NLC versus nanoemulsions: effect on physiological skin parameters during regular in vivo application and impact on drug penetration
Publication date: Available online 9 August 2018Source: International Journal of PharmaceuticsAuthor(s): Martin Wolf, Victoria Klang, Tatjana Stojcic, Carola Fuchs, Michael Wolzt, Claudia ValentaAbstractNanostructured lipid carriers (NLC) and nano-sized emulsions based on monoacyl-phosphatidylcholine (MAPL) were tested for their effect on physiological skin parameters in vivo during daily application over four weeks. The influence of the basic formulations on transepidermal water loss (TEWL), skin hydration, sebum content and pH was determined once per week and after a recovery period of three weeks. In addition, confocal ...
Source: International Journal of Pharmaceutics - August 9, 2018 Category: Drugs & Pharmacology Source Type: research

Mesoporous Silica Nanoparticles for Enhanced Lidocaine Skin Delivery
Publication date: Available online 3 August 2018Source: International Journal of PharmaceuticsAuthor(s): Shohreh Nafisi, Naghmeh Samadi, Mahboubeh Houshiar, Howard I MaibachAbstractLidocaine's (Lido) low water solubility and negligible tissue uptake limit its bioavailability when applied to the skin. Nanoparticulate systems would help address these issues; therefore, lidocaine inclusion complexes with mesoporous silica nanoparticles (MSNs) were prepared and the effect of MCM41 surface functionalization with positively charged amino-propyl groups on the molecule properties studied. It is expected that positively c...
Source: International Journal of Pharmaceutics - August 3, 2018 Category: Drugs & Pharmacology Source Type: research

Longitudinal PET/CT evaluation of TNBS-induced Inflammatory Bowel Disease rat model
In this study, IBD was induced in rats using 2,4,6-trinitrobenzenesulfonic acid (TNBS) and longitudinal [18F]FDG PET/CT scans were conducted to assess disease progression post-TNBS administration. Afterwards, [18F]FDG PET/CT scans were carried out after treatment with methylprednisolone to validate the model.In non-treated rats, SUVmax (Standardized Uptake Value) rapidly increased after IBD induction, being particularly significant (p
Source: International Journal of Pharmaceutics - August 3, 2018 Category: Drugs & Pharmacology Source Type: research

Optimization of β-Cyclodextrin Consolidated Micellar Dispersion for Promoting the Transcorneal Permeation of a Practically Insoluble Drug
Publication date: Available online 3 August 2018Source: International Journal of PharmaceuticsAuthor(s): Sinar Sayed, Ibrahim Elsayed, Maha M. IsmailAbstractDevelopment of efficient ocular drug delivery system for antifungal drugs becomes a must nowadays to face and eradicate the widely spread ophthalmic fungal infections. Itraconazole, a triazole antifungal, is struggling to penetrate the cornea and subsequently, its efficacy is limited. The aim of this study was to enhance itraconazole corneal penetration through utilizing the minimum surfactant amount in presence of β-cyclodextrin which acted as a dissolution and p...
Source: International Journal of Pharmaceutics - August 3, 2018 Category: Drugs & Pharmacology Source Type: research

3D printed drug products: Non-destructive dose verification using a rapid point-and-shoot approach
Publication date: Available online 2 August 2018Source: International Journal of PharmaceuticsAuthor(s): Sarah J Trenfield, Alvaro Goyanes, Richard Telford, David Wilsdon, Martin Rowland, Simon Gaisford, Abdul W BasitAbstractThree-dimensional printing (3DP) has the potential to cause a paradigm shift in pharmaceuticals, enabling personalised medicines to be produced on-demand. To facilitate integration into healthcare, non-destructive characterisation techniques are required to ensure final product quality. Here, the use of process analytical technologies (PAT), including near infrared spectroscopy (NIR) and Raman confocal...
Source: International Journal of Pharmaceutics - August 2, 2018 Category: Drugs & Pharmacology Source Type: research

