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International Journal of Pharmaceutics

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https://www.readbyqxmd.com/read/28818458/colonic-delivery-of-indometacin-loaded-pga-co-pdl-microparticles-coated-with-eudragit-l100-55-from-fast-disintegrating-tablets
#1
Hesham M Tawfeek, Ahmed A H Abdellatif, Thomas J Dennison, Afzal R Mohmmed, Younis Sadiq, Imran Y Saleem
The aim of this work was to investigate the efficient targeting and delivery of indometacin (IND), as a model anti-inflammatory drug to the colon for treatment of inflammatory bowel disease. We prepared fast disintegrating tablets (FDT) containing IND encapsulated within poly(glycerol-adipate-co-ɷ-pentadecalactone), PGA-co-PDL, microparticles and coated with Eudragit L100-55 at different ratios (1:1.5, 1:1, 1:0.5). Microparticles encapsulated with IND were prepared using an o/w single emulsion solvent evaporation technique and coated with Eudragit L-100-55 via spray drying...
August 14, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28811118/prediction-and-characterization-of-the-stability-enhancing-effect-of-the-cherry-tag%C3%A2-in-highly-concentrated-protein-solutions-by-complex-rheological-measurements-and-md-simulations
#2
Pascal Baumann, Marie-Therese Schermeyer, Hannah Burghardt, Cathrin Dürr, Jonas Gärtner, Jürgen Hubbuch
Solution stability attributes are one of the key parameters within the production and launching phase of new biopharmaceuticals. Instabilities of active biological compounds can reduce the yield of biopharmaceutical productions, and may induce undesired reactions in patients, such as immunogenic rejections. Protein solution stability thus needs to be engineered and monitored throughout production and storage. In contrast to the gold standard of long-term storage experiments applied in industry, novel experimental and in silico molecular dynamics tools for predicting protein solution stability can be applied within several minutes or hours...
August 12, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28811117/bilayered-buccal-films-as-child-appropriate-dosage-form-for-systemic-administration-of-propranolol
#3
Angela Abruzzo, Fiore Pasquale Nicoletta, Francesco Dalena, Teresa Cerchiara, Barbara Luppi, Federica Bigucci
Buccal mucosa has emerged as an attractive site for systemic administration of drug in paediatric patients. This route is simple and non-invasive, even if the saliva wash-out effect and the relative permeability of the mucosa can reduce drug absorption. Mucoadhesive polymers represent a common employed strategy to increase the contact time of the formulation at the application site and to improve drug absorption. Among the different mucoadhesive dosage forms, buccal films are particularly addressed for paediatric population since they are thin, adaptable to the mucosal surface and able to offer an exact and flexible dose...
August 12, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28807566/electrospun-collagen-based-nanofibres-a-sustainable-material-for-improved-antibiotic-utilisation-in-tissue-engineering-applications
#4
Ivan J Hall Barrientos, Eleonora Paladino, Peter Szabó, Sarah Brozio, Peter J Hall, Charles I Oseghale, Melissa K Passarelli, Susan J Moug, Richard A Black, Clive G Wilson, Romana Zelkó, Dimitrios A Lamprou
For the creation of scaffolds in tissue engineering applications, it is essential to control the physical morphology of fibres and to choose compositions which do not disturb normal physiological function. Collagen, the most abundant protein in the human body, is a well-established biopolymer used in electrospinning compositions. It shows high in-vivo stability and is able to maintain a high biomechanical strength over time. In this study, the effects of collagen type I in polylactic acid-drug electrospun scaffolds for tissue engineering applications are examined...
August 11, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28803939/bubble-generating-nano-lipid-carriers-for-ultrasound-ct-imaging-guided-efficient-tumor-therapy
#5
Nan Zhang, Jia Li, Ruirui Hou, Jiangnan Zhang, Pei Wang, Xinyang Liu, Zhenzhong Zhang
Ideal therapeutic effectiveness of chemotherapy is obtained only when tumor cells are exposed to a maximal drug concentration, which is often hindered by dose-limiting toxicity. We designed a bubble-generating liposomal delivery system by introducing ammonium bicarbonate and gold nanorods into folic acid-conjugated liposomes to allow both multimodal imaging and the local release of drug (doxorubicin) with hyperthermia. The key component, ammonium bicarbonate, allows a controlled, rapid release of doxorubicin to provide an effective drug concentration in the tumor microenvironment...
