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International Journal of Pharmaceutics

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https://www.readbyqxmd.com/read/27915009/exploring-gastrointestinal-variables-affecting-drug-and-formulation-behavior-methodologies-challenges-and-opportunities
#1
REVIEW
Bart Hens, Maura Corsetti, Robin Spiller, Luca Marciani, Tim Vanuytsel, Jan Tack, Arjang Talattof, Gordon L Amidon, Mirko Koziolek, Werner Weitschies, Clive G Wilson, Roelof J Bennink, Joachim Brouwers, Patrick Augustijns
Various gastrointestinal (GI) factors affect drug and formulation behavior after oral administration, including GI transfer, motility, pH and GI fluid volume and composition. An in-depth understanding of these physiological and anatomical variables is critical for a continued progress in oral drug development. In this review, different methodologies (invasive versus non-invasive) to explore the impact of physiological variables on formulation behavior in the human GI tract are presented, revealing their strengths and limitations...
November 30, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27915008/sensitivity-analysis-of-a-pharmaceutical-tablet-production-process-from-the-control-engineering-perspective
#2
Jakob Rehrl, Arlin Gruber, Johannes G Khinast, Martin Horn
This paper presents a sensitivity analysis of a pharmaceutical direct compaction process. Sensitivity analysis is an important tool for gaining valuable process insights and designing a process control concept. Examining its results in a systematic manner makes it possible to assign actuating signals to controlled variables. This paper presents mathematical models for individual unit operations, on which the sensitivity analysis is based. Two sensitivity analysis methods are outlined: (i) based on the so-called Sobol indices and (ii) based on the steady-state gains and the frequency response of the proposed plant model...
November 30, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27915007/effect-of-the-oral-administration-of-nanoencapsulated-quercetin-on-a-mouse-model-of-alzheimer-s-disease
#3
Lina Clara Gayoso E Almendra Ibiapina, 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 quercetin in zein nanoparticles (NPQ), that significantly improves the oral absorption and bioavailability of the flavonoid, as potential oral treatment for AD. For this purpose, SAMP8 mice were orally treated for two months with either NPQ (25mg/kg every 48hours) or a solution of quercetin (Q; 25mg/kg daily)...
November 30, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27915006/predicting-optimal-wet-granulation-parameters-for-extrusion-spheronisation-of-pharmaceutical-pellets-using-a-mixer-torque-rheometer
#4
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 torque produced during wet massing in the MTR, L/S(maxT), was 0.8 for the low solubility APIs, which decreased to 0...
November 30, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27913241/evaluation-of-highly-branched-cyclic-dextrin-in-inhalable-particles-of-combined-antibiotics-for-the-pulmonary-delivery-of-anti-tuberculosis-drugs
#5
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 of two anti-tuberculosis drugs (isoniazid and rifampicin). Fine particles of untreated active pharmaceutical ingredients (APIs) and combination products using excipients were prepared by spray drying...
November 29, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27913240/activity-of-vancomycin-release-from-bioinspired-coatings-of-hydroxyapatite-or-tio2-nanotubes
#6
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 obtained by electrochemical anodization. Surface morphology, compositional and structural data confirm the incorporation of vancomycin into the layers and drug release profiles for vancomycin evaluate their release ability...
November 29, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27913239/strategy-for-assessment-of-the-colloidal-and-biological-stability-of-h1n1-influenza-a-viruses
#7
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 remaining biological activity of H1N1 influenza viruses under various conditions after an incubation of 40 days...
November 29, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27908629/evaluation-of-the-cytotoxicity-genotoxicity-and-mucus-permeation-capacity-of-several-surface-modified-poly-anhydride-nanoparticles-designed-for-oral-drug-delivery
#8
T Iglesias, A López de Cerain, Juan Manuel 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 the harsh environment, reduce the drug's toxicity and, by virtue of surface modification, to enhance or reduce their mucus permeability and the bioadhesion to specific target cells...
November 28, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27899320/preparation-characterization-and-in-vivo-pharmacokinetic-study-of-pvp-modified-oleanolic-acid-liposomes
#9
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 dispersion method coupled with sonication. Several properties of the PVP-modified OA liposomes (PVPOALs), including surface morphology, particle size, zeta potential and entrapment efficiency were extensively characterized...
November 27, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27894988/experimental-observations-and-dissipative-particle-dynamic-simulations-on-microstructures-of-ph-sensitive-polymer-containing-amorphous-solid-dispersions
#10
Mengchi Sun, Bingyu Li, Yanchun Li, Yangdan Liu, Qi Liu, Hailun Jiang, Zhonggui He, Yongshan Zhao, Jin Sun
Amorphous solid dispersion (ASD) technique is an effective strategy to increase the dissolution rate of poorly soluble drugs. However, it is inherently unstable, and the molecular basis for achieving kinetic stability is not well understood. 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...
November 25, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27894987/a-novel-approach-for-dry-powder-coating-of-pellets-with-ethylcellulose-part-i-evaluation-of-film-formulation-and-process-set-up
#11
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 reach the target temperature a liquid plasticizer, oleic acid (OA), was introduced in the coating formulation...
