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International Journal of Pharmaceutics

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https://www.readbyqxmd.com/read/28323102/preparation-of-core-crosslinked-linear-dendritic-copolymer-micelles-with-enhanced-stability-and-their-application-for-drug-solubilisation
#1
Zhengyuan Zhou, Robert T Forbes, Antony D'Emanuele
In this study we explore the preparation of core-crosslinked micelles of linear-dendritic methoxy-poly(ethylene glycol) (MPEG)-co-poly(ester-sulfide) (PES) polymers to improve the stability of such polymeric micelle systems against premature disintegration and drug release. A series of MPEG-PES copolymers were synthesised via stepwise reactions of acetylation and thiol-ene photoreaction. Surface tension measurement showed that the copolymers with ethenyl surface groups could self-associate in dilute aqueous solutions to form micelles...
March 18, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28323101/mixtures-of-hyaluronic-acid-and-liposomes-for-drug-delivery-phase-behavior-microstructure-and-mobility-of-liposomes
#2
Naila El Kechai, Sandrine Geiger, Arianna Fallacara, Ingrid Cañero Infante, Valérie Nicolas, Evelyne Ferrary, Nicolas Huang, Amélie Bochot, Florence Agnely
Hyaluronic acid liposomal gels have previously demonstrated in vivo their great potential for drug delivery. Elucidating their phase behavior and structure would provide a better understanding of their use properties. This work evaluates the microstructure and the phase behavior of mixtures of hyaluronic acid (HA) and liposomes and their impact on the vesicle mobility. HA concentration and surface properties of liposomes (positively or negatively charged, neutral, with a polyethylene glycol corona) are varied while the liposome concentration remains constant...
March 18, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28323099/nanohydrogel-with-n-n-bis-acryloyl-cystine-crosslinker-for-high-drug-loading
#3
Marcin Mackiewicz, Jan Romanski, Ewa Drozd, Beata Gruber-Bzura, Piotr Fiedor, Zbigniew Stojek, Marcin Karbarz
Substantially improved hydrogel particles based on poly(N-isopropylacrylamide) (pNIPA) have been obtained. First, as a result of replacing commercially available N,N'-bis(acryloyl)cystamine (BAC), the crosslinker, with acryloyl derivative of cystine containing a carboxylic group (BISS), the hydrogel particles acquired improved stability vs. ionic strength and allowed further chemical modification of the chains, including the attachment of drug molecules. Next, a redox-initiated aqueous precipitation polymerization via the semi-batch method was used...
March 18, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28323098/an-innovative-method-for-the-preparation-of-high-api-loaded-hollow-spherical-granules-for-use-in-controlled-release-formulation
#4
Takumi Asada, Mitsuaki Kobiki, Yasushi Ochiai, Yasunori Iwao, Shigeru Itai
The aim of this study was to prepare controlled-release (CR) granules with suitable particle strength, flowability, particle size distribution (PSD) and density characteristics for blending with other excipients. We also wanted these CR granules to contain large quantities of active pharmaceutical ingredient (API). A high shear mixer was used to mix an API with various polymers at various feed ratios, and the resulting granulated materials were sprayed with solvent. The wet granules were dried using a fluidized bed dryer to give CR granules...
March 18, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28323100/reflectometric-monitoring-of-the-dissolution-process-of-thin-polymeric-films
#5
Riikka Laitinen, Jukka Räty, Kristiina Korhonen, Jarkko Ketolainen, Kai-Erik Peiponen
Pharmaceutical thin films are versatile drug-delivery platforms i.e. allowing transdermal, oral, sublingual and buccal administration. However, dissolution testing of thin films is challenging since the commonly used dissolution tests for conventional dosage forms correspond rather poorly to the physiological conditions at the site of administration. Here we introduce a traditional optical reflection method for monitoring the dissolution behavior of thin polymeric films. The substances, e.g. drug molecules, released from the film generate an increase in the refractive index in the liquid medium which can be detected by reflectance monitoring...
