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

Short-duration ocular iontophoresis of ionizable aciclovir prodrugs: A new approach to treat herpes simplex infections in the anterior and posterior segments of the eye
The objective was to investigate (trans)corneal and transscleral iontophoresis of biolabile amino acid ester prodrugs of aciclovir (ACV-X, X = Arg, Gly and Trp) as a means to increase ocular bioavailability of ACV. Prodrugs displayed tissue-dependent susceptibility to hydrolysis. Iontophoresis of ACV-Arg, ACV-Gly and ACV-Trp (5 mM, 0.5 mA/cm2) for 5 min followed by 55 min passive diffusion resulted in appreciable corneal deposition (21.5 ± 5.1, 14.1 ± 2.0 and 5.3 ± 0.6 nmol/cm2, respectively) and transcorneal per...
Source: International Journal of Pharmaceutics - December 23, 2017 Category: Drugs & Pharmacology Source Type: research

Development of rectal self-emulsifying suspension of a moisture-labile water-soluble drug
The objective was to use the oily phase of the system to formulate a liquid, non-aqueous product while obtaining the advantages of self-emulsification, rapid contact with the rectal mucosa and rapid absorption post-administration. Ceftriaxone was used as a model drug and the human bile salt sodium chenodeoxycholate was used as an absorption enhancer. After preliminary screening of 23 excipients, based on their emulsification ability and emulsion fineness in binary and ternary mixtures, a full factorial design was used to screen different formulations of three preselected excipients. The optimal formulation contained 60% of...
Source: International Journal of Pharmaceutics - December 23, 2017 Category: Drugs & Pharmacology Source Type: research

New insights on the influence of manufacturing conditions and molecular weight on phase-separated films intended for controlled release
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): Helene Andersson Moore, Mariagrazia Marucci, Linda Härdelin, Johan Hjärtstam, Mats Stading, Christian von Corswant, Anette Larsson The aim of this work was to investigate how manufacturing conditions influence phase-separated films of ethyl cellulose (EC) and hydroxypropyl cellulose (HPC) with different molecular weights of HPC. Two HPC grades, SSL and M, with weight average molecular weights (Mw) of 30×103 g/mol and 365×103 g/mol, respectively, were combined with EC 10 cps (70:30w/w EC/HPC...
Source: International Journal of Pharmaceutics - December 23, 2017 Category: Drugs & Pharmacology Source Type: research

PET/CT imaging of 3D printed devices in the gastrointestinal tract of rodents
The objective of this pilot study was to explore the intestinal behaviour of four different polymer-based devices fabricated using FDM 3DP technology in rats. Small capsular devices of 8.6 mm in length and 2.65 mm in diameter were printed from polyvinyl alcohol-polyethylene glycol graft-copolymer (PVA-PEG copolymer, Kollicoat IR), hydroxypropylcellulose (HPC, Klucel), ethylcellulose (EC, Aqualon N7) and hypromellose acetate succinate (HPMCAS, Aquasolve-LG). A smaller sized device, 3.2 mm in length and 2.65 mm in diameter, was also prepared with HPMCAS to evaluate the cut off size of gastric empt...
Source: International Journal of Pharmaceutics - December 23, 2017 Category: Drugs & Pharmacology Source Type: research

Current and novel approaches for control of dental biofilm
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): Trinette Fernandes, Chintan Bhavsar, Sujata Sawarkar, Anisha D’souza Insights in oral demographics have revealed that a significant percentage of population faces chronic incidences of oral diseases. The innervation of these oral manifestations is required because untreated conditions may lead to bone loss in the oral cavity and systemic complications. Conventional treatments include surgery of the affected area followed by its management and/or treatment with antibiotics. However, widely used antibiotics ...
Source: International Journal of Pharmaceutics - December 23, 2017 Category: Drugs & Pharmacology Source Type: research

Insights on animal models to investigate inhalation therapy: Relevance for biotherapeutics
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): A. Guillon, T. Sécher, L.A. Dailey, L. Vecellio, M. de Monte, M. Si-Tahar, P. Diot, C.P. Page, N. Heuzé-Vourc’h Acute and chronic respiratory diseases account for major causes of illness and deaths worldwide. Recent developments of biotherapeutics opened a new era in the treatment and management of patients with respiratory diseases. When considering the delivery of therapeutics, the inhaled route offers great promises with a direct, non-invasive access to the diseased organ and has already p...
Source: International Journal of Pharmaceutics - December 23, 2017 Category: Drugs & Pharmacology Source Type: research

