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International Journal of Pharmaceutics

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https://www.readbyqxmd.com/read/29343428/development-and-pre-clinical-evaluation-in-the-swine-model-of-a-mucosal-vaccine-tablet-for-human-influenza-viruses-a-proof-of-concept-study
#1
V Busignies, G Simon, G Mollereau, O Bourry, V Mazel, M Rosa-Calatrava, P Tchoreloff
Liquid vaccine formulations present some disadvantages such as stability problems, cold chain requirement or administration by trained personnel. Vaccine formulated as tablets would present a wide range of progress such as an increase stability that would facilitate the administration, the distribution and the storage of vaccine formulations. This work investigates the possibility to develop a mucosal tablet vaccine for human influenza viruses. The tablets were tested in vitro for biological efficacy and stability and in vivo in swine as a model for influenza A virus immunity...
January 14, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29341921/computational-hydrodynamic-comparison-of-a-mini-vessel-and-a-usp-2-dissolution-testing-system-to-predict-the-dynamic-operating-conditions-for-similarity-of-dissolution-performance
#2
Bing Wang, Gerard Bredael, Piero M Armenante
The hydrodynamics characteristics of a mini vessel and a USP 2 dissolution testing system were obtained and compared to predict the tablet-liquid mass transfer coefficient from velocity distributions near the tablet and establish the dynamic operating conditions under which dissolution in mini vessels could be conducted to generate concentration profiles similar to those in the USP 2. Velocity profiles were obtained experimentally using Particle Image Velocimetry (PIV). Computational Fluid Dynamics (CFD) was used to predict the velocity distribution and strain rate around a model tablet...
January 13, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29341920/effect-of-structural-factors-on-release-profiles-of-camptothecin-from-block-copolymer-conjugates-with-high-load-of-drug
#3
Andrzej Plichta, Sebastian Kowalczyk, Ewa Olędzka, Marcin Sobczak, Marcin Strawski
The aim of the present work was the synthesis and study the kinetics and profiles of camptothecin (CPT) release form block co- and ter-polymer conjugates comprising polylactide (PLA) segments and CPT moieties, structurally diverse by degrees of branching, content of D-PLA units and poly(ethylene glycol) methyl ether methacrylate (PEGMA). Six PLA, non-toxic macroinitiators (MIs), terminated with α-bromoester were synthesized. MIs were subjected to polymerization of CPT methacrylic derivative (CPTMA) with PEGMA at various ratios...
January 13, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29341919/performance-of-an-acoustically-mixed-pharmaceutical-dry-powder-delivered-from-a-novel-inhaler
#4
Ryoma Tanaka, Naoyuki Takahashi, Yasuaki Nakamura, Yusuke Hattori, Kazuhide Ashizawa, Makoto Otsuka
No abstract text is available yet for this article.
January 13, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29341918/asymmetric-flow-field-flow-fractionation-for-the-characterization-of-globule-size-distribution-in-complex-formulations-a-cyclosporine-ophthalmic-emulsion-case
#5
Haiou Qu, Jiang Wang, Yong Wu, Jiwen Zheng, Yellela S R Krishnaiah, Mohammad Absar, Stephanie Choi, Muhammad Ashraf, Celia N Cruz, Xiaoming Xu
Commonly used characterization techniques such as cryogenic-transmission electron microscopy (cryo-TEM) and batch-mode dynamic light scattering (DLS) are either time consuming or unable to offer high resolution to discern the poly-dispersity of complex drug products like cyclosporine ophthalmic emulsions. Here, a size-based separation and characterization method for globule size distribution using an asymmetric flow field flow fractionation (AF4) is reported for comparative assessment of cyclosporine ophthalmic emulsion drug products (model formulation) with a wide size span and poly-dispersity...