November 25, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27890621/nasal-drug-delivery-design-of-a-novel-mucoadhesive-and-in-situ-gelling-polymer
#12
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 mediated amide bond formation. The resulting conjugate was characterized with respect to the amount of coupled ligand, the in situ gelling behavior, mucoadhesive properties and stability towards oxidation...
November 24, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27889588/preparation-and-properties-evaluation-of-a-novel-ph-sensitive-liposomes-based-on-imidazole-modified-cholesterol-derivatives
#13
Liang Ju, Fang Cailin, Wu Wenlan, Yu Pinghua, Gao Jiayu, Li Junbo
As a new kind of drug carries, pH-sensitive liposomes have been widely studied in tumor therapy for their advantages of target ability and sustained-release. Here, we synthesized a pH-sensitive material, N-(3-Aminopropyl)imidazole-cholesterol (IM-Chol) and prepared a novel pH-sensitive liposomes using IM-Chol and phosphatidylcholine. IM-Chol was synthesized through amidation reaction between the amino group of N-(3-Aminopropyl)imidazole and acyl chloride group of cholesteryl chloroformate in a weak base solution...
November 23, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27889587/pharmaceutical-technology-can-turn-a-traditional-drug-dexamethasone-into-a-first-line-ocular-medicine-a-global-perspective-and-future-trends
#14
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 dexamethasone delivery systems have been designed in an attempt to achieve sustained release and targeting. The FDA has approved dexamethasone implants for the treatment of macular edema secondary to retinal vein occlusion and posterior segment noninfectious uveitis...
November 23, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27889586/surfactant-effect-on-the-physicochemical-characteristics-of-cationic-solid-lipid-nanoparticles
#15
Chiara Botto, Nicolò Mauro, Erika Amore, Elisabetta Martorana, Gaetano Giammona, Maria Luisa Bondì
Solid lipid nanoparticles (SLNs) may be considered as a new approach for therapeutics for many diseases. In addition to drug delivery, their use as non-viral vectors for gene delivery can be obtained by including cationic lipids, which provide a positive surface potential that favors binding to the nucleic acids as DNA, siRNA, miRNA, etc. In fact, the addition of cationic surfactants is indispensable for obtaining nanoparticles with surface positive charge. 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...
November 23, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27887884/calcium-phosphate-nanoparticles-functionalized-with-alendronate-conjugated-polyethylene-glycol-peg-for-the-treatment-of-bone-metastasis
#16
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-conjugated poly (ethylene glycol) 2000 material (ALN-PEG2k-ALN). The ALN-PEG2k-ALN was characterized using (1)H NMR and (31)P NMR and FTIR...
November 22, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27887883/nanoprecipitated-catestatin-released-from-pharmacologically-active-microcarriers-pams-exerts-pro-survival-effects-on-msc
#17
C Angotti, M C Venier-Julienne, C Penna, S Femminò, L Sindji, C Paniagua, C N Montero-Menei, P Pagliaro
Catestatin (CST), a fragment of Chromogranin-A, exerts angiogenic, arteriogenic, vasculogenic and cardioprotective effects. CST is a very promising agent for revascularization purposes, in "NO-OPTION" patients. However, peptides have a very short half-life after administration and must be conveniently protected. Fibronectin-coated pharmacologically active microcarriers (FN-PAM), are biodegradable and biocompatible polymeric microspheres that can convey mesenchymal stem cell (MSCs) and therapeutic proteins delivered in a prolonged manner...
November 22, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27884715/improved-sustained-release-of-antigen-from-immunostimulatory-dna-hydrogel-by-electrostatic-interaction-with-chitosan
#18
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 enhance the potency of the sDNA hydrogel via improvement of its sustained release property, we selected chitosan, a biocompatible cationic polymer which electrostatically interacts with DNA, and mixed it with the sDNA hydrogel...
November 21, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27884714/carrier-particle-design-for-stabilization-and-isolation-of-drug-nanoparticles
#19
Teresa Tierney, Katalin Bodnár, Åke Rasmuson, Sarah Hudson
Nanoparticles of poorly water-soluble drugs were prepared in suspension via antisolvent precipitation in order to improve their dissolution behaviour. Insoluble, surface-functionalized, micron-range, clay carrier particles were employed for the dual purpose of stabilizing the nanoparticles in suspended state, and facilitating their unhindered isolation to solid state; often a challenging step in nanoparticle production. The carrier particles, which were functionalized with an optimal level of cationic polymer (protamine), attracted negatively-charged nanoparticles to their surface as a uniform and segregated nanoparticle layer, at drug loadings up to 9% w/w...
November 21, 2016: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/27884713/paclitaxel-loaded-polymeric-nanoparticles-combined-with-chronomodulated-chemotherapy-on-lung-cancer-in-vitro-and-in-vivo-evaluation
#20
Jie Hu, Shaozhi Fu, Qiuxia Peng, YunWei Han, Jie Xie, Ning Zan, Yue Chen, Juan Fan
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-dependent effect...
November 21, 2016: International Journal of Pharmaceutics
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