Milling induced amorphisation and recrystallization of α-lactose monohydrate
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Maria Badal Tejedor, Samaneh Pazesh, Niklas Nordgren, Michael Schuleit, Mark W. Rutland, Göran Alderborn, Anna Millqvist-Fureby Preprocessing of pharmaceutical powders is a common procedure to condition the materials for a better manufacturing performance. However, such operations may induce undesired material properties modifications when conditioning particle size through milling, for example. Modification of both surface and bulk material structure will change the material properties, thus affe...
Source: International Journal of Pharmaceutics - December 22, 2017 Category: Drugs & Pharmacology Source Type: research

From benchtop to pilot scale –experimental study and computational assessment of a hot-melt extrusion scale-up of a solid dispersion of dipyridamole and copovidone
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Damir E. Zecevic, Rachel C. Evans, Katharina Paulsen, Karl G. Wagner The aim of our work was to study and define a computationally-based adiabatic scale-up methodology for a hot-melt extrusion (HME) process to produce an amorphous solid dispersion (ASD). As a drug product becomes commercially viable, there is a need for scaling up the manufacturing process. In the case of HME used for the formation of ASDs, scale-up can be challenging due to the fundamental differences in how heat is generated in extru...
Source: International Journal of Pharmaceutics - December 22, 2017 Category: Drugs & Pharmacology Source Type: research

Fast and non-destructive pore structure analysis using terahertz time-domain spectroscopy
This study derives a new quantitative parameter, S a , to describe the anisotropy in pore structure of pharmaceutical tablets based on terahertz time-domain spectroscopy measurements. The S a parameter analysis was applied to three different data sets including tablets with only one excipient (functionalised calcium carbonate), samples with one excipient (microcrystalline cellulose) and one drug (indomethacin), and a complex formulation (granulated product comprising several excipients and one drug). The overall porosity, tablet thickness, initial particle size distribution as well as the granule density were all found to ...
Source: International Journal of Pharmaceutics - December 22, 2017 Category: Drugs & Pharmacology Source Type: research

Size characterization of lipid-based self-emulsifying pharmaceutical excipients during lipolysis using Taylor dispersion analysis with fluorescence detection
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Joseph Chamieh, Habib Merdassi, Jean-Christophe Rossi, Vincent Jannin, Frédéric Demarne, Hervé Cottet Self-emulsifying drug delivery systems based on lipids have gained in interest in recent years due to their capacity to enhance the bioavailability of poorly water soluble drugs. Their oral intake suggests that they will be in contact with gastric and pancreatic enzymes during their passage through the gastrointestinal tract. The study of the evolution of such systems in the presen...
Source: International Journal of Pharmaceutics - December 21, 2017 Category: Drugs & Pharmacology Source Type: research

Active intestinal drug absorption and the solubility-permeability interplay
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Daniel Porat, Arik Dahan The solubility-permeability interplay deals with the question: what is the concomitant effect on the drug’s apparent permeability when increasing the apparent solubility with a solubility-enabling formulation? The solubility and the permeability are closely related, exhibit certain interplay between them, and ongoing research throughout the past decade shows that treating the one irrespectively of the other may be insufficient. The aim of this article is to provide an ove...
Source: International Journal of Pharmaceutics - December 20, 2017 Category: Drugs & Pharmacology Source Type: research

Drug nanocrystals – Versatile option for formulation of poorly soluble materials
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Leena Peltonen, Jouni Hirvonen Poor solubility of drug compounds is a great issue in drug industry today and decreasing particle size is one efficient and simple way to overcome this challenge. Drug nanocrystals are solid nanosized drug particles, which are covered by a stabilizer layer. In nanoscale many physical properties, like compound solubility, are different from the solubility of bulk material, and due to this drug nanocrystals can reach supersaturation as compared to thermodynamic solubility. ...
Source: International Journal of Pharmaceutics - December 20, 2017 Category: Drugs & Pharmacology Source Type: research

