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Pharmaceutical Research

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https://www.readbyqxmd.com/read/28527126/polycaprolactone-based-nanoparticles-loaded-with-indomethacin-for-anti-inflammatory-therapy-from-preparation-to-ex-vivo-study
#1
Waisudin Badri, Karim Miladi, Sophie Robin, Céline Viennet, Qand Agha Nazari, Géraldine Agusti, Hatem Fessi, Abdelhamid Elaissari
PURPOSE: This work focused on the preparation of polycaprolactone based nanoparticles containing indomethacin to provide topical analgesic and anti-inflammatory effect for symptomatic treatment of inflammatory diseases. Indomethacin loaded nanoparticles are prepared for topical application to decrease indomethacin side effects and administration frequency. Oppositely to already reported works, in this research non-invasive method has been used for the enhancement of indomethacin dermal drug penetration...
May 19, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28523384/the-need-for-restructuring-the-disordered-science-of-amorphous-drug-formulations
#2
REVIEW
Khadijah Edueng, Denny Mahlin, Christel A S Bergström
The alarming numbers of poorly soluble discovery compounds have centered the efforts towards finding strategies to improve the solubility. One of the attractive approaches to enhance solubility is via amorphization despite the stability issue associated with it. Although the number of amorphous-based research reports has increased tremendously after year 2000, little is known on the current research practice in designing amorphous formulation and how it has changed after the concept of solid dispersion was first introduced decades ago...
May 18, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28516400/sytematic-investigation-of-the-role-of-surfactant-composition-and-choice-of-oil-design-of-a-nanoemulsion-based-adjuvant-inducing-concomitant-humoral-and-cd4-t-cell-responses
#3
Signe Tandrup Schmidt, Malene Aaby Neustrup, Stine Harloff-Helleberg, Karen Smith Korsholm, Thomas Rades, Peter Andersen, Dennis Christensen, Camilla Foged
PURPOSE: Induction of cell-mediated immune (CMI) responses is crucial for vaccine-mediated protection against difficult vaccine targets, e.g., Chlamydia trachomatis (Ct). Adjuvants are included in subunit vaccines to potentiate immune responses, but many marketed adjuvants stimulate predominantly humoral immune responses. Therefore, there is an unmet medical need for new adjuvants, which potentiate humoral and CMI responses. The purpose was to design an oil-in-water nanoemulsion adjuvant containing a synthetic CMI-inducing mycobacterial monomycoloyl glycerol (MMG) analogue to concomitantly induce humoral and CMI responses...
May 17, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28512718/development-of-in-vitro-in-vivo-correlation-for-potassium-chloride-extended-release-tablet-formulation-using-urinary-pharmacokinetic-data
#4
Rajendar K Mittapalli, Patrick Marroum, Yihong Qiu, Kathleen Apfelbaum, Hao Xiong
PURPOSE: To develop and validate a Level A in vitro-in vivo correlation (IVIVC) for potassium chloride extended-release (ER) formulations. METHODS: Three prototype ER formulations of potassium chloride with different in vitro release rates were developed and their urinary pharmacokinetic profiles were evaluated in healthy subjects. A mathematical model between in vitro dissolution and in vivo urinary excretion, a surrogate for measuring in vivo absorption, was developed using time-scale and time-shift parameters...
May 16, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28508123/photochemically-controlled-drug-dosing-from-a-polymeric-scaffold
#5
Louise Donnelly, John G Hardy, Sean P Gorman, David S Jones, Nicola J Irwin, Colin P McCoy
PURPOSE: To develop the first photoactive biomaterial coating capable of controlled drug dosing via inclusion of synthesised drug-3,5-dimethoxybenzoin (DMB) conjugates in a poly(2-methyoxyethyl acrylate) (pMEA) scaffold. METHODS: Flurbiprofen- and naproxen-DMB conjugates were prepared via esterification and characterised via NMR spectroscopy and mass spectrometry following chromatographic purification. Conjugate photolysis was investigated in acetonitrile solution and within the pMEA matrix following exposure to low-power 365 nm irradiation...
