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

Nanoparticle-loaded hydrogels as a pathway for enzyme-triggered drug release in ophthalmic applications
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): Michelle Åhlén, Gopi Krishna Tummala, Albert Mihranyan The aim of this study was to develop nanoparticle loaded hydrogel based contact lenses that could be used for ocular drug delivery. Two potential contact lens platforms for controlled ophthalmic drug delivery were developed by incorporating chitosan-poly (acrylic acid) nanoparticles into polyvinyl alcohol (PVA) hydrogels and in-situ gelled nanoparticles and cellulose nanocrystals (CNC) in PVA lenses. The nanoparticles were shown to disintegrate ...
Source: International Journal of Pharmaceutics - November 28, 2017 Category: Drugs & Pharmacology Source Type: research

Reclaiming hijacked phagosomes: Hybrid nano-in-micro encapsulated MIAP peptide ensures host directed therapy by specifically augmenting phagosome-maturation and apoptosis in TB infected macrophage cells
We describe the potential of nano-encapsulated synthetic Magainin-I analog peptide (MIAP) as Host Directed Therapy against TB. Micron-sized inhalable platform “Porous Nanoparticle Aggregates Particles (PNAP)” with nano-scale physiognomies were developed to improve the delivery of MIAP-peptide to the lungs and enhance its stability. This particle engineering enabled more control over aerodynamic characteristics and bioactive release. Antimicrobial and mechanistic studies were carried out against virulent H37Rv TB bacteria. These MIAP-PNAP nano-assemblies demonstrated dose and time dependent antibacterial action ...
Source: International Journal of Pharmaceutics - November 28, 2017 Category: Drugs & Pharmacology Source Type: research

Failure of active targeting by a cholesterol-anchored ligand and improvement by altering the lipid composition to prevent ligand desorption
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): Shoshiro Yamamoto, Yu Sakurai, Hideyoshi Harashima Although anti-angiogenic therapy is predicted to be an effective therapy for treating cancer, selectively targeting tumor endothelial cells (TECs), and not normal endothelial cells, remains a major obstacle. Modifying a drug carrier with a targeting ligand is a popular strategy for developing an active-targeting type drug delivery system (DDS). We previously reported that a cyclo(Arg-Gly-Asp-D-Phe-Lys) (cRGD)-equipped liposome that contains encapsulated siRNA (R...
Source: International Journal of Pharmaceutics - November 28, 2017 Category: Drugs & Pharmacology Source Type: research

Sustained-release multiparticulates for oral delivery of a novel peptidic ghrelin agonist: Formulation design and in vitro characterization
This study describes the generation of a high load capacity pellet formulation for sustained release of a freely water-soluble dairy-derived hydrolysate, FHI-2571. The activity of this novel peptidic ghrelin receptor agonist is reported using in vitro calcium mobilization assays. Conventional extrusion spheronization was then used to prepare peptide-loaded pellets which were subsequently coated with ethylcellulose (EC) film coats using a fluid bed coating system in bottom spray (Wurster) mode. Aqueous-based EC coating dispersions produced mechanically brittle coats which fractured due to osmotic pressure build-up within pe...
Source: International Journal of Pharmaceutics - November 28, 2017 Category: Drugs & Pharmacology Source Type: research

A simple and rapid measurement method of encapsulation efficiency of doxorubicin loaded liposomes by direct injection of the liposomal suspension to liquid chromatography
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): Eiichi Yamamoto, Shota Miyazaki, Chiaki Aoyama, Masaru Kato A simple and rapid chromatographic measurement method for determining doxorubicin (DOX) encapsulation efficiency (EE) into PEGylated liposomes using nanoparticle exclusion chromatography (nPEC) was developed. In this work, Doxil® and two PEGylated liposomes spiked with DOX were employed as model liposomes, and unencapsulated DOX was measured by high performance liquid chromatography with diode-array detector using an N-vinylpyrrolidone modified nPEC...
Source: International Journal of Pharmaceutics - November 26, 2017 Category: Drugs & Pharmacology Source Type: research

Temperature-sensitive copolymer-coated fluorescent mesoporous silica nanoparticles as a reactive oxygen species activated drug delivery system
In this study, a temperature and ROS-responsive drug delivery system ROSP@MSN based on mesoporous silica nanoparticles has been designed and synthesized by taking advantage of 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzyl acrylate modified polymers (ROSP) as “nano-valve”, which can respond selectively to cancer exclusive microenvironment and implement targeted drug release. Due to the superior temperature-sensitive properties of ROSP, ROSP@MSN could achieve cargo loading in cold water, and subsequently close the pore by raising temperature to obtain ROSP@MSN@DOX. Upon the stimulus of ROS, ROSP@MSN@DOX s...
Source: International Journal of Pharmaceutics - November 25, 2017 Category: Drugs & Pharmacology Source Type: research

