Release characteristics of cellulose sulphate capsules and production of cytokines from encapsulated cells
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Brian Salmons, Walter H. GunzburgAbstractThe size and speed of release of proteins of different sizes from standard cellulose sulphate capsules (Cell-in-a-Box®) was investigated. Proteins with molecular weights of up to around 70kD can be released. The conformation, charge and concentration of the protein being released play a role in the release kinetics. Small proteins such as cytokines can be easily released. The ability to produce cytokines at a sustained and predefined level from encapsulated cells genet...
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

Optimizing feed frame design and tableting process parameters to increase die-filling uniformity on a high-speed rotary tablet press
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): W. Grymonpré, V. Vanhoorne, B. Van Snick, B. Blahova Prudilova, F. Detobel, J.P. Remon, T. De Beer, C. VervaetAbstractDespite the high quantities of tablets produced daily, many tableting processes are still operated at sub-optimal settings and hence lack the necessary flexibility to mitigate for possible process deviations. However, to ensure this flexibility on tableting throughput it is important to select the most robust feed frame design and settings regarding die-filling. In this research study, four...
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

Radioactive holmium phosphate microspheres for cancer treatment
In conclusion, this study shows that stable radioactive HoPO4-MS can be prepared with suitable properties to be used for cancer therapy.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

Evaluation of novel formulations of d-β-hydroxybutyrate and melatonin in a rat model of hemorrhagic shock
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Andrea Wolf, Seema Thakral, Kristine E. Mulier, Raj Suryanarayanan, Gregory J BeilmanAbstractd-β-hydroxybutyrate and melatonin (BHB/MLT) infusion improves survival in hemorrhagic shock models. The original BHB/MLT formulation contains dimethyl sulfoxide (DMSO) to increase melatonin solubility. We formulated BHB/MLT solutions wherein DMSO was replaced either with 10% polyvinylpyrrolidone (BHB/MLT/PVP) or with 5% hydroxypropyl-β-cyclodextrin/2.5% PVP/2.5% polyethylene glycol 400 (BHB/MLT/CD). Safety and e...
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

Entangled and colloidally stable microcrystalline cellulose matrices in controlled drug release
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Yujiao Dong, Heli Paukkonen, Wenwen Fang, Eero Kontturi, Timo Laaksonen, Päivi LaaksonenAbstractDrug release from a new type of matrix material consisting of partially fibrillated microcrystalline cellulose was investigated. A mechanical treatment of novel AaltoCell™ cellulose microcrystals caused partial opening of the nanofibrillary structure of the cellulose particles and entanglement of individual particles led into formation of an elastic network of microcrystalline cellulose. The rheological prop...
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

Characterization of the suspension stability of pharmaceuticals using a shadowgraphic imaging method
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Hui Wang, Penny Tan, David Barona, Grace Li, Susan Hoe, David Lechuga-Ballesteros, David S. Nobes, Reinhard VehringAbstractA new shadowgraphic imaging method and an associated instrument for analyzing the physical stability of pharmaceutical suspensions are introduced in this paper. The new suspension tester consists mainly of a high-resolution camera that takes sequential shadowgraphic images of emulsions or suspensions and a 2D collimated LED for simultaneous whole-sample illumination in bright field. A built-i...
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

Contact lenses with dual drug delivery for the treatment of bacterial conjunctivitis
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Furqan A. Maulvi, Sulabh S. Singhania, Ankita R. Desai, Manish R. Shukla, Aniruddha S. Tannk, Ketan M. Ranch, Bhavin A. Vyas, Dinesh O. ShahAbstractCurrently, bacterial conjunctivitis is treated by frequent administration of antibiotic eye drop solutions, which is tedious and patient noncompliant. Contact lenses could be ideal medical devices to sustain the release of ophthalmic drugs, but the incorporation of the latter can alter the optical and physical properties of the lenses. In addition, many contact lens u...
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

Formulation of delivery systems with risperidone based on biodegradable terpolymers
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Artur Turek, Aleksandra Borecka, Henryk Janeczek, Michał Sobota, Janusz KasperczykAbstractRisperidone is applied in oral dosage formulations in the treatment of mental diseases. Current trends point toward parenteral delivery systems based on poly(lactide-co-glycolide), with wafers or rods being the more attractive option than the routinely used intramuscular suspension with microparticles. The aim of our work was to study the utility of solution casting and hot melt extrusion in the formulation of wafers and ro...
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