Pharmacokinetics and Pharmacodynamics of High Doses of Inhaled Dry Powder Drugs
Publication date: Available online 2 August 2018Source: International Journal of PharmaceuticsAuthor(s): Manolya Kukut Hatipoglu, Anthony J. Hickey, Lucila Garcia-ContrerasAbstractFor many years, administration of drugs by inhalation has been the mainstay treatment for obstructive respiratory disorders such as asthma and chronic obstructive pulmonary disease. Antibiotics and other drugs have been administered for decades as aerosols to treat other pulmonary disease in a clinical setting, but it was until the early 1980’s that colistin was formally marketed as a solution for nebulization in Europe (Colomycin, Pharmax,...
Source: International Journal of Pharmaceutics - August 2, 2018 Category: Drugs & Pharmacology Source Type: research

Applications of mesoporous silica in biosensing and controlled release of insulin
Publication date: 5 October 2018Source: International Journal of Pharmaceutics, Volume 549, Issues 1–2Author(s): Maria Sönmez, Denisa Ficai, Anton Ficai, Laurentia Alexandrescu, Mihai Georgescu, Roxana Trusca, Dana Gurau, Mihail Aurel Titu, Ecaterina AndronescuAbstractThe development of new oral insulin delivery systems could bring significant benefits to insulin-dependent patients due to the simplicity of the method, avoidance of pain caused by parenteral administration and maintenance of optimal therapeutic levels for a longer period. However, administration of such therapeutic proteins orally remains a challe...
Source: International Journal of Pharmaceutics - August 2, 2018 Category: Drugs & Pharmacology Source Type: research

Model development and prediction of particle size distribution, density and friability of a comilling operation in a continuous pharmaceutical manufacturing process
Publication date: Available online 1 August 2018Source: International Journal of PharmaceuticsAuthor(s): Nirupaplava Metta, Maxim Verstraeten, Michael Ghijs, Ashish Kumar, Elisabeth Schafer, Ravendra Singh, Thomas De Beer, Ingmar Nopens, Philippe Cappuyns, Ivo Van Assche, Marianthi Ierapetritou, Rohit RamachandranAbstractThe comilling process plays an important role in solid oral dosage manufacturing. In this process, the granulated products are comminuted to the required size distribution through collisions created from a rotating impeller. In addition to predicting particle size distribution, there is a need to predict o...
Source: International Journal of Pharmaceutics - August 2, 2018 Category: Drugs & Pharmacology Source Type: research

Editorial Board
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - August 2, 2018 Category: Drugs & Pharmacology Source Type: research

Pickering nano-emulsion as a nanocarrier for pH-triggered drug release
This study investigates the formulation of surfactant-free Pickering nano-emulsions able to release a drug at specific pH, in order to enhance its oral bioavailability. The stabilizing nanoparticles composed of magnesium hydroxide, were obtained by nano-precipitation method. The oil-in-water Pickering nano-emulsions stabilized with Mg(OH)2 nanoparticles, and encapsulating a model of hydrophobic drug (ibuprofen) were formulated following a high-energy process, using a sonication probe. The experimental approach explored the impact of all formulation parameters, composition and size of Mg(OH)2 nanoparticles, on the physico-c...
Source: International Journal of Pharmaceutics - August 1, 2018 Category: Drugs & Pharmacology Source Type: research

Exosomes derived from TRAIL-engineered mesenchymal stem cells with effective anti-tumor activity in a mouse melanoma model
Publication date: Available online 31 July 2018Source: International Journal of PharmaceuticsAuthor(s): Fazileh Hosseini Shamili, Houshang Rafatpanah Bayegi, Zahra Salmasi, Kayvan Sadri, Mahmoud Mahmoudi, Mahmoudreza Kalantari, Mohammad Ramezani, Khalil AbnousGraphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - August 1, 2018 Category: Drugs & Pharmacology Source Type: research

Optimization of Linalool-loaded Solid Lipid Nanoparticles using Experimental Factorial Design and Long-term Stability Studies with a New Centrifugal Sedimentation Method
Publication date: Available online 31 July 2018Source: International Journal of PharmaceuticsAuthor(s): Irina Pereira, Zielińska, Nuno R. Ferreira, Amélia M. Silva, Eliana B. SoutoAbstractLinalool (C10H18O), also known as 3, 7-dimethyl-1, 6-octadien-3-ol, is the most common acyclic monoterpene tertiary alcohol present in essential oils of several aromatic plant species. Previous studies indicate that linalool is a valuable compound with a wide range of therapeutic properties. The promising therapeutic effects of linalool are however limited by its poor water solubility and volatility. Recently, the encapsulation of...
Source: International Journal of Pharmaceutics - August 1, 2018 Category: Drugs & Pharmacology Source Type: research