January 13, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29341917/a-novel-method-for-the-production-of-core-shell-microparticles-by-inverse-gelation-optimized-with-artificial-intelligent-tools
#6
Rosalia Rodríguez-Dorado, Mariana Landín, Ayça Altai, Paola Russo, Rita P Aquino, Pasquale Del Gaudio
Numerous studies have been focused on hydrophobic compounds encapsulation as oils. In fact, oils can provide numerous health benefits as synergic ingredient combined with other hydrophobic active ingredients. However, stable microparticles for pharmaceutical purposes are difficult to achieve when commonly techniques are used. In this work, sunflower oil was encapsulated in calcium-alginate capsules by prilling technique in co-axial configuration. Core-shell beads were produced by inverse gelation directly at the nozzle using w/o emulsion containing aqueous calcium chloride solution in sunflower oil pumped through the inner nozzle while an aqueous alginate solution, coming out from the annular nozzle, produced the bead shell...
January 13, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29341916/effects-of-surfactant-based-permeation-enhancers-on-mannitol-permeability-histology-and-electrogenic-ion-transport-responses-in-excised-rat-colonic-mucosae
#7
Sam Maher, Joanne Heade, Fiona McCartney, Seona Waters, Sinéad B Bleiel, David J Brayden
Surfactant-based intestinal permeation enhancers (PEs) are constituents of several oral macromolecule formulations in clinical trials. This study examined the interaction of a test panel of surfactant-based PEs with isolated rat colonic mucosae mounted in Ussing chambers in an attempt to determine if increases in transepithelial permeability can be separated from induction of mucosal perturbation. The aim was to assess the effects of PEs on (i) apparent permeability coefficient (Papp) of [14C]-mannitol on (ii) histology score and (iii) short-circuit current (ΔIsc) responses to a cholinomimetic (carbachol, CCh)...
January 13, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29341915/influence-of-ligands-property-and-particle-size-of-gold-nanoparticles-on-the-protein-adsorption-and-corresponding-targeting-ability
#8
Wei Xiao, Jingyuan Xiong, Shuang Zhang, Yang Xiong, Huajin Zhang, Huile Gao
Nanoparticulated vesicles were widely used for carriers of drugs and imaging probes. To improve the targeting delivery efficiency of these vesicles, ligands were often functionalized onto their surfaces. However, the interaction between vesicles and plasma proteins may cover the ligands and hinder the targeting delivery. It is important to address the potential influence of ligands modification on plasma protein adsorption and the following targeting delivery. In this study, two common used ligands were chosen as the model: transferrin and RGD peptide...
January 13, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29341914/is-there-a-correlation-between-the-glass-forming-ability-of-a-drug-and-its-supersaturation-propensity
#9
Lasse Ingerslev Blaabjerg, Eleanor Lindenberg, Korbinian Löbmann, Holger Grohganz, Thomas Rades
The use of an enabling formulation technique, such as amorphization of a poorly water-soluble crystalline drug, can result in supersaturation with respect to the crystalline form of the drug and thus potentially in a higher degree of absorption after oral administration. The ease with which such drugs can be amorphized is known as their glass forming ability (GFA). In this study, a potential correlation between GFA and supersaturation propensity is investigated. The GFA of 23 different drugs was determined by melt quenching or milling the crystalline drugs to obtain their respective amorphous forms...
January 13, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29341913/characterisation-of-pore-structures-of-pharmaceutical-tablets-a-review
#10
REVIEW
Daniel Markl, Alexa Strobel, Rüdiger Schlossnikl, Johan Bøtker, Prince Bawuah, Cathy Ridgway, Jukka Rantanen, Thomas Rades, Patrick Gane, Kai-Erik Peiponen, J Axel Zeitler
Traditionally, the development of a new solid dosage form is formulation-driven and less focus is put on the design of a specific microstructure for the drug delivery system. However, the compaction process particularly impacts the microstructure, or more precisely, the pore architecture in a pharmaceutical tablet. Besides the formulation, the pore structure is a major contributor to the overall performance of oral solid dosage forms as it directly affects the liquid uptake rate, which is the very first step of the dissolution process...