Low molecular-weight hyaluronan as a cryoprotectant for the storage of microencapsulated cells
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): H. Gurruchaga, L. Saenz del Burgo, G. Orive, R.M. Hernandez, J. Ciriza, J.L. PedrazAbstractThe low-temperature storage of therapeutic cell-based products plays a crucial role in their clinical translation for the treatment of diverse diseases. Although dimethylsulfoxide (DMSO) is the most successful cryoprotectant in slow freezing of microencapsulated cells, it has shown adverse effects after cryopreserved cell-based products implantation. Therefore, the search of alternative non-toxic cryoprotectants for encapsu...
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

DPI formulations for high dose applications – Challenges and opportunities
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Regina Scherließ, Christian EtschmannAbstractThis opinion piece gives reasons for high dose DPI applications, points out challenges and shows opportunities and possible solutions for high dose DPI. This piece of work shall set the stage for more in-depth reviews of state of the art and research papers addressing the challenges of high dose DPI which shall be included in the special issue of IJP. (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

New insights on the structure of hexagonally faceted platelets from hydrophobically modified chitosan and α-cyclodextrin
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Zeeshan Ahmed, Sophia Malli, Raul Diaz-Salmeron, Pierre-Louis Destruel, Antonio Da Costa, Jean-Michel Guigner, Florence Porcher, Benoit Baptiste, Gilles Ponchel, Kawthar BouchemalAbstractA new class of non-spherical particles was recently designed in our research group by mixing a polysaccharide grafted with fatty acids and α-cyclodextrin in water. Because their flat surfaces, and according to their size, particles are called micro- or nano-platelets. Here, we varied the composition of fatty acids grafted o...
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

Smart liposomal drug delivery for treatment of oxidative stress model in human embryonic stem cell-derived retinal pigment epithelial cells
In this study, we suggested an antioxidant delivery system based on redox-sensitive liposome composed of phospholipids and a diselenide centered alkyl chain. Dynamic light scattering assessment indicated that the liposomes had an average size of 140 nm with a polydispersity index below 0.2. The percentage of encapsulation efficiency of the liposomes was calculated by high-performance liquid chromatography. The carriers were loaded with N-acetyl cysteine as a model antioxidant drug. We demonstrated responsiveness of the nanocarrier and its efficiency in drug delivery in an oxidative stress model of human embryonic stem ce...
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

Are phytosomes a superior nanodelivery system for the antioxidant rutin?
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Hanh T.H. Vu, Sarah M. Hook, Scheyla D. Siqueira, Anette Müllertz, Thomas Rades, Arlene McDowellAbstractRutin, a strong antioxidant, has been implicated in the prevention of liver inflammation. However, low solubility and permeability through the gut wall limit development of rutin as a therapeutic agent for oral administration. Phytosomes are described as lipid nanocarriers with a complexation between the phospholipid headgroups and entrapped phytochemicals. The aim of this research was to compare the struc...
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

In situ fabrication of mesoporous silica-coated silver-gold hollow nanoshell for remotely controllable chemo-photothermal therapy via phase-change molecule as gatekeepers
This study reports a new strategy for in situ fabrication of plasmonic hollow silver-gold nanoshell (with resonance tuned to NIR region) encased in the hollow mesoporous silica as an efficient platform to efficiently and precisely regulate the release of 5-fluorouracil (anticancer drug) for prostate cancer therapy and photothermal therapy. The mesopores were capped with thermosensitive phase-change material lauric acid, which allowed for remote, precise, and spatiotemporal control of drug release via external heating or photothermal heating of plasmonic silver-gold nanoshell via NIR laser irradiation. The system was nanome...
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

Intra-articular nonviral gene therapy in mucopolysaccharidosis I mice
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Juliana Bidone, Roselena Silvestri Schuh, Mirian Farinon, Édina Poletto, Gabriela Pasqualim, Patrícia Gnieslaw de Oliveira, Michelle Fraga, Ricardo Machado Xavier, Guilherme Baldo, Helder Ferreira Teixeira, Ursula MatteAbstractMucopolysaccharidosis type I (MPS I) is caused by the lysosomal accumulation of glycosaminoglycans (GAGs) due to the deficiency of the enzyme alpha-L-iduronidase (IDUA). Currently available treatments may improve several clinical manifestations, but they have limited effects o...
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

