Porous microspheres: Synthesis, characterisation and applications in pharmaceutical & medical fields
Publication date: 5 September 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(s): Debabrata Ghosh Dastidar, Sourabh Saha, Moumita ChowdhuryAbstractPorous 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 ...
Source: International Journal of Pharmaceutics - July 10, 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 2018Source: International Journal of Pharmaceutics, Volume 548, Issue 1Author(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 SheddenAbstractOver the past decade, formulation predictive dissolution (fPD) testing has gained increasing attention. Another mindset is pushed forward where scientists in our field are more confident to...
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

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 10, 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 10, 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 10, 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 10, 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 10, 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 10, 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 10, 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 10, 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 10, 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 10, 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 10, 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 10, 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 10, 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 10, 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 10, 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 10, 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 10, 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 10, 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 10, 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 10, 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 10, 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 10, 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 10, 2018 Category: Drugs & Pharmacology Source Type: research

Audible Acoustic Emission Data Analysis for Drug Content Prediction during Tableting Processes
Publication date: Available online 9 July 2018Source: International Journal of PharmaceuticsAuthor(s): Ryoma Tanaka, Kenta Kojima, Yusuke Hattori, Kazuhide Ashizawa, Makoto OtsukaGraphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

Treatment merits of Latanoprost/Thymoquinone – encapsulated liposome for glaucomatus rabbits
Publication date: Available online 8 July 2018Source: International Journal of PharmaceuticsAuthor(s): Heba Mohamed Fahmy, Engy Abd El-Malek Saeed Saad, Neveen Moustafa Sabra, Amal Ahmed El-Gohary, Faten Fathy Mohamed, Mohamed Hassaneen GaberAbstractElevation of the intraocular pressure (IOP) is recognized as a risk factor for glaucoma development. Latanoprost (LAT) is a prostaglandin analog used to reduce the (IOP). Thymoquinone (TQ) is a major bioactive ingredient of Nigella sativa. The aim of this study was to develop novel liposomal drug carriers for ocular delivery of LAT, TQ and a mixture of them to investigate their...
Source: International Journal of Pharmaceutics - July 9, 2018 Category: Drugs & Pharmacology Source Type: research

Functionalized carbon nanotubes as emerging delivery system for the treatment of cancer
Publication date: Available online 8 July 2018Source: International Journal of PharmaceuticsAuthor(s): Shubhangi Mahajan, Abhimanyu Patharkar, Kaushik Kuche, Rahul Maheshwari, Pran Kishore Deb, Kiran Kalia, Rakesh K. TekadeAbstractIn recent time, carbon nanotubes (CNTs) have gained vital importance for pharmaceutical formulation scientist for delivering drugs and genes, owing to their excellent surface properties. For example, their aspect ratio is thought to be responsible for their excellent cell penetration aptitude; anisotropic conductivity/semi-conductivity along their axis is ideal for integration with nervous and mu...
Source: International Journal of Pharmaceutics - July 8, 2018 Category: Drugs & Pharmacology Source Type: research

Stabilization of unilamellar catanionic vesicles induced by β-cyclodextrins: a strategy for a tunable drug delivery depot
This study focuses on the impact of β-cyclodextrins for the stabilization of SDS/CTAB catanionic vesicles. Molar ratio and sample preparation procedures have been investigated to evaluate the temperature stability of catanionic vesicles. Diffusion and spectroscopic techniques evidenced that when β-cyclodextrins are added, unilamellar structures are stabilized above the multilamellar-unilamellar vesicles critical temperature. The results evidence encouraging perspectives for the use of vesicular nanoresevoirs for drug depot applications.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 7, 2018 Category: Drugs & Pharmacology Source Type: research

A novel nasal almotriptan loaded solid lipid nanoparticles in mucoadhesive in situ gel formulation for brain targeting: Preparation, characterization and in vivo evaluation
Publication date: Available online 6 July 2018Source: International Journal of PharmaceuticsAuthor(s): Nancy Abdel Hamid Abou Youssef, Abeer Ahmed Kassem, Ragwa Mohamed Farid, Fatma Ismail, Magda Abd Elsamea EL-Massik, Nabila Ahmed BoraieAbstractThis work aimed at designing efficient safe delivery system for intranasal (IN) brain targeting of the water soluble anti- migraine drug Almotriptan malate (ALM). Solid lipid nanoparticles (SLNs) were prepared by w/o/w double emulsion-solvent evaporation method. Selection of the optimized SLNs formula was based on evaluating particle size (PS), poly dispersity index (PDI) and entra...
Source: International Journal of Pharmaceutics - July 7, 2018 Category: Drugs & Pharmacology Source Type: research