August 10, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28803938/organoids-as-preclinical-models-to-improve-intraperitoneal-chemotherapy-effectiveness-for-colorectal-cancer-patients-with-peritoneal-metastases-preclinical-models-to-improve-hipec
#6
P Roy, C Canet-Jourdan, M Annereau, O Zajac, M Gelli, S Broutin, L Mercier, A Paci, F Lemare, M Ducreux, D Elias, D Malka, V Boige, D Goéré, F Jaulin
BACKGROUND: Peritoneal metastases (PM), corresponding to tumor implants into the peritoneal cavity, are associated with impaired prognosis and low responsiveness to systemic chemotherapy. A new therapeutic approach has dramatically changed the prognosis of patients with PM from colorectal cancer (CRC), consisting in the association of a complete cytoreductive surgery followed by intraperitoneal chemotherapy associated to hyperthermia (HIPEC). Many drugs have been administered intraperitoneally, but no clear consensus has been approved...
August 10, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28802795/atomic-layer-deposition-a-novel-method-for-the-ultrathin-coating-of-minitablets
#7
Jaana Hautala, Tommi Kääriäinen, Pekka Hoppu, Marianna Kemell, Jyrki Heinämäki, David Cameron, Steven George, Anne Mari Juppo
We introduce atomic layer deposition (ALD) as a novel method for the ultrathin coating (nanolayering) of minitablets. The effects of ALD coating on the tablet characteristics and taste masking were investigated and compared with the established coating method. Minitablets containing bitter tasting denatonium benzoate were coated by ALD using three different TiO2 nanolayer thicknesses (number of deposition cycles). The established coating of minitablets was performed in a laboratory-scale fluidized-bed apparatus using four concentration levels of aqueous Eudragit(®) E coating polymer...
August 9, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28802794/a-novel-and-organic-solvent-free-preparation-of-solid-lipid-nanoparticles-using-natural-biopolymers-as-natural-emulsifier-and-stabilizer
#8
Jingyi Xue, Taoran Wang, Qiaobin Hu, Mingyong Zhou, Yangchao Luo
In this work, a new and novel organic solvent-free and synthetic surfactant-free method was reported to fabricate stable solid lipid nanoparticles (SLNs) from stearic acid, sodium caseinate (NaCas) and pectin, as well as water. Melted stearic acid was directly emulsified into an aqueous phase containing NaCas and pectin, followed by pH adjustment and thermal treatment to induce the formation of a compact and dense polymeric coating which stabilized SLNs. The preparation procedures and formulations were comprehensively optimized...
August 9, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28802793/pickering-emulsions-stabilized-by-biodegradable-block-copolymer-micelles-for-controlled-topical-drug-delivery
#9
Faiza Laredj-Bourezg, Marie-Alexandrine Bolzinger, Jocelyne Pelletier, Yves Chevalier
Surfactant-free biocompatible and biodegradable Pickering emulsions were investigated as vehicles for skin delivery of hydrophobic drugs. O/w emulsions of medium-chain triglyceride (MCT) oil droplets loaded with all-trans retinol as a model hydrophobic drug were stabilized by block copolymer nanoparticles: either poly(lactide)-block-poly(ethylene glycol) (PLA-b-PEG) or poly(caprolactone)-block-poly(ethylene glycol) (PCL-b-PEG). Those innovative emulsions were prepared using two different processes allowing drug loading either inside oil droplets or inside both oil droplets and non-adsorbed block copolymer nanoparticles...
August 9, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28801109/modelling-and-understanding-powder-flow-properties-and-compactability-of-selected-active-pharmaceutical-ingredients-excipients-and-physical-mixtures-from-critical-material-properties
#10
Zelalem Ayenew Worku, Dinesh Kumar, João Victor Gomes, Yunliang He, Brian Glennon, Kiran A Ramisetty, Åke C Rasmuson, Peter O'Connell, Kieran Gallagher, Trevor Woods, Nalini R Shastri, Anne-Marie Healy
The development of solid dosage forms and manufacturing processes are governed by complex physical properties of the powder and the type of pharmaceutical unit operation the manufacturing processes employs. Suitable powder flow properties and compactability are crucial bulk level properties for tablet manufacturing by direct compression. It is also generally agreed that small scale powder flow measurements can be useful to predict large scale production failure. In this study, predictive multilinear regression models were effectively developed from critical material properties to estimate static powder flow parameters from particle size distribution data for a single component and for binary systems...
