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Molecular Pharmaceutics

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https://www.readbyqxmd.com/read/28700237/rgd-modified-albumin-nanoconjugates-for-targeted-delivery-of-a-porphyrin-photosensitizer
#1
Fang Li, Yan Zhao, Chengqiong Mao, Yi Kong, Xin Ming
Advances in photodynamic therapy of cancer have been restrained by lack of cancer specificity and side effects to normal tissues. Molecularly targeted photodynamic therapy can achieve higher cancer specificity by combination of active cancer targeting and localized laser activation. We aimed to use albumin as a carrier to prepare targeted nanoconjugates that are selective to cancer cells and smaller than conventional nanoparticles for superior tumor penetration. IRDye 700DX (IR700), a porphyrin photosensitizer, was covalently conjugated to human serum albumin that was also linked with tumor-targeting RGD peptides...
July 25, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28737945/preliminary-pet-study-of-18-f-fc119s-in-normal-and-alzheimer-s-disease-models
#2
Se Jong Oh, Min Hwan Kim, Sang Jin Han, Kyung Jun Kang, In Ok Ko, YoungSoo Kim, Ji Ae Park, Jae Yong Choi, Kyo Chul Lee, Dae Yoon Chi, Yong Jin Lee, Kyeong Min Kim
To evaluate the efficacy of (18)F-FC119S as a positron emission tomography (PET) radiopharmaceutical for the imaging of Alzheimer's disease (AD), we studied the drug absorption characteristics and (18)F-FC119S distribution in normal mice. In addition, we evaluated the specificity of (18)F-FC119S for β-amyloid (Aβ) in the AD group of an APP/PS1 mouse model and compared it with that in the wild-type (WT) group. (18)F-FC119S exhibited the characteristics of rapid brain uptake and washout patterns in the normal mice...
July 24, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28737925/lipid-bilayer-gated-mesoporous-silica-nanocarriers-for-tumor-targeted-delivery-of-zoledronic-acid-in-vivo
#3
Diti Desai, Jixi Zhang, Jouko Sandholm, Jaakko Lehtimäki, Tove Grönroos, Johanna Tuomela, Jessica M Rosenholm
Zoledronic acid (ZOL) is a nitrogen-containing bisphosphonate used for the treatment of bone diseases and calcium metabolism. Anticancer activity of ZOL has been established, but its extraskeletal effects are limited due to its rapid uptake and accumulation to bone hydroxyapatite. In this work, we report on the development of tethered lipid bilayer-gated mesoporous silica nanocarriers (MSNs) for the incorporation, retention and intracellular delivery of ZOL. The in vitro anticancer activity of ZOL-loaded nanocarriers was evaluated by cell viability assay and live-cell imaging...
July 24, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28737923/co-silencing-intestinal-transglutaminase-2-and-interleukin-15-using-gelatin-based-nanoparticles-in-an-in-vitro-model-of-celiac-disease
#4
Husain Attarwala, Valerie Clausen, Prasoon Chaturvedi, Mansoor M Amiji
In this study, we have developed type B gelatin-based nanoparticle based siRNA delivery system for silencing of intestinal transglutaminase-2 (TG2) and interleukin-15 (IL-15) genes in cultured human intestinal epithelial cells (Caco-2) and murine alveolar macrophage cells (J774A.1). Small interfering RNA (siRNA) targeting the TG2 or IL-15 gene was encapsulated within gelatin nanoparticles using ethanol-water solvent displacement method. Size, charge and morphology of gelatin nanoparticles were evaluated using Zetasizer instrument and transmission electron microscopy...