The novel immunogenic chimeric peptide vaccine to elicit potent cellular and mucosal immune responses against HTLV-1
This study reports on the immunogenicity assessment of a novel chimeric peptide vaccine including Tax, gp21, gp46, and gag immunodominant epitopes of human T-cell lymphotropic virus type 1 (HTLV-1) to induce immunity against HTLV-1 after subcutaneous (SC) or intranasal administration in a mice model. Additionally, to elevate the efficacy of the HTLV-1 vaccine, the chimera was physically mixed with monophosphoryl lipid A (MPLA) or ISCOMATRIX (IMX) adjuvants. For this purpose, the ISCOMATRIX with a size range of 40 to 60 nm were prepared using lipid film hydration method. Our investigation revealed that the mixture of IMX an...
Source: International Journal of Pharmaceutics - August 1, 2018 Category: Drugs & Pharmacology Source Type: research

A redispersible dry emulsion system with simvastatin prepared via fluid bed layering as a means of dissolution enhancement of a lipophilic drug
Publication date: Available online 1 August 2018Source: International Journal of PharmaceuticsAuthor(s): Mitja Pohlen, Luka Pirker, Matevž Luštrik, Rok DreuAbstractThe purpose of the study was to develop a redispersible dry emulsion, containing a lipophilic, poorly water soluble model drug simvastatin, by employing fluid bed coating technology. The presented dry emulsion manufacturing approach produces pellets in a way, where a layer of the dry emulsion is applied to a neutral core. In the preliminary formulation development phase 1-oleoyl-rac-glycerol was chosen as the oily lipid phase, based on the high drug solu...
Source: International Journal of Pharmaceutics - August 1, 2018 Category: Drugs & Pharmacology Source Type: research

Glutathione-responsive self-delivery nanoparticles assembled by curcumin dimer for enhanced intracellular drug delivery
Publication date: Available online 31 July 2018Source: International Journal of PharmaceuticsAuthor(s): Huabing Zhang, Yubin Zhang, Yilin Chen, Ying Zhang, Yange Wang, Yinying Zhang, Liang Song, Beili Jiang, Guanghao Su, Yang Li, Zhenqing HouAbstractPoor water solubility, short half-life, and low drug efficacy posed a challenge for clinical application of curcumin (CUR). In this work, a kind of CUR prodrug was synthesized by coupling two CUR molecules with a mono-thioether linker for glutathione (GSH)-responsive drug delivery. The synthesized CUR prodrug (CUR-S-CUR dimer) could self-assemble into the homogeneous spherical ...
Source: International Journal of Pharmaceutics - July 31, 2018 Category: Drugs & Pharmacology Source Type: research

Aspartame as a co-former in co-amorphous systems
In conclusion, aspartame has been shown to be a promising co-former in co-amorphous systems, superior to the single amino acids or their mixtures.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 31, 2018 Category: Drugs & Pharmacology Source Type: research

Carrier free indomethacin microparticles for dry powder inhalation
In conclusion, a promising powder formulation for DPIs has been developed to treat, locally and systemically, inflammatory diseases.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 30, 2018 Category: Drugs & Pharmacology Source Type: research

Recent advancements in oral administration of insulin-loaded liposomal drug delivery systems for diabetes mellitus
Publication date: Available online 30 July 2018Source: International Journal of PharmaceuticsAuthor(s): Chun Y. Wong, Hani Al-Salami, Crispin R. DassAbstractDiabetes is a chronic medical condition, which is characterised by high blood sugar level. Exogenous insulin is commonly administered subcutaneously for the management of diabetes. However, daily injections of insulin could result in poor patient compliance and various side-effects. Although oral administration offers benefits, insulin is vulnerable to enzymatic degradation, chemical instability and poor gastrointestinal absorption. There is an absence of reviews on in...
Source: International Journal of Pharmaceutics - July 30, 2018 Category: Drugs & Pharmacology Source Type: research