Edaravone, a cytoprotective drug, enhances transgene expression mediated by lipoplexes in HepG2 cells and mice
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Shu Wang, Shintaro Fumoto, Hirotaka Miyamoto, Masakazu Tanaka, Koyo NishidaAbstractA requirement of gene therapy is efficient nucleic acid delivery. However, the application of cationic liposomes to gene therapy is restricted by their inefficient transfection capacity, which may be caused by cytotoxicity. This cytotoxicity is highly dependent on cationic lipid-induced reactive oxygen species (ROS). Here, to provide cellular protection, we used edaravone, an efficacious anti-oxidative drug, to scavenge ROS during ...
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

Development of phospholipid nanoparticles encapsulating 3-O-cetyl ascorbic acid and tocopherol acetate (TA-Cassome) for improving their skin accumulation
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Tomoka Fushimi, Tomonobu Uchino, Yasunori Miyazaki, Ichiro Hatta, Miyuki Asano, Hiyori Fujino, Rie Suzuki, Shun Fujimori, Daichi Kamiya, Yoshiyuki KagawaAbstractPhospholipid nanoparticles (PNs) encapsulating vitamin C and E derivatives, 3-O-cetyl ascorbic acid (CA) and tocopherol acetate (TA), respectively, were examined using the film rehydration and extrusion method. PN formulations (TA-Cassome) were prepared by mixing CA, soya phosphatidylcholine (Soya PC), sodium cholate, and TA at a molar ratio of 20/80/5/6....
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

Mediterranean essential oils as precious matrix components and active ingredients of lipid nanoparticles
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): C. Carbone, C. Martins-Gomes, C. Caddeo, A.M. Silva, T. Musumeci, R. Pignatello, G. Puglisi, E.B. SoutoAbstractEssential oils are recognized as valuable active pharmaceutical ingredients attributed to a set of biological properties, which include antibacterial, antifungal, antiviral, antioxidant, anticancer, immune-modulatory, analgesic and anti-inflammatory activities. Their use in pharmaceutics is however compromised by their limited water solubility and low physicochemical stability (i.e. volatility, oxidation...
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

Hierarchical supramolecular platelets from hydrophobically-modified polysaccharides and α-cyclodextrin: Effect of hydrophobization and α-cyclodextrin concentration on platelet formation
The objective of this investigation is to tune platelet formation by modifying these two parameters, independently on polysaccharide composition. A systematic study was conducted by varying polysaccharide type (dextran, pullulan, amylopectin), degree of substitution (DS:0.1–5.6%) and α-cyclodextrin concentration (0–10 wt%) for a fixed concentration of polysaccharide esterified with palmitoyl groups (1 wt%). Characterizations include ATR-FTIR, elemental analysis, solid state 13C NMR and transmission electron microscopy. Abundant and well-organized hexagonal platelets were obtained with high DS (4.2&nda...
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

Preparation of spray dried submicron particles: Part B – Particle recovery by electrostatic precipitation
In conclusion, an ESP customized for collecting particles in the range of 0.1–1 µm was designed, built and tested, and collection efficiencies higher than 99% were achieved for submicron particle size distributions. For a robust process continuous cleaning of the charging stage is necessary.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

Development and characterization of gemcitabine hydrochloride loaded lipid polymer hybrid nanoparticles (LPHNs) using central composite design
The objective of this study was to design and optimize gemcitabine hydrochloride loaded LPHNs based on the central composite design approach. PLGA 50:50/PLGA 65:35 mass ratio (w/w), soya phosphatidylcholine (SPC)/polymer mass ratio (%, w/w) and amount of DSPE-PEG were chosen as the investigated independent variables. The LPHNs were prepared with modified double emulsion solvent evaporation method and characterized by testing their particle size, encapsulation efficiency, and cumulative release. The composition of optimal formulation was determined as 1,5 (w/w) PLGA 50:50/PLGA 65:35 mass ratio, 30% (w/w) SPC/polymer mass ra...
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

Considerations in preparing for clinical studies of inhaled rifampicin to enhance tuberculosis treatment
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Prakash Khadka, Jack Dummer, Philip C. Hill, Shyamal C. DasAbstractDrug delivery via the inhaled route has advantages for treating local and systemic diseases. Pulmonary drug delivery may have potential in treating tuberculosis (TB), which is mainly localised in the lung (pulmonary tuberculosis ∼75%) while also affecting other organs (extra-pulmonary tuberculosis). Currently, rifampicin, a first-line anti-tubercular drug, is given orally and the maximum daily oral dose is the lesser of 10 mg/kg or 600 mg....
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

