Induction of Au-methotrexate conjugates by sugar molecules: production, assembly mechanism, and bioassay studies
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): 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...
Source: International Journal of Pharmaceutics - January 31, 2018 Category: Drugs & Pharmacology Source Type: research

Process analytical technology in continuous manufacturing of a commercial pharmaceutical product
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Jenny M. Vargas, Sarah Nielsen, Vanessa Cárdenas, Anthony Gonzalez, Efrain Y. Aymat, Elvin Almodovar, Gustavo Classe, Yleana Colón, Eric Sanchez, Rodolfo J. Romañach The implementation of process analytical technology and continuous manufacturing at an FDA approved commercial manufacturing site is described. In this direct compaction process the blends produced were monitored with a Near Infrared (NIR) spectroscopic calibration model developed with partial least squares (PLS) regressio...
Source: International Journal of Pharmaceutics - January 31, 2018 Category: Drugs & Pharmacology Source Type: research

Hydrogels based on poly(methyl vinyl ether-co-maleic acid) and Tween 85 for sustained delivery of hydrophobic drugs
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Eneko Larrañeta, Laura Barturen, Michael Ervine, Ryan F. Donnelly Hydrogels based on poly(methyl vinyl ether-co-maleic acid) and Tween 85 were prepared for hydrophobic drug delivery. The hydrogels were synthesized following a simple procedure carried out in solid state. The process did not require the use of any solvent and, as it is based on an esterification reaction, no toxic by-products were obtained. The resulting hydrogels contained Tween 85 inside the structure and due to the amphiphilic natu...
Source: International Journal of Pharmaceutics - January 31, 2018 Category: Drugs & Pharmacology Source Type: research

Performance of an acoustically mixed pharmaceutical dry powder delivered from a novel inhaler
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Ryoma Tanaka, Naoyuki Takahashi, Yasuaki Nakamura, Yusuke Hattori, Kazuhide Ashizawa, Makoto OtsukaGraphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 31, 2018 Category: Drugs & Pharmacology Source Type: research

Semifluorinated alkane based systems for enhanced corneal penetration of poorly soluble drugs
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®. Precorneal residence of the four test vehicles containing the hyd...
Source: International Journal of Pharmaceutics - January 31, 2018 Category: Drugs & Pharmacology Source Type: research

A novel method for the production of core-shell microparticles by inverse gelation optimized with artificial intelligent tools
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): 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-alg...
Source: International Journal of Pharmaceutics - January 31, 2018 Category: Drugs & Pharmacology Source Type: research

Molecular-level elucidation of saccharin-assisted rapid dissolution and high supersaturation level of drug from Eudragit ® E solid dispersion
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): 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...
Source: International Journal of Pharmaceutics - January 31, 2018 Category: Drugs & Pharmacology Source Type: research

In vivo controlled release of fenretinide from long-acting release depots for chemoprevention of oral squamous cell carcinoma recurrence
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Kari Nieto, Ping Pei, Daren Wang, Susan R. Mallery, Steven P. Schwendeman Local, long-acting release fenretinide (4HPR) millicylindrical implants were prepared and evaluated for their release kinetics in vivo and their ability to suppress oral cancer tumor explant growth. Poly(lactic-co-glycolic acid)(PLGA) implants were prepared as a function of drug loading and the presence of various excipients (pore-formers, solubilizers, crystallization inhibitors) to enhance release of the insoluble 4HPR. Release kin...
Source: International Journal of Pharmaceutics - January 31, 2018 Category: Drugs & Pharmacology Source Type: research

Characterisation of pore structures of pharmaceutical tablets: A review
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): 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 t...
Source: International Journal of Pharmaceutics - January 31, 2018 Category: Drugs & Pharmacology Source Type: research

An efficient PEGylated gene delivery system with improved targeting: Synergism between octaarginine and a fusogenic peptide
In this study, we describe the development of PEGylated CPP-based gene carrier with an improved targeting and a high transfection activity. The system was prepared by condensing DNA with a polycation followed by coating with a lipid envelope containing the octaarginine (R8) peptide as a model CPP. R8-modified nanoparticles produced high transfection activities, but the efficiency was reduced by PEG shielding. The reduced activity could be fully restored by the addition of a targeting ligand and a pH-sensitive fusogenic peptide. The efficiency of the proposed system is quite high, even in the presence of serum, and shows im...
Source: International Journal of Pharmaceutics - January 21, 2018 Category: Drugs & Pharmacology Source Type: research

