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Pharmaceutical Research

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https://www.readbyqxmd.com/read/28326459/preparation-and-evaluation-of-plga-coated-capsaicin-magnetic-nanoparticles
#1
Mrudhula Baskaran, Padmamalini Baskaran, Navamoney Arulsamy, Baskaran Thyagarajan
PURPOSE: Drugs used in the treatment of diseases can cause several unwanted systemic side effects. A site-specific drug delivery system can eliminate such consequences by delivering drugs to certain target areas of the body where therapeutic effects are required. Here we present the preparation and evaluation of magnetic nanoparticles of capsaicin, the active ingredient in chili peppers, coated with poly-L-lactide co-glycolide (PLGA), a FDA-approved biodegradable bioavailable polymer...
March 21, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28326458/vitamin-e-rich-nanoemulsion-enhances-the-antitumor-efficacy-of-low-dose-paclitaxel-by-driving-th1-immune-response
#2
Jun Ye, Wujun Dong, Yanfang Yang, Huazhen Hao, Hengfeng Liao, Bangyuan Wang, Xue Han, Yiqun Jin, Xuejun Xia, Yuling Liu
PURPOSE: To overcome the drawbacks of high dose regimen and improve the outcomes of chemotherapy at a low dose, an immunotherapeutic nanoemulsion based combination of chemotherapeutic agent (paclitaxel) with immunomodulatory agent (vitamin E) was developed and evaluated for their antitumor effect against breast cancer. METHODS: A total of five nanoemulsions loaded with various content of vitamin E were prepared and characterized. The immunoregulatory effects of vitamin E along with the overall antitumor efficacy of vitamin E-rich nanoemulsion with a low dose of paclitaxel were investigated through in vitro and in vivo experiments...
March 21, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28321609/the-cytotoxic-action-of-cytochrome-c-cardiolipin-nanocomplex-cyt-cl-on-cancer-cells-in-culture
#3
Yury A Vladimirov, Can Sarisozen, Georgy K Vladimirov, Nina Filipczak, Anastasia M Polimova, Vladimir P Torchilin
PURPOSE: The effect of existing anti-cancer therapies is based mainly on the stimulation of apoptosis in cancer cells. Here, we have demonstrated the ability of a catalytically-reactive nanoparticle-based complex of cytochrome c with cardiolipin (Cyt-CL) to induce the apoptosis and killing of cancer cells in a monolayer cell culture. METHODS: Cyt-CL nanoparticles were prepared by complexing CytC with different molar excesses of CL. Following characterization, cytotoxicity and apoptosis inducing effects of nanoparticles were investigated...
March 20, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28315084/multiple-lipid-nanoparticles-mln-a-new-generation-of-lipid-nanoparticles-for-drug-delivery-systems-lamivudine-mln-experimental-design
#4
Suellen M T Cavalcanti, Cláudia Nunes, Sofia A C Lima, José L Soares-Sobrinho, Salette Reis
PURPOSE: An optimized methodology for the development of a new generation of lipid nanoparticles, the multiple lipid nanoparticles (MLN) is described. MLN have characteristics between nanostructured lipid carriers (NLC) and multiple emulsions (W/O/W), but without the outer aqueous phase. METHODS: The production is based on a hot homogenization method combined with high shear and ultrasonication. The antiretroviral agent lamivudine (3TC), was loaded in the MLN. For comparison purposes, NLC-3TC formulation was also developed and physico-chemically characterized by the same parameters as MLN-3TC...
March 17, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28315083/achieving-the-promise-of-therapeutic-extracellular-vesicles-the-devil-is-in-details-of-therapeutic-loading
#5
REVIEW
Dhruvitkumar S Sutaria, Mohamed Badawi, Mitch A Phelps, Thomas D Schmittgen
Extracellular vesicles (EVs) represent a class of cell secreted organelles which naturally contain biomolecular cargo such as miRNA, mRNA and proteins. EVs mediate intercellular communication, enabling the transfer of functional nucleic acids from the cell of origin to the recipient cells. In addition, EVs make an attractive delivery vehicle for therapeutics owing to their increased stability in circulation, biocompatibility, low immunogenicity and toxicity profiles. EVs can also be engineered to display targeting moieties on their surfaces which enables targeting to desired tissues, organs or cells...