Enhanced glioma therapy by synergistic inhibition of autophagy and tyrosine kinase activity
Publication date: 30 January 2018 Source:International Journal of Pharmaceutics, Volume 536, Issue 1 Author(s): Xuhui Wang, Yue Qiu, Qianwen Yu, Hui Li, Xiaoxiao Chen, Man Li, Yang Long, Yayuan Liu, Libao Lu, Jiajing Tang, Zhirong Zhang, Qin He Autophagy is a lysosomal degradation pathway that acts as a cytoprotective mechanism causing treatment resistance in various cancer cells. Recent studies showed that hydroxychloroquine can inhibit the latter step of autophagy and therefore enhance the anti-glioma efficiency of ZD6474, a tyrosine kinase inhibitor. However, the nonselective distribution of ZD6474 in vivo and the low ...
Source: International Journal of Pharmaceutics - November 25, 2017 Category: Drugs & Pharmacology Source Type: research

Lipid coated chitosan-DNA nanoparticles for enhanced gene delivery
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Elias Baghdan, Shashank Reddy Pinnapireddy, Boris Strehlow, Konrad H. Engelhardt, Jens Schäfer, Udo Bakowsky Chitosan as a polycationic non-viral vector for gene delivery has the advantage of being a biocompatible and biodegradable polymer. However, without laborious chemical modifications to its structure, it is of limited use as a gene delivery vehicle due to its low ability to efficiently transfect under physiological conditions. To address this problem, we developed novel liposome encapsulated ...
Source: International Journal of Pharmaceutics - November 24, 2017 Category: Drugs & Pharmacology Source Type: research

Incorporation of surface-modified dry micronized poorly water-soluble drug powders into polymer strip films
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Lu Zhang, Yidong Li, Manal Abed, Rajesh N. Davé Recent work has established polymer strip films as a robust platform for delivery of poorly water-soluble drugs via slurry casting, in particular using stable drug nanosuspensions. Here, a simpler, robust method to directly incorporate dry micronized poorly water-soluble drug, fenofibrate (FNB), is introduced. As a major novelty, simultaneous surface modification using hydrophilic silica along with micronization was done using fluid energy mill (FEM...
Source: International Journal of Pharmaceutics - November 24, 2017 Category: Drugs & Pharmacology Source Type: research

Protein-alginate complexes as pH-/ion-sensitive carriers of proteins
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Vida Rahmani, Heather Sheardown Protein-alginate complexes were prepared with the objective of quantifying the influence of the parameters such as protein characteristics on the final complex properties and their dissociation rates. Cytochrome C, lysozyme, myoglobin, chymotrypsin, and bovine serum albumin were used as model proteins for preparing the complexes and physical properties such as composition, average diameter, and zeta potential of the complexes formed were measured. In addition, protein rel...
Source: International Journal of Pharmaceutics - November 24, 2017 Category: Drugs & Pharmacology Source Type: research

Polymer-based nanoparticles loaded with a TLR7 ligand to target the lymph node for immunostimulation
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Jérôme Widmer, Cédric Thauvin, Inès Mottas, Van Nga Nguyen, Florence Delie, Eric Allémann, Carole Bourquin Small-molecule agonists for the Toll-like receptors (TLR) 7 and 8 are effective for the immunotherapy of skin cancer when used as topical agents. Their systemic use has however been largely unsuccessful due to dose-limiting toxicity. We propose a polymer-based nanodelivery system to target resiquimod, a TLR7 ligand, to the lymph node in order to focus the immunosti...
Source: International Journal of Pharmaceutics - November 23, 2017 Category: Drugs & Pharmacology Source Type: research

Exploring gold nanoparticles interaction with mucins: A spectroscopic-based study
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Nadia Barbero, Martina Coletti, Federico Catalano, Sonja Visentin The interaction between two mucin types (mucin from porcine stomach – PGM and mucin from bovine submaxillary glands – BSM) and gold nanoparticles (GNPs) of various size (5, 20 and 40 nm) and functionalization (with cysteamine or thioglycolic acid) was studied under physiological conditions, in order to investigate the affinity of the nanoparticles to the proteins. Different methods are employed to monitor the interactio...
Source: International Journal of Pharmaceutics - November 23, 2017 Category: Drugs & Pharmacology Source Type: research

Penta-block copolymer microspheres: Impact of polymer characteristics and process parameters on protein release
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Minh-Quan Le, Fabien Violet, Cédric Paniagua, Xavier Garric, Marie-Claire Venier-Julienne Here, we aimed to develop protein loaded microspheres (MSs) using penta-block PLGA-based copolymers to obtain sustained and complete protein release. We varied MS morphology and studied the control of protein release. Lysozyme was used as a model protein and MSs were prepared using the solid-in-oil-in-water emulsion solvent extraction method. We synthesized and studied various penta-block PLGA-based copolyme...
Source: International Journal of Pharmaceutics - November 23, 2017 Category: Drugs & Pharmacology Source Type: research

