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International Journal of Pharmaceutics

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https://www.readbyqxmd.com/read/30218827/potential-role-of-stromal-collagen-in-cystine-crystallization-in-cystinosis-patients
#1
Phillip Dixon, Keith Christopher, Anuj Chauhan
Cystinosis is a genetic disease that leads to the accumulation of intracellular cystine crystals in all organs including cornea due to the loss of cystine efflux transporters in the lysosome of the cells. While the mechanism for formation of intracellular cystine is well understood for most organs, it does not explain many observations for crystal accumulation in the cornea of cystinosis patients. First, the crystals in cornea are extracellular and needle-like with several hundred microns length which is in sharp contrast with the rectangular or hexagonal crystals found throughout other organs...
September 12, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/30218826/reconstituted-spray-dried-phenytoin-loaded-nanocapsules-improve-the-in-vivo-phenytoin-anticonvulsant-effect-and-the-survival-time-in-mice
#2
Edilene Gadelha de Oliveira, Aline Marquez Cardoso, Karina Paese, Karine Coradini, Clarissa Vasconcelos de Oliveira, Adriana Raffin Pohlmann, Mauro Schneider Oliveira, Sílvia Stanisçuaski Guterres, Ruy Carlos Ruver Beck
This study evaluated the in vivo anticonvulsant effect of a spray-dried powder for reconstitution containing phenytoin-loaded lipid-core nanocapsules. The effect of chitosan coating on redispersibility, gastrointestinal stability, and drug release from nanoparticles was evaluated during the development of the powders. Maltodextrin was used as adjuvant in the spray-drying process. Chitosan coating played an important role in redispersibility, and large particles (> 100 μm) were obtained using the highest concentration of solids in the feed...
September 12, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/30218825/determination-of-intestinal-permeability-using-in-situ-perfusion-model-in-rats-challenges-and-advantages-to-bcs-classification-applied-to-digoxin
#3
Tamires Guedes Caldeira, Alejandro Ruiz-Picazo, Isabel Lozoya-Agullo, Dênia Antunes Saúde-Guimarães, Marta González-Álvarez, Jacqueline de Souza, Isabel González-Álvarez, Marival Bermejo
The purpose of this work was to describe the closed loop in situ perfusion method in rats and to compare the difficulties and advantages with other methods proposed by regulatory agencies for BCS classification and finally to illustrate its application to evaluate the permeability of digoxin at relevant clinical concentrations. Digoxin was evaluated at two concentration levels: 1.0 μg/ml (with and without sodium azide 65.0 μg/ml) and 6.0 μg/ml. These concentrations correspond to the ratio of the highest dose strength (0...
September 12, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/30217769/prevention-of-corneal-neovascularization-by-subconjunctival-injection-of-avastin-%C3%A2-loaded-thermosensitive-hydrogels-in-rabbit-model
#4
Xu Xu, Jing Yu, Hui Shi, Jie Zhang, Xingyi Li
The antibody avastin® (Ava) has been clinically to treat various intraocular neovascular diseases, but suffering from the rapid clearance and short shelf-life of Ava in the requirement of frequent administration. In the present study, we reports the sustained release of Ava from a thermosensitive hydrogel based on poly(ethylene glycol)-poly(ɛ-caprolactone)-poly(ethylene glycol) (PECE) copolymer for the control of corneal neovascularization in rabbit model. Ava were physically mixed with PECE aqueous solution at 4°C, and resulting Ava-PECE solution showed a sol-gel transition at physiological temperature (37°C)...
September 11, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/30217768/polyvinylpyrrolidone-affects-thermal-stability-of-drugs-in-solid-dispersions
#5
Yasmine Ben Osman, Tatsiana Liavitskaya, Sergey Vyazovkin
The present study explores the hypothesis that a polymer can affect the thermal stability of a drug in solid polymer-drug dispersions. The hypothesis is tested in a systematic fashion by combining isoconversional kinetic analysis with thermogravimetric measurements on several solid dispersions. Experimental systems involve three drugs: indomethacin (IMC), felodipine (FD), and nifedipine (ND) and their solid dispersions with polyvinylpyrrolidone (PVP). It is found that PVP stabilizes IMC but destabilizes FD and ND...
