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International Journal of Pharmaceutics

Jelena Djuris, Stoja Milovanovic, Djordje Medarevic, Vladimir Dobricic, Aleksandra Dapčević, Svetlana Ibric
Solid dispersions production is one of the substantial approaches for improvement of poor drug solubility. Additionally, supercritical fluid assisted method for preparation of solid dispersions can offer many advantages in comparison to the conventional melting or solvent-evaporation methods. Miscibility analysis provides valuable guidance for selection of the most appropriate polymeric carrier for dispersion of the drug of interest. In addition to the increased drug release rate, solid dispersions should have proper mechanical attributes in order to be successfully formulated in the final solid dosage form such as tablet...
November 8, 2018: International Journal of Pharmaceutics
Bahez Gareb, Gerard Dijkstra, Jos G W Kosterink, Henderik W Frijlink
Up to 50% of Crohn's disease and ulcerative colitis patients suffer from ileo-colonic inflammation. Topically delivered budesonide is an effective treatment but in vitro as well as clinical data suggest that oral formulations currently used in clinical practice are not optimal to treat the ileo-colon. The aim of this in vitro study was to develop ileo-colonic-targeted zero-order sustained-release tablets containing 3 mg or 9 mg budesonide. Targeted delivery was achieved by coating the tablets with the ColoPulse technology (ColoPulse 3 mg or ColoPulse 9 mg, respectively)...
November 8, 2018: International Journal of Pharmaceutics
Russell P Watt, Hetal Khatri, Andrew R G Dibble
Injectability is a term related to the ease of parenteral administration of a dosing solution, and includes dose preparation, dose administration, ergonomics related to these procedures, pain of injection, and other adverse events at the injection site. This article focuses on force measurements related to injectability, namely: force to expel syringe contents (expulsion force - a mimic for in vivo injection force), needle-penetration force, and needle-bending force, and these results are supplemented by expulsion time measurements with 18 participants, as well as injections in a porcine model...
November 7, 2018: International Journal of Pharmaceutics
Isabell Speer, Vincent Lenhart, Maren Preis, Jörg Breitkreutz
Prolonged drug release provided by multiple-unit dosage forms is highly beneficial to enhance the compliance and safety of the pharmacotherapy even for patients with swallowing deficiencies. To facilitate the intake for these patients, multiple-unit tablets and capsules have to be crushed or opened. An attempt to overcome these issues has been made by the introduction of orodispersible films (ODFs), which rapidly disintegrate within the oral cavity and facilitate the intake of oral solid dosage forms. The aim of this study was to develop a rapidly disintegrating ODF with prolonged release properties by incorporation of small-sized micropellets (MPs)...
November 7, 2018: International Journal of Pharmaceutics
Eleonora Pereverzeva, Ivan Treschalin, Mikhail Treschalin, Diana Arantseva, Yulia Ermolenko, Natalya Kumskova, Olga Maksimenko, Vadim Balabanyan, Jörg Kreuter, Svetlana Gelperina
Doxorubicin loaded in poloxamer 188-coated PLGA nanoparticles (Dox-NP+P188) was shown to produce a high antitumor effect against the experimental orthotopic 101.8 glioblastoma in rats upon intravenous administration. The objective of the present study was to evaluate the acute and chronic toxicity of this nanoformulation. The parent drug was used as a reference formulation. Acute toxicity of doxorubicin-loaded nanoparticles in mice and rats was similar to that of free doxorubicin. The chronic toxicity study was conducted in Chinchilla rabbits; the treatment regimen consisted of 30 daily intravenous injections using two dosage levels: 0...
November 7, 2018: International Journal of Pharmaceutics
Roshni Iyer, Aneetta E Kuriakose, Serkan Yaman, Lee-Chun Su, Dingying Shan, Jian Yang, Jun Liao, Liping Tang, Subhash Banerjee, Hao Xu, Kytai T Nguyen
Nanoparticles (NPs) can be used to locally deliver anti-restenosis drugs when they are infused directly to the injured arteries after intervention procedures such as angioplasty. However, the efficacy of transferring NPs via infusion to the arterial wall is limited, at least partially, due to poor NP retention on the inner artery wall. To improve NP retention, angioplasty balloons coated with drug-loaded NPs were fabricated via either layer-by-layer (LbL) electrostatic coating or acrylic-based hydrogel (AAH) coating techniques...
November 5, 2018: International Journal of Pharmaceutics
Osama Madkhali, George Mekhail, Shawn D Wettig
Gelatin nanoparticles (GNPs) are one of the most extensively used natural polymers for gene therapy. With advantages of being biodegradable, biocompatible, low cost and easily modified, gelatin holds great promise as a non-viral system for gene delivery. This review examines various methods of preparation of modified gelatin nanoparticles and considers how these modifications apply to gene delivery. The article discusses cationic gelatin, PEGylated gelatin, thiolated gelatin, alendronate gelatin, and EGFR gelatin nanoparticles...