Anti-Adherent Biomaterials for Prevention of Catheter Biofouling
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Colin P. McCoy, Nicola J. Irwin, Louise Donnelly, David S. Jones, John G. Hardy, Louise Carson Medical device-associated infections present a leading global healthcare challenge, and effective strategies to prevent infections are urgently required. Herein, we present an innovative anti-adherent hydrogel copolymer as a candidate catheter coating with complementary hydrophobic drug-carrying and eluting capacities. The amphiphilic block copolymer, Poloxamer 188, was chemically-derivatized with methacryloyl...
Source: International Journal of Pharmaceutics - November 23, 2017 Category: Drugs & Pharmacology Source Type: research

Development and characterization of an organic solvent free, proliposomal formulation of Busulfan using quality by design approach
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Dhawal Chobisa, Ketan Patel, Jasmin Monpara, Mayank Patel, Pradeep Vavia Parenteral administration of Busulfan (BU) conquers the bioavailability and biovariability related issues of oral BU by maintaining the plasma drug concentration in therapeutic range with minimal fluctuations thereby significantly reducing the side effects. Busulfex® is the only commercially available parenteral formulation of BU composed of organic solvents N, N-dimethylacetamide and polyethylene glycol 400. Since, BU is highl...
Source: International Journal of Pharmaceutics - November 21, 2017 Category: Drugs & Pharmacology Source Type: research

Particle agglomeration of chitosan –magnesium aluminum silicate nanocomposites for direct compression tablets
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Rapee Khlibsuwan, Thaned Pongjanyakul Exfoliated nanocomposites of chitosan-magnesium aluminum silicate (CS-MAS) particles are characterized by good compressibility but poor flowability. Thus, the aims of this study were to investigate agglomerates of CS-MAS nanocomposites prepared using the agglomerating agents water, ethanol, or polyvinylpyrrolidone (PVP) for flowability enhancement and to evaluate the agglomerates obtained as direct compression fillers for tablets. The results showed that the additio...
Source: International Journal of Pharmaceutics - November 21, 2017 Category: Drugs & Pharmacology Source Type: research

Investigating cascade impactor performance using a modified 3D printed induction port
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Kai Berkenfeld, Michael Bernauer, Jason T. McConville, Alf Lamprecht Based on a computer tomographic scan of a human trachea, a modified induction port (mIP), for use with the Next Generation Cascade Impactor, was manufactured using 3D printing technology. Standard United States Pharmacopoeia IP (USPIP) was compared to the mIP and a 3D printed version of the USPIP (USP3DIP) by analyzing different types of commercial salbutamol formulations for inhalation. Increased retention of particles in the mIP was ...
Source: International Journal of Pharmaceutics - November 21, 2017 Category: Drugs & Pharmacology Source Type: research

Interactions between a poorly soluble cationic drug and sodium dodecyl sulfate in dissolution medium and their impact on in vitro dissolution behavior
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Zongyun Huang, Shuchi Parikh, William P. Fish In the pharmaceutical industry, in vitro dissolution testing ofsolid oral dosage forms is a very important tool for drug development and quality control. However, ion-pairing interaction between the ionic drugand surfactants in dissolution medium often occurs, resulting in inconsistent and incomplete drug release. The aim of this study is toevaluate the effects ofsodium dodecyl sulfate (SDS) mediated medium onthe dissolution behaviors of a poorly soluble cat...
Source: International Journal of Pharmaceutics - November 21, 2017 Category: Drugs & Pharmacology Source Type: research

Improvement of intestinal absorption of curcumin by cyclodextrins and the mechanisms underlying absorption enhancement
In this study, the effects of various cyclodextrins on the intestinal absorption of curcumin were evaluated in rat intestine by an in situ closed-loop method. Among the tested cyclodextrins, 50 mM α-cyclodextrin significantly enhanced the absorption of curcumin without inducing any intestinal toxicity. The analysis of cellular transport across Caco-2 cell monolayers showed that 50 mM α-cyclodextrin reduced the transepithelial electrical resistance value of cell monolayers and improved the permeability of 5(6)-carboxyfluorescein, a poorly absorbable drug, which is mainly transported via a paracellu...
Source: International Journal of Pharmaceutics - November 21, 2017 Category: Drugs & Pharmacology Source Type: research

Hyaluronan-decorated liposomes as drug delivery systems for cutaneous administration
Publication date: 15 January 2018 Source:International Journal of Pharmaceutics, Volume 535, Issues 1–2 Author(s): Silvia Franzé, Alessandro Marengo, Barbara Stella, Paola Minghetti, Silvia Arpicco, Francesco Cilurzo The work aimed to evaluate the feasibility to design hyaluronic acid (HA) decorated flexible liposomes to enhance the skin penetration of nifedipine. Egg phosphatidylcholine (e-PC) based transfersomes (Tween 80) and transethosomes (ethanol) were prepared. HA was reacted with 1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine (HA-DPPE) and two molar ratios (0.5 and 3%) of conjugate with respect to e...
Source: International Journal of Pharmaceutics - November 20, 2017 Category: Drugs & Pharmacology Source Type: research