Spherical neutral gold nanoparticles improve anti-inflammatory response, oxidative stress and fibrosis in alcohol-methamphetamine-induced liver injury in rats
This study aimed to elucidate the anti-inflammatory, anti-oxidant and antifibrotic effects of gold nanoparticles (GNPs) in rats subjected to liver injury with ethanol and Methamphetamine (METH). The liver injury was induced by gavage administrations of 30% alcoholic solution (7 g/kg) once a day during 28 days, followed by METH (10 mg/kg) on the 20th and 28th days of treatment. GNPs treatment (724.96 µg/kg) during the ethanol and METH exposure was associated with reduced steatosis, hepatic cord degeneration, fibrosis and necrosis. Furthermore, there was a reduction in biochemical markers of liver damage and ...
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

Mediterranean essential oils as precious matrix components and active ingredients of lipid nanoparticles
Publication date: 5 September 2018 Source:International Journal of Pharmaceutics, Volume 548, Issue 1 Author(s): C. Carbone, C. Martins-Gomes, C. Caddeo, A.M. Silva, T. Musumeci, R. Pignatello, G. Puglisi, E.B. Souto Essential oils are recognized as valuable active pharmaceutical ingredients attributed to a set of biological properties, which include antibacterial, antifungal, antiviral, antioxidant, anticancer, immune-modulatory, analgesic and anti-inflammatory activities. Their use in pharmaceutics is however compromised by their limited water solubility and low physicochemical stability (i.e. volatility, oxidation). In...
Source: International Journal of Pharmaceutics - July 4, 2018 Category: Drugs & Pharmacology Source Type: research

Dose administration maneuvers and patient care in tobramycin dry powder inhalation therapy
Publication date: 5 September 2018 Source:International Journal of Pharmaceutics, Volume 548, Issue 1 Author(s): Francesca Buttini, Anna Giulia Balducci, Gaia Colombo, Fabio Sonvico, Serena Montanari, Giovanna Pisi, Alessandra Rossi, Paolo Colombo, Ruggero Bettini The purpose of this work was to study a new dry powder inhaler (DPI) of tobramycin capable to simplify the dose administration maneuvers to maximize the cystic fibrosis (CF) patient care in antibiotic inhalation therapy. For the purpose, tobramycin/sodium stearate powder (TobraPS) having a high drug content, was produced by spray drying, characterized and the ae...
Source: International Journal of Pharmaceutics - July 4, 2018 Category: Drugs & Pharmacology Source Type: research

Development of phospholipid nanoparticles encapsulating 3-O-cetyl ascorbic acid and tocopherol acetate (TA-Cassome) for improving their skin accumulation
Publication date: 5 September 2018 Source:International Journal of Pharmaceutics, Volume 548, Issue 1 Author(s): Tomoka Fushimi, Tomonobu Uchino, Yasunori Miyazaki, Ichiro Hatta, Miyuki Asano, Hiyori Fujino, Rie Suzuki, Shun Fujimori, Daichi Kamiya, Yoshiyuki Kagawa Phospholipid nanoparticles (PNs) encapsulating vitamin C and E derivatives, 3-O-cetyl ascorbic acid (CA) and tocopherol acetate (TA), respectively, were examined using the film rehydration and extrusion method. PN formulations (TA-Cassome) were prepared by mixing CA, soya phosphatidylcholine (Soya PC), sodium cholate, and TA at a molar ratio of 20/80/5/6. Glyc...
Source: International Journal of Pharmaceutics - July 4, 2018 Category: Drugs & Pharmacology Source Type: research

Low molecular-weight hyaluronan as a cryoprotectant for the storage of microencapsulated cells
Publication date: 5 September 2018 Source:International Journal of Pharmaceutics, Volume 548, Issue 1 Author(s): H. Gurruchaga, L. Saenz del Burgo, G. Orive, R.M. Hernandez, J. Ciriza, J.L. Pedraz The low-temperature storage of therapeutic cell-based products plays a crucial role in their clinical translation for the treatment of diverse diseases. Although dimethylsulfoxide (DMSO) is the most successful cryoprotectant in slow freezing of microencapsulated cells, it has shown adverse effects after cryopreserved cell-based products implantation. Therefore, the search of alternative non-toxic cryoprotectants for encapsulated...
Source: International Journal of Pharmaceutics - July 4, 2018 Category: Drugs & Pharmacology Source Type: research