March 17, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28323097/direct-comparison-between-millifluidic-and-bulk-mixing-platform-in-the-synthesis-of-amorphous-drug-polysaccharide-nanoparticle-complex
#6
Bingxue Dong, Kunn Hadinoto
Amorphous drug-polysaccharide nanoparticle complex (or drug nanoplex) had emerged as an ideal supersaturating delivery system of poorly-soluble drugs attributed to its many attractive characteristics. Herein we presented for the first time direct comparison between two nanoplex synthesis platforms, i.e. millifluidics and bulk mixing, representing continuous and batch production modes, respectively. They were compared by the resultant nanoplex's (1) physical characteristics (size, zeta potential, and payload), (2) preparation efficiency, (3) storage stability, (4) dissolution rate/supersaturation generation, and (5) production consistency...
March 16, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28323096/nanoparticles-as-safe-and-effective-delivery-systems-of-antifungal-agents-achievements-and-challenges
#7
REVIEW
Ghareb M Soliman
Invasive fungal infections are becoming a major health concern in several groups of patients leading to severe morbidity and mortality. Moreover, cutaneous fungal infections are a major cause of visits to outpatient skin clinics. Despite the availability of several effective agents in the antifungal drug arena, their therapeutic outcome is less than optimal due to limitations related to drug physicochemical properties and toxicity. For instance, poor aqueous solubility limits the formulations options and efficacy of several azole antifungal drugs while toxicity limits the benefits of many other drugs...
March 16, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28323095/megalin-targeted-enhanced-transfection-efficiency-in-cultured-human-hk-2-renal-tubular-proximal-cells-using-aminoglycoside-carboxyalkyl-polyethylenimine-containing-nanoplexes
#8
Fatemeh Oroojalian, Ali Hossein Rezayan, Wayne Thomas Shier, Khalil Abnous, Mohammad Ramezani
Non-viral vectors are of interest as therapeutic gene delivery agents in gene therapy, because they are simple to prepare, easy to modify and have definable safety profiles compared to viral vectors. The potential of gene therapy in the treatment of renal diseases is limited by a lack of effective kidney-targeted gene delivery systems. Aminoglycoside antibiotics gentamicin and neomycin were connected by amide linkages to carboxyl groups on carboxyalkylated-PEI25 (25kDa PEI) or carboxyalkylated-PEI10 (10kDa PEI)...
March 16, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28323094/denatured-protein-coated-docetaxel-nanoparticles-alterable-drug-state-and-cytosolic-delivery
#9
Li Zhang, Qingqing Xiao, Yiran Wang, Chenshuang Zhang, Wei He, Lifang Yin
Many lead compounds have a low solubility in water, which substantially hinders their clinical application. Nanosuspensions have been considered a promising strategy for the delivery of water-insoluble drugs. Here, denatured soy protein isolate (SPI)-coated docetaxel nanosuspensions (DTX-NS) were developed using an anti-solvent precipitation-ultrasonication method to improve the water-solubility of DTX, thus improving its intracellular delivery. DTX-NS, with a diameter of 150 to 250nm and drug-loading up to 18...
March 16, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28315716/critical-material-attributes-cmas-of-strip-films-loaded-with-poorly-water-soluble-drug-nanoparticles-iii-impact-of-drug-nanoparticle-loading
#10
Scott M Krull, Jacqueline Moreno, Meng Li, Ecevit Bilgili, Rajesh N Davé
Polymer strip films have emerged as a robust platform for poorly water-soluble drug delivery. However, the common conception is that films cannot exceed low drug loadings, mainly due to poor drug stability, slow release, and film brittleness. This study explores the ability to achieve high loadings of poorly water-soluble drug nanoparticles in strip films while retaining good mechanical properties and enhanced dissolution rate. Aqueous suspensions containing up to 30wt% griseofulvin nanoparticles were prepared via wet stirred media milling and incorporated into hydroxypropyl methylcellulose (HPMC) films...