Effect of drug incorporation technique and polymer combination on the performance of biopolymeric antifungal buccal films
Publication date: Available online 6 July 2018Source: International Journal of PharmaceuticsAuthor(s): G. Tejada, M.C. Lamas, L. Svetaz, C.J. Salomón, V.A. Alvarez, D. LeonardiAbstractNumerous films with a dissolved or dispersed active principle within a polymeric matrix have been described in literature. However, the incorporation of solid crystals into the films may influence several relevant properties. Additionally, it has been reported that different polymeric matrices lead to films presenting a different performance. The aim of this work was to evaluate the effect of the combination of chitosan with carrageena...
Source: International Journal of Pharmaceutics - July 7, 2018 Category: Drugs & Pharmacology Source Type: research

Competing for Water: A New Approach to Understand Disintegrant Performance
In this study, water uptake and force development as well as water sorption experiments were performed of tablets containing either a soluble or an insoluble filler, one of four different binders, and one of four different disintegrants. For both fillers, one disintegrant performed distinctly worse than the others. For the insoluble filler, dibasic calcium phosphate (DCP), sodium starch glycolate resulted in the longest disintegration, for the soluble filler, lactose, croscarmellose sodium performed worst. Based on the experimental results, the authors introduce the competition-for-water hypotheses, which takes into consid...
Source: International Journal of Pharmaceutics - July 7, 2018 Category: Drugs & Pharmacology Source Type: research

3D printed medicines: A new branch of digital healthcare
This article reviews the current state-of-the-art in FDM technology for medical and pharmaceutical research, including its use for personalised treatments and interconnection within digital health networks. The outstanding challenges are also discussed, with a focus on the future developments that are required to facilitate its integration within pharmacies and hospitals.Graphical abstract (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 7, 2018 Category: Drugs & Pharmacology Source Type: research

Characterization of a smart pH-cleavable PEG polymer towards the development of dual pH-sensitive liposomes
Publication date: Available online 4 July 2018Source: International Journal of PharmaceuticsAuthor(s): Manju Kanamala, Brian D. Palmer, William R. Wilson, Zimei WuAbstractTo facilitate the development of PEG-cleavable pH-sensitive liposomes (CL-pPSL), this study aimed to fully characterize a new pH-sensitive polymer, PEGB-Hz-CHEMS. Polyethylene glycol (PEG) functionalised with 4-carboxybenzaldehyde (PEGB) was linked to cholesteryl hemisuccinate (CHEMS) via an acid labile hydrazide–hydrazone hybrid bond (–CO–NH–N=CH–) to form PEGB-Hz-CHEMS. The polymer was post-inserted into DOPE/CHEMS liposome...
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

In-situ forming PLGA implants for intraocular dexamethasone delivery
Publication date: Available online 4 July 2018Source: International Journal of PharmaceuticsAuthor(s): C. Bode, H. Kranz, F. Siepmann, J. SiepmannAbstractDifferent types of in-situ forming implants based on poly(lactic-co-glycolic acid) (PLGA) and N-methyl-pyrrolidone (NMP) were prepared for controlled ocular delivery of dexamethasone. The impact of the volume of the release medium, initial drug content, polymer molecular weight and PLGA concentration on the resulting drug release kinetics were studied and explained based on a thorough physico-chemical characterization of the systems. This included for instance the monitor...
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

Implication of linker length on cell cytotoxicity, pharmacokinetic and toxicity profile of gemcitabine-docetaxel combinatorial dual drug conjugate
Publication date: Available online 4 July 2018Source: International Journal of PharmaceuticsAuthor(s): Varun Kushwah, Sameer S. Katiyar, Ashish Kumar Agrawal, Isha Saraf, Inder Pal Singh, Dimitrios A. Lamprou, Ramesh C. Gupta, Sanyog JainAbstractThe present study investigates effect of linkers [zero length (without linker), short length linker (glycine and lysine) and long length linker (PEG1000, PEG2000 and PEG3500)] on pharmacokinetics and toxicity of docetaxel (DTX) and gemcitabine (GEM) bio-conjugates. Conjugates were synthesized via carbodiimide chemistry and characterized by 1H-NMR and FTIR. Conjugation of DTX and GE...
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