Effect of structural factors on release profiles of camptothecin from block copolymer conjugates with high load of drug
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): 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 synth...
Source: International Journal of Pharmaceutics - January 21, 2018 Category: Drugs & Pharmacology Source Type: research

3D extrusion printing of high drug loading immediate release paracetamol tablets
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Shaban A. Khaled, Morgan R. Alexander, Ricky D. Wildman, Martin J. Wallace, Sonja Sharpe, Jae Yoo, Clive J. Roberts The manufacture of immediate release high drug loading paracetamol oral tablets was achieved using an extrusion based 3D printer from a premixed water based paste formulation. The 3D printed tablets demonstrate that a very high drug (paracetamol) loading formulation (80% w/w) can be printed as an acceptable tablet using a method suitable for personalisation and distributed manufacture. Parace...
Source: International Journal of Pharmaceutics - January 20, 2018 Category: Drugs & Pharmacology Source Type: research

Nanogel-DFO conjugates as a model to investigate pharmacokinetics, biodistribution, and iron chelation in vivo
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): 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 b...
Source: International Journal of Pharmaceutics - January 19, 2018 Category: Drugs & Pharmacology Source Type: research

Stability, biocompatibility and antioxidant activity of PEG-modified liposomes containing resveratrol
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Carla Caddeo, Laura Pucci, Morena Gabriele, Claudia Carbone, Xavier Fernàndez-Busquets, Donatella Valenti, Ramon Pons, Antonio Vassallo, Anna Maria Fadda, Maria Manconi The present investigation reports the development of PEG-modified liposomes for the delivery of naturally occurring resveratrol. PEG-modified liposomes were prepared by direct sonication of the phospholipid aqueous dispersion, in the presence of two PEG-surfactants. Small, spherical, unilamellar vesicles were produced, as demonstrate...
Source: International Journal of Pharmaceutics - January 13, 2018 Category: Drugs & Pharmacology Source Type: research

Probing the particulate microstructure of the aerodynamic particle size distribution of dry powder inhaler combination products
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): M.W. Jetzer, B.D. Morrical, M. Schneider, S. Edge, G. Imanidis The in-vitro aerosol performance of two combination dry powder inhaler (DPI) products, Foster® NEXThaler® and Seretide® Diskus® were investigated with single particle aerosol mass spectrometry (SPAMS). The in-vitro pharmaceutical performance is markedly different for both inhalers. Foster® NEXThaler® generates a higher fine particle fraction (FPF <5 μm) and a much higher relative extra fine particle fraction ...
Source: International Journal of Pharmaceutics - January 12, 2018 Category: Drugs & Pharmacology Source Type: research

Controllable encapsulation of α-mangostin with quaternized β-cyclodextrin grafted chitosan using high shear mixing
In this study, the inclusion complex formation between α-mangostin and water-soluble quaternized β-CD grafted-chitosan (QCD-g-CS) was investigated. Inclusion complex formation with encapsulation efficiency (%EE) of 5, 15 and 75% can be varied using high speed homogenizer. Tuning %EE plays a role on physicochemical and biological properties of α-mangostin/QCD-g-CS complex. Molecular dynamics simulations indicate that α-mangostin is included within the hydrophobic β-CD cavity and being absorbed on the QCD-g-CS surface, with these results being confirmed by Fourier transform infrared (FTIR) spectro...
Source: International Journal of Pharmaceutics - January 12, 2018 Category: Drugs & Pharmacology Source Type: research

Optimized tableting for extremely oxygen-sensitive probiotics using direct compression
Publication date: 1 March 2018 Source:International Journal of Pharmaceutics, Volume 538, Issues 1–2 Author(s): Rania Allouche, Sébastien Dupont, Alexandre Charriau, Patrick Gervais, Laurent Beney, Odile Chambin Faecalibacterium prausnitzii was previously recognized for its intestinal anti-inflammatory activities and it has been shown less abundant in patients with chronic intestinal diseases. However, the main problems encountered in the use of this interesting anaerobic microorganism are firstly its high sensitivity to the oxygen and secondly, its ability to reach the large intestine alive as targeted site....
Source: International Journal of Pharmaceutics - January 12, 2018 Category: Drugs & Pharmacology Source Type: research