August 8, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28801108/breaching-barriers-in-glioblastoma-part-ii-targeted-drug-delivery-and-lipid-nanoparticles
#11
REVIEW
Ana Miranda, María Blanco-Prieto, João Sousa, Alberto Pais, Carla Vitorino
Tailored nanocarriers have gained huge research focus for brain drug delivery, aimed at combating several neuro-oncological conditions, such as the glioblastoma multiforme (GBM). The progress of knowledge on the pathogenesis of GBM has allowed identifying the major hurdles for efficient treatment, encompassing biological interfaces (blood-brain barrier and blood-brain tumour barrier), specificities of tumour microenvironment, as well as both bulk and glioma stem cell subpopulations. These findings provided new insights into the molecular basis of GBM, being a strong driving force behind development of targeted nanomedicines in this area...
August 8, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28801107/nanoprecipitation-process-from-encapsulation-to-drug-delivery
#12
REVIEW
Claudia Janeth Martínez Rivas, Mohamad Tarhini, Waisudin Badri, Karim Miladi, Hélène Greige-Gerges, Qand Agha Nazari, Sergio Arturo Galindo Rodríguez, Rocío Álvarez Román, Hatem Fessi, Abdelhamid Elaissari
Drugs encapsulation is a suitable strategy in order to cope with the limitations of conventional dosage forms such as unsuitable bioavailability, stability, taste, and odor. Nanoprecipitation technique has been used in the pharmaceutical and agricultural research as clean alternative for other drug carrier formulations. This technique is based on precipitation mechanism. Polymer precipitation occurs after the addition of a non-solvent to a polymer solution in four steps mechanism: supersaturation, nucleation, growth by condensation, and growth by coagulation that leads to the formation of polymer nanoparticles or aggregates...
August 8, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28797969/bioactive-mesoporous-silica-nanostructures-with-anti-microbial-and-anti-biofilm-properties
#13
Paul Cătălin Balaure, Bianca Boarca, Roxana Cristina Popescu, Diana Savu, Roxana Trusca, Bogdan Ștefan Vasile, Alexandru Mihai Grumezescu, Alina Maria Holban, Alexandra Bolocan, Ecaterina Andronescu
The increasing rate of antibiotic resistant bacteria associated with nosocomial infections in severely ill patients has urged the need for new antibacterial therapies. Nanostructured materials represent emerging innovative approaches to controlled delivery of different antimicrobial drugs. Delivery systems encapsulating natural compounds with antibacterial effects, such as essential oils have shown a great potential. Herein we report the development of SiO2 mesoporous nanosystems loaded with eucalyptus (EUC), orange (ORA), and cinnamon (CIN) essential oils...
August 7, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28797968/a-polychromatic-turbidity-microplate-assay-to-distinguish-discovery-stage-drug-molecules-with-beneficial-precipitation-properties
#14
John Morrison, Michelle Nophsker, Paul Elzinga, Maria Donoso, Hyunsoo Park, Roy Haskell
A material sparing microplate screening assay was developed to evaluate and compare the precipitation of discovery stage drug molecules as a function of time, concentration and media composition. Polychromatic turbidity time course profiles were collected for cinnarizine, probucol, dipyridamole as well as BMS-932481, and compared with turbidity profiles of monodisperse particle size standards. Precipitation for select sample conditions were further characterized at several time points by size, morphology, amount and form via laser diffraction, microscopy, size based particle counting and X-ray diffraction respectively...
August 7, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28797967/multipurpose-tenofovir-disoproxil-fumarate-electrospun-fibers-for-the-prevention-of-hiv-1-and-hsv-2-infections-in-vitro
#15
Kevin M Tyo, Hung R Vuong, Danial A Malik, Lee B Sims, Houda Alatassi, Jinghua Duan, Walter H Watson, Jill M Steinbach-Rankins
Sexually transmitted infections affect hundreds of millions of people worldwide. Both human immunodeficiency virus (HIV-1 and -2) and herpes simplex virus-2 (HSV-2) remain incurable, urging the development of new prevention strategies. While current prophylactic technologies are dependent on strict user adherence to achieve efficacy, there is a dearth of delivery vehicles that provide discreet and convenient administration, combined with prolonged-delivery of active agents. To address these needs, we created electrospun fibers (EFs) comprised of FDA-approved polymers, poly(lactic-co-glycolic acid) (PLGA) and poly(DL-lactide-co-ε-caprolactone) (PLCL), to provide sustained-release and in vitro protection against HIV-1 and HSV-2...
