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High-throughput screening and scale-up of cocrystals using resonant acoustic mixing
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Karthik Nagapudi, Evelyn Yanez Umanzor, Colin Masui This paper explores the effectiveness of resonant acoustic mixing RAM for screening and scale up of cocrystals. 16 cocrystal systems were selected as test cases based on previous literature precedent. A 96 well plate set up in conjunction with zirconia beads was used for cocrystal screening using RAM. A success rate of 80% was obtained in the screen for plates containing solvent or solvent plus Zirconia beads. A proof of concept production of hydrated an...
Source: International Journal of Pharmaceutics - March 1, 2017 Category: Drugs & Pharmacology Source Type: research

New gonadotropin-releasing hormone glycolipids with direct antiproliferative activity and gonadotropin-releasing potency
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Pegah Varamini, Friederike M. Mansfeld, Ashwini Kumar Giddam, Frederik Steyn, Istvan TothGraphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - March 1, 2017 Category: Drugs & Pharmacology Source Type: research

Design of novel injectable in-situ forming scaffolds for non-surgical treatment of periapical lesions: In-vitro and in-vivo evaluation
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Rehab N. Shamma, Nermeen A. Elkasabgy, Azza A. Mahmoud, Shaimaa I. Gawdat, Mohamed M. Kataia, Mohamed A. Abdel Hamid Periapical lesions are considered one of the common pathological conditions affecting alveolar bone. The primary focus of this study was to investigate the effectiveness of formulating an injectable in-situ forming scaffold-loaded with risedronate (bone resorption inhibitor) and with lornoxicam (anti-inflammatory drug) for the non-surgical treatment of periapical lesions. The scaffolds were...
Source: International Journal of Pharmaceutics - February 28, 2017 Category: Drugs & Pharmacology Source Type: research

Physical key properties of antibiotic-free, PLGA/HPMC-based in-situ forming implants for local periodontitis treatment
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): K. Agossa, M. Lizambard, T. Rongthong, E. Delcourt-Debruyne, J. Siepmann, F. Siepmann In-situ forming implants (ISFI) offer an interesting potential for the treatment of periodontitis, allowing for time-controlled drug release directly at the site of action (which is difficult to reach). For this purpose, ISFI loaded with antibiotics have been reported in the literature. But the use of antibiotic drugs at low doses over prolonged periods of time can lead to the development of bacterial resistances. This r...
Source: International Journal of Pharmaceutics - February 28, 2017 Category: Drugs & Pharmacology Source Type: research

Computational fluid dynamics (CFD) studies of a miniaturized dissolution system
In this study we used computational fluid dynamics to simulate and investigate the hydrodynamics in a novel miniaturized dissolution method for parenteral formulations. The dissolution method is based on a rotating disc system and uses a rotating sample reservoir which is separated from the remaining dissolution medium by a nylon screen. Sample reservoirs of two sizes were investigated (SR6 and SR8) and the hydrodynamic studies were performed at rotation rates of 100, 200 and 400rpm. The overall fluid flow was similar for all investigated cases, with a lateral upward spiraling motion and central downward motion in the form...
Source: International Journal of Pharmaceutics - February 26, 2017 Category: Drugs & Pharmacology Source Type: research

Patients ’ appropriateness, acceptability, usability and preferences for pharmaceutical preparations: Results from a literature review on clinical evidence
In conclusion, more interdisciplinary scientific efforts are required to develop and increase research in understanding patient needs and preferences. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 26, 2017 Category: Drugs & Pharmacology Source Type: research

Application of halloysite clay nanotubes as a pharmaceutical excipient
This study reports the development composite tablets based on 50wt.% of the drug loaded halloysite mixed with 45wt.% of microcrystalline cellulose. Powder flow and compressibility properties of halloysite (angle of repose, Carr’s index, Hausner ratio, Brittle Fracture Index, tensile strength) indicate that halloysite is an excellent tablet excipient. Halloysite tubes can also be filled with nifedipine with ca. 6wt.% loading efficiency and sustained release from the nanotubes. Tablets prepared with drug loaded halloysite allowed for almost zero order nifedipine release for up to 20h. Nifedipine trapped in the nanotube...
Source: International Journal of Pharmaceutics - February 24, 2017 Category: Drugs & Pharmacology Source Type: research