May 15, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28508122/a-trivalent-enzymatic-system-for-uricolytic-therapy-of-hprt-deficiency-and-lesch-nyhan-disease
#6
Luca Ronda, Marialaura Marchetti, Riccardo Piano, Anastasia Liuzzi, Romina Corsini, Riccardo Percudani, Stefano Bettati
PURPOSE: Because of the evolutionary loss of the uricolytic pathway, humans accumulate poorly soluble urate as the final product of purine catabolism. Restoration of uricolysis through enzyme therapy is a promising treatment for severe hyperuricemia caused by deficiency of hypoxanthine-guanine phosphoribosyltransferase (HPRT). To this end, we studied the effect of PEG conjugation on the activity and stability of the enzymatic complement required for conversion of urate into the more soluble (S)-allantoin...
May 15, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28493100/characterization-of-temperature-profiles-in-skin-and-transdermal-delivery-system-when-exposed-to-temperature-gradients-in-vivo-and-in-vitro
#7
Qian Zhang, Michael Murawsky, Terri LaCount, Jinsong Hao, Gerald B Kasting, Bryan Newman, Priyanka Ghosh, Sam G Raney, S Kevin Li
PURPOSE: Performance of a transdermal delivery system (TDS) can be affected by exposure to elevated temperature, which can lead to unintended safety issues. This study investigated TDS and skin temperatures and their relationship in vivo, characterized the effective thermal resistance of skin, and identified the in vitro diffusion cell conditions that would correlate with in vivo observations. METHODS: Experiments were performed in humans and in Franz diffusion cells with human cadaver skin to record skin and TDS temperatures at room temperature and with exposure to a heat flux...
May 10, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28493099/anti-inflammatory-therapeutic-effect-of-adiponectin-gene-delivery-using-a-polymeric-carrier-in-an-acute-lung-injury-model
#8
Chunxian Piao, Jeong Hyun Park, Minhyung Lee
PURPOSE: Adiponectin (APN) is an adipokine with anti-inflammatory and cytoprotective effects. In this study, the therapeutic effect of APN gene delivery using a polymeric carrier was evaluated in an acute lung injury (ALI) model. METHODS: Polyethylenimine (2 kDa, PEI2K), PEI25K (25 kDa), polyamidoamine (generation 2, PAMG2), dexamethasone-conjugated PEI2k (PEI2K-Dexa), and dexamethasone-conjugated PAMG2 (PAMG2-Dexa) were evaluated in vitro and in vivo as gene carriers...
May 10, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28493098/personalized-therapeutics-and-pharmacogenomics-integral-to-personalized-health-care
#9
EDITORIAL
Wolfgang Sadee
No abstract text is available yet for this article.
May 10, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28484975/a-clinical-cassette-dosing-study-for-evaluating-the-contribution-of-hepatic-oatps-and-cyp3a-to-drug-drug-interactions
#10
Takashi Yoshikado, Kazuya Maeda, Sawako Furihata, Hanano Terashima, Takeshi Nakayama, Keiko Ishigame, Kazunobu Tsunemoto, Hiroyuki Kusuhara, Ken-Ichi Furihata, Yuichi Sugiyama
PURPOSE: To demonstrate the relative importance of organic anion-transporting polypeptides (OATPs) and cytochrome P450 3A (CYP3A) in the hepatic elimination of substrate drugs. METHODS: A cocktail of subtherapeutic doses of bosentan, repaglinide, clarithromycin, darunavir, simeprevir, and midazolam (CYP3A probe) was administered orally to eight healthy volunteers. Rifampicin (OATP inhibitor; 600 mg, p.o.) and itraconazole (CYP3A inhibitor; 200 mg, i.v.) were coadministered with the cocktail in the second and third phases, respectively...