Optical diagnostics studies of air flow and powder fluidisation in Nexthaler®. Part II: Use of fluorescent imaging to characterise transient release of fines from a dry powder inhaler
Publication date: 5 October 2018Source: International Journal of Pharmaceutics, Volume 549, Issues 1–2Author(s): C. Merusi, G. Brambilla, E.J. Long, G.K. Hargrave, H.K. VersteegAbstractThe fine particle fraction is a key indicator of therapeutic effectiveness of inhaled pharmaceutical aerosols. This paper presents a fluorescence imaging technique to visualise and characterise the emission of active pharmaceutical ingredient (API) fines in model formulations containing coarse lactose carrier and 1.5–2 μm diameter fluorescent microspheres (model API fines). A two-camera arrangement was used to acquire simult...
Source: International Journal of Pharmaceutics - July 30, 2018 Category: Drugs & Pharmacology Source Type: research

Inline Acoustic Monitoring to Determine Fluidized Bed Performance During Pharmaceutical Coating
Publication date: Available online 29 July 2018Source: International Journal of PharmaceuticsAuthor(s): Allan Carter, Lauren BriensGraphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 30, 2018 Category: Drugs & Pharmacology Source Type: research

Inkjet Printing of T3 and T4 Oral Drug Combinations as a Novel Strategy for Hypothyroidism
In this study, a two-cartridge TIJ printer was modified such that it could print separate solutions of T3 and T4. Dose adjustments were achieved by printing solutions adjacent to each other, enabling therapeutic T3 (15–50 μg) and T4 dosages (60–180 μg) to be successfully printed. Excellent linearity was observed between the theoretical and measured dose for both T3 and T4 (R2 = 0.982 and 0.985, respectively) by changing the length of the print objective (Y-value). Rapid disintegration of the ODFs was achieved (
Source: International Journal of Pharmaceutics - July 30, 2018 Category: Drugs & Pharmacology Source Type: research

Dendrimers: A versatile nanocarrier for drug delivery and targeting
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Atul P. Sherje, Mrunal Jadhav, Bhushan R. Dravyakar, Darshana KadamAbstractDendrimers are novel polymeric nanoarchitectures characterized by hyper-branched 3D-structure having multiple functional groups on the surface that increases their functionality and make them versatile and biocompatible. Their unique properties like nanoscale uniform size, high degree of branching, polyvalency, water solubility, available internal cavities and convenient synthesis approaches make them promising agent for biological and dru...
Source: International Journal of Pharmaceutics - July 28, 2018 Category: Drugs & Pharmacology Source Type: research

Gel formation of puerarin and mechanistic study during its cooling process
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Zunting Pang, Yuanfeng Wei, Ningning Wang, Jianjun Zhang, Yuan Gao, Shuai QianAbstractRecently, low molecular weight gelators are getting increasing interests in pharmaceutical field. In the current study, puerarin (PUE), a natural and bioactive flavonoid from the plant Pueraria lobata, was found to be able to gelate water to form hydrogel during cooling down process of its hot solution. In order to explore its gelation mechanism, the crystallization process, characterization, interaction force, morphology, rheol...
Source: International Journal of Pharmaceutics - July 28, 2018 Category: Drugs & Pharmacology Source Type: research

Subcutaneous administration of Lyso-phosphatidylserine nanoparticles induces immunological tolerance towards Factor VIII in a Hemophilia A mouse model
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Fiona Y. Glassman, Sathy V. Balu-IyerAbstractA major complication with enzyme replacement therapy of Factor VIII (FVIII) in Hemophilia A (HA) is the development of anti-drug antibodies. Recently, we have shown that FVIII administration in the presence of heterogeneous phosphatidylserine (PS) nanoparticles derived from a natural source induces tolerance to FVIII, suggesting that PS converts an immunogen to a tolerogen. However, the specific structural features responsible for the immune-regulatory properties of PS...
Source: International Journal of Pharmaceutics - July 28, 2018 Category: Drugs & Pharmacology Source Type: research

Gluing Pills Technology: A novel route to multilayer tablet manufacturing
This study shows the feasibility of the GPT for manufacturing of robust MLT, emphasizing its potential in terms of real-time production of individualized fixed-dose combinations and application in both translational pharmaceutics and personalized medicine.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 28, 2018 Category: Drugs & Pharmacology Source Type: research