Novel enzyme formulations for improved pharmacokinetic properties and anti-inflammatory efficacies
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Lan Yang, Shenglei Yan, Yonghong Zhang, Xueyuan Hu, Qi Guo, Yuming Yuan, Jingqing Zhang Anti-inflammatory enzymes promote the dissolution and excretion of sticky phlegm, clean the wound surface and accelerate drug diffusion to the lesion. They play important roles in treating different types of inflammation and pain. Currently, various formulations of anti-inflammatory enzymes are successfully prepared to improve the enzymatic characteristics, pharmacokinetic properties and anti-inflammatory efficacies...
Source: International Journal of Pharmaceutics - January 10, 2018 Category: Drugs & Pharmacology Source Type: research

Accelerated full-thickness wound healing via sustained bFGF delivery based on a PVA/chitosan/gelatin hydrogel incorporating PCL microspheres
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Amir Shamloo, Morteza Sarmadi, Zahra Aghababaie, Manouchehr Vossoughi Herein, a hybrid hydrogel/microsphere system is introduced for accelerated wound healing by sustained release of basic fibroblast growth factor (bFGF). The hydrogel is composed of a mixture of PVA, gelatin and chitosan. The double-emulsion-solvent-evaporation method was utilized to obtain microspheres composed of PCL, as the organic phase, and PVA, as the aqueous phase. Subsequently, various in-vitro and in-vivo assays were performed...
Source: International Journal of Pharmaceutics - January 10, 2018 Category: Drugs & Pharmacology Source Type: research

Zinc delivery from non-woven fibres within a therapeutic nipple shield
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Theresa Maier, Rebekah L. Scheuerle, Daniel Markl, Sylvaine Bruggraber, Axel Zeitler, Ljiljana Fruk, Nigel K.H. Slater A Therapeutic Nipple Shield (TNS) was previously developed to respond to the global need for new infant therapeutic delivery technologies. However, the release efficiency for the same Active Pharmaceutical Ingredient (API) from different therapeutic matrices within the TNS formulation has not yet been investigated. To address this, in-vitro release of elemental zinc into human milk fro...
Source: International Journal of Pharmaceutics - January 10, 2018 Category: Drugs & Pharmacology Source Type: research

Enhancing the solubility and bioavailability of poorly water-soluble drugs using supercritical antisolvent (SAS) process
This article also presents an overview of the main aspects of the SAS-assisted particle precipitation process, its mechanism, and parameters, as well as our own experiences, recent advances, and trends in development. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 10, 2018 Category: Drugs & Pharmacology Source Type: research

A novel lactoferrin-modified stealth liposome for hepatoma-delivery of triiodothyronine
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Rosa Pireddu, Monica Pibiri, Donatella Valenti, Chiara Sinico, Anna Maria Fadda, Gabriella Simbula, Francesco Lai Triiodothyronine (T3), a thyroid hormone synthesized and secreted by the thyroid gland, plays an essential role in morphogenesis and differentiation through interaction with its nuclear receptors (TRs). However, there are increasing evidences for its role in hepatocellular carcinoma (HCC) suppression. The aim of this work was to develop an effective hepatocellular carcinoma targeting drug d...
Source: International Journal of Pharmaceutics - January 5, 2018 Category: Drugs & Pharmacology Source Type: research

Mucus adhesion- and penetration-enhanced liposomes for paclitaxel oral delivery
In conclusion, the dual functional CS-TGA-PF liposomes with mucus adhesion- and permeation-enhanced properties could be used as a promising nanodrug delivery system for PTX oral delivery. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 5, 2018 Category: Drugs & Pharmacology Source Type: research

Mucus-PVPA (mucus Phospholipid Vesicle-based Permeation Assay): An artificial permeability tool for drug screening and formulation development
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Margherita Falavigna, Mette Klitgaard, Christina Brase, Selenia Ternullo, Nataša Škalko-Basnet, Gøril Eide Flaten The mucus layer covering all mucosal surfaces in our body is the first barrier encountered by drugs before their potential absorption through epithelial tissues, and could thus affect the drugs’ permeability and their effectiveness. Therefore, it is of key importance to have in vitro permeability models that can mimic this specific environment. For this purpose, t...
Source: International Journal of Pharmaceutics - January 5, 2018 Category: Drugs & Pharmacology Source Type: research