January 13, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29341912/quantitative-estimation-of-phenytoin-sodium-disproportionation-in-the-formulations-using-vibration-spectroscopies-and-multivariate-methodologies
#11
Sathish Dharani, Ziyaur Rahman, Sogra F Barakh Ali, Hamideh Afrooz, Mansoor A Khan
Phenytoin sodium (PS) has tendency to convert to its base form; phenytoin base (PHT) during manufacturing, packaging, shelf life and in-use conditions that can influence its clinical performance. The objective of the present work was to develop a non-destructive, quick and easy analytical method for quantification of PHT in the drug product. A formulation was prepared containing the excipients present in the commercial capsule formulation of PS. Formulation containing either 100% PHT or PS was prepared and these formulations were mixed in different proportion to achieve 0-100% PHT matrices...
January 13, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29341911/an-efficient-pegylated-gene-delivery-system-with-improved-targeting-synergism-between-octaarginine-and-a-fusogenic-peptide
#12
Ikramy A Khalil, Hideyoshi Harashima
Because of their ability to translocate different cargos into cells, arginine-rich cell penetrating peptides (CPPs) are promising vehicles for drug and gene delivery. The use of CPP-based carriers, however, is hampered by the lack of specificity and by interactions with negative serum components. Polyethylene glycol (PEG) is used to decrease such non-specific interactions, albeit its use is associated with reduced transfection efficiency. In this study, we describe the development of PEGylated CPP-based gene carrier with an improved targeting and a high transfection activity...
January 13, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29341910/isomalt-and-its-diastereomer-mixtures-as-stabilizing-excipients-with-freeze-dried-lactate-dehydrogenase
#13
Anna-Kaisa Tuderman, Clare J Strachan, Anne M Juppo
The purpose of this research was to study isomalt as a protein-stabilizing excipient with lactate dehydrogenase (LDH) during freeze-drying and subsequent storage and compare it to sucrose, a standard freeze-drying excipient. Four different diastereomer mixtures of isomalt were studied. The stability of the protein was studied with a spectrophotometric enzyme activity test and circular dichroism after freeze-drying and after 21 days of storage at 16% RH. Physical stability was analyzed with differential scanning calorimetry and Karl Fischer titration...
January 13, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29341909/nanogel-dfo-conjugates-as-a-model-to-investigate-pharmacokinetics-biodistribution-and-iron-chelation-in-vivo
#14
Yan Wang, Zhi Liu, Tien-Min Lin, Shaurya Chanana, May P Xiong
Deferoxamine (DFO) to treat iron overload (IO) has been limited by toxicity issues and short circulation times and it would be desirable to prolong circulation to improve non-transferrin bound iron (NTBI) chelation. In addition, DFO is currently unable to efficiently target the large pool of iron in the liver and spleen. Nanogel-Deferoxamine conjugates (NG-DFO) can prove useful as a model to investigate the pharmacokinetic (PK) properties and biodistribution (BD) behavior of iron-chelating macromolecules and their overall effect on serum ferritin levels...
January 13, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29341908/induction-of-au-methotrexate-conjugates-by-sugar-molecules-production-assembly-mechanism-and-bioassay-studies
#15
Wei-Yuan Wang, Xiu-Fen Zhao, Xiao-Han Ju, Ping Liu, Jing Li, Ya-Wen Tang, Shu-Ping Li, Xiao-Dong Li, Fu-Gui Song
Au-methotrexate (Au-MTX) conjugates induced by sugar molecules were produced by a simple, one-pot, hydrothermal growth method. Herein, the Au(III)-MTX complexes were used as the precursors to form Au-MTX conjugates. Addition of different types of sugar molecules with abundant hydroxyl groups resulted in the formation of Au-MTX conjugates featuring distinct characteristics that could be explained by the diverse capping mechanisms of sugar molecules. That is, the instant-capping mechanism of glucose favored the generation of peanut-like Au-MTX conjugates with high colloidal stability while the post-capping mechanism of dextran and sucrose resulted in the production of Au-MTX conjugates featuring excellent near-infrared (NIR) optical properties with a long-wavelength plasmon resonance near 630-760 nm...