Novel salts of dipicolinic acid as viscosity modifiers for high concentration antibody solutions
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Peng Ke, Iris L. Batalha, Andrew Dobson, Esther Tejeda-Montes, Sofia Ekizoglou, Graham Christie, James McCabe, Christopher F. van der WalleAbstractConcentrated monoclonal antibody (mAb) solutions can lead to high viscosity as a result of protein-protein interactions and pose challenges for manufacture. Dipicolinic acid (DPA, pyridine-2,6-dicarboxylic acid) is a potential excipient for reduction of protein solution viscosity and here we describe new DPA salts with improved aqueous solubility. Crystallinity and sol...
Source: International Journal of Pharmaceutics - July 28, 2018 Category: Drugs & Pharmacology Source Type: research

Solid state 13C NMR spectroscopy provides direct evidence for reaction between ethinyl estradiol and a silicone elastomer vaginal ring drug delivery system
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Clare F. McCoy, David C. Apperley, Bruce Variano, Heather Sussman, Daniel Loeven, Peter Boyd, R. Karl MalcolmAbstractSteroid molecules have a long history of incorporation into silicone elastomer materials for controlled release drug delivery applications. Previously, based on in vitro release testing and drug content analysis, we demonstrated indirectly that the contraceptive progestin levonorgestrel (LNG) chemically and irreversibly binds to addition cure silicone elastomers, presumably via a hydrosilylation re...
Source: International Journal of Pharmaceutics - July 28, 2018 Category: Drugs & Pharmacology Source Type: research

Nanoparticle formulations that allow for sustained delivery and brain targeting of the neuropeptide oxytocin
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Rokon Uz Zaman, Nihal S. Mulla, Keegan Braz Gomes, Cherilyn D'Souza, Kevin Sean Murnane, Martin J. D'SouzaAbstractOxytocin is a promising candidate for the treatment of social-deficit disorders such as Autism Spectrum Disorder, but oxytocin cannot readily pass the blood-brain barrier. Moreover, oxytocin requires frequent dosing as it is rapidly metabolized in blood. We fabricated four polymeric nanoparticle formulations using poly(lactic-co-glycolic acid) (PLGA) or bovine serum albumin (BSA) as the base material....
Source: International Journal of Pharmaceutics - July 28, 2018 Category: Drugs & Pharmacology Source Type: research

Audible acoustic emission data analysis for active pharmaceutical ingredient concentration prediction during tableting processes
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Ryoma Tanaka, Kenta Kojima, Yusuke Hattori, Kazuhide Ashizawa, Makoto OtsukaGraphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 28, 2018 Category: Drugs & Pharmacology Source Type: research

Dosing challenges in respiratory therapies
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Stewart Yeung, Daniela Traini, David Lewis, Paul M. YoungAbstractThe pulmonary route of administration has been commonly used for local lung conditions such as asthma and chronic obstructive pulmonary disease (COPD). Recently, with the advent of new technologies available for both formulation and device design, molecules usually delivered at high doses, such as antibiotics and insulin to treat cystic fibrosis (CF) and diabetes, respectively, can now be delivered by inhalation as a dry powder. These molecules are ...
Source: International Journal of Pharmaceutics - July 28, 2018 Category: Drugs & Pharmacology Source Type: research

Sulindac encapsulation and release from functional poly(HEMA) microparticles prepared in supercritical carbon dioxide
Publication date: Available online 26 July 2018Source: International Journal of PharmaceuticsAuthor(s): Rahmet Parilti, Raphaël Riva, Steven M. Howdle, Christine Dupont-Gillain, Christine JeromeAbstractSulindac loaded poly(HEMA) cross-linked microparticles were synthesized via one-pot free-radical dispersion polymerisation in supercritical carbon dioxide (scCO2) in presence of photocleavable diblock stabilisers based on polyethylene oxide (PEO) and poly(heptadecafluorodecyl acrylate) (PFDA) bearing a o-nitrobenzyl photosensitive junction (hv) (PEO-hv-PFDA), and ethylene glycol dimethacrylate (EGDMA) as cross-linker. P...
Source: International Journal of Pharmaceutics - July 26, 2018 Category: Drugs & Pharmacology Source Type: research