Amorphous Magnesium Carbonate Nanoparticles with Strong Stabilizing Capability for Amorphous Ibuprofen
This study demonstrates, for the first time, the ability to stabilize an API in the amorphous state using a solid dispersion of magnesium carbonate nanoparticles within the API. Specifically, high proportions of ibuprofen were able to be stabilized in the amorphous state using as little as 17% wt/wt amorphous magnesium carbonate nanoparticles, and drug release rates 83 times faster than from the crystalline state were achieved. Biocompatibility of the nanoparticles was demonstrated in vitro using Human dermal fibroblasts and stability of the nanocomposite formulation was verified with a storage time of six months. The succ...
Source: International Journal of Pharmaceutics - July 6, 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 6, 2018 Category: Drugs & Pharmacology Source Type: research

Corrigendum to “In vitro and preclinical assessment of an intranasal spray formulation of parathyroid hormone PTH 1–34 for the treatment of osteoporosis” [Int. J. Pharm. 535 (2018) 113–119]
Publication date: Available online 5 July 2018Source: International Journal of PharmaceuticsAuthor(s): Allan J. Williams, Faron Jordan, Gareth King, Andrew L. Lewis, Lisbeth Illum, Tahir Masud, Alan C. Perkins, Richard G. Pearson (Source: International Journal of Pharmaceutics)
Source: International Journal of Pharmaceutics - July 6, 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: Available online 5 July 2018Source: International Journal of PharmaceuticsAuthor(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 is uncle...
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

Lipid-coated Superparamagnetic Nanoparticles for Thermoresponsive Cancer Treatment
Publication date: Available online 5 July 2018Source: International Journal of PharmaceuticsAuthor(s): Ayat A. Allam, Sarah J. Potter, Sergey L. Bud'ko, Donglu Shi, Dina F. Mohamed, Fawzia S. Habib, Giovanni M. PaulettiAbstractPoor aqueous solubility, chemical instability, and indiscriminate cytotoxicity have limited clinical development of camptothecin (CPT) as potent anticancer therapeutic. This research aimed at fabricating thermoresponsive nanocomposites that enhance solubility and stability of CPT in aqueous milieu and enable stimulus-induced drug release using magnetic hyperthermia. 1,2-Dipalmitoyl-sn-glycero-3-phosp...
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

A stimuli-responsive insulin delivery system based on reversible phenylboronate modified cyclodextrin with glucose triggered host-guest interaction
In this study, a smart drug carrier that can release insulin depending on the changes in blood glucose levels was designed. Combining two popular molecules through facile synthetic processes, a drug carrier of reversible phenylboronate group modified cyclodextrin (β-CD-EPDME) was fabricated. The drug carrier is composed of cyclodextrin, which can encapsulate insulin, and phenylboronate, which is sensitive to the cis-diols in some saccharides. Moreover, β-CD-EPDME can successfully encapsulate insulin and almost completely release insulin in the presence of glucose. The detached phenylboronic acid moiety triggered ...
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

Preparation of Spray Dried Submicron Particles: Part A – Particle Generation by Aerosol Conditioning
Publication date: Available online 5 July 2018Source: International Journal of PharmaceuticsAuthor(s): Ramona Strob, Adrian Dobrowolski, Gerhard Schaldach, Peter Walzel, Markus ThommesAbstractThe preparation of submicron-sized particles is relevant in chemical, food and pharmaceutical applications. In pharmaceutics, spray dried submicron-sized particles (0.1-1 µm) can increase the dissolution rate as well as the solubility of poorly water-soluble drugs. Since the particle size during spray drying is mainly influenced by the droplet size, the preparation of uniform droplets smaller than 3 µm is of part...
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