The effect of mechanical dry coating with magnesium stearate on flowability and compactibility of plastically deforming microcrystalline cellulose powders
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Jaana Koskela, David A.V. Morton, Peter J. Stewart, Anne M. Juppo, Satu Lakio Mechanofusion is a dry coating method that can be used to improve the flowability of cohesive powder by coating host particles with a lubricant, for example magnesium stearate (MgSt). It has been shown previously that fragmenting material can under some circumstances be mechanofused with MgSt without impairing compactibility of the powder and without reducing the dissolution rate of the resulting tablets. However, the effects...
Source: International Journal of Pharmaceutics - December 20, 2017 Category: Drugs & Pharmacology Source Type: research

Efficiency of resveratrol-loaded sericin nanoparticles: Promising bionanocarriers for drug delivery
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Kunat Suktham, Thongchai Koobkokkruad, Tuksadon Wutikhun, Suvimol Surassmo Sericin protein nanoparticles are a biocompatible, bio-viable class of nanocarriers gaining prominence in drug delivery system. This research aimed to investigate the suitability fabrication of silk protein (SP) nanoparticles for loading with resveratrol (RSV) via a solventless precipitation technique. The addition of 0.5% (w/v) pluronic surfactant proved optimal for SP nanoparticle fabrication, with obtained nanoparticles being...
Source: International Journal of Pharmaceutics - December 19, 2017 Category: Drugs & Pharmacology Source Type: research

Generic patches containing fentanyl: In vitro equivalence and abuse deterrent evaluation according to EMA and FDA guidelines
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Cristina Padula, Silvia Pescina, Sara Nicoli, Patrizia Santi The aim of this work was to characterize in vitro and ex vivo the performances of Durogesic and of two bioequivalent generic products, by evaluating: (a) fentanyl release; (b) fentanyl permeation across porcine skin and (c) fentanyl ease of extraction. Additional characteristics studied are the effect of temperature and skin integrity, applied individually or combined, to check a possible synergism. The two generic patches resulted equivalent...
Source: International Journal of Pharmaceutics - December 19, 2017 Category: Drugs & Pharmacology Source Type: research

Design and characterization of a perivascular PLGA coated PET mesh sustaining the release of atorvastatin for the prevention of intimal hyperplasia
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Ioanna Mylonaki, Orio Trosi, Eric Allémann, Marlène Durand, Olivier Jordan, Florence Delie Following vascular bypass interventions, autologous saphenous vein grafts are prone to fail due to intimal hyperplasia development. An atorvastatin (ATV)-eluting tubular mesh coated with poly(d,l-lactide-co-glycolisde) acid (PLGA) was designed for perivascular application, in order to prevent the development of this pathology. Formulation parameters such as PLGA molecular weight, concentration of AT...
Source: International Journal of Pharmaceutics - December 19, 2017 Category: Drugs & Pharmacology Source Type: research

The artificial membrane insert system as predictive tool for formulation performance evaluation
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Philippe Berben, Joachim Brouwers, Patrick Augustijns In view of the increasing interest of pharmaceutical companies for cell- and tissue-free models to implement permeation into formulation testing, this study explored the capability of an artificial membrane insert system (AMI-system) as predictive tool to evaluate the performance of absorption-enabling formulations. Firstly, to explore the usefulness of the AMI-system in supersaturation assessment, permeation was monitored after induction of differe...
Source: International Journal of Pharmaceutics - December 16, 2017 Category: Drugs & Pharmacology Source Type: research

Nano-scale and molecular-level understanding of wet-milled indomethacin/poloxamer 407 nanosuspension with TEM, suspended-state NMR, and Raman measurements
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Yosuke Kuroiwa, Kenjirou Higashi, Keisuke Ueda, Keiji Yamamoto, Kunikazu Moribe We investigated the formation and stabilization mechanisms of indomethacin (IMC)/poloxamer 407 nanosuspensions. Stable nanosuspensions were prepared via 24 h wet-milling of three IMC forms (γ form, α form, and amorphous) with poloxamer 407. Cryogenic-transmission electron microscopy images of nanoparticles obtained using γ-form IMC indicated a rhombic-plate shape. In contrast, needle-like nanoparticles w...
Source: International Journal of Pharmaceutics - December 16, 2017 Category: Drugs & Pharmacology Source Type: research