November 5, 2018: International Journal of Pharmaceutics
Sergey Zaichik, Christian Steinbring, Cagri Caliskan, Andreas Bernkop-Schnürch
The aim of this study was to develop a self-emulsifying drug delivery system (SEDDS) containing the glycopeptide antibiotic vancomycin (VAN) with improved intestinal mucosa permeating properties in order to increase oral drug absorption. VAN was effectively incorporated into SEDDS increasing the lipophilicity of the drug via hydrophobic ion pairing (HIP) with cetyltrimethylammonium bromid (CTAB). Newly developed SEDDS formulations containing VAN/CTAB complex were characterized with respect to droplet size, polydispersity index and zeta potential...
November 5, 2018: International Journal of Pharmaceutics
Janske Nel, Céline M Desmet, Benoit Driesschaert, Patrick Saulnier, Laurent Lemaire, Bernard Gallez
Oxygen is essential in physiology and pathophysiology. Electron Paramagnetic Resonance (EPR) oximetry, using oxygen sensitive paramagnetic materials, could be attractive for measuring oxygen in tissues. The aim of the present study was to assess the properties of lipid nanocapsules (LNCs) loaded with the nitroxide tempo-benzoate (TB) or tetrathiatriarylmethyl (TAM) radicals. LNCs loaded with the EPR probes were successfully prepared by the phase inversion process leading to nanocapsules of about 60 nm. LNCs protected the TB radical against reduction in vitro...
November 3, 2018: International Journal of Pharmaceutics
Pengfei Gu, Zhenguang Liu, Yaqin Sun, Ning Ou, Yuanliang Hu, Jiaguo Liu, Yi Wu, Deyun Wang
Nanoparticles (NPs)-based vaccine delivery systems are widely used for their ability to control the release of antigens and promote immune responses against cancer or infectious diseases. In this study, the immunopotentiator Angelica sinensis polysaccharide (ASP) and model protein antigen ovalbumin (OVA) were encapsulated into Poly(lactic-co-glycolic acid) (PLGA) to formulate the novel NPs-based vaccine delivery system (ASP-PLGA/OVA). These formulations were subcutaneously administered to mice, then the magnitude and kinetics of antibody and cellular immune responses were assessed...
November 3, 2018: International Journal of Pharmaceutics
Eun-Ju Hyun, Mohammad Nazmul Hasan, Sung Hun Kang, Sungpil Cho, Yong-Kyu Lee
Oral siRNA delivery is an ideal way to translate siRNA therapeutic effects in the clinic due to its ability to be administered in convenient and multiple dosages. However, an effective oral delivery system requires overcoming both a hostile gastrointestinal (GI) environment and non-specific targeting. Here, an HTsRP-NC system is a new oral siRNA delivery system consisting of a siRNA/protamine (sRP) nano-complex protected by a multi-functional hyaluronic acid-taurocholic acid (HA-TCA) conjugate. The HTsRP-NC promotes cell penetration and enhances endosomal escape in cancer cells...
November 3, 2018: International Journal of Pharmaceutics
Haley McFall, Sandeep Sarabu, Vijaykumar Shankar, Suresh Bandari, S Narasimha Murthy, Karl Kolter, Nigel Langley, Dong Wuk Kim, Michael A Repka
The objective of this study was to formulate aripiprazole (ARI)-loaded pH-modulated solid dispersions (SD) to enhance solubility, dissolution, and bioavailability via hot-melt extrusion (HME) technology. Kollidon® 12 PF (PVP) and succinic acid (SA) were selected after solubility screenings of various polymers and acidifiers. Several formulations, varying in screw speed and drug/polymer/acidifier ratios, were extruded using an 11 mm twin-screw extruder and were investigated for the effect of these variables...
November 2, 2018: International Journal of Pharmaceutics
Satoshi Uchiyama, Samira Dahesh, Victor Nizet, Jack Kessler
Staphylococcus aureus, a leading cause of serious human infections in both healthcare and community settings, is increasingly difficult to control due to expanding resistance to multiple antibiotic classes. Methicillin-resistant S. aureus (MRSA) strains have disseminated on a global scale and are associated with adverse patient outcomes, increased hospital stays, and significant economic costs to the healthcare system. A proximal step in S. aureus infection is colonization of the nasal mucosa, and effective strategies to decolonize high risk patients to reduce the risk of invasive infection and nosocomial spread represent an important clinical priority...