Effect of absorption-modifying excipients, hypotonicity, and enteric neural activity in an in vivo model for small intestinal transport
Publication date: Available online 26 July 2018Source: International Journal of PharmaceuticsAuthor(s): D. Dahlgren, C. Roos, A. Lundqvist, C. Tannergren, M. Sjöblom, E. Sjögren, H. LennernäsAbstractThe small intestine mucosal barrier is physiologically regulated by the luminal conditions, where intestinal factors, such as diet and luminal tonicity, can affect mucosal permeability. The intestinal barrier may also be affected by absorption-modifying excipients (AME) in oral drug delivery systems. Currently, there is a gap in the understanding of how AMEs interact with the physiological regulation of intestina...
Source: International Journal of Pharmaceutics - July 26, 2018 Category: Drugs & Pharmacology Source Type: research

Investigation of miscibility estimation methods between indomethacin and poly(vinylpyrrolidone-co-vinyl acetate)
Publication date: 5 October 2018Source: International Journal of Pharmaceutics, Volume 549, Issues 1–2Author(s): Romina Pezzoli, John G. Lyons, Noel Gately, Clement L. HigginbothamAbstractThe investigation of the miscibility between active pharmaceutical ingredients (API’s) and polymeric excipients is of great interest for the formulation and development of amorphous solid dispersions, especially in the context of the prediction of the stability of these systems. Two different methods were applied to determine the miscibility between model compounds poly(vinylpyrrolidone-co-vinyl acetate) (PVPVA) and indomethac...
Source: International Journal of Pharmaceutics - July 26, 2018 Category: Drugs & Pharmacology Source Type: research

Extemporaneous Preparation Strategy for Early Phase Clinical Studies
Publication date: Available online 25 July 2018Source: International Journal of PharmaceuticsAuthor(s): Rampurna P. Gullapalli, Carolyn L. Mazzitelli, Christina M. Charriez, David J. Carpenter, Rebecca D. Crean, Bobbie Carter, Phil PereraAbstractExtemporaneous preparations (EPs) of investigational drugs, which are compounded at the clinical study site by a pharmacist, are being increasingly used in early phase clinical studies to accelerate the development of new medicines. The successful application of EP strategies in clinical studies requires ‘fit-for-purpose’ formulation design and preparation processes, as...
Source: International Journal of Pharmaceutics - July 26, 2018 Category: Drugs & Pharmacology Source Type: research

Topical delivery of climbazole to mammalian skin
Publication date: Available online 25 July 2018Source: International Journal of PharmaceuticsAuthor(s): Miguel Paz-Alvarez, Paul D.A. Pudney, Jonathan Hadgraft, Majella E. LaneAbstractDandruff is a common condition, affecting up to half the global population of immunocompetent adults at some time during their lives and it has been highly correlated with the over-expression of the fungus Malassezia spp. Climbazole (CBZ) is used as an antifungal and preservative agent in many marketed formulations for the treatment of dandruff. While the efficacy of CBZ in vitro and in vivo has previously been reported, limited information h...
Source: International Journal of Pharmaceutics - July 26, 2018 Category: Drugs & Pharmacology Source Type: research

Engineering of budesonide-loaded lipid-polymer hybrid nanoparticles using a quality-by-design approach
Publication date: Available online 25 August 2017Source: International Journal of PharmaceuticsAuthor(s): Donglei Leng, Kaushik Thanki, Elias Fattal, Camilla Foged, Mingshi YangAbstractChronic obstructive pulmonary disease (COPD) is a complex disease, characterized by persistent airflow limitation and chronic inflammation. The purpose of this study was to design lipid-polymer hybrid nanoparticles (LPNs) loaded with the corticosteroid, budesonide, which could potentially be combined with small interfering RNA (siRNA) for COPD management. Here, we prepared LPNs based on the biodegradable polymer poly(dl-lactic-co-glycolic ac...
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Nucleic acid loading and fluorescent labeling of isolated extracellular vesicles requires adequate purification
Publication date: Available online 12 October 2017Source: International Journal of PharmaceuticsAuthor(s): Stephan Stremersch, Toon Brans, Kevin Braeckmans, Stefaan De Smedt, Koen RaemdonckAbstractExtracellular vesicles (EVs) are nanosized vesicular structures released by cells to communicate with one another. The growing interest in the (patho)physiological function and potential pharmaceutical application of these vesicles is accompanied by a vast number of new research groups entering this research field and a plethora of different protocols to separate EVs from non-vesicular components. This lack of uniformity often ge...
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Fabrication and characterization of gefitinib-releasing polyurethane foam as a coating for drug-eluting stent in the treatment of bronchotracheal cancer
In conclusion, we have fabricated drug-loaded PU foams that are suitable for bronchotracheal stent coating.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