Cytotoxicity of polycations: Relationship of molecular weight and the hydrolytic theory of the mechanism of toxicity
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Bryn D. Monnery, Michael Wright, Rachel Cavill, Richard Hoogenboom, Sunil Shaunak, Joachim H.G. Steinke, Maya Thanou The mechanism of polycation cytotoxicity and the relationship to polymer molecular weight is poorly understood. To gain an insight into this important phenomenon a range of newly synthesised uniform (near monodisperse) linear polyethylenimines, commercially available poly(l-lysine)s and two commonly used PEI-based transfectants (broad 22kDa linear and 25kDa branched) were tested for their c...
Source: International Journal of Pharmaceutics - February 24, 2017 Category: Drugs & Pharmacology Source Type: research

Modulation mechanism of the stratum corneum structure during permeation of surfactant-based rigid and elastic vesicles
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Tomonobu Uchino, Ichiro Hatta, Yasunori Miyazaki, Tomoya Onai, Takuto Yamazaki, Fuyoko Sugiura, Yoshiyuki Kagawa We evaluated the interaction between human stratum corneum (SC) and surfactant-based rigid or elastic vesicles during permeation using synchrotron X-ray diffraction to obtain the mechanism action of surfactant-based vesicles for enhanced skin permeation. The effects of vesicle elasticity on the interaction with SC were also investigated. Changes in the small-angle X-ray diffraction peaks of the...
Source: International Journal of Pharmaceutics - February 24, 2017 Category: Drugs & Pharmacology Source Type: research

Improving the dissolution rate of hydrophobic drugs through encapsulation in porous lactose as a new biocompatible porous carrier
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Amirali Ebrahimi, Morteza Saffari, Timothy Langrish T he dissolution rates of indomethacin (IMC) and nifedipine (NIF) as poorly water-soluble model drugs have been significantly improved by encapsulating their molecules in the porous structure of engineered-particles of lactose as a new biocompatible porous carrier. The formulation method used in this study utilized a template-based spray-drying technique for in-situ production of porous lactose followed by two solvent-based drug-loading methods: (i) adso...
Source: International Journal of Pharmaceutics - February 24, 2017 Category: Drugs & Pharmacology Source Type: research

In situ hybrid nano drug delivery system (IHN-DDS) of antiretroviral drug for simultaneous targeting to multiple viral reservoirs: An in vivo proof of concept
In conclusion, IHN-DDS systems could be a promising approach for simultaneous multisite targeting and could provide therapeutic benefits in complete eradication of HIV infections. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 24, 2017 Category: Drugs & Pharmacology Source Type: research

In situ determination of the saturation solubility of nanocrystals of poorly soluble drugs for dermal application
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Miriam Colombo, Sven Staufenbiel, Eckart Rühl, Roland Bodmeier The aim of this study was to determine, in situ, the saturation solubility and dissolution rate of nanocrystals of three poorly water-soluble drugs for dermal application. The nanocrystals were prepared by wet bead milling. Their size could be controlled by various process parameters. The saturation solubility was measured in water or in the presence of surfactant at 32°C with a Sirius® inForm based on in situ UV–vis spectro...
Source: International Journal of Pharmaceutics - February 24, 2017 Category: Drugs & Pharmacology Source Type: research

An equation for the prediction of human skin permeability of neutral molecules, ions and ionic species
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Keda Zhang, Michael H. Abraham, Xiangli Liu Experimental values of permeability coefficients, as log Kp, of chemical compounds across human skin were collected by carefully screening the literature, and adjusted to 37°C for the effect of temperature. The values of log Kp for partially ionized acids and bases were separated into those for their neutral and ionic species, forming a total data set of 247 compounds and species (including 35 ionic species). The obtained log Kp values have been regressed ag...
Source: International Journal of Pharmaceutics - February 24, 2017 Category: Drugs & Pharmacology Source Type: research

Improving the dissolution properties of curcumin using dense gas antisolvent technology
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Firman Kurniawansyah, Lisa Quachie, Raffaella Mammucari, Neil R. Foster The dissolution properties of curcumin are notoriously poor and hinder its bioavailability. To improve its dissolution properties, curcumin has been formulated with methyl-β-cyclodextrin and polyvinylpyrrolidone by the atomized rapid injection solvent extraction (ARISE) system. The compounds were co-precipitated from organic solutions using carbon dioxide at 30°C and 95bar as the antisolvent. Curcumin formulations were also p...
Source: International Journal of Pharmaceutics - February 24, 2017 Category: Drugs & Pharmacology Source Type: research