Loading of polymyxin B onto anionic mesoporous silica nanoparticles retains antibacterial activity and enhances biocompatibility
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Zahra Gounani, Mohammad A. Asadollahi, Rikke L. Meyer, Ayyoob Arpanaei Polymyxin B is a polycationic antibiotic used as the last line treatment against antibiotic-resistant Gram negative bacteria. However, application of polymyxin B is limited because of its toxicity effects. Herein, we used bare and surface modified mesoporous silica nanoparticles (MSNs) with an average diameter of 72.29 ± 8.17 nm as adsorbent for polymyxin B to improve its therapeutic properties. The polymyxin B adsorpti...
Source: International Journal of Pharmaceutics - January 5, 2018 Category: Drugs & Pharmacology Source Type: research

Notorious but not understood: How liquid-air interfacial stress triggers protein aggregation
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Ellen Koepf, Simon Eisele, Rudolf Schroeder, Gerald Brezesinski, Wolfgang Friess Protein aggregation is a major challenge in the development of biopharmaceuticals. As the pathways of aggregation are manifold, good understanding of the mechanisms behind is essential. Particularly, the presence of liquid-air interfaces has been identified to trigger the formation of large protein particles. Investigations of two monoclonal antibodies (IgGs) at the liquid-air interface exhibited the formation of a highly ...
Source: International Journal of Pharmaceutics - January 5, 2018 Category: Drugs & Pharmacology Source Type: research

Real-time process monitoring in a semi-continuous fluid-bed dryer – microwave resonance technology versus near-infrared spectroscopy
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Johanna Peters, Andreas Teske, Wolfgang Taute, Claas Döscher, Michael Höft, Reinhard Knöchel, Jörg Breitkreutz The trend towards continuous manufacturing in the pharmaceutical industry is associated with an increasing demand for advanced control strategies. It is a mandatory requirement to obtain reliable real-time information on critical quality attributes (CQA) during every process step as the decision on diversion of material needs to be performed fast and automatically. Where po...
Source: International Journal of Pharmaceutics - January 5, 2018 Category: Drugs & Pharmacology Source Type: research

Real time release testing of tablet content and content uniformity
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Daniel J. Goodwin, Sander van den Ban, Mike Denham, Ian Barylski A comprehensive commercial control strategy for tablet content and content uniformity focussed on the unit operation of compression is presented and is proposed to enable real time release for these critical quality attributes. The control strategy is based on process understanding, process control through compaction force weight control on the tablet press, periodic checks of mean and individual tablet weight combined with at-line testin...
Source: International Journal of Pharmaceutics - January 5, 2018 Category: Drugs & Pharmacology Source Type: research

OAT1 and OAT3 also mediate the drug-drug interaction between piperacillin and tazobactam
In conclusion, piperacillin and tazobactam are the substrates of hOAT1/3, and OAT1/3 mediate the DDI between piperacillin and tazobactam. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 5, 2018 Category: Drugs & Pharmacology Source Type: research

Development and in vivo evaluation of a novel lyophilized formulation for the treatment of hemorrhagic shock
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Seema Thakral, Andrea Wolf, Gregory J. Beilman, Raj Suryanarayanan Hemorrhagic shock, caused by trauma, is a leading cause of preventable death. A combination treatment of d-β-hydroxybutyrate (BHB) and melatonin (MLT), in dimethyl sulfoxide - water, increased survival. A freeze-dried BHB–MLT formulation, with a short reconstitution time, has been developed. This intravenous formulation, prepared with an aqueous vehicle, completely eliminated dimethyl sulfoxide, thereby avoiding the potential...
Source: International Journal of Pharmaceutics - January 5, 2018 Category: Drugs & Pharmacology Source Type: research

Development of poloxamer gel formulations via hot-melt extrusion technology
In conclusion, the hot-melt extrusion technology could be successfully employed to develop poloxamer gels by overcoming the drawbacks associated with the conventional techniques. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - January 5, 2018 Category: Drugs & Pharmacology Source Type: research

Effect of high pressure homogenization on the structure and the interfacial and emulsifying properties of β-lactoglobulin
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Ali Ali, Isabelle Le Potier, Nicolas Huang, Véronique Rosilio, Monique Cheron, Vincent Faivre, Isabelle Turbica, Florence Agnely, Ghozlene Mekhloufi The effect of high pressure homogenization (HPH) on the structure of β-lactoglobulin (β-lg) was studied by combining spectroscopic, chromatographic, and electrophoretic methods. The consequences of the resulting structure modifications on oil/water (O/W) interfacial properties were also assessed. Moderated HPH treatment (100 MPa/4 cycles...
Source: International Journal of Pharmaceutics - January 5, 2018 Category: Drugs & Pharmacology Source Type: research