Development of solidified self-microemulsifying drug delivery systems containing l-tetrahydropalmatine: Design of experiment approach and bioavailability comparison
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Nguyen-Thach Tung, Cao-Son Tran, Thi-Minh-Hue Pham, Hoang-Anh Nguyen, Tran-Linh Nguyen, Sang-Cheol Chi, Dinh-Duc Nguyen, Thi-Bich-Huong Bui The study first aimed to apply a design of experiment (DoE) approach to investigate the influences of excipients on the properties of liquid self-microemulsifying drug delivery system (SMEDDS) and SMEDDS loaded in the pellet (pellet-SMEDDS) containing l-tetrahydropalmatine (l-THP). Another aim of the study was to compare the bioavailability of l-THP suspension, liq...
Source: International Journal of Pharmaceutics - December 15, 2017 Category: Drugs & Pharmacology Source Type: research

Point of use production of liposomal solubilised products
Publication date: 15 February 2018 Source:International Journal of Pharmaceutics, Volume 537, Issues 1–2 Author(s): Swapnil Khadke, Peter Stone, Aleksey Rozhin, Jerome Kroonen, Yvonne Perrie With the progression towards personalised and age-appropriate medicines, the production of drug loaded liposomes at the point of care would be highly desirable. In particular, liposomal solubilisation agents that can be produced rapidly and easily would provide a new option in personalised medicines. Such a process could also be used as a rapid tool for the formulation and pre-clinical screening of low soluble drugs. Within this...
Source: International Journal of Pharmaceutics - December 14, 2017 Category: Drugs & Pharmacology Source Type: research

Conductive vancomycin-loaded mesoporous silica polypyrrole-based scaffolds for bone regeneration
In this study, we have developed bone scaffolds composed of hydroxyapaptite (HAp), gelatin and mesoporous silica, all recognized as promising materials in bone tissue engineering due to favorable biocompatibility, osteoconductivity and drug delivery potential, respectively. These materials were coupled with conductive polypyrrole (PPy) polymer to create a novel bone scaffold for regenerative medicine. Conductive and non-conductive scaffolds were made by slurry casting method and loaded with a model antibiotic, vancomycin (VCM). Their properties were compared in different experiments in which scaffolds containing PPy showed...
Source: International Journal of Pharmaceutics - December 6, 2017 Category: Drugs & Pharmacology Source Type: research

Multivariate modeling of diffuse reflectance infrared fourier transform (DRIFT) spectra of mixtures with low-content polymorphic impurities with analysis of outliers
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): Slobodan Šašić, Andrew Gilkison, Mark Henson Diffuse Reflectance Fourier Transform Infrared Spectroscopy (DRIFTS)-based multivariate models were developed to quantify the content of two polymorphic impurities in mixtures with the desired active pharmaceutical ingredient (API) form, with the impurities not exceeding 2% wt/wt. In addition, close attention was paid to the outlier detection criteria: Q residuals; Hotelling T2; and score bi-plot. While reasonably accurate results were obtained for the ...
Source: International Journal of Pharmaceutics - December 6, 2017 Category: Drugs & Pharmacology Source Type: research

The efficiency and mechanism of N-octyl-O, N-carboxymethyl chitosan-based micelles to enhance the oral absorption of silybin
This study demonstrates the preparation of a silybin-loaded N-octyl-O, N-carboxymethyl chitosan micelle (OCC-SLB) to enhance the oral absorption efficiency of silybin (SLB) and investigate the related mechanisms of enhancement. Firstly, the physicochemical properties of OCC and OCC-SLB micelles, including critical micelle concentration (CMC), particle size, zeta potential, drug-loading, etc., were determined. Results of pharmacokinetic studies on rats then confirmed a desirable enhancement in the oral bioavailability of SLB by OCC-SLB micelles compared with a stock SLB suspension solution. Subsequently, uptake studies on t...
Source: International Journal of Pharmaceutics - December 2, 2017 Category: Drugs & Pharmacology Source Type: research