Influence of preparation pathway on the glass forming ability
This study investigates the correlation of the GFA between these two pathways. Eighteen compounds were chosen and their GFA was investigated by determining the critical cooling rate and the minimal milling time. It was observed that drugs, which turned amorphous upon cooling from the melt at slow cooling rates also had a low minimal milling time and vice versa. It was found that the GFA of the studied set of drugs was inherent and independent of the preparation method. It can be concluded that a drug with low critical cooling rate will also have a low minimal milling time and is thus a good glass former. Graphical abstract...
Source: International Journal of Pharmaceutics - February 24, 2017 Category: Drugs & Pharmacology Source Type: research

Laser deposition of poly(3-hydroxybutyric acid-co-3-hydroxyvaleric acid) – lysozyme microspheres based coatings with anti-microbial properties
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): V. Grumezescu, A.M. Holban, L.E. Sima, M.B. Chiritoiu, G.N. Chiritoiu, A.M. Grumezescu, L. Ivan, F. Safciuc, F. Antohe, C. Florica, C.R. Luculescu, M.C. Chifiriuc, G. Socol The purpose of this study was to obtain, characterize and evaluate the cytotoxicity and antimicrobial activity of coatings based on poly(3-hydroxybutyric acid-co-3-hydroxyvaleric acid) – Lysozyme (P(3HB-3HV)/Lys) and P(3HB-3HV) – Polyethylene glycol – Lysozyme (P(3HB-3HV)/PEG/Lys) spheres prepared by Matrix Assisted P...
Source: International Journal of Pharmaceutics - February 24, 2017 Category: Drugs & Pharmacology Source Type: research

Parameters affecting the transscleral delivery of two positively charged proteins of comparable size
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Maria Aurora Grimaudo, Elena Tratta, Silvia Pescina, Cristina Padula, Patrizia Santi, Sara Nicoli Apart from molecular weight and net surface charge, there are other macromolecule-related factors that could, in principle, influence their diffusion across biological tissues, such as shape, conformability, water solubility and surface charge distribution. Lysozyme and cytochrome c, proteins with comparable molecular weight, isoelectric point and net surface charge in physiological conditions (approx. +7.8),...
Source: International Journal of Pharmaceutics - February 24, 2017 Category: Drugs & Pharmacology Source Type: research

Potential of single cationic amino acid molecule “Arginine” for stimulating oral absorption of insulin
In this study, we found that arginine is a key cationic amino acid for delivering insulin across intestinal epithelial barriers and hopefully accelerating the clinical development of oral insulin delivery systems. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 24, 2017 Category: Drugs & Pharmacology Source Type: research

Exosomes as novel bio-carriers for gene and drug delivery
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Xin-Chi Jiang, Jian-Qing Gao Clinical treatments have stalled in certain diseases due to a lack of proper therapeutic delivery systems. Recent studies have identified exosomes for their potential use as cell-free therapies, which may provide a novel mechanism for solving this problem. Exosomes are nanoscale extracellular vesicles that can transport rich cargos of proteins, lipids, DNA, and RNA. It is increasingly recognized that exosomes play a complex role in not only the physiological conditions but als...
Source: International Journal of Pharmaceutics - February 24, 2017 Category: Drugs & Pharmacology Source Type: research

Increased intestinal permeation and modulation of presystemic metabolism of resveratrol formulated into self-emulsifying drug delivery systems
In conclusion, our data suggests that oil-in-water nanoemulsions prepared from SEDDS dispersions of medium-chain lipids could be promising formulations for enhancing oral delivery of resveratrol. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 23, 2017 Category: Drugs & Pharmacology Source Type: research

Non-viral vectors based on magnetoplexes, lipoplexes and polyplexes for VEGF gene delivery into central nervous system cells
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Ilia Villate-Beitia, Gustavo Puras, Cristina Soto-Sánchez, Mireia Agirre, Edilberto Ojeda, Jon Zarate, Eduardo Fernández, José Luis Pedraz Nanotechnology based non-viral vectors hold great promise to deliver therapeutic genes into the central nervous system (CNS) in a safe and controlled way. Vascular endothelial growth factor (VEGF) is a potential therapeutic gene candidate for CNS disorders due to its specific roles in brain angiogenesis and neuroprotection. In this work, we elabora...
Source: International Journal of Pharmaceutics - February 23, 2017 Category: Drugs & Pharmacology Source Type: research