Microparticles, microcapsules and microspheres: A review of recent developments and prospects for oral delivery of insulin
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Chun Y. Wong, Hani Al-Salami, Crispin R. Dass Diabetes mellitus is a chronic metabolic health disease affecting the homeostasis of blood sugar levels. However, subcutaneous injection of insulin can lead to patient non-compliance, discomfort, pain and local infection. Sub-micron sized drug delivery systems have gained attention in oral delivery of insulin for diabetes treatment. In most of the recent literature, the terms “microparticles” and “nanoparticle” refer to particles whe...
Source: International Journal of Pharmaceutics - January 5, 2018 Category: Drugs & Pharmacology Source Type: research

Development and in-vitro characterization of nanoemulsions loaded with paclitaxel/ γ-tocotrienol lipid conjugates
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): Ahmed Abu-Fayyad, Mohammad M. Kamal, Jennifer L. Carroll, Ana-Maria Dragoi, Robert Cody, James Cardelli, Sami Nazzal Vitamin E TPGS is a tocopherol (α-T) based nonionic surfactant that was used in the formulation of the Tocosol™ paclitaxel nanoemulsion, which was withdrawn from phase III clinical trials. Unlike tocopherols, however, the tocotrienol (T3) isomers of vitamin E were found to have innate anticancer activity and were shown to potentiate the antitumor activity of paclitaxel. The primary obj...
Source: International Journal of Pharmaceutics - December 23, 2017 Category: Drugs & Pharmacology Source Type: research

Surface engineered excipients: I. improved functional properties of fine grade microcrystalline cellulose
The objective of this paper is to examine the feasibility of using dry coating based surface modification of microcrystalline cellulose, Avicel PH-105, to produce an engineered fine grade (<30 μm) excipient that has all three desired properties. Using a material sparing high-intensity vibrational mixer, Avciel PH-105 is dry coated with 1 wt% Aerosil 200, selected due to its relatively higher dispersive surface energy and lower particle size amongst other silica choices. The results indicated that as expected, the bulk density and flowability are significantly improved, while there was an appreciable...
Source: International Journal of Pharmaceutics - December 23, 2017 Category: Drugs & Pharmacology Source Type: research

Antibacterial effect and DNA delivery using a combination of an arsonium-containing lipophosphoramide with an N-heterocyclic carbene-silver complex – Potential benefits for cystic fibrosis lung gene therapy
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): Angélique Mottais, Mathieu Berchel, Yann Sibiril, Véronique Laurent, Deborah Gill, Stephen Hyde, Paul-Alain Jaffrès, Tristan Montier, Tony Le Gall Cystic Fibrosis (CF), the most common chronic genetic disorder among the Caucasian population, is a life-threatening disease mainly due to respiratory failures resulting from chronic infections and inflammation. Although research in the pharmacological field has recently made significant progress, gene therapy still remains a promising strategy to...
Source: International Journal of Pharmaceutics - December 23, 2017 Category: Drugs & Pharmacology Source Type: research

3D printing of high drug loaded dosage forms using thermoplastic polyurethanes
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): G. Verstraete, A. Samaro, W. Grymonpré, V. Vanhoorne, B. Van Snick, M.N. Boone, T. Hellemans, L. Van Hoorebeke, J.P. Remon, C. Vervaet It was the aim of this study to develop high drug loaded (>30%, w/w), thermoplastic polyurethane (TPU)-based dosage forms via fused deposition modelling (FDM). Model drugs with different particle size and aqueous solubility were pre-processed in combination with diverse TPU grades via hot melt extrusion (HME) into filaments with a diameter of 1.75 ±&th...
Source: International Journal of Pharmaceutics - December 23, 2017 Category: Drugs & Pharmacology Source Type: research

QR encoded smart oral dosage forms by inkjet printing
In this study we demonstrate, for the first time, the applicability of IJP in the production of edible dosage forms in the pattern of a quick response (QR) code. This printed pattern contains the drug itself and encoded information relevant to the patient and/or healthcare professionals. IJP of the active pharmaceutical ingredient (API)-containing ink in the pattern of QR code was performed onto a newly developed porous and flexible, but mechanically stable substrate with a good absorption capacity. The printing did not affect the mechanical properties of the substrate. The actual drug content of the printed dosage forms w...
Source: International Journal of Pharmaceutics - December 23, 2017 Category: Drugs & Pharmacology Source Type: research