E-selectin targeted immunoliposomes for rapamycin delivery to activated endothelial cells
In this study we developed anti-E-selectin immunoliposomes for targeted delivery to E-selectin over-expressing tumor necrosis factor-α (TNF-α) activated endothelial cells. Liposomes composed of 1,2-dipalmitoyl-sn-glycero-3.;hosphocholine (DPPC), Cholesterol, and 1,2-Distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethyleneglycol)-2000]-maleimide (DSPE-PEG-Mal) were loaded with rapamycin via lipid film hydration, after which they were further functionalized by coupling N-succinimidyl-S-acetylthioacetate (SATA)-modified mouse anti human E-selectin antibodies to the distal ends of the maleimidyl (Mal)-PE...
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

PLGA-PEG nanoparticles for targeted delivery of the mTOR/PI3kinase inhibitor dactolisib to inflamed endothelium
In conclusion, E-selectin targeted nanoparticles have a high potential in delivering the potent mTOR/pI3K inhibitor dactolisib to inflamed endothelial cells and are an interesting nanomedicine for anti-inflammatory therapy.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Functionalized PLA polymers to control loading and/or release properties of drug-loaded nanoparticles
In this study, we sought to show the possibility of influencing these properties by modifying the structure of the constituting polymer. Seven non-functionalized or functionalized PLA polymers were specifically designed and synthesized by microwave-assisted ring-opening polymerization of d,l-lactide. They presented short hydrophobic and/or hydrophilic groups thanks to the use of C20 aliphatic chain, mPEG1000, sorbitan esters (Spans®) or polysorbates (Tweens®), their PEGylated analogues, as initiators. Then, seven types of drug-loaded nanoparticles (NP) were prepared from these polymers and compared in terms of phys...
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Influence of cholesterol inclusion on the doxorubicin release characteristics of lysolipid-based thermosensitive liposomes
Publication date: Available online 7 November 2017Source: International Journal of PharmaceuticsAuthor(s): Negar Sadeghi, Roel Deckers, Burcin Ozbakir, Sohail Akthar, Robbert Jan Kok, Twan Lammers, Gert StormAbstractFast hyperthermia (i.e. 39–42 °C) triggered doxorubicin release from lysolipid-containing thermosensitive liposomes (LTSL) in the tumor vasculature has been demonstrated to result in considerable enhancement of bioavailable drug levels in heated tumor tissue in preclinical tumor models. However, there is also significant leakage of doxorubicin already at 37 °C in the bloodstream, mak...
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Relationship between polarities of antibiotic and polymer matrix on nanoparticle formulations based on aliphatic polyesters
Publication date: Available online 11 November 2017Source: International Journal of PharmaceuticsAuthor(s): J.A.S. Ritsema, E.M.A. Herschberg, S.E. Borgos, C. Løvmo, R. Schmid, Y.M. te Welscher, G. Storm, C.F. van NostrumAbstractIn the field of nanomedicine, nanoparticles are developed to target antibiotics to sites of bacterial infection thus enabling adequate drug exposure and decrease development of resistant bacteria. In the present study, we investigated the encapsulation of two antibiotics with different polarity into different PEGylated polymeric nanoparticles based on aliphatic polyesters, to obtain a better...
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Critical evaluation of quantification methods for oligonucleotides formulated in lipid nanoparticles
Publication date: Available online 21 December 2017Source: International Journal of PharmaceuticsAuthor(s): Erik Oude Blenke, Martijn J.W. Evers, Volker Baumann, Johannes Winkler, Gert Storm, Enrico MastrobattistaAbstractThere is a very large variety in the types of nanoparticulate lipid formulations for oligonucleotides, and remarkably, also a very large heterogeneity in the methods that are used for analyzing oligonucleotide load, encapsulation efficiency and oligonucleotide release. Furthermore, a literature survey showed that the extent to which these procedures are reported in scientific literature varies greatly, wit...
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Tablets made from paper