PEGylation prolongs the pulmonary retention of an anti-IL-17A Fab ’ antibody fragment after pulmonary delivery in three different species
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Danielle Freches, Harshad P. Patil, Maria Machado Franco, Catherine Uyttenhove, Sam Heywood, Rita Vanbever The PEGylation of antibody fragments has been shown to greatly prolong their residence time in the lungs in mice. The purpose of this research was to confirm the effect of PEGylation in higher animal species, that is, the rat and the rabbit. An anti-IL-17A Fab’ antibody fragment was conjugated to a two-armed 40kDa polyethylene glycol (PEG) via site-selective thiol PEGylation. PEGylation did not...
Source: International Journal of Pharmaceutics - February 23, 2017 Category: Drugs & Pharmacology Source Type: research

Effects of storage conditions on the stability of spray dried, inhalable bacteriophage powders
This study aimed to develop inhalable powders containing phages active against antibiotic-resistant Pseudomonas aeruginosa for pulmonary delivery. A Pseudomonas phage, PEV2, was spray dried into powder matrices comprising of trehalose (0–80%), mannitol (0–80%) and l-leucine (20%). The resulting powders were stored at various relative humidity (RH) conditions (0, 22 and 60% RH) at 4°C. The phage stability and in vitro aerosol performance of the phage powders were examined at the time of production and after 1, 3 and 12 months storage. After spray drying, a total of 1.3 log titer reduction in phage was observ...
Source: International Journal of Pharmaceutics - February 23, 2017 Category: Drugs & Pharmacology Source Type: research

Design and evaluation of antibiotic releasing self- assembled scaffolds at room temperature using biodegradable polymer particles
Publication date: 30 March 2017 Source:International Journal of Pharmaceutics, Volume 520, Issues 1–2 Author(s): Prasad Admane, Jatin Gupta, Ancy I.J., Robin Kumar, Amulya K. Panda Biodegradable polymer-based drug-eluting implants offer many advantages such as predictable drug release kinetics, safety, and acceptable drug loading under ambient conditions. Herein, we describe fabrication and evaluation of antibiotic loaded scaffolds for localized delivery and tissue engineering applications. PDLLA particles entrapping gentamycin were formulated using solvent evaporation method and used for scaffold fabrication. Optim...
Source: International Journal of Pharmaceutics - February 20, 2017 Category: Drugs & Pharmacology Source Type: research

Multiwalled carbon nanotubes for drug delivery: Efficiency related to length and incubation time
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Niccolò Sciortino, Stefano Fedeli, Paolo Paoli, Alberto Brandi, Paola Chiarugi, Mirko Severi, Stefano Cicchi Batches of oxidized multiwalled carbon nanotubes differing in length were adopted to prepare two drug delivery systems (DDS) loaded with doxorubicin. The different internalization of the two batches, verified by atomic emission spectroscopy onto cell lysates, was also confirmed by the different toxicity of the same DDS loaded with doxorubicin. In vitro experiments evidenced, after 48h of inc...
Source: International Journal of Pharmaceutics - February 20, 2017 Category: Drugs & Pharmacology Source Type: research

Influence of peptide dendrimers and sonophoresis on the transdermal delivery of ketoprofen
This study demonstrates that arginine terminated peptide dendrimers combined with sonophoresis can effectively improve the transdermal permeation of ketoprofen. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 20, 2017 Category: Drugs & Pharmacology Source Type: research

A single microfluidic chip with dual surface properties for protein drug delivery
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Mehrdad Bokharaei, Katayoun Saatchi, Urs O. Häfeli Principles of double emulsion generation were incorporated in a glass microfluidic chip fabricated with two different surface properties in order to produce protein loaded polymer microspheres. The microspheres were produced by integrating two microfluidic flow focusing systems and a multi-step droplet splitting and mixing system into one chip. The chip consists of a hydrophobic and a hydrophilic section with two different heights, 12μm and 45μ...
Source: International Journal of Pharmaceutics - February 20, 2017 Category: Drugs & Pharmacology Source Type: research