May 8, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28470471/expression-and-activity-of-breast-cancer-resistance-protein-bcrp-abcg2-in-human-distal-lung-epithelial-cells-in-vitro
#11
Sabrina Nickel, Mohammed Ali Selo, Juliane Fallack, Caoimhe G Clerkin, Hanno Huwer, Nicole Schneider-Daum, Claus-Michael Lehr, Carsten Ehrhardt
PURPOSE: Breast cancer resistance protein (BCRP/ABCG2) has previously been identified with high expression levels in human lung. The subcellular localisation and functional activity of the transporter in lung epithelia, however, remains poorly investigated. The aim of this project was to study BCRP expression and activity in freshly isolated human alveolar epithelial type 2 (AT2) and type 1-like (AT1-like) cells in primary culture, and to compare these findings with data obtained from the NCI-H441 cell line...
May 3, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28466393/improved-stability-and-enhanced-oral-bioavailability-of-atorvastatin-loaded-stearic-acid-modified-gelatin-nanoparticles
#12
Deepanshu Shilpi, Varun Kushwah, Ashish Kumar Agrawal, Sanyog Jain
PURPOSE: The present study evaluates the effects of stearic acid conjugation with gelatin and, its pharmaceutical potential to formulate novel atorvastatin (AT) loaded nanoparticles. METHOD: AT loaded stearic acid modified gelatin nanoparticles (AT-MG NPs) were prepared via two-step desolvation method with extensive optimization of different process variables. Further, the developed nanoparticles where evaluated against in vitro Caco-2 cell model and in vivo bioavailability...
May 2, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28466392/preemptive-panel-based-pharmacogenetic-testing-the-time-is-now
#13
Kristin W Weitzel, Larisa H Cavallari, Lawrence J Lesko
While recent discoveries have paved the way for the use of genotype-guided prescribing in some clinical environments, significant debate persists among clinicians and researchers about the optimal approach to pharmacogenetic testing in clinical practice. One crucial factor in this debate surrounds the timing and methodology of genotyping, specifically whether genotyping should be performed reactively for targeted genes when a single drug is prescribed, or preemptively using a panel-based approach prior to drug prescribing...
May 2, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28455777/insights-into-nano-and-micron-scale-phase-separation-in-amorphous-solid-dispersions-using-fluorescence-based-techniques-in-combination-with-solid-state-nuclear-magnetic-resonance-spectroscopy
#14
Hitesh S Purohit, James D Ormes, Sugandha Saboo, Yongchao Su, Matthew S Lamm, Amanda K P Mann, Lynne S Taylor
PURPOSE: Miscibility between the drug and the polymer in an amorphous solid dispersion (ASD) is considered to be one of the most important factors impacting the solid state stability and dissolution performance of the active pharmaceutical ingredient (API). The research described herein utilizes emerging fluorescence-based methodologies to probe (im)miscibility of itraconazole (ITZ)-hydroxypropyl methylcellulose (HPMC) ASDs. METHODS: The ASDs were prepared by solvent evaporation with varying evaporation rates and were characterized by steady-state fluorescence spectroscopy, confocal imaging, differential scanning calorimetry (DSC), and solid state nuclear magnetic resonance (ssNMR) spectroscopy...
April 28, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28432535/exploring-the-carbamazepine-interaction-with-human-pregnane-x-receptor-and-effect-on-abcc2-using-in-vitro-and-in-silico-approach
#15
Gurpreet K Grewal, Khuraijam D Singh, Neha Kanojia, Chitra Rawat, Samiksha Kukal, Ajay Jajodia, Anshika Singhal, Richa Misra, Selvaraman Nagamani, Karthikeyan Muthusamy, Ritushree Kukreti
PURPOSE: Over expression of ATP-binding cassette transporters is considered one of the major reasons for non-responsiveness to antiepileptic drugs. Carbamazepine (CBZ), one of first line antiepileptic drug is known to influence ABCC2 expression but its exact molecular mechanism is unknown. METHODS: We investigated the effect of CBZ on expression of ABCC2 and pregnane X receptor (PXR) in HepG2 cell line and compared with hyperforin (agonist of PXR) and ketoconazole (antagonist of PXR) through realtime PCR and western blot assay...