March 17, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28299534/interdependence-of-dosage-form-microstructure-and-performance
#6
J Axel Zeitler, Thomas Rades
No abstract text is available yet for this article.
March 15, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28289997/innovative-microcapsules-for-pancreatic-%C3%AE-cells-harvested-from-mature-double-transgenic-mice-cell-imaging-viability-induced-glucose-stimulated-insulin-measurements-and-proinflammatory-cytokines-analysis
#7
Armin Mooranian, Ryu Tackechi, Emma Jamieson, Grant Morahan, Hani Al-Salami
PURPOSE: Recently we demonstrated that microencapsulation of a murine pancreatic β-cell line using an alginate-ursodeoxycholic acid (UDCA) matrix produced microcapsules with good stability and cell viability. In this study, we investigated if translation of this formulation to microencapsulation of primary β-cells harvested from mature double-transgenic healthy mice would also generate stable microcapsules with good cell viability. METHODS: Islets of Langerhans were isolated from Ngn3-GFP/RIP-DsRED mice by intraductal collagenase P digestion and density gradient centrifugation, dissociated into single cells and the β-cell population purified by Fluorescence Activated Cell Sorting...
March 13, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28283859/combination-of-sedds-and-preactivated-thiomer-technology-incorporation-of-a-preactivated-thiolated-amphiphilic-polymer-into-self-emulsifying-delivery-systems
#8
Gergely Hetényi, Janine Griesser, Isabelle Nardin, Andreas Bernkop-Schnürch
PURPOSE: The aim of the study was to create novel mucoadhesive drug delivery systems by incorporating amphiphilic hydrophobically modified, thiolated and preactivated polymers (preactivated thiomers) into self-emulsifying drug delivery systems (SEDDS). METHODS: L-Cysteine methyl ester was covalently attached to the polymeric backbone of Pemulen TR-2 and preactivated using 2-mercaptonicotinic acid (2-MNA). These thiomers were incorporated in a concentration of 0...
March 10, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28281205/transmembrane-domain-single-nucleotide-polymorphisms-impair-expression-and-transport-activity-of-abc-transporter-abcg2
#9
Noora Sjöstedt, Jeroen J M W van den Heuvel, Jan B Koenderink, Heidi Kidron
PURPOSE: To study the function and expression of nine naturally occurring single-nucleotide polymorphisms (G406R, F431L, S441N, P480L, F489L, M515R, L525R, A528T and T542A) that are predicted to reside in the transmembrane regions of the ABC transporter ABCG2. METHODS: The transport activity of the variants was tested in inside-out membrane vesicles from Sf9 insect and human derived HEK293 cells overexpressing ABCG2. Lucifer Yellow and estrone sulfate were used as probe substrates of activity...
March 9, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28281204/erratum-to-effect-of-crystallinity-on-electrostatic-charging-in-drypowder-inhaler-formulations
#10
Jennifer Wong, Philip Chi Lip Kwok, Tim Noakes, Ali Fathi, Fariba Dehghani, Hak-Kim Chan
No abstract text is available yet for this article.
March 9, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28271248/network-reconstruction-reveals-that-valproic-acid-activates-neurogenic-transcriptional-programs-in-adult-brain-following-traumatic-injury
#11
Gerald A Higgins, Patrick Georgoff, Vahagn Nikolian, Ari Allyn-Feuer, Brian Pauls, Richard Higgins, Brian D Athey, Hasan E Alam
OBJECTIVES: To determine the mechanism of action of valproic acid (VPA) in the adult central nervous system (CNS) following traumatic brain injury (TBI) and hemorrhagic shock (HS). METHODS: Data were analyzed from different sources, including experiments in a porcine model, data from postmortem human brain, published studies, public and commercial databases. RESULTS: The transcriptional program in the CNS following TBI, HS, and VPA treatment includes activation of regulatory pathways that enhance neurogenesis and suppress gliogenesis...