September 11, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/30217767/dry-powder-inhaler-formulations-of-poorly-water-soluble-itraconazole-a-balance-between-in-vitro-dissolution-and-in-vivo-distribution-is-necessary
#6
Zhengwei Huang, Ling Lin, Cushla Mc Goverin, Hu Liu, Lili Wang, Qi Tony Zhou, Ming Lu, Chuanbin Wu
No abstract text is available yet for this article.
September 11, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/30217766/comparative-study-of-the-therapeutic-effect-of-doxorubicin-and-resveratrol-combination-on-2d-and-3d-spheroids-cell-cultures-models
#7
Andreia S Barros, Elisabete C Costa, Ana S Nunes, Duarte de Melo-Diogo, Ilídio J Correia
The assessment of drug-combinations for pancreatic cancer treatment is usually performed in 2D cell cultures. In this study, the therapeutic effect and the synergistic potential of a particular drug-combination towards 2D and 3D cell cultures of pancreatic cancer were compared for the first time. Thus, the effect of Doxorubicin:Resveratrol (DOX:RES) combinations (at molar ratios ranging from 5:1 to 1:5) in the viability of PANC-1 cells cultured as 2D monolayers and as 3D spheroids was analyzed. The results showed that the cells' viability was more affected when DOX:RES combinations containing higher contents of RES (1:2 to 1:5 molar ratios) were used...
September 11, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/30213683/directing-the-nanoparticle-formation-by-the-combination-with-small-molecular-assembly-and-polymeric-assembly-for-topical-suppression-of-ocular-inflammation
#8
Jinhai Huang, Xinxin Yu, Yanfang Zhou, Renshu Zhang, Qianqian Song, Qinmei Wang, Xingyi Li
In this paper, we presented a simple yet versatile strategy to generate a high drug payload nanoparticles by the combination with small molecular assembly and polymeric assembly for topical suppression of ocular inflammation. Upon physical mixing of the succinated triamcinolone acetonide (TA-SA) supramolecular hydrogel with the poly (ethylene glycol)-poly (ɛ-caprolactone)-poly (ethylene glycol) (PECE) aqueous solution at 37°C, TA-SA/PECE nanoparticles formed spontaneously and characterized thoroughly by transmission electron microscopy (TEM), X-ray diffraction (XRD) and differential scanning calorimetry (DSC)...
September 10, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/30205128/personalized-orodispersible-films-by-hot-melt-ram-extrusion-3d-printing
#9
Umberto M Musazzi, Francesca Selmin, Marco A Ortenzi, Garba Khalid Mohammed, Silvia Franzé, Paola Minghetti, Francesco Cilurzo
This work demonstrates the feasibility of the extemporaneous preparation of maltodextrins orodispersible films (ODF) by hot-melt ram-extrusion 3D printing. This method consists of three simple technological operations which can be also implemented in a pharmacy setting. First, maltodextrins, drug, and other excipients are mixed in a mortar and wetted with the plasticizer (i.e. glycerine). Then, the mixture is fed in the chamber of the ram-extruder and heated. ODF are individually printed on the packaging material foil and sealed without further manipulations...
September 8, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/30205127/improved-anticancer-efficacy-of-doxorubicin-mediated-by-human-derived-cell-penetrating-peptide-dnp2
#10
Yucheng Xiang, Wei Shan, Yuan Huang
Although cell penetrating peptides (CPPs) have been extensively studied as an approach to deliver anti-cancer drugs into the tumor cells for the last 30 years, no FDA-approved CPP-based drugs are available, implying that the existing CPPs may have less efficiency in human or have side effects such as toxicity. Herein, we established a tumor targeting drug delivery system by attaching a human-derived cell-penetrating peptide dNP2 (CKIKKVKKKGRKKIKKVKKKGRK) to N-(2-hydroxypropyl)-methacrylamide (HPMA) copolymer doxorubicin conjugates...