Publication date: Available online 1 June 2018Source: International Journal of PharmaceuticsAuthor(s): Florian Stumpf, Cornelia M. KeckAbstractThe possibility to compress ordinary paper into tablets was systematically investigated in this study. Results proved that tablets can be made from paper, independent of the type of paper used. The tablets appear shiny and with a smooth surface. The pharmaceutical quality was acceptable, i.e. all tablets fulfilled the requirements for tablets according to the European Pharmacopeia. Drug-loaded tablets were produced by compression of drug-loaded paper. Drug loading did not alter the ...
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Selected contributions from the 10th European Workshop on Particulate Systems, Copenhagen 19th–20th January 2017
Publication date: Available online 6 June 2018Source: International Journal of PharmaceuticsAuthor(s): C. Foged (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Monoolein cubic phases containing cinnamic acid, poly(ethyleneimine) and gold nanoparticle and their UV- and NIR-responsive release property
Publication date: Available online 19 June 2018Source: International Journal of PharmaceuticsAuthor(s): Danbi Park, Jin-Chul KimAbstractUV and NIR-responsive monoolein cubic phase was prepared by including poly(ethyleneimine) (PEI)/cinnamic acid (CA) conjugate and gold nanoparticle (GNP) within its structure. UV irradiation elevated significantly the release % of Auramine O loaded in cubic phase containing PEI/CA, possibly because of the trans-to-cis isomerization of CA. NIR irradiation also increased significantly the release % of FITC-dextran loaded in cubic phase containing PEI/CA. The release % of the dye loaded in cub...
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Exploring gastric drug absorption in fasted and fed state rats
In this study, an in situ gastric bolus administration model was used to study the gastric absorption of pharmaceutical compounds in fasted and fed state rats. Three drugs [paracetamol (neutral), diclofenac (acidic) and posaconazole (basic)] were administered directly into the stomach as solution (paracetamol and diclofenac) or suspension (posaconazole). Transfer to the intestine was blocked by ligating the pylorus; as a reference, non-ligated conditions were used. Blood samples were collected and gastric absorption was assessed by the appearance of compounds in the systemic circulation. Paracetamol and diclofenac were rea...
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Direct Quantification of Unencapsulated Doxorubicin in Liposomal Doxorubicin Formulations Using Capillary Electrophoresis
In this study, a capillary electrophoresis (CE) with UV-Vis detection method was developed for the simultaneous separation and quantification of unencapsulated drug from liposome-associated drug using a doxorubicin-containing liposome formulation as the model drug. CE separates the unencapsulated drug and liposomal drugs based on their electrophoretic mobility under the electric field. Liposomal drugs were diluted to the appropriate concentrations with running buffer or 5% dextrose before hydrodynamic sample injection. Using a high-sensitivity detection cell, the doxorubicin detection sensitivity was enhanced about 10-fold...
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research

Optical diagnostics studies of air flow and powder fluidisation in Nexthaler® Part II: Use of fluorescent imaging to characterise transient release of fines from a dry powder inhaler
Publication date: Available online 11 July 2018Source: International Journal of PharmaceuticsAuthor(s): C. Merusi, G. Brambilla, E.J. Long, G.K. Hargrave, H.K. VersteegAbstractThe fine particle fraction is a key indicator of therapeutic effectiveness of inhaled pharmaceutical aerosols. This paper presents a fluorescence imaging technique to visualise and characterise the emission of active pharmaceutical ingredient (API) fines in model formulations containing coarse lactose carrier and 1.5-2 μm diameter fluorescent microspheres (model API fines). A two-camera arrangement was used to acquire simultaneous images of spatia...
Source: International Journal of Pharmaceutics - July 25, 2018 Category: Drugs & Pharmacology Source Type: research