Development and in vivo evaluation of an innovative “Hydrochlorothiazide-in Cyclodextrins-in Solid Lipid Nanoparticles” formulation with sustained release and enhanced oral bioavailability for potential hypertension treatment in pediatrics
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Marzia Cirri, Natascia Mennini, Francesca Maestrelli, Paola Mura, Carla Ghelardini, Lorenzo di Cesare Mannelli An innovative pediatric oral formulation of hydrochlorothiazide (HCT) (2mg/mL), endowed with improved bioavailability and sustained release properties and suitable for the hypertension treatment in pediatric patients, was developed by combining the drug-cyclodextrin complexation and the incorporation of the complex into Solid Lipid Nanoparticles (SLN). Precirol®ATO5-based SLN, with two differ...
Source: International Journal of Pharmaceutics - February 20, 2017 Category: Drugs & Pharmacology Source Type: research

Comparison of the physical characteristics of monodisperse non-ionic surfactant vesicles (NISV) prepared using different manufacturing methods
In this study, we have compared the physical characteristics of NISV prepared using two conventional methods (thin-film hydration method and heating method) with a recently introduced microfluidic method. The resulting particles from these methods were assessed for their physical characteristics and in vitro cytotoxicity. Through microfluidics, nano-sized NISV were prepared in seconds, through rapid and controlled mixing of two miscible phases (lipids dissolved in alcohol and an aqueous medium) in a microchannel, without the need of a size reduction step, as required for the conventional methods. Stability studies over two...
Source: International Journal of Pharmaceutics - February 20, 2017 Category: Drugs & Pharmacology Source Type: research

Nano-encapsulation of a novel anti-Ran-GTPase peptide for blockade of regulator of chromosome condensation 1 (RCC1) function in MDA-MB-231 breast cancer cells
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Yusuf A. Haggag, Kyle B. Matchett, El-Habib Dakir, Paul Buchanan, Mohammed A. Osman, Sanaa A. Elgizawy, Mohamed El-Tanani, Ahmed M. Faheem, Paul A. McCarron Ran is a small ras-related GTPase and is highly expressed in aggressive breast carcinoma. Overexpression induces malignant transformation and drives metastatic growth. We have designed a novel series of anti-Ran-GTPase peptides, which prevents Ran hydrolysis and activation, and although they display effectiveness in silico, peptide activity is subopti...
Source: International Journal of Pharmaceutics - February 20, 2017 Category: Drugs & Pharmacology Source Type: research

Artificial neural network modelling of continuous wet granulation using a twin-screw extruder
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Saeed Shirazian, Manuel Kuhs, Shaza Darwish, Denise Croker, Gavin M. Walker Computational modelling of twin-screw granulation was conducted by using an artificial neural network (ANN) approach. Various ANN configurations were considered with changing hidden layers, nodes and activation functions to determine the optimum model for the prediction of the process. The neural networks were trained using experimental data obtained for granulation of pure microcrystalline cellulose using a 12mm twin-screw extrud...
Source: International Journal of Pharmaceutics - February 20, 2017 Category: Drugs & Pharmacology Source Type: research

Successful application of large microneedle patches by human volunteers
We describe, for the first time, the design, production and evaluation of large microneedle patches. Such systems, based on 16 individual microneedle arrays (needle height 600μm), were prepared from aqueous blends of 15% w/w Gantrez® S97 and 7.5% w/w poly(ethyleneglycol) 10,000Da. Ester-based crosslinking was confirmed by FTIR and mechanical strength was good. Insertion depths in a validated skin model were approximately 500μm. Ten human volunteers successfully self-inserted the microneedles of these larger patches in their skin, following appropriate instruction, as confirmed by transepidermal water loss measure...
Source: International Journal of Pharmaceutics - February 20, 2017 Category: Drugs & Pharmacology Source Type: research

Assessment of surface caking of powders using the ball indentation method
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Qinqin Chen, Umair Zafar, Mojtaba Ghadiri, Jinfeng Bi Powder caking is a ubiquitous problem, which could significantly decrease product quality and lead to economic losses. Hence it is important to know the conditions under which it occurs. The caking behaviour of three powder materials (PVP, HPC and CaHPO4) has been investigated by the ball indentation method (BIM) as affected by relative humidity (RH), temperature and time. The resistance to powder flow, as indicated by the hardness is measured by a bal...
Source: International Journal of Pharmaceutics - February 20, 2017 Category: Drugs & Pharmacology Source Type: research