Edaravone, a cytoprotective drug, enhances transgene expression mediated by lipoplexes in HepG2 cells and mice
Publication date: 5 September 2018 Source:International Journal of Pharmaceutics, Volume 548, Issue 1 Author(s): Shu Wang, Shintaro Fumoto, Hirotaka Miyamoto, Masakazu Tanaka, Koyo Nishida A requirement of gene therapy is efficient nucleic acid delivery. However, the application of cationic liposomes to gene therapy is restricted by their inefficient transfection capacity, which may be caused by cytotoxicity. This cytotoxicity is highly dependent on cationic lipid-induced reactive oxygen species (ROS). Here, to provide cellular protection, we used edaravone, an efficacious anti-oxidative drug, to scavenge ROS during trans...
Source: International Journal of Pharmaceutics - July 3, 2018 Category: Drugs & Pharmacology Source Type: research

Intra-articular nonviral gene therapy in mucopolysaccharidosis I mice
Publication date: 5 September 2018 Source:International Journal of Pharmaceutics, Volume 548, Issue 1 Author(s): Juliana Bidone, Roselena Silvestri Schuh, Mirian Farinon, Édina Poletto, Gabriela Pasqualim, Patrícia Gnieslaw de Oliveira, Michelle Fraga, Ricardo Machado Xavier, Guilherme Baldo, Helder Ferreira Teixeira, Ursula Matte Mucopolysaccharidosis type I (MPS I) is caused by the lysosomal accumulation of glycosaminoglycans (GAGs) due to the deficiency of the enzyme alpha-L-iduronidase (IDUA). Currently available treatments may improve several clinical manifestations, but they have limited effects on joi...
Source: International Journal of Pharmaceutics - June 30, 2018 Category: Drugs & Pharmacology Source Type: research

In situ fabrication of mesoporous silica-coated silver-gold hollow nanoshell for remotely controllable chemo-photothermal therapy via phase-change molecule as gatekeepers
This study reports a new strategy for in situ fabrication of plasmonic hollow silver-gold nanoshell (with resonance tuned to NIR region) encased in the hollow mesoporous silica as an efficient platform to efficiently and precisely regulate the release of 5-fluorouracil (anticancer drug) for prostate cancer therapy and photothermal therapy. The mesopores were capped with thermosensitive phase-change material lauric acid, which allowed for remote, precise, and spatiotemporal control of drug release via external heating or photothermal heating of plasmonic silver-gold nanoshell via NIR laser irradiation. The system was nanome...
Source: International Journal of Pharmaceutics - June 30, 2018 Category: Drugs & Pharmacology Source Type: research

Formulation of delivery systems with risperidone based on biodegradable terpolymers
Publication date: 5 September 2018 Source:International Journal of Pharmaceutics, Volume 548, Issue 1 Author(s): Artur Turek, Aleksandra Borecka, Henryk Janeczek, Michał Sobota, Janusz Kasperczyk Risperidone is applied in oral dosage formulations in the treatment of mental diseases. Current trends point toward parenteral delivery systems based on poly(lactide-co-glycolide), with wafers or rods being the more attractive option than the routinely used intramuscular suspension with microparticles. The aim of our work was to study the utility of solution casting and hot melt extrusion in the formulation of wafers and rods wi...
Source: International Journal of Pharmaceutics - June 30, 2018 Category: Drugs & Pharmacology Source Type: research

Are phytosomes a superior nanodelivery system for the antioxidant rutin?
Publication date: 5 September 2018 Source:International Journal of Pharmaceutics, Volume 548, Issue 1 Author(s): Hanh T.H. Vu, Sarah M. Hook, Scheyla D. Siqueira, Anette Müllertz, Thomas Rades, Arlene McDowell Rutin, a strong antioxidant, has been implicated in the prevention of liver inflammation. However, low solubility and permeability through the gut wall limit development of rutin as a therapeutic agent for oral administration. Phytosomes are described as lipid nanocarriers with a complexation between the phospholipid headgroups and entrapped phytochemicals. The aim of this research was to compare the structure ...
Source: International Journal of Pharmaceutics - June 30, 2018 Category: Drugs & Pharmacology Source Type: research

Contact lenses with dual drug delivery for the treatment of bacterial conjunctivitis
Publication date: 5 September 2018 Source:International Journal of Pharmaceutics, Volume 548, Issue 1 Author(s): Furqan A. Maulvi, Sulabh S. Singhania, Ankita R. Desai, Manish R. Shukla, Aniruddha S. Tannk, Ketan M. Ranch, Bhavin A. Vyas, Dinesh O. Shah Currently, bacterial conjunctivitis is treated by frequent administration of antibiotic eye drop solutions, which is tedious and patient noncompliant. Contact lenses could be ideal medical devices to sustain the release of ophthalmic drugs, but the incorporation of the latter can alter the optical and physical properties of the lenses. In addition, many contact lens users ...
Source: International Journal of Pharmaceutics - June 30, 2018 Category: Drugs & Pharmacology Source Type: research