January 13, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29341907/molecular-level-elucidation-of-saccharin-assisted-rapid-dissolution-and-high-supersaturation-level-of-drug-from-eudragit%C3%A2-e-solid-dispersion
#16
Keisuke Ueda, Harunobu Kanaya, Kenjirou Higashi, Keiji Yamamoto, Kunikazu Moribe
In this work, the effect of saccharin (SAC) addition on the dissolution and supersaturation level of phenytoin (PHT)/Eudragit® E (EUD-E) solid dispersion (SD) at neutral pH was examined. The PHT/EUD-E SD showed a much slower dissolution of PHT compared to the PHT/EUD-E/SAC SD. EUD-E formed a gel layer after the dispersion of the PHT/EUD-E SD into an aqueous medium, resulting in a slow dissolution of PHT. Pre-dissolving SAC in the aqueous medium significantly improved the dissolution of the PHT/EUD-E SD. Solid-state 13C NMR measurements showed an ionic interaction between the tertiary amino group of EUD-E and the amide group of SAC in the EUD-E gel layer...
January 13, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29339249/semifluorinated-alkane-based-systems-for-enhanced-corneal-penetration-of-poorly-soluble-drugs
#17
Priyanka Agarwal, Dieter Scherer, Bernhard Günther, Ilva D Rupenthal
Semifluorinated alkanes (SFAs) are amphiphilic liquids that can dissolve hydrophobic drugs to form clear solutions. This study evaluated the potential of two SFAs to act as vehicle for topical ocular drug delivery. After confirming ocular safety, an ex vivo corneal penetration model was developed to determine drug distribution and corneal bioavailability. Hydrophobic dye distribution in the different corneal layers was visualised under a confocal microscope. Corneal bioavailability of cyclosporine A (CsA) dissolved in perfluorobutylpentane (F4H5) or perfluorohexyloctane (F6H8) was compared to commercially available CsA ophthalmic emulsions, Restasis® and Ikervis®...
January 12, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29339248/recent-trends-of-nanomedicinal-approaches-in-clinics
#18
REVIEW
Fahima Dilnawaz, Sarbari Acharya, Sanjeeb Kumar Sahoo
Nanotechnology has become the indispensable cutting edge science providing solutions to many problems associated with human being. The application of nanotechnology associated to human health "nanomedicine" has revolutionized the drug delivery system by providing improved pharmacological and therapeutic properties of drugs. These advantageous effects of drug loaded nanocarrier systems are embraced by the pharmaceutical industries for the development of different effective nanocarriers. Currently, several drug loaded nanoformulations are approved by the Food and Drug Administration (FDA), and some of them are undergoing clinical trials for the human use...
January 12, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29339247/self-emulsifying-peptide-drug-delivery-systems-how-to-make-them-highly-mucus-permeating
#19
Janine Griesser, Gergely Hetényi, Hatice Kadas, Frédéric Demarne, Vincent Jannin, Andreas Bernkop-Schnürch
AIM: It was the aim of this study to evaluate the mucus permeating properties of self-emulsifying drug delivery systems (SEDDS) exhibiting different size and zeta potential. METHODS: Various SEDDS were prepared and characterized regarding droplet size, zeta potential and stability. Desmopressin was incorporated as model peptide drug and log P (SEDDS/water) was determined. Thereafter, mucus permeation studies with freshly isolated porcine mucus via Transwell method were performed...
January 12, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29337185/proliposome-tablets-manufactured-using-a-slurry-driven-lipid-enriched-powders-development-characterization-and-stability-evaluation
#20
Iftikhar Khan, Sakib Yousaf, Sneha Subramanian, Mohamed Albed Alhnan, Waqar Ahmed, Abdelbary Elhissi
Proliposome powders were prepared via a slurry method using sorbitol or D-mannitol as carbohydrate carriers in 1:10 or 1:15 w/w lipid phase to carrier ratios. Soya phosphatidylcholine (SPC) and cholesterol were employed as a lipid phase and Beclometasone dipropionate (BDP) was incorporated as a model drug. Direct compaction using a Minipress was applied on the lipid-enriched powder in order to manufacture proliposome tablets. Sorbitol-based proliposome tablets in a 1:15 w/w ratio were found to be the best formulation as it exhibited excellent powder flowability with an angle of repose of 25...
January 11, 2018: International Journal of Pharmaceutics
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