September 8, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/30201294/tocopherol-loaded-transfersomes-in-vitro-antioxidant-activity-and-efficacy-in-skin-regeneration
#11
Carla Caddeo, Maria Letizia Manca, Josè Esteban Peris, Iris Usach, Octavio Diez-Sales, Maria Matos, Xavier Fernàndez-Busquets, Anna Maria Fadda, Maria Manconi
Transfersomes were prepared by using different polysorbates (i.e., Tween 20, 40, 60 and 80) and loaded with tocopherol acetate, a naturally-occurring phenolic compound with antioxidant activity. The vesicles showed unilamellar morphology, small size (∼85 nm), low polydispersity index (≤0.27), and high entrapment efficiency, which increased as a function of the length of the Tween fatty acid chain (from 72% to 90%). The long-term stability of the formulations was evaluated by means of the Turbiscan™ technology, which indicated their good stability, irrespective of the Tween used...
September 7, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/30009984/polysorbate-20-non-ionic-surfactant-enhances-retinal-gene-delivery-efficiency-of-cationic-niosomes-after-intravitreal-and-subretinal-administration
#12
Ilia Villate-Beitia, Idoia Gallego, Gema Martínez-Navarrete, Jon Zárate, Tania López-Méndez, Cristina Soto-Sánchez, Edorta Santos-Vizcaíno, Gustavo Puras, Eduardo Fernández, José Luis Pedraz
The success of non-viral vectors based on cationic niosomes for retinal gene delivery applications depends on the ability to achieve persistent and high levels of transgene expression, ideally from a single administration. In this work, we studied the effect of the non-ionic surfactant component of niosomes in their transfection efficiency in rat retina. For that purpose, three niosome formulations that only differed in the non-ionic tensioactives were elaborated. Niosomes contained: cationic lipid 1,2-di-O-octadecenyl-3-trimethylammonium propane (DOTMA), helper lipid squalene and polysorbate 20, polysorbate 80 or polysorbate 85...
September 7, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/30196142/loading-studies-of-the-anticancer-drug-camptothecin-into-dual-stimuli-sensitive-nanoparticles-stability-scrutiny
#13
Nieves Iglesias, Elsa Galbis, M Jesús Díaz-Blanco, M-Violante de-Paz, Juan A Galbis
In recent years, the preparation of valuable drug delivery systems (DDS) from self-assembled amphiphilic copolymers has attracted much attention since these nanomaterials provide new opportunities to solve problems such as the lack of solubility in water of lipophilic drugs, improve their bioavailability, prolong their circulation time and decrease the side effects associated with their administration. In the current study two types of biocompatible pH-responsive nanoparticles derived from poly(2-hydroxyethyl methacrylate) (pHEMA) have been used as drug nano-carriers, being one of them core cross-linked to circumvent their instability upon dilution in human fluids...
September 6, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/30196141/lipid-bilayer-coated-nanogels-allow-for-sustained-release-and-enhanced-internalization
#14
Chao Qin, Yaqi Lv, Chaoran Xu, Jingjing Li, Lifang Yin, Wei He
Nanoparticle drug delivery system improves the therapeutic efficacy of a drug; however, achieving sustained release from nanoparticles is challenging, owing to the increase of surface area and pronounced burst release. In this study, by incorporating an organogel of 12-hydroxystearic acid (12-HSA) into lipid-bilayers, a gel-liposomal formulation was developed to sustain drug release over time. The lipid-bilayer-coated nanogels (LBCNs) with a particle size of approximately 200 nm and with a core-shell structure had an entrapment efficiency of up to 80% for paclitaxel...
September 6, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/30196140/downscaling-of-the-tableting-process-feasibility-of-miniaturized-forced-feeders-on-a-high-speed-rotary-tablet-press
#15
W Grymonpré, B Blahova Prudilova, V Vanhoorne, B Van Snick, F Detobel, J P Remon, T De Beer, C Vervaet
With the current transformation of the pharmaceutical industry towards continuous manufacturing, there is an inherent need to embrace this concept already during the early stages of drug formulation. Therefore, this research paper investigated the feasibility of using miniaturized forced feeders on a high-speed rotary tablet press with the intention of downscaling the tableting process. Forced feeders with a reduced volume (up to 46% compared to the conventional two-compartment forced feeder) were designed by either sealing one compartment (i...