Mesoporous systems for poorly soluble drugs – recent trends
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): Joakim Riikonen, Wujun Xu, Vesa-Pekka Lehto When poor aqueous solubility of active pharmaceutical ingredients is encountered during a drug formulation process, the toolbox typically utilized contains pharmaceutical salts, co-crystals, solid dispersions, cyclodextrins, lipids, liposomes and nanocrystals etc. Especially in the pharmaceutical industry, the option which confers the greatest benefit with the lowest risk is usually chosen. Several factors affect the final decision, but new technologies should also be ...
Source: International Journal of Pharmaceutics - December 2, 2017 Category: Drugs & Pharmacology Source Type: research

Novel sulforaphane-enabled self-microemulsifying delivery systems (SFN-SMEDDS) of taxanes: Formulation development and in vitro cytotoxicity against breast cancer cells
This study highlighted the unique properties of SFN and its potential use in reformulating taxanes with high drug load and significantly lower excipient content than the commercial products. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - December 2, 2017 Category: Drugs & Pharmacology Source Type: research

Multivariate analysis for the optimization of microfluidics-assisted nanoprecipitation method intended for the loading of small hydrophilic drugs into PLGA nanoparticles
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): E. Chiesa, R. Dorati, T. Modena, B. Conti, I. Genta Design of Experiment-assisted evaluation of critical process (total flow rate, TFR, flow rate ratio, FRR) and formulation (polymer concentration and structure, drug:polymer ratio) variables in a novel microfluidics-based device, a staggered herringbone micromixer (SHM), for poly(lactic-co-glycolic acid) copolymer (PLGA) nanoparticles (NPs) manufacturing was performed in order to systematically evaluate and mathematically describe their effects on NPs sizes and ...
Source: International Journal of Pharmaceutics - December 2, 2017 Category: Drugs & Pharmacology Source Type: research

HPMA copolymer conjugate with pirarubicin: In vitro and ex vivo stability and drug release study
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): Waliul Islam, Jun Fang, Tomas Etrych, Petr Chytil, Karel Ulbrich, Akihiro Sakoguchi, Katsuki Kusakabe, Hiroshi Maeda We have developed a tumor environment-responsive polymeric anticancer prodrug containing pirarubicin (THP) conjugated to N-(2-hydroxypropyl) methacrylamide copolymer (PHPMA), [P-THP], through a spacer containing pH-sensitive hydrazone bond, that showed remarkable therapeutic effect against various tumor models and in a human pilot study. Toward clinical development, here we report THP release prof...
Source: International Journal of Pharmaceutics - November 29, 2017 Category: Drugs & Pharmacology Source Type: research

Liposomes encapsulating native and cyclodextrin enclosed paclitaxel: Enhanced loading efficiency and its pharmacokinetic evaluation
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): Priyanka Bhatt, Rohan Lalani, Imran Vhora, Sushilkumar Patil, Jitendra Amrutiya, Ambikanandan Misra, Rajashree Mashru Combination strategy involving cyclodextrin (CD) complexation and liposomal system was investigated for Paclitaxel (PTX) to improve loading. Complexation was done using 2,6-di-O-methylbetacyclodextrin (DMβCD). Sterically stabilized double loaded PEGylated liposomes (DLPLs) containing PTX and PTX-DMβCD complex were prepared by thin film hydration. Physicochemical characterization of comp...
Source: International Journal of Pharmaceutics - November 29, 2017 Category: Drugs & Pharmacology Source Type: research

Rational design of polysorbate 80 stabilized human serum albumin nanoparticles tailored for high drug loading and entrapment of irinotecan
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): Neetika Taneja, Kamalinder K. Singh Human serum albumin (HSA) nanoparticles are considered to be versatile carrier of anticancer agents in efficiently delivering the drug to the tumor site without causing any toxicity. The aim of the study was to develop stable HSA nanoparticles (NPs) of drug irinotecan (Iro) having slightly water solubility and moderate HSA binding. A novel strategy of employing a hydrophilic non-ionic surfactant polysorbate 80 which forms protein-polysorbate 80 complex with increased affinity ...
Source: International Journal of Pharmaceutics - November 28, 2017 Category: Drugs & Pharmacology Source Type: research