Characterization of the suspension stability of pharmaceuticals using a shadowgraphic imaging method
Publication date: 5 September 2018 Source:International Journal of Pharmaceutics, Volume 548, Issue 1 Author(s): Hui Wang, Penny Tan, David Barona, Grace Li, Susan Hoe, David Lechuga-Ballesteros, David S. Nobes, Reinhard Vehring A new shadowgraphic imaging method and an associated instrument for analyzing the physical stability of pharmaceutical suspensions are introduced in this paper. The new suspension tester consists mainly of a high-resolution camera that takes sequential shadowgraphic images of emulsions or suspensions and a 2D collimated LED for simultaneous whole-sample illumination in bright field. A built-in ult...
Source: International Journal of Pharmaceutics - June 30, 2018 Category: Drugs & Pharmacology Source Type: research

Entangled and colloidally stable microcrystalline cellulose matrices in controlled drug release
Publication date: 5 September 2018 Source:International Journal of Pharmaceutics, Volume 548, Issue 1 Author(s): Yujiao Dong, Heli Paukkonen, Wenwen Fang, Eero Kontturi, Timo Laaksonen, Päivi Laaksonen Drug release from a new type of matrix material consisting of partially fibrillated microcrystalline cellulose was investigated. A mechanical treatment of novel AaltoCell™ cellulose microcrystals caused partial opening of the nanofibrillary structure of the cellulose particles and entanglement of individual particles led into formation of an elastic network of microcrystalline cellulose. The rheological propertie...
Source: International Journal of Pharmaceutics - June 30, 2018 Category: Drugs & Pharmacology Source Type: research

Evaluation of novel formulations of d- β-hydroxybutyrate and melatonin in a rat model of hemorrhagic shock
Publication date: 5 September 2018 Source:International Journal of Pharmaceutics, Volume 548, Issue 1 Author(s): Andrea Wolf, Seema Thakral, Kristine E. Mulier, Raj Suryanarayanan, Gregory J Beilman d-β-hydroxybutyrate and melatonin (BHB/MLT) infusion improves survival in hemorrhagic shock models. The original BHB/MLT formulation contains dimethyl sulfoxide (DMSO) to increase melatonin solubility. We formulated BHB/MLT solutions wherein DMSO was replaced either with 10% polyvinylpyrrolidone (BHB/MLT/PVP) or with 5% hydroxypropyl-β-cyclodextrin/2.5% PVP/2.5% polyethylene glycol 400 (BHB/MLT/CD). Safety and effica...
Source: International Journal of Pharmaceutics - June 30, 2018 Category: Drugs & Pharmacology Source Type: research

Radioactive holmium phosphate microspheres for cancer treatment
In conclusion, this study shows that stable radioactive HoPO4-MS can be prepared with suitable properties to be used for cancer therapy. Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - June 30, 2018 Category: Drugs & Pharmacology Source Type: research

Formulation predictive dissolution (fPD) testing to advance oral drug product development: An introduction to the US FDA funded ‘21st Century BA/BE’ project
Publication date: 5 September 2018 Source:International Journal of Pharmaceutics, Volume 548, Issue 1 Author(s): Bart Hens, Patrick Sinko, Nicholas Job, Meagan Dean, Jozef Al-Gousous, Niloufar Salehi, Robert M. Ziff, Yasuhiro Tsume, Marival Bermejo, Paulo Paixão, James G. Brasseur, Alex Yu, Arjang Talattof, Gail Benninghoff, Peter Langguth, Hans Lennernäs, William L. Hasler, Luca Marciani, Joseph Dickens, Kerby Shedden, Duxin Sun, Gregory E. Amidon, Gordon L. Amidon Over the past decade, formulation predictive dissolution (fPD) testing has gained increasing attention. Another mindset is pushed forward where sc...
Source: International Journal of Pharmaceutics - June 30, 2018 Category: Drugs & Pharmacology Source Type: research

Smart liposomal drug delivery for treatment of oxidative stress model in human embryonic stem cell-derived retinal pigment epithelial cells
In this study, we suggested an antioxidant delivery system based on redox-sensitive liposome composed of phospholipids and a diselenide centered alkyl chain. Dynamic light scattering assessment indicated that the liposomes had an average size of 140 nm with a polydispersity index below 0.2. The percentage of encapsulation efficiency of the liposomes was calculated by high-performance liquid chromatography. The carriers were loaded with N-acetyl cysteine as a model antioxidant drug. We demonstrated responsiveness of the nanocarrier and its efficiency in drug delivery in an oxidative stress model of human embryonic stem ce...
Source: International Journal of Pharmaceutics - June 28, 2018 Category: Drugs & Pharmacology Source Type: research