March 7, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28251425/a-review-of-disintegration-mechanisms-and-measurement-techniques
#12
REVIEW
Daniel Markl, J Axel Zeitler
Pharmaceutical solid dosage forms (tablets or capsules) are the predominant form to administer active pharmaceutical ingredients (APIs) to the patient. Tablets are typically powder compacts consisting of several different excipients in addition to the API. Excipients are added to a formulation in order to achieve the desired fill weight of a dosage form, to improve the processability or to affect the drug release behaviour in the body. These complex porous systems undergo different mechanisms when they come in contact with physiological fluids...
March 1, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28251424/visualization-and-non-destructive-quantification-of-inkjet-printed-pharmaceuticals-on-different-substrates-using-raman-spectroscopy-and-raman-chemical-imaging
#13
Magnus Edinger, Daniel Bar-Shalom, Jukka Rantanen, Natalja Genina
PURPOSE: The purpose of this study was to investigate the applicability of Raman spectroscopy for visualization and quantification of inkjet-printed pharmaceuticals. METHODS: Haloperidol was used as a model active pharmaceutical ingredient (API), and a printable ink base containing lactic acid and ethanol was developed. Inkjet printing technology was used to apply haloperidol ink onto three different substrates. Custom-made inorganic compacts and dry foam, as well as marketed paracetamol tablets were used as the substrates...
March 1, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28247168/high-penetration-of-paclitaxel-in-abdominal-wall-of-rabbits-after-hyperthermic-intraperitoneal-administration-of-nab-paclitaxel-compared-to-standard-paclitaxel-formulation
#14
Federico Coccolini, Fabio Acocella, Lavinia Morosi, Stefano Brizzola, Matteo Ghiringhelli, Marco Ceresoli, Enrico Davoli, Luca Ansaloni, Maurizio D'Incalci, Massimo Zucchetti
PURPOSE: Paclitaxel (PTX) is currently used in combination with cisplatin for Hyperthermic Intraperitoneal Chemotherapy (HIPEC) for the treatment of peritoneal carcinomatosis. Albumin-bound PTX is a promising new drug for HIPEC because of its easy solubility in aqueous perfusion medium and possibly because of the tendency of albumin to cross physiological barriers and accumulate in tumor tissue. METHODS: We tested the feasibility of using nab-paclitaxel in rabbits treated by HIPEC for 60 min compared with the classical formulation at an equivalent PTX dose...
February 28, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28243955/development-of-a-level-a-in-vitro-in-vivo-correlation-for-veliparib-abt-888-extended-release-tablet-formulation
#15
Rajendar K Mittapalli, Silpa Nuthalapati, Alyssa E Delke DeBord, Hao Xiong
PURPOSE: The aim of the current manuscript is to develop and validate a level A in vitro-in vivo correlation (IVIVC) for veliparib extended-release (ER) tablet formulations. METHODS: The in vitro release profiles of veliparib formulations were determined using USP Dissolution Apparatus 2 with 900 mL of 0.1 N HCl at 75 rpm. In a clinical study, 24 subjects with solid tumors received one of the ER formulations (200 mg): fast (Formulation A), intermediate (Formulation B), and slow (Formulation C), and two 100 mg immediate release capsules (Formulation D)...