Production of cocrystals in an excipient matrix by spray drying
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): David Walsh, Dolores R. Serrano, Zelalem Ayenew Worku, Brid A. Norris, Anne Marie Healy Spray drying is a well-established scale-up technique for the production of cocrystals. However, to the best of our knowledge, the effect of introducing a third component into the feed solution during the spray drying process has never been investigated. Cocrystal formation in the presence of a third component by a one-step spray drying process has the potential to reduce the number of unit operations which are required to pr...
Source: International Journal of Pharmaceutics - December 23, 2017 Category: Drugs & Pharmacology Source Type: research

Characterization of the coating and tablet core roughness by means of 3D optical coherence tomography
This study demonstrates the use of optical coherence tomography (OCT) to simultaneously characterize the roughness of the tablet core and coating of pharmaceutical tablets. OCT is a high resolution non-destructive and contactless imaging methodology to characterize structural properties of solid dosage forms. Besides measuring the coating thickness, it also facilitates the analysis of the tablet core and coating roughness. An automated data evaluation algorithm extracts information about coating thickness, as well as tablet core and coating roughness. Samples removed periodically from a pan coating process were investigate...
Source: International Journal of Pharmaceutics - December 23, 2017 Category: Drugs & Pharmacology Source Type: research

Xanthan gum as a rate-controlling polymer for the development of alcohol resistant matrix tablets and mini-tablets
In this study, xanthan gum was chosen as rate-controlling polymer for the development of alcohol resistant matrix formulations and theophylline as model drug. Two polymer particle sizes (75 and 180μm) and concentrations (30 and 60% w/w) were used to assess their influence on the in-vitro drug release from directly compressed tablets and mini-tablets, in 0% and 40% ethanol for 2h (pH 1.2). For both, tablets and mini-tablets, by using 60% xanthan gum similar dissolution profiles in hydrous and hydroalcoholic media were obtained, independently of the polymer particle size. By decreasing the polymer concentration a risk of ...
Source: International Journal of Pharmaceutics - December 23, 2017 Category: Drugs & Pharmacology Source Type: research

Effects of solvents on skin absorption of nonvolatile lipophilic and polar solutes under finite dose conditions
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): Rattikorn Intarakumhaeng, Apipa Wanasathop, S. Kevin Li The effects of solvents upon the deposition of a moderately lipophilic solute on skin and skin permeation were investigated previously. The present study was a continuing effort to investigate the effects of solvents on finite dose skin absorption of nonvolatile lipophilic and polar solutes and examine the relationships between solute physicochemical properties, solvent effects, and skin absorption of these solutes after solvent deposition. Skin permeation ...
Source: International Journal of Pharmaceutics - December 23, 2017 Category: Drugs & Pharmacology Source Type: research

Characterization and in vivo efficacy of a heptapeptide ODT formulation for the treatment of neurogenic bladder dysfunction
The objective of this study was to develop oral disintegrating tablet (ODT) formulations of a heptapeptide, [Lys5,MeLeu9,Nle10]-NKA(4–10), for the treatment of neurogenic bladder dysfunction. A design of experiment approach was applied to determine the optimal ratio of chosen excipients: gelatin (X1), glycine (X2), and sorbitol (X3). These formulations were optimized for efficacy studies to produce ODTs exhibiting rapid disintegration times (Y1) and appropriate structural integrity (Y2) using JMP® 12.0.1 software. Based on theoretically predicted values from 12 experimental runs, the optimal ODT formulation was d...
Source: International Journal of Pharmaceutics - December 23, 2017 Category: Drugs & Pharmacology Source Type: research

Parameter study of shipping conditions for the ready-to-use application of a 3D human hemicornea construct in drug absorption studies
In this study, a shipping protocol for our 3D human hemicornea (HC) construct should be developed to provide quality-maintaining shipping conditions and to allow its ready-to-use application in drug absorption studies. First, the effects of single and multiple parameters, such as the type of shipping container, storage temperature and CO2 supply, were investigated under controlled laboratory conditions by assessing cell viability via MTT dye reaction and epithelial barrier properties via transepithelial electrical resistance (TEER) measurements. These investigations showed that TEER is more susceptible to shipping paramete...
Source: International Journal of Pharmaceutics - December 23, 2017 Category: Drugs & Pharmacology Source Type: research