DPI formulations for high dose applications – Challenges and opportunities
Publication date: 5 September 2018 Source:International Journal of Pharmaceutics, Volume 548, Issue 1 Author(s): Regina Scherließ, Christian Etschmann This opinion piece gives reasons for high dose DPI applications, points out challenges and shows opportunities and possible solutions for high dose DPI. This piece of work shall set the stage for more in-depth reviews of state of the art and research papers addressing the challenges of high dose DPI which shall be included in the special issue of IJP. (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - June 28, 2018 Category: Drugs & Pharmacology Source Type: research

Optimizing feed frame design and tableting process parameters to increase die-filling uniformity on a high-speed rotary tablet press
Publication date: 5 September 2018 Source:International Journal of Pharmaceutics, Volume 548, Issue 1 Author(s): W. Grymonpré, V. Vanhoorne, B. Van Snick, B. Blahova Prudilova, F. Detobel, J.P. Remon, T. De Beer, C. Vervaet Despite the high quantities of tablets produced daily, many tableting processes are still operated at sub-optimal settings and hence lack the necessary flexibility to mitigate for possible process deviations. However, to ensure this flexibility on tableting throughput it is important to select the most robust feed frame design and settings regarding die-filling. In this research study, four padd...
Source: International Journal of Pharmaceutics - June 28, 2018 Category: Drugs & Pharmacology Source Type: research

New insights on the structure of hexagonally faceted platelets from hydrophobically modified chitosan and α-cyclodextrin
Publication date: 5 September 2018 Source:International Journal of Pharmaceutics, Volume 548, Issue 1 Author(s): Zeeshan Ahmed, Sophia Malli, Raul Diaz-Salmeron, Pierre-Louis Destruel, Antonio Da Costa, Jean-Michel Guigner, Florence Porcher, Benoit Baptiste, Gilles Ponchel, Kawthar Bouchemal A new class of non-spherical particles was recently designed in our research group by mixing a polysaccharide grafted with fatty acids and α-cyclodextrin in water. Because their flat surfaces, and according to their size, particles are called micro- or nano-platelets. Here, we varied the composition of fatty acids grafted on chi...
Source: International Journal of Pharmaceutics - June 27, 2018 Category: Drugs & Pharmacology Source Type: research

Porous microspheres: Synthesis, characterisation and applications in pharmaceutical & amp; medical fields
Publication date: 5 September 2018 Source:International Journal of Pharmaceutics, Volume 548, Issue 1 Author(s): Debabrata Ghosh Dastidar, Sourabh Saha, Moumita Chowdhury Porous microspheres have interconnective external and internal pores leading to very low mass density and enormous specific surface area, enabling them to have excellent adsorption capabilities. Due to this uniqueness over traditional microsphere, they find extensive pharmaceutical applications. Porous microspheres are very promising for gastro retentive drug delivery, alveoli targeted drug delivery, high-speed chromatography, development of tissue regen...
Source: International Journal of Pharmaceutics - June 27, 2018 Category: Drugs & Pharmacology Source Type: research

Release characteristics of cellulose sulphate capsules and production of cytokines from encapsulated cells
Publication date: 5 September 2018 Source:International Journal of Pharmaceutics, Volume 548, Issue 1 Author(s): Brian Salmons, Walter H. Gunzburg The size and speed of release of proteins of different sizes from standard cellulose sulphate capsules (Cell-in-a-Box®) was investigated. Proteins with molecular weights of up to around 70kD can be released. The conformation, charge and concentration of the protein being released play a role in the release kinetics. Small proteins such as cytokines can be easily released. The ability to produce cytokines at a sustained and predefined level from encapsulated cells geneticall...
Source: International Journal of Pharmaceutics - June 24, 2018 Category: Drugs & Pharmacology Source Type: research

Spherical neutral gold nanoparticles improve anti-inflammatory response, oxidative stress and fibrosis in alcohol-methamphetamine-induced liver injury in rats
This study aimed to elucidate the anti-inflammatory, anti-oxidant and antifibrotic effects of gold nanoparticles (GNPs) in rats subjected to liver injury with ethanol and Methamphetamine (METH). The liver injury was induced by gavage administrations of 30% alcoholic solution (7 g/kg) once a day during 28 days, followed by METH (10 mg/kg) on the 20th and 28th days of treatment. GNPs treatment (724.96 µg/kg) during the ethanol and METH exposure was associated with reduced steatosis, hepatic cord degeneration, fibrosis and necrosis. Furthermore, there was a reduction in biochemical markers of liver damage and ...
Source: International Journal of Pharmaceutics - June 23, 2018 Category: Drugs & Pharmacology Source Type: research