Surface-modified particles loaded with CaMKII inhibitor protect cardiac cells against mitochondrial injury
Publication date: 30 March 2017 Source:International Journal of Pharmaceutics, Volume 520, Issues 1–2 Author(s): Amaraporn Wongrakpanich, Angie S. Morris, Sean M. Geary, Mei-ling A. Joiner, Aliasger K. Salem An excess of calcium (Ca2+) influx into mitochondria during mitochondrial re-energization is one of the causes of myocardial cell death during ischemic/reperfusion injury. This overload of Ca2+ triggers the mitochondrial permeability transition pore (mPTP) opening which leads to programmed cell death. During the ischemic/reperfusion stage, the activated Ca2+/calmodulin-dependent protein kinase II (CaMKII) enzyme...
Source: International Journal of Pharmaceutics - February 16, 2017 Category: Drugs & Pharmacology Source Type: research

Effect of gel formation on the dissolution behavior of clarithromycin tablets
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Koki Inukai, Kei Takiyama, Shuji Noguchi, Yasunori Iwao, Shigeru Itai Clarithromycin (CAM) is a macrolide antibiotic that is widely used at clinical sites. We found that release of CAM is suppressed when tablets of CAM were exposed to an external solvent containing carboxylate buffers such as citrate. The suppressed release of CAM can be attributed to the formation of gels on the tablet surfaces, which inhibits penetration of the solvent into the tablet and thus disintegration of the tablets. Delayed disi...
Source: International Journal of Pharmaceutics - February 16, 2017 Category: Drugs & Pharmacology Source Type: research

Core-interlayer-shell Fe3O4@mSiO2@lipid-PEG-methotrexate nanoparticle for multimodal imaging and multistage targeted chemo-photodynamic therapy
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Guihua Liu, Jinyuan Ma, Yang Li, Qi Li, Chunhua Tan, Hua Song, Shuhui Cai, Dengyue Chen, Zhenqing Hou, Qing Chen, Xuan Zhu Multimodal imaging-guided multistage targeted synergistic combination therapy possesses many advantages including increased tumoricidal effect, reduced toxicity, and retarded drug resistance. Herein, we have elaborately developed a core-interlayer-shell structure Fe3O4@mSiO2@lipid-PEG-methotrexatenanoparticle(FMLM), in which the Fe3O4 core could be used for magnet-stimulate-response d...
Source: International Journal of Pharmaceutics - February 16, 2017 Category: Drugs & Pharmacology Source Type: research

Relating emulsion stability to interfacial properties for pharmaceutical emulsions stabilized by Pluronic F68 surfactant
We report measurements of dynamic emulsion drop size, zeta potential, and creaming time, as well as dynamic interfacial tension and interfacial viscoelasticity. Experiments show that with 1wt% Pluronic F68, soybean oil emulsions were the most stable with no creaming over six months, followed by isopropyl myristate, octanoic acid, and then ethyl butyrate. The eventual destabilization occurred due to the rising of large drops which formed through Ostwald ripening and coalescence. While Ostwald ripening is important, it is not the dominant destabilization mechanism for the time scale of interest in pharmaceutical emulsions. T...
Source: International Journal of Pharmaceutics - February 16, 2017 Category: Drugs & Pharmacology Source Type: research

Humidity induced phase transformation of poloxamer 188 and its effect on physical stability of amorphous solid dispersion of AMG 579, a PDE10A inhibitor
Publication date: 15 April 2017 Source:International Journal of Pharmaceutics, Volume 521, Issues 1–2 Author(s): Qiong Wu, Michael T. Kennedy, Karthik Nagapudi, Y.-H. Kiang Poloxamer 188, a commonly used emulsifying and solubilizing agent, was found to be the cause of crystallization of an investigational drug, AMG 579, from its amorphous solid dispersion at accelerated storage conditions. Investigation of this physical stability issue included thorough characterization of poloxamer 188 at non-ambient conditions. At 40°C, poloxamer 188 becomes deliquescent above relative humidity of 75%. Upon returning to ambien...
Source: International Journal of Pharmaceutics - February 16, 2017 Category: Drugs & Pharmacology Source Type: research

Hydrophobic ion pairing: Key to highly payloaded self-emulsifying peptide drug delivery systems
Conclusion Following the procedure described herein payloads >10% can be achieved for peptide drugs in SEDDS. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 15, 2017 Category: Drugs & Pharmacology Source Type: research