September 6, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/30196139/effect-of-excipients-on-encapsulation-and-release-of-insulin-from-spray-dried-solid-lipid-microparticles
#16
Chengyu Wu, Marco van de Weert, Stefania G Baldursdottir, Mingshi Yang, Huiling Mu
The study aimed at investigating the potential of spray drying method for encapsulation of protein drugs into solid lipid microparticles (MP) and evaluating effects of excipients on encapsulation and release of protein from MP. After transformation of model protein insulin to insulin-phospholipid complex, it was dissolved together with lipid excipients in organic solvent, which was spray-dried to form solid lipid MP. Polymeric MP with D, L-lactic-co-glycolic acid (PLGA) were prepared similarly. Around 90% of insulin was encapsulated in glycerol monostearate MP and glycerol distearate MP, whereas the encapsulation efficiency was 60% and 35% for tristearate (TG18) MP and tribehenate (TG22) MP, respectively...
September 6, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/30195082/vaginal-bifidobacterium-breve-for-preventing-urogenital-infections-development-of-delayed-release-mucoadhesive-oral-tablets
#17
Barbara Giordani, Luz Maria Melgoza, Carola Parolin, Claudio Foschi, Antonella Marangoni, Angela Abruzzo, Francesco Dalena, Teresa Cerchiara, Federica Bigucci, Barbara Luppi, Beatrice Vitali
Bifidobacteria are predominant microorganisms in the intestinal flora, but at the same time represent a subdominant group of the vaginal microbiota. For this reason, oral administration of these probiotic bacteria can provide beneficial effect for both intestinal and urogenital ecosystems. The first aim of this study was to test the strain Bifidobacterium breve BC204, isolated from a vaginal swab of a healthy woman, for its capability to adhere to human cells, to survive to gastric acids and bile salts and to exert antimicrobial activities...
September 5, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/30195081/investigation-on-the-impact-of-powder-arching-in-small-die-filling
#18
Hui Ping Goh, Paul Wan Sia Heng, Celine Valeria Liew
The flow of particulate materials is critical during processes such as mixing, compression and packing. Non-cohesive arching, a feature characteristic of coarse and free-flowing particles, has been studied extensively for silos and hoppers. However, the arching of powders during die fill has received much less attention. In this study, die fill performance of coarse and free-flowing nonpareils was evaluated using a specially designed die filling device in order to investigate the impact of non-cohesive arching during die fill under gravity flow...
September 5, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/30195080/manufacturing-and-characterization-of-long-acting-levonorgestrel-intrauterine-systems
#19
Quanying Bao, Bing Gu, Claire F Price, Yuan Zou, Yan Wang, Darby Kozak, Stephanie Choi, Diane J Burgess
Mirena® is long-acting (5 years) contraceptive intrauterine device. It is composed of a hollow cylindrical drug reservoir (containing Levonorgestrel and polydimethylsiloxane), which is covered with a release rate controlling silicone membrane. This structure presents a manufacturing challenge and to date, there have been no literature reports on the manufacturing, product design and quality evaluation of these hollow cylindrical intrauterine devices. It is vital to develop a reproducible and robust manufacturing process for these long-acting intrauterine devices or systems to obtain an understanding the in vitro and in vivo performance of such drug-device combinations...
September 5, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/30194012/in-vivo-evaluation-of-chitosan-based-local-delivery-systems-for-atorvastatin-in-treatment-of-periodontitis
#20
A Işılay Özdoğan, Yağmur D İlarslan, Kemal Kösemehmetoğlu, Gülçin Akca, H Burak Kutlu, Elnur Comerdov, Alper Iskit, Sevda Şenel
Periodontitis is a local inflammatory disease initiated by bacteria accumulation and results in cytokine mediated alveolar bone resorption and tissue destruction. In this study, the effect of locally delivered atorvastatin (2% w/v) containing chitosan formulations in the treatment of periodontitis was evaluated in rats with ligature induced periodontitis. The levels of interleukin-1beta (IL-1β), IL-6, IL-8, IL-10, transforming growth factor-β1 (TGF-β1), TGF-β2 and TGF-β3 were measured after treatment with formulations...
September 5, 2018: International Journal of Pharmaceutics
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