August 7, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28789886/an-advanced-technique-using-an-electronic-taste-sensing-system-to-evaluate-the-bitterness-of-orally-disintegrating-films-and-the-evaluation-of-model-films
#16
Yoshiko Takeuchi, Rina Usui, Hidekazu Ikezaki, Kohei Tahara, Hirofumi Takeuchi
Taste detection systems using electronic sensors are needed in the field of pharmaceutical design. The aim of this study was to propose an advanced technique using a taste-sensing system to evaluate the bitterness of an orally disintegrating film (ODF) samples. In this system, a solid film sample is kept in the test medium with stirring, and the sensor output is recorded. Model films were prepared using a solution-casting method with a water-soluble polymer such as pullulan, HPMC, HPC or PVP as film formers, and donepezil hydrochloride and quinine hydrochloride as model bitter-tasting active pharmaceutical ingredients (APIs)...
August 5, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28789885/ultra-thin-hydro-films-based-on-lactose-crosslinked-fish-gelatin-for-wound-healing-applications
#17
Alaitz Etxabide, Claudia Vairo, Edorta Santos-Vizcaino, Pedro Guerrero, Jose Luis Pedraz, Manoli Igartua, Koro de la Caba, Rosa Maria Hernandez
This study focuses on the development and characterization of an ultra thin hydro-film based on lactose-mediated crosslinking of fish gelatin by Maillard reaction. Lactose results in the only efficient crosslinker able to produce resistant to handling hydro-films when compared to conventional crosslinkers such as glutaraldehyde or genipin (tested at 25 and 37°C in phosphate buffer saline solution (PBS)).The disappearance of the peak related to the N-containing groups (XPS) and the images obtained by SEM and AFM demonstrate the highly ordered nano-scaled structure of lactose-crosslinked gelatin, confirming the crosslinking efficiency...
August 5, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28782582/development-and-in-vitro-characterization-of-a-papain-loaded-mucolytic-self-emulsifying-drug-delivery-system-sedds
#18
Christina Leichner, Claudia Menzel, Flavia Laffleur, Andreas Bernkop-Schnürch
The aim of the study was to create a self-emulsifying drug delivery system (SEDDS) with mucolytic properties based on incorporated papain for improved mucus permeation. In order to increase the lipophilicity of the enzyme and to dissolve it in SEDDS, hydrophobic ion pairing with sodium deoxycholate in a molar ratio of 20:1 (surfactant: enzyme) was performed. The yield of precipitated papain was 86.8±2.7% and the ion pair was loaded into the formulations to 1% (m/m). Suitable formulations were chosen according to their properties to dissolve the ion pair and characterized regarding droplet size and polydispersity index...
August 3, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28779987/a-novel-technique-for-the-visualization-of-tablet-punch-surfaces-characterization-of-surface-modification-wear-and-sticking
#19
Claudia Al-Karawi, Thomas Kaiser, Claudia S Leopold
The surface quality of tablets is strongly related to the surface quality of the tablet punch. Therefore, regular control of the punch surfaces is needed to determine the surface properties, the wear status and sticking tendency of the punches. The aim of the present study was to develop and evaluate a new technique to visualize and evaluate tablet punch surfaces using high-resolution impression molding combined with 3D surface analysis. Standardized 3D surface texture parameters were analyzed by principal component analysis (PCA) to characterized differently surface-modified punches, punches with different wear status and the sticking pattern on the punch surfaces...
August 3, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28779986/gas-adsorption-on-commercial-magnesium-stearate-effects-of-degassing-conditions-on-nitrogen-bet-surface-area-and-isotherm-characteristics
#20
Darren P Lapham, Julie L Lapham
Commercial grades of magnesium stearate have been analysed by nitrogen adsorption having been pre-treated at temperatures between 30°C and 110°C and in the as-received state. Characteristics of nitrogen adsorption/desorption isotherms are assessed through the linearity of low relative pressure isotherm data and the BET transform plot together with the extent of isotherm hysteresis. Comparison is made between thermal gravimetric analysis and mass loss on drying. Features of gas adsorption isotherms considered atypical are identified and possible causes presented...
August 2, 2017: International Journal of Pharmaceutics
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