March 15, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28315384/the-absorption-enhancer-sodium-deoxycholate-promotes-high-gene-transfer-in-skeletal-muscles
#11
Christian Leborgne, Debborah Alimi-Guez, Nelly El Shafey, Laetitia van Wittenberghe, Pascal Bigey, Daniel Scherman, Antoine Kichler
Gene delivery to skeletal muscle is a promising strategy for the treatment of muscle disorders and for the systemic secretion of therapeutic proteins. In addition, muscle is an attractive target tissue because it is easily accessible. However, very few synthetic vectors proved capable of surpassing naked DNA mediated muscle gene transfer. In fact, only neutral copolymers, in particular poloxamers, demonstrated capacities to increase transgene expression in skeletal muscles. Here, we studied in vitro and in vivo behaviour of different bile salts...
March 14, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28302515/orodispersible-films-towards-drug-delivery-in-special-populations
#12
REVIEW
Mariagiovanna Scarpa, Sven Stegemann, Wen-Kai Hsiao, Heinz Pichler, Simon Gaisford, Massimo Bresciani, Amrit Paudel, Mine Orlu
Orodispersible films (ODF) hold promise as a novel delivery method, with the potential to deliver tailored therapies to different patient populations. Together with the current trends and potential therapeutic areas such technology can address, some of the unmet needs in terms of quality aspects and manufacturing of conventional and novel (printed) ODF are discussed. Overall, this article aims to stimulate further research to fill the current knowledge gap between manufacturing and administration requirements of ODF targeting specific patient subpopulations such as geriatrics...
March 13, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28300630/functionalized-single-walled-carbon-nanotubes-cellular-uptake-biodistribution-and-applications-in-drug-delivery
#13
Zixian Li, Andre Luis Branco de Barros, Daniel Cristian Ferreira Soares, Sara Nicole Moss, Laleh Alisaraie
The unique properties of single-walled carbon nanotubes (SWNTs) enable them to play important roles in many fields. One of their functional roles is to transport cargo into the cell. SWNTs are able to traverse amphipathic cell membranes due to their large surface area, flexible interactions with cargo, customizable dimensions, and surface chemistry. The cargoes delivered by SWNTs include peptides, proteins, nucleic acids, as well as drug molecules for therapeutic purpose. The drug delivery functions of SWNTs have been explored over the past decade...
March 11, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28300629/insights-into-caco-2-cell-culture-structure-using-coherent-anti-stokes-raman-scattering-cars-microscopy
#14
Jukka Saarinen, Erkan Sözeri, Sara J Fraser-Miller, Leena Peltonen, Hélder A Santos, Antti Isomäki, Clare J Strachan
We have used coherent anti-Stokes Raman scattering (CARS) microscopy as a novel and rapid, label-free and non-destructive imaging method to gain structural insights into live intestinal epithelial cell cultures used for drug permeability testing. Specifically we have imaged live Caco-2 cells in (bio)pharmaceutically relevant conditions grown on membrane inserts. Imaging conditions were optimized, including evaluation of suitable membrane materials and media solutions, as well as tolerable laser powers for non-destructive imaging of the live cells...
March 11, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28286081/in-vitro-evaluation-of-the-genotoxicity-of-poly-anhydride-nanoparticles-designed-for-oral-drug-delivery
#15
T Iglesias, M Dusinska, N El Yamani, J M Irache, A Azqueta, A López de Cerain
In the last years, the development of nanomaterials has significantly increased due to the immense variety of potential applications in technological sectors, such as medicine, pharmacy and food safety. Focusing on the nanodevices for oral drug delivery, poly(anhydride) nanoparticles have received extensive attention due to their unique properties, such us their capability to develop intense adhesive interactions within the gut mucosa, their modifiable surface and their biodegradable and easy-to-produce profile...