Impact breakage of pharmaceutical tablets
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): C. Hare, T. Bonakdar, M. Ghadiri, J. Strong Tablets are the most common solid dosage form of pharmaceutical active ingredients due to their ease of use. Their dissolution behaviour depends on the particle size distribution and physicochemical properties of the formulation, and the compression process, which need to be optimised for producing consistently robust tablets, as weaker tablets are often prone to breakage during production, transport and end use. Tablet strength is typically determined by diametric com...
Source: International Journal of Pharmaceutics - December 23, 2017 Category: Drugs & Pharmacology Source Type: research

Effect of particle size, polydispersity and polymer degradation on progesterone release from PLGA microparticles: Experimental and mathematical modeling
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): Carlos Busatto, Juan Pesoa, Ignacio Helbling, Julio Luna, Diana Estenoz Poly(lactic-co-glycolic acid) (PLGA) microparticles containing progesterone were prepared by the solvent extraction/evaporation and microfluidic techniques. Microparticles were characterized by their size distribution, encapsulation efficiency, morphology and thermal properties. The effect of particle size, polydispersity and polymer degradation on the in vitro release of the hormone was studied. A triphasic release profile was observed for ...
Source: International Journal of Pharmaceutics - December 23, 2017 Category: Drugs & Pharmacology Source Type: research

Investigation of microemulsion and microemulsion gel formulations for dermal delivery of clotrimazole
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): Ji Zhang, Bozena B. Michniak-Kohn Dermal delivery of hydrophobic drugs by microemulsion (ME) formulations and effect from ME microstructures were studied. Anti-fungal drug, clotrimazole (CLOT), was used as the model compound. ME formulations possessing different microstructures were prepared using a ME system that contains isopropyl myristate as oil, Labrasol and Cremophor EL as surfactant and co-surfactant, and water. Permeation experiments on human cadaver skin were conducted for ME and the control formulation...
Source: International Journal of Pharmaceutics - December 23, 2017 Category: Drugs & Pharmacology Source Type: research

Impact of non-binder ingredients and molecular weight of polymer binders on heat assisted twin screw dry granulation
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): Y. Liu, M.R. Thompson, K.P. O’Donnell Two grades of commercial AFFINISOL™ HPMC HME were used as polymer binders to explore the influence of polymer viscosity and concentration on a novel heat assisted dry granulation process with a twin screw extruder. Contributions of other non-binder ingredients in the formulations were also studied for lactose, microcrystalline cellulose and an active pharmaceutical ingredient of caffeine. As sensitive indicators of processing conditions that expose the drug to hi...
Source: International Journal of Pharmaceutics - December 23, 2017 Category: Drugs & Pharmacology Source Type: research

Performance indicators for carrier-based DPIs: Carrier surface properties for capsule filling and API properties for in vitro aerosolisation
This study investigates engineered carrier, as well as engineered API particles, and shows that there are distinct performance indicators of particle engineering for carrier-based dry powder inhalers (DPIs). Spray dried (SDSS) and jet-milled (JMSS) salbutamol sulphate (SS) was blended with untreated α-lactose monohydrate (LAC_R) and α-lactose monohydrate engineered (LAC_E). Subsequent capsule filling was performed with different process settings on a dosator nozzle capsule filling machine in order to reach a target fill weight of 20–25 mg. To evaluate the performance of the different mixtures, in v...
Source: International Journal of Pharmaceutics - December 23, 2017 Category: Drugs & Pharmacology Source Type: research

DEM based computational model to predict moisture induced cohesion in pharmaceutical powders
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): Raj Mukherjee, Chen Mao, Sayantan Chattoraj, Bodhisattwa Chaudhuri Pharmaceutical powder flow can alter significantly based on the exposed humidity conditions, and lack of computational models to predict the same may undermine process development, optimization, and scale-up performances. A Discrete Element Model (DEM) is proposed to predict the effects of humidity on pharmaceutical powder flow by altering the cohesive forces based on granular bond numbers in simple hopper geometries. Experiments analogous to the...
Source: International Journal of Pharmaceutics - December 23, 2017 Category: Drugs & Pharmacology Source Type: research