Development of orally-deliverable DNA hydrogel by microemulsification and chitosan coating
In this study, we aimed to develop DNA hydrogel microspheres (Dgel-MS) coated with chitosan to improve their stability. Chitosan-coated Dgel-MS (Cs-Dgel-MS) was prepared by emulsifying Dgel to obtain the D-gel core, followed by mixing with microemulsions of chitosan for electrostatic coating. Fluorescence imaging of Cs-Dgel-MS labeled with fluorescent dyes showed that Dgel-MS (approximately 30 μm) was coated with chitosan. The recovery efficiency of Alexa Fluor 488-DNA was 87.4 ± 7.5%. To load a phosphorothioate CpG oligodeoxynucleotide into Dgel, a modified Dgel (mDgel) was designed and fluorescein isothio...
Source: International Journal of Pharmaceutics - June 19, 2018 Category: Drugs & Pharmacology Source Type: research

All-atomistic molecular dynamics (AA-MD) studies and pharmacokinetic performance of PAMAM-dendrimer-furosemide delivery systems
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): Daniel P. Otto, Melgardt M. de Villiers Improvement of problematic dissolution and solubility properties of a model drug, furosemide, was investigated for poly(amidoamine) (PAMAM) dendrimer complexes of the drug. Full and half generation dendrimers with amino and ester terminals respectively, were studied. In vitro release performance of these complexes was investigated at drug loads ranging 5–60% using simulated gastric fluids. Full generation dendrimers accommodated higher drug loads, outperforme...
Source: International Journal of Pharmaceutics - June 19, 2018 Category: Drugs & Pharmacology Source Type: research

Hot melt extrusion of ion-exchange resin for taste masking
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): David Cheng Thiam Tan, Jeremy Jianming Ong, Rajeev Gokhale, Paul Wan Sia Heng Taste masking is important for some unpleasant tasting bioactives in oral dosage forms. Among many methods available for taste-masking, use of ion-exchange resin (IER) holds promise. IER combined with hot melt extrusion (HME) may offer additional advantages over solvent methods. IER provides taste masking by complexing with the drug ions and preventing drug dissolution in the mouth. Drug-IER complexation approaches described in...
Source: International Journal of Pharmaceutics - June 19, 2018 Category: Drugs & Pharmacology Source Type: research

Influence of lidocaine forms (salt vs. freebase) on properties of drug –eudragit® L100-55 extrudates prepared by reactive melt extrusion
This study examines the preparation of sustained-release lidocaine polyelectrolyte complex using reactive melt extrusion. Eudragit L100-55 was selected as the ionic polymer. The influence of drug forms (freebase vs. hydrochloride salt) on lidocaine–Eudragit L100-55 interactions, physical stability, and dissolution properties of extrudates was investigated. It was confirmed by DSC, FT-IR and Raman spectroscopy that polyelectrolyte could only form via the acid–base reaction between Eudragit L100-55 and lidocaine freebase. Due to this ionic interaction, the lidocaine extrudate was physically more stable than the l...
Source: International Journal of Pharmaceutics - June 19, 2018 Category: Drugs & Pharmacology Source Type: research

Lipidation of polyethylenimine-based polyplex increases serum stability of bioengineered RNAi agents and offers more consistent tumoral gene knockdown in vivo
Publication date: 25 August 2018 Source:International Journal of Pharmaceutics, Volume 547, Issues 1–2 Author(s): Qian-Yu Zhang, Pui Yan Ho, Mei-Juan Tu, Joseph L. Jilek, Qiu-Xia Chen, Su Zeng, Ai-Ming Yu Recently we have established a novel approach to produce bioengineered noncoding RNA agents (BERAs) in living cells that carry target RNAi molecules (e.g., siRNA and miRNA) and thus act as “prodrugs”. Using GFP-siRNA-loaded BERA (BERA/GFP-siRNA) as a model molecule, this study was to define the in vitro and in vivo knockdown efficiency of BERAs delivered by liposome-polyethylenimine nanocomplex (lipopol...
Source: International Journal of Pharmaceutics - June 18, 2018 Category: Drugs & Pharmacology Source Type: research