April 21, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28421307/an-efficient-and-rapid-method-to-monitor-the-oxidative-degradation-of-protein-pharmaceuticals-probing-tyrosine-oxidation-with-fluorogenic-derivatization
#16
Rupesh Bommana, Olivier Mozziconacci, Y John Wang, Christian Schöneich
PURPOSE: The loss of potency of protein therapeutics can be linked to the oxidation of specific amino acid residues leading to a great variety of oxidative modifications. The comprehensive identification of these oxidative modifications requires high-resolution mass spectrometry analysis, which requires time and expensive resources. Here, we propose a fluorogenic derivatization method of oxidized Tyr and Phe yielding benzoxazole derivatives, as an orthogonal technique for the rapid screening of protein oxidation...
April 18, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28421306/breast-cancer-resistance-protein-and-multidrug-resistance-protein-2-regulate-the-disposition-of-acacetin-glucuronides
#17
Huangyu Jiang, Jia Yu, Haihui Zheng, Jiamei Chen, Jinjun Wu, Xiaoxiao Qi, Ying Wang, Xinchun Wang, Ming Hu, Lijun Zhu, Zhongqiu Liu
PURPOSE: To determine the mechanism responsible for acacetin glucuronide transport and the bioavailability of acacetin. METHODS: Area under the curve (AUC), clearance (CL), half-life (T1/2) and other pharmacokinetic parameters were determined by the pharmacokinetic model. The excretion of acacetin glucuronides was evaluated by the mouse intestinal perfusion model and the Caco-2 cell model. RESULTS: In pharmacokinetic studies, the bioavailability of acacetin in FVB mice was 1...
April 18, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28405914/cyclosporine-a-loaded-electrospun-poly-d-l-lactic-acid-poly-ethylene-glycol-nanofibers-drug-carriers-utilizable-in-local-immunosuppression
#18
Jakub Sirc, Zuzana Hampejsova, Jana Trnovska, Petr Kozlik, Jakub Hrib, Radka Hobzova, Alena Zajicova, Vladimir Holan, Zuzana Bosakova
PURPOSE: The present study aims to prepare poly(D,L-lactic acid) (PLA) nanofibers loaded by the immunosuppressant cyclosporine A (CsA, 10 wt%). Amphiphilic poly(ethylene glycol)s (PEG) additives were used to modify the hydrophobic drug release kinetics. METHODS: Four types of CsA-loaded PLA nanofibrous carriers varying in the presence and molecular weight (MW) of PEG (6, 20 and 35 kDa) were prepared by needleless electrospinning. The samples were extracted for 144 h in phosphate buffer saline or tissue culture medium...
April 12, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28405913/in-vitro-transport-activity-and-trafficking-of-mrp2-abcc2-polymorphic-variants
#19
Xia Wen, Melanie S Joy, Lauren M Aleksunes
PURPOSE: Multidrug resistance-associated protein 2 (MRP2/ABCC2) is an efflux pump that removes drugs and chemicals from cells. We sought to characterize the expression, trafficking and in vitro activity of seven single nucleotide polymorphisms (SNPs) in the ABCC2 gene. METHODS: ABCC2 SNPs were generated using site-directed mutagenesis and stably expressed in Flp-In HEK293 cells, which allows targeted insertion of transgenes within the genome. Total and cell surface expression of MRP2 as well as accumulation of substrates (calcein AM and 5(6)-carboxy-2',7'-dichlorofluorescein diacetate, CDCF) were quantified in cells or inverted membrane vesicles expressing wild-type (WT) or variant forms...
April 12, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28405912/continuous-transdermal-delivery-of-l-dopa-based-on-a-self-assembling-nanomicellar-system
#20
Amnon C Sintov, Haim V Levy, Igor Greenberg
PURPOSE: When levodopa (L-DOPA) is administered orally, it is eliminated from the body very quickly resulting in a series of sharp fluctuations in its blood concentrations. These frequent changes in blood levels are considered to be responsible for the development of late motor complications and dyskinesias, which are troubling clinical and treatment issues in Parkinson's disease. Transdermal drug delivery is a patient-compliant method for delivering therapeutics into the systemic circulation in a continuous and controlled manner...
April 12, 2017: Pharmaceutical Research
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