A novel in situ silver/hyaluronan bio-nanocomposite fabrics for wound and chronic ulcer dressing: In vitro and in vivo evaluations
Publication date: 30 March 2017 Source:International Journal of Pharmaceutics, Volume 520, Issues 1–2 Author(s): A.M. Abdel-Mohsen, J. Jancar, R.M. Abdel-Rahman, L. Vojtek, P. Hyršl, M. Dušková, H. Nejezchlebová In-situ formed hyaluronan/silver (HA/Ag) nanoparticles (NPs) were used to prepare composite fibers/fabrics for the first time. Different concentrations of silver nitrate (1, 2mg/100ml) were added at ambient temperature to sodium hyaluronate solution (40mg/ml), then the pH was increased to 8 by adding sodium hydroxide. The in-situ formed HA/Ag-NPs were used to prepare fibers/nonwov...
Source: International Journal of Pharmaceutics - February 13, 2017 Category: Drugs & Pharmacology Source Type: research

Understanding the mechanisms underlying pulsating aerosol delivery to the maxillary sinus: In vitro tests and computational simulations
Conclusion Results of this study verified the hypothesis of resonance being the mechanism for enhanced particle deposition in the maxillary sinus. A better knowledge of the relationship between sinus dosages, pulsating frequency, and nasal morphometry is essential for improving the design of intrasinus delivery devices. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - February 13, 2017 Category: Drugs & Pharmacology Source Type: research

Salt disproportionation: A material science perspective
Publication date: 30 March 2017 Source:International Journal of Pharmaceutics, Volume 520, Issues 1–2 Author(s): Naveen K. Thakral, Ron C. Kelly While screening the counter-ions for salt selection for an active pharmaceutical substance, there is often an uncertainty about disproportionation of the salt and hence physical stability of the final product formulation to provide adequate shelf life. Several examples of disproportionation reactions are reviewed to explain the concepts of pHmax, microenvironmental pH, and buffering capacity of excipients and APIs to gain mechanistic understanding of disproportionation reac...
Source: International Journal of Pharmaceutics - February 13, 2017 Category: Drugs & Pharmacology Source Type: research

Lipid nanovehicles with adjustable surface properties for overcoming multiple barriers simultaneously in oral administration
Publication date: 30 March 2017 Source:International Journal of Pharmaceutics, Volume 520, Issues 1–2 Author(s): Lei Wu, Min Liu, Wei Shan, Yi Cui, Zhirong Zhang, Yuan Huang Lipid nanoparticles (LNs) are widely investigated for oral drug delivery, and for achieving significant advantages in colloidal stability, biocompatibility and scaled-up possibility. However, researchers face challenge of developing methods to improve the ability of LNs in overcoming multiple barriers (i.e., mucus and epithelium barrier) in gastrointestinal (GI) tract because of the contradictory requirement of nanoparticle (NP) surface properti...
Source: International Journal of Pharmaceutics - February 11, 2017 Category: Drugs & Pharmacology Source Type: research

Photosensitizer-mediated mitochondria-targeting nanosized drug carriers: Subcellular targeting, therapeutic, and imaging potentials
Publication date: 30 March 2017 Source:International Journal of Pharmaceutics, Volume 520, Issues 1–2 Author(s): Yeon Su Choi, Kiyoon Kwon, Kwonhyeok Yoon, Kang Moo Huh, Han Chang Kang Mitochondria-targeting drug carriers have considerable potential because of the presence of many molecular drug targets in the mitochondria and their pivotal roles in cellular viability, metabolism, maintenance, and death. To compare the mitochondria-targeting abilities of triphenylphosphonium (TPP) and pheophorbide a (PhA) in nanoparticles (NPs), this study prepared mitochondria-targeting NPs using mixtures of methoxy poly(ethylene g...
Source: International Journal of Pharmaceutics - February 10, 2017 Category: Drugs & Pharmacology Source Type: research

Cellular internalization and transport of biodegradable polyester dendrimers on a model of the pulmonary epithelium and their formulation in pressurized metered-dose inhalers
Publication date: 30 March 2017 Source:International Journal of Pharmaceutics, Volume 520, Issues 1–2 Author(s): Rodrigo S. Heyder, Qian Zhong, Reinaldo C. Bazito, Sandro R.P. da Rocha The purpose of this study was to evaluate the effect of generation and surface PEGylation of degradable polyester-based dendrimers nanocarriers on their interactions with an in vitro model of the pulmonary epithelium as well as to assess the ability to formulate such carriers in propellant-based, portable oral-inhalation devices to determine their potential for local and systemic delivery of drugs to and through the lungs. Hydroxyl (-...
Source: International Journal of Pharmaceutics - February 10, 2017 Category: Drugs & Pharmacology Source Type: research