Surface-induced crystallization of pharmaceuticals and biopharmaceuticals: A review
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Fiora Artusio, Roberto PisanoAbstractDespite the wide occurrence of crystallization in the pharmaceutical industry, deep understanding and fine control of the process remain a tricky issue. Nevertheless, the successful manufacturing of finished pharmaceutical products, as well as the structural determination of biopharmaceuticals, depend on the size, form, shape and purity of the crystals. The ability of substrates with precise chemistry and topological features to induce nucleation has been thoroughly ass...
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

Nanostructured lipid carriers-based drug delivery for treating various lung diseases: A State‐of‐the‐Art Review
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Tulshidas S. Patil, Ashwini S. DeshpandeAbstractAccording to the list published by the WHO for global top ten causes of death, lung diseases contribute nearly one-third of the total mortality. The current treatment on lung diseases provide only symptomatic relief rather than restoring the complete lung functions. Nanostructured lipid carriers-based drug delivery system (NLCs-based DDS) provide a breakthrough in treating various lung diseases.This review provides the readers with background information for ...
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

Pharmaceutical cocrystallization techniques. Advances and challenges
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Marisa Rodrigues, Bárbara Baptista, João Almeida Lopes, Mafalda Cruz SarraguçaAbstractCocrystals are homogenous (single-phase) crystalline structures composed by two or more components in a definite stoichiometric ratio bonded together by noncovalent bonds. Pharmaceutical industry has been showing interest in cocrystals due to their ability to improve active pharmaceutical ingredients (API’s) properties, such as solubility, dissolution, bioavailability, stability and processabili...
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

Promising nanotherapy in treating leishmaniasis
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Aline de Souza, Débora Soares Souza Marins, Samir Leite Mathias, Lis Marie Monteiro, Megumi Nishitani Yukuyama, Cauê Benito Scarim, Raimar Löbenberg, Nádia Araci Bou-ChacraAbstractLeishmaniases are infectious diseases caused by an intracellular protozoan in humans by 20 different species of Leishmania among more than 53 species. There are at least twelve million cases of infections worldwide and three hundred and fifty million people are at risk in at least 98 developing countries ...
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

Chemical modifications of insulin: Finding a compromise between stability and pharmaceutical performance
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Mohsen Akbarian, Younes Ghasemi, Vladimir N. Uversky, Reza YousefiAbstractInsulin, a key peptide hormone that conjointly with its receptor regulates blood glucose levels, is used as the major means to treat diabetes. This therapeutic hormone may undergo different chemical modifications during industrial processes, pharmaceutical formulation, and through its endogenous storage in the pancreatic β-cells. Insulin is highly sensitive to the environmental stresses and easily undergoes structural changes, b...
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

Nanoemulsion containing 8-methoxypsoralen for topical treatment of dermatoses: Development, characterization and ex vivo permeation in porcine skin
Publication date: 25 August 2018Source: International Journal of Pharmaceutics, Volume 547, Issues 1–2Author(s): Catarina Amorim Oliveira, Marcos Martins Gouvêa, Gabriel Ramos Antunes, Zaida Maria Faria de Freitas, Flávia Ferreira de Carvalho Marques, Eduardo Ricci-JuniorAbstractOral therapy with 8-methoxypsoralen (8-MOP) may cause major side effects, whereas the topical treatment might not be much effective due to the low penetration induced by typical formulations. Therefore, the objectives of this work are the development and characterization of a nanoemulsion (NE) containing 8-MOP together with an ex...
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research

Enhanced cellular uptake and osteogenic differentiation efficiency of melatonin by inclusion complexation with 2-hydroxypropyl β-cyclodextrin
In this study, an inclusion complex of MLT with 2-hydroxypropyl β-cyclodextrin (HP-β-CD) was prepared to improve the water solubility, and the osteogenic differentiation ability of the inclusion complex was investigated in MC3T3-E1 cells. The formation of HP-β-CD/MLT inclusion complex was confirmed by 1H and 13C nuclear magnetic resonance spectroscopy and wide-angle X-ray diffraction. The water solubility of MLT increased linearly upon addition of HP-β-CD because of the formation of the inclusion complex. Additionally, treatment of the cells with HP-β-CD/MLT inclusion complex showed higher uptake a...
Source: International Journal of Pharmaceutics - July 6, 2018 Category: Drugs & Pharmacology Source Type: research