July 24, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28737409/low-buffer-capacity-and-alternating-motility-along-the-human-gastrointestinal-tract-implications-for-in-vivo-dissolution-and-absorption-of-ionizable-drugs
#5
Bart Hens, Yasuhiro Tsume, Marival Bermejo, Paulo Paixao, Mark Koenigsknecht, Jason R Baker, William L Hasler, R Lionberger, Jianghong Fan, Joseph Dickens, Kerby A Shedden, Bo Wen, Jeffrey Wysocki, Raimar Löbenberg, Allen Lee, Ann F Fioritto, Gregory E Amidon, Alex Yu, Gail Benninghoff, Niloufar Salehi, Arjang Talattof, Duxin Sun, Gordon L Amidon
In this study, we determined the pH and buffer capacity of human gastrointestinal (GI) fluids (aspirated from the stomach, duodenum, proximal jejunum and mid/distal jejunum) as a function of time, from 37 healthy subjects after oral administration of an 800 mg immediate-release tablet of ibuprofen (reference listed drug; RLD) under typical prescribed bioequivalence (BE) study protocol conditions in both fasted and fed state (simulated by ingestion of a liquid meal). Simultaneously, motility was continuously monitored using water-perfused manometry...
July 24, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28737406/preclinical-effect-of-absorption-modifying-excipients-on-rat-intestinal-transport-of-five-model-compounds-and-the-intestinal-barrier-marker-51-cr-edta
#6
David Dahlgren, Carl Roos, Anders Lundqvist, Peter Langguth, Christer Tannergren, Markus Sjöblom, E Sjögren, H Lennernas
There is a renewed interest from the pharmaceutical field to develop oral formulations of compounds such as peptides, oligonucleotides, and polar drugs. However, these often suffer from insufficient absorption across the intestinal mucosal barrier. One approach to circumvent this problem is the use of absorption modifying excipient(s) (AME). This study determined the absorption enhancing effect of four AMEs (sodium dodecyl sulfate, caprate, chitosan, N-acetylcysteine) on five model compounds in a rat jejunal perfusion model...
July 24, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28737403/validation-of-dissolution-testing-with-biorelevant-media-an-orbito-study
#7
James Mann, Jennifer B Dressman, Karin Rosenblatt, Lee Ashworth, Uwe Muenster, Kerstin Frank, Paul Hutchins, James Williams, Lukas Klumpp, Kristina Wielockx, Philippe Berben, Patrick Augustijns, Rene Holm, Michael Hofmann, Sanjaykumar Patel, Stefania Beato, Krista Ojala, Irena Tomaszewska, Jean-Luc Bruel, James Butler
BACKGROUND: Dissolution testing with biorelevant media has become widespread in the pharmaceutical industry as a means of better understanding how drugs and formulations behave in the gastrointestinal tract. Until now, however, there have been few attempts to gauge the reproducibility of results obtained with these methods. PURPOSE: The aim of this study was to determine the inter-laboratory reproducibility of biorelevant dissolution testing, using the paddle apparatus (USP 2)...
July 24, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28737398/in-vivo-mechanisms-of-intestinal-drug-absorption-from-aprepitant-nanoformulations
#8
Carl Roos, David Dahlgren, Staffan Berg, Jan Westergren, Bertil Abrahamsson, Christer Tannergren, E Sjögren, H Lennernas
Over recent decades there has been an increase in the proportion of BCS class II and IV drug candidates in industrial drug development. To overcome the biopharmaceutical challenges associated with the less favorable properties of solubility and/or intestinal permeation of these substances, the development of formulations containing nanosuspensions of the drugs has been suggested. The intestinal absorption of aprepitant from two nanosuspensions (20 µM and 200 µM total concentrations) in phosphate buffer, one nanosuspension (200 µM) in fasted-state simulated intestinal fluid (FaSSIF), and one solution (20 µM) in FaSSIF was investigated in the rat single-pass intestinal perfusion model...
July 24, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28731350/gastric-and-duodenal-ethanol-concentrations-after-intake-of-alcoholic-beverages-in-postprandial-conditions
#9
Jari Rubbens, Danny Riethorst, Joachim Brouwers, Kris Wolfs, Erwin Adams, Jan Tack, Patrick Augustijns
INTRODUCTION: This study determined intraluminal ethanol concentrations (stomach and duodenum) in fed healthy volunteers after the consumption of common alcoholic beverages (beer, wine and whisky). The results of this study were compared with a previous study in fasted volunteers. MATERIALS AND METHODS: Five healthy volunteers were recruited in a cross-over study. The fed state was simulated by ingestion of 250 mL of Nutridrink Compact® Neutral. Volunteers subsequently consumed two standard units of beer (Stella Artois®, 500 mL, 5...