A three-dimensional assemblage of gingiva-derived mesenchymal stem cells and NO-releasing microspheres for improved differentiation
Publication date: 30 March 2017 Source:International Journal of Pharmaceutics, Volume 520, Issues 1–2 Author(s): Shobha Regmi, Jiafu Cao, Shiva Pathak, Biki Gupta, Bijay Kumar Poudel, Pham Thanh Tung, Simmyung Yook, Jun-Beom Park, Chul Soon Yong, Jong Oh Kim, Jin-Wook Yoo, Jee-Heon Jeong Stem cell therapy is an attractive approach to bone tissue regeneration. Nitric oxide (NO) has been reported to facilitate osteogenic differentiation of stem cells. To enhance osteogenic differentiation of gingiva-derived mesenchymal stem cells (GMSCs), we designed a method for in situ delivery of exogenous NO to these cells. A NO d...
Source: International Journal of Pharmaceutics - February 10, 2017 Category: Drugs & Pharmacology Source Type: research

Photosensitizer-eluting nanofibers for enhanced photodynamic therapy of wounds: A preclinical study in immunocompromized rats
Publication date: 30 March 2017 Source:International Journal of Pharmaceutics, Volume 520, Issues 1–2 Author(s): Labiba El-Khordagui, Nesma El-Sayed, Sally Galal, Hanan El-Gowelli, Hoda Omar, Moustafa Mohamed Electrospun nanofibers (NFs) as drug delivery/tissue regeneration template and antimicrobial photodynamic therapy (APDT) have been widely investigated as two different approaches to enhance wound healing. In the present study, the two approaches were combined in a single platform for greater healing enhancement potentials. Composite photosensitizer-eluting NFs were developed using a polyhydrohybutyrate/polyethy...
Source: International Journal of Pharmaceutics - February 10, 2017 Category: Drugs & Pharmacology Source Type: research

Humidity affects the morphology of particles emitted from beclomethasone dipropionate pressurized metered dose inhalers
Publication date: 30 March 2017 Source:International Journal of Pharmaceutics, Volume 520, Issues 1–2 Author(s): James W. Ivey, Pallavi Bhambri, Tanya K. Church, David A. Lewis, Mark T. McDermott, Shereen Elbayomy, Warren H. Finlay, Reinhard Vehring The effects of propellant type, cosolvent content, and air humidity on the morphology and solid phase of the particles produced from solution pressurized metered dose inhalers containing the corticosteroid beclomethasone dipropionate were investigated. The active ingredient was dissolved in the HFA propellants 134a and 227ea with varying levels of the cosolvent ethanol a...
Source: International Journal of Pharmaceutics - February 10, 2017 Category: Drugs & Pharmacology Source Type: research

Curcumin complexation with cyclodextrins by the autoclave process: Method development and characterization of complex formation
Publication date: 30 March 2017 Source:International Journal of Pharmaceutics, Volume 520, Issues 1–2 Author(s): Turki Al Hagbani, Sami Nazzal One approach to enhance curcumin (CUR) aqueous solubility is to use cyclodextrins (CDs) to form inclusion complexes where CUR is encapsulated as a guest molecule within the internal cavity of the water-soluble CD. Several methods have been reported for the complexation of CUR with CDs. Limited information, however, is available on the use of the autoclave process (AU) in complex formation. The aims of this work were therefore to (1) investigate and evaluate the AU cycle as a ...
Source: International Journal of Pharmaceutics - February 10, 2017 Category: Drugs & Pharmacology Source Type: research

In vitro permeation and disposition of niacinamide in silicone and porcine skin of skin barrier-mimetic formulations
In this study, three doses (5, 20 and 50μL per cm2) of two NIA containing oil-in-water skin barrier-mimetic formulations were evaluated in silicone membrane and porcine ear skin and compared with a commercial control formulation. Permeation studies were conducted over 24h in Franz cells and at the end of the experiment membranes were washed and niacinamide was extracted. For the three doses, retention or deposition of NIA was generally higher in porcine skin compared with silicone membrane, consistent with the hydrophilic nature of the active. Despite the control containing a higher amount of active, comparable amounts ...
Source: International Journal of Pharmaceutics - February 10, 2017 Category: Drugs & Pharmacology Source Type: research