November 2, 2018: International Journal of Pharmaceutics
Mohamad Jamal Altamimi, Kim Wolff, Ali Nokhodchi, Gary P Martin, Paul G Royall
Lactose, a disaccharide is a ubiquitous excipient in many pharmaceutical formulations which exists in two anomeric forms; either as α- or β-lactose. The anomers have different properties which can affect their application. Nevertheless, batches of lactose products are widely produced by many manufacturers, and is available in many grades. However, the anomeric content of these batches has not been accurately characterized and reported previously. Therefore, the aim of this study was to analyse a set of 19 commercially available samples of lactose using a novel H1 -NMR technique to establish a library showing the anomeric content of a large range of lactose products...
November 2, 2018: International Journal of Pharmaceutics
Marek Šoltys, Pavel Kovačík, Ondřej Dammer, Josef Beránek, František Štěpánek
Increasing the dissolution rate of poorly water-soluble active pharmaceutical ingredients (APIs) is a key strategy used for improving their oral bioavailability. One of the formulation approaches is API loading to mesoporous carrier particles, which can increase the dissolution rate through the combination of improved powder wettability and dispersion, higher surface area, and API conversion from crystalline to the amorphous state. From the formulation process point of view, the maximum achievable drug loading is a crucial parameter, which depends on the loading method...
November 2, 2018: International Journal of Pharmaceutics
V Mazel, H Diarra, P Tchoreloff
Tablets final properties are mainly determined during the compaction process by the evolution of the stresses applied to the powder. Any process or product parameter that may influence this stress evolution may have a direct impact on the tablet final properties. In this article, we studied the influence of the friction between the tooling and the powder on the evolution of the die-wall pressure during compaction using flat and concave punches. Experimental studies were performed on microcrystalline cellulose as well as numerical studies using finite element method (FEM) simulation...
November 2, 2018: International Journal of Pharmaceutics
Steven Woolford, Mandy Tran, Agnes NguyenPho, Martin K McDermott, Berk Oktem, Samanthi Wickramasekara
Drug coated balloons (DCBs) have proven to be a suitable alternative for the treatment of cardiovascular diseases. They allow for uniform delivery of an antiproliferative drug to the stenotic site without permanent implantation of the device in the patient's body. There are, however, regulatory concerns regarding the lack of data associated with variable drug delivery to the target site, which can be related to the coating process. This study describes the process for an in-house micro-pipetting coating method that incorporates a laboratory-developed coating equation for determining optimal coating parameters...
November 2, 2018: International Journal of Pharmaceutics
José L Soriano-Ruiz, Ana C Calpena-Capmany, Cristina Cañadas-Enrich, Nuria Bozal-de Febrer, Joaquim Suñer-Carbó, Eliana B Souto, Beatriz Clares-Naveros
Clotrimazole (CLT) was formulated in a nanoemulsion (NE) for the topical treatment of candidiasis consisting of 10% labrafac® lipophile, 60% labrasol® :capryol® 90 mixture (ratio 4:1) and 30% propylene glycol. Physicochemical properties, stability, rheology, in vitro drug release, ex vivo drug permeation through human skin and porcine buccal, sublingual and vaginal mucosae, antifungal efficacy, as well as in vivo skin tolerance were evaluated. 1% CLT-NE (CLT-NE1) and 2% CLT-NE (CLT-NE2) exhibited 153±17...
November 2, 2018: International Journal of Pharmaceutics
Simo Näkki, Julie T-W Wang, Jianwei Wu, Li Fan, Jimi Rantanen, Tuomo Nissinen, Mikko I Kettunen, Matilda Backholm, Robin H A Ras, Khulosud T Al-Jamal, Vesa-Pekka Lehto, Wujun Xu
The inability of traditional chemotherapeutics to reach cancer tissue reduces the treatment efficacy and leads to adverse effects. A multifunctional nanovector was developed consisting of porous silicon, superparamagnetic iron oxide, calcium carbonate, doxorubicin and polyethylene glycol. The particles integrate magnetic properties with the capacity to retain drug molecules inside the pore matrix at neutral pH to facilitate drug delivery to tumor tissues. The MRI applicability and pH controlled drug release were examined in vitro together with in-depth material characterization...
November 1, 2018: International Journal of Pharmaceutics
Bilal Ahmed, Cameron J Brown, Thomas McGlone, Deborah L Bowering, Jan Sefcik, Alastair J Florence
Wet milling coupled with crystallisation has considerable potential to deliver enhanced control over particle attributes. The effect of process conditions and wet mill configuration on particle size, shape and surface energy has been investigated on acetaminophen using a seeded cooling crystallisation coupled with a wet mill unit generating size controlled acetaminophen crystals through an interchangeable rotor-tooth configuration. The integrated wet milling crystallisation platform incorporates inline focused beam reflectance measurement (FBRM) and particle vision measurement (PVM) for in-depth understanding of particle behaviour under high-shear conditions...
October 31, 2018: International Journal of Pharmaceutics
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