February 27, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28236061/the-routine-clinical-use-of-pharmacogenetic-tests-what-it-will-require
#16
REVIEW
Mafalda M Dias, Michael J Sorich, Andrew Rowland, Michael D Wiese, Ross A McKinnon
Pharmacogenetic testing aims to personalize drug therapy with a view to optimising drug efficacy and minimise toxicity. However, despite the potential benefits, pharmacogenetic testing is mostly confined to specialised medical areas, laboratories and centres. Widespread integration into routine clinical practice has been limited by a complex set of issues including regulatory and reimbursement frameworks, evidence of clinical utility and clinician perspectives, practices and education. Here we assess the current barriers to widespread clinical uptake and identify the key issue necessary to address to accelerate routine testing...
February 24, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28224388/ocular-safety-of-intravitreal-clindamycin-hydrochloride-released-by-plga-implants
#17
Gabriella M Fernandes-Cunha, Silvia Ligório Fialho, Gisele Rodrigues da Silva, Armando Silva-Cunha, Min Zhao, Francine Behar-Cohen
BACKGROUND: Drug ocular toxicity is a field that requires attention. Clindamycin has been injected intravitreally to treat ocular toxoplasmosis, the most common cause of eye posterior segment infection worldwide. However, little is known about the toxicity of clindamycin to ocular tissues. We have previously showed non intraocular toxicity in rabbit eyes of poly(lactic-co-glycolic acid) (PLGA) implants containing clindamycin hydrochloride (CLH) using only clinical macroscotopic observation...
February 21, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28224387/evaluation-of-the-ros-inhibiting-activity-and-mitochondrial-targeting-of-phenolic-compounds-in-fibroblast-cells-model-system-and-enhancement-of-efficiency-by-natural-deep-eutectic-solvent-nades-formulation
#18
Erwann Durand, Jérôme Lecomte, Rashmi Upasani, Béatrice Chabi, Christelle Bayrasy, Bruno Baréa, Elodie Jublanc, Martyn J Clarke, David J Moore, Jonathan Crowther, Chantal Wrutniak-Cabello, Pierre Villeneuve
PURPOSE: Many phenolics have already been tested for their antioxidant activities using in vitro methods. However, such assays do not consider the complexity of real cellular systems, and most of the phenolics characterized with such assays shows disappointing results when evaluated in cells. Accordingly, there is a need to develop effective screening methods. METHODS: Antioxidants were first evaluated by CAT assay and then, evaluated for their ability (i) to reduce the level of ROS using fluorescent probe, (ii) to cross fibroblast cell membranes using confocal microscopy, and (iii) to target mitochondria...
February 21, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28213842/determination-of-the-porosity-of-plga-microparticles-by-tracking-their-sedimentation-velocity-using-a-flow-imaging-microscope-flowcam
#19
A S Sediq, S K D Waasdorp, M R Nejadnik, M M C van Beers, J Meulenaar, R Verrijk, W Jiskoot
PURPOSE: To investigate whether particle sedimentation velocity tracking using a flow imaging microscope (FlowCAM) can be used to determine microparticle porosity. METHODS: Two different methods were explored. In the first method the sedimentation rate of microparticles was tracked in suspending media with different densities. The porosity was calculated from the average apparent density of the particles derived by inter- or extrapolation to the density of a suspending medium in which the sedimentation velocity was zero...
February 17, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28205004/maturation-of-oxycodone-pharmacokinetics-in-neonates-and-infants-a-population-pharmacokinetic-model-of-three-clinical-trials
#20
Pyry Välitalo, Merja Kokki, Veli-Pekka Ranta, Klaus T Olkkola, Andrew C Hooker, Hannu Kokki
PURPOSE: The aim of the current population pharmacokinetic study was to quantify oxycodone pharmacokinetics in children ranging from preterm neonates to children up to 7 years of age. METHODS: Data on intravenous or intramuscular oxycodone administration were obtained from three previously published studies (n = 119). The median [range] postmenstrual age of the subjects was 299 days [170 days-7.8 years]. A population pharmacokinetic model was built using 781 measurements of oxycodone plasma concentration...
February 15, 2017: Pharmaceutical Research
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