March 9, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28286080/electrospun-protein-nanofibers-in-healthcare-a-review
#16
REVIEW
S Babitha, Lakra Rachita, K Karthikeyan, Ekambaram Shoba, Indrakumar Janani, Balan Poornima, K Purna Sai
Electrospun nanofibers are being utilized for a wide range of healthcare applications. A plethora of natural and synthetic polymers are exploited for their ability to be electrospun and replace the complex habitat provided by the extracellular matrix for the cells. The fabrication of nanofibers can be tuned to act as a multicarrier system to deliver drugs, growth factors and health supplements etc. in a sustained manner. Owing to its pliability, nanofibers reached its heights in tissue engineering and drug delivery applications...
March 9, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28286079/multifractal-and-mechanical-analysis-of-amorphous-solid-dispersions
#17
Camille Adler, Alexandra Teleki, Martin Kuentz
The formulation of lipophilic and hydrophobic compounds is a challenge for the pharmaceutical industry and it requires the development of complex formulations. Our first aim was to investigate hot-melt extrudate microstructures by means of multifractal analysis using scanning electron microscopy imaging. Since the microstructure can affect solid dosage form performance such as mechanical properties, a second objective was to study the influence of the type of adsorbent and of the presence of an amorphous compound on extrudate hardness...
March 9, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28284921/engineered-particles-demonstrate-improved-flow-properties-at-elevated-drug-loadings-for-direct-compression-manufacturing
#18
Andrea N Trementozzi, Cheuk-Yui Leung, Frederick Osei-Yeboah, Erwin Irdam, Yiqing Lin, J Michael MacPhee, Pierre Boulas, Shyam B Karki, Peter N Zawaneh
Optimizing powder flow and compaction properties is critical for ensuring a robust tablet manufacturing process. The impact of flow and compaction properties of the active pharmaceutical ingredient (API) becomes progressively significant for higher drug load formulations, and for scaling up manufacturing processes. This study demonstrated that flow properties of a powder blend can be improved through API particle engineering, without critically impacting blend tabletability at elevated drug loadings. In studying a jet milled API (D50=24μm) and particle engineered wet milled API (D50=70μm and 90μm), flow functions of all API lots were similarly poor despite the vast difference in average particle size (ffc<4)...
March 8, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28284920/tensile-and-shear-methods-for-measuring-strength-of-bilayer-tablets
#19
Shao-Yu Chang, Jian-Xin Li, Changquan Calvin Sun
Both shear and tensile measurement methods have been used to quantify interfacial bonding strength of bilayer tablets. The shear method is more convenient to perform, but reproducible strength data requires careful control of the placement of tablet and contact point for shear force application. Moreover, data obtained from the shear method depend on the orientation of the bilayer tablet. Although more time-consuming to perform, the tensile method yields data that are straightforward to interpret. Thus, the tensile method is preferred in fundamental bilayer tableting research to minimize ambiguity in data interpretation...
March 8, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28284919/nanostructured-monolinolein-miniemulsions-as-delivery-systems-role-of-the-internal-mesophase-on-cytotoxicity-and-cell-internalization
#20
Samuel Guillot, Fabienne Méducin, Kristina Poljak, Virginie Malard, Alexandra Foucault-Collet, Sébastien Serieye, Chantal Pichon
Recent advances in nanoparticle systems for improved drug delivery display a great potential for the administration of active molecules. Here, lipid miniemulsions with various internal nanostructures were loaded with the chemotherapeutic agent Paclitaxel. The goal is to assess the impact of internal structures on their efficiency. Previously the structure, the stability and the physico-chemical properties of those carriers were characterized. Modalities of action were addressed by the evaluation of their effects on the tumor cells viability, their cellular uptake by flow cytometry and confocal microscopy detection of fluorescently labeled nanostructured miniemulsions...
March 8, 2017: International Journal of Pharmaceutics
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