-film hydration; an active drug loading method was developed with the aid of solubilizers. Cytotoxicity was evaluated...
Source: International Journal of Pharmaceutics - November 27, 2016 Category: Drugs & Pharmacology Source Type: research

Polyethylenimine-functionalized carbon nanotubes tagged with AS1411 aptamer for combination gene and drug delivery into human gastric cancer cells
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Sahar Taghavi, Azadeh Hashem Nia, Khalil Abnous, Mohammad Ramezani In this project, synergistic cancer cell death was achieved by a targeted delivery system comprising Bcl-xL-specific shRNA and a very low DOX content, which simultaneously activated an intrinsic apoptotic pathway. A modified branched polyethylenimine (PEI 10kDa) was grafted through polyethylene glycol (PEG) linker to carboxylated single-walled carbon nanotubes (SWCNT) to serve as a vehicle for shRNA delivery. The SWNT-PEG-PEI conjugate w...
Source: International Journal of Pharmaceutics - November 27, 2016 Category: Drugs & Pharmacology Source Type: research

Paclitaxel-loaded polymeric nanoparticles combined with chronomodulated chemotherapy on lung cancer: In vitro and in vivo evaluation
The objective of our study was to examine the anti-tumor effect of paclitaxel (PTX)-loaded polymeric nanoparticles (PTX-NPs) combined with circadian chronomodulated chemotherapy. Our intention was to screen out the best time of the day for the drug to be administered. PTX-NPs with a diameter of approximately 168nm were prepared through a thin film dispersion technique. The PTX in PTX-NPs showed an initial fast release subsequently a slower and sustained release. The cytotoxicity of chronomodulated administration of PTX-NPs in vitro confirmed that its cytotoxic effect was lower than that of PTX injection, and showed a time-...
Source: International Journal of Pharmaceutics - November 24, 2016 Category: Drugs & Pharmacology Source Type: research

Needleless coaxial electrospinning: A novel approach to mass production of coaxial nanofibers
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Lucie Vysloužilová, Matej Buzgo, Pavel Pokorný, Jiří Chvojka, Andrea Míčková, Michala Rampichová, Jiří Kula, Karel Pejchar, Martin Bílek, David Lukáš, Evžen Amler Herein, we describe a simple spinneret setup for needleless coaxial electrospinning that exceeds the limited production capacity of current approaches. The proposed weir spinneret enables coaxial electrospinning from free liquid surface. This approach leads to the forma...
Source: International Journal of Pharmaceutics - November 24, 2016 Category: Drugs & Pharmacology Source Type: research

Development of flexible nanocarriers for siRNA delivery into tumor tissue
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Hyunkyung Jung, Yuri Shimatani, Mahadi Hasan, Kohei Uno, Susumu Hama, Kentaro Kogure Various non-viral delivery systems for small interfering RNAs (siRNA) have been developed. Such delivery systems generally exhibit tightly formed spherical structures. While such carriers have demonstrated good transfection activity in mono-layered cell systems, effects against solid tumors are often less apparent and difficult to demonstrate, likely due to the rigid structures of the carriers, which may prevent penetra...
Source: International Journal of Pharmaceutics - November 24, 2016 Category: Drugs & Pharmacology Source Type: research

γ-Cyclodextrin
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Phennapha Saokham, Thorsteinn Loftsson γ-Cyclodextrin (γCD) is a cyclic oligosaccharide formed by bacterial digestion of starch and used as solubilizing agent and stabilizer in a variety of pharmaceutical and food products. γCD is a large (molecular weight 1297Da) hydrophilic molecule that does not readily permeate biological membranes and is rapidly digested by bacteria in the gastrointestinal tract. In humans γCD is metabolized by α-amylase that is found in, for example, ...
Source: International Journal of Pharmaceutics - November 24, 2016 Category: Drugs & Pharmacology Source Type: research

Application of DoE approach in the development of mini-capsules, based on biopolymers and manuka honey polar fraction, as powder formulation for the treatment of skin ulcers
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Marika Tenci, Silvia Rossi, Maria Cristina Bonferoni, Giuseppina Sandri, Irene Mentori, Cinzia Boselli, Antonia Icaro Cornaglia, Maria Daglia, Anna Marchese, Carla Caramella, Franca Ferrari The aim of the present work was the development of a powder formulation for the delivery of manuka honey (MH) bioactive components in the treatment of chronic skin ulcers. In particular pectin (PEC)/chitosan glutamate (CS)/hyaluronic acid (HA) mini-capsules were obtained by inverse ionotropic gelation in presence of ...
Source: International Journal of Pharmaceutics - November 24, 2016 Category: Drugs & Pharmacology Source Type: research

Spherical agglomerates of lactose with enhanced mechanical properties
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Dejan Lamešić, Odon Planinšek, Zoran Lavrič, Ilija Ilić The aim of this study was to prepare spherical agglomerates of lactose and to evaluate their physicochemical properties, flow properties, particle friability and compaction properties, and to compare them to commercially available types of lactose for direct compression (spray-dried, granulated and anhydrous β-lactose). Porous spherical agglomerates of α-lactose monohydrate with radially arranged prism-like primary parti...
Source: International Journal of Pharmaceutics - November 22, 2016 Category: Drugs & Pharmacology Source Type: research

Microencapsulated SLN: An innovative strategy for pulmonary protein delivery
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Diana P Gaspar, Carmen Serra, Paulo R Lino, Lídia Gonçalves, Pablo Taboada, Carmen Remuñán-López, António J Almeida Associating protein with nanoparticles is an interesting strategy to improve their bioavailability and biological activity. Solid lipid nanoparticles (SLN) have been sought as carriers for therapeutic proteins transport to the lung epithelium. Nevertheless, because of their low inertia, nanoparticles intended for pulmonary application usually escap...
Source: International Journal of Pharmaceutics - November 21, 2016 Category: Drugs & Pharmacology Source Type: research

Lipid vesicular nanocarrier: Quick encapsulation efficiency determination and transcutaneous application
Publication date: 10 January 2017 Source:International Journal of Pharmaceutics, Volume 516, Issues 1–2 Author(s): Yibang Zhang, Weibeng Ng, Xue Feng, Fangying Cao, Huaxi Xu Nanoscale delivery systems have been widely investigated to overcome the penetration barrier of stratum corneum for effective transcutaneous application. The aim of this study is the development of effective vesicular formulations of ovalbumin and saponin which are able to promote penetration through the skin layers. Three kinds of vesicular formulations have been investigated as carriers, including liposomes, transfersomes and ethosomes, in whi...
Source: International Journal of Pharmaceutics - November 21, 2016 Category: Drugs & Pharmacology Source Type: research

Polymeric nanospheres for topical delivery of vitamin D3
This study investigates the potential application of polymeric nanospheres (known as TyroSpheres) as a formulation carrier for topical delivery of cholecalciferol (i.e., Vitamin D3, VD3) with the goal to improve the skin delivery and stability of VD3. High drug loading and binding efficiencies were obtained for VD3 when loaded in TyroSpheres. VD3 was released from TyroSpheres in a sustained manner and was delivered across the stratum corneum, which occurred independent of the initial drug loading. An ex vivo skin distribution study showed that TyroSphere formulations delivered 3–10μg of active into the epidermis w...
Source: International Journal of Pharmaceutics - November 19, 2016 Category: Drugs & Pharmacology Source Type: research