July 21, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28728419/apoferritin-nanocage-for-brain-targeted-doxorubicin-delivery
#10
Zhijiang Chen, Meifang Zhai, Xiang Yang Xie, Yue Zhang, Siyu Ma, Zhiping Li, Fanglin Yu, Baoquan Zhao, Min Zhang, Yang Yang, Xingguo Mei
An ideal brain-targeted nanocarrier must be sufficiently potent to penetrate the blood-brain barrier (BBB) and sufficiently competent to target the cells of interest with adequate optimized physiochemical features and biocompatibility. However, it is an enormous challenge to the researchers to organize the abovementioned properties into a single nanocarrier particle. New frontiers in nanomedicine are advancing the research of new biomaterials. Herein, we demonstrate a straightforward strategy for brain targeting by encapsulating doxorubicin (DOX) into a naturally available and unmodified apoferritin nanocage (DOX-loaded APO)...
July 20, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28728415/-177-lu-labelled-cyclic-minigastrin-analogues-with-therapeutic-activity-in-cck2r-expressing-tumours-preclinical-evaluation-of-a-kit-formulation
#11
Christine Rangger, Maximilian Klingler, Lajos Balogh, Zita Pöstényi, Andras Polyak, Dariusz Pawlak, Renata Mikołajczak, Elisabeth von Guggenberg
Minigastrin (MG) analogues specifically target cholecystokinin-2 receptors (CCK2R) expressed in different tumours and enable targeted radiotherapy of advanced and disseminated disease when radiolabelled with a beta emitter such as (177)Lu. Especially truncated MG analogues missing the penta-Glu sequence are associated with low kidney retention and seem therefore most promising for therapeutic use. Based on [D-Glu1,desGlu2-6]MG (MG11) we have designed the two cyclic MG analogues cyclo1,9[γ-D-Glu1,desGlu2-6,D-Lys9]MG (cyclo-MG1) and cyclo1,9[γ-D-Glu1,desGlu2-6,D-Lys9,Nle11]MG (cyclo-MG2)...
July 20, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28727430/renal-clearable-peptide-functionalized-nagdf4-nanodots-for-high-efficiency-tracking-orthotopic-colorectal-tumor-in-mouse
#12
Hongda Chen, Xiaodong Li, Fuyao Liu, Huimao Zhang, Zhenxin Wang
The effective delivery of bioimaging probes to a selected cancerous tissue has extensive significance for biological studies and clinical investigations. Herein, the peptide functionalized NaGdF4 nanodots (termed as, pPeptide-NaGdF4 nanodots) have been prepared for highly efficient magnetic resonance imaging (MRI) of tumor by formation of Gd-phosphonate coordinate bonds among hydrophobic NaGdF4 nanodots (4.2 nm in diameter) with mixed phosphorylated peptide ligands including a tumor targeting phosphopeptide and a cell penetrating phosphopeptide...
July 20, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28726424/self-encapsulating-poly-lactic-co-glycolic-acid-plga-microspheres-for-intranasal-vaccine-delivery
#13
Brittany A Bailey, Kashappa-Goud H Desai, Lukasz J Ochyl, Susan M Ciotti, James J Moon, Steven P Schwendeman
Herein we describe a formulation of self-encapsulating poly(lactic-co-glycolic acid) (PLGA) microspheres for vaccine delivery. Self-healing encapsulation is a novel encapsulation method developed by our group that enables the aqueous loading of large molecules into pre-made PLGA microspheres. Calcium phosphate (CaHPO4) adjuvant gel was incorporated into the microspheres as a protein-trapping agent for improved encapsulation of antigen. Microspheres were found to have a median size of 7.05 ± 0.31 µm, with a w/w loading of 0...
July 20, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28665620/multifunctional-desferrichrome-analogues-as-versatile-89-zr-iv-chelators-for-immunopet-probe-development
#14
Casey J Adams, Justin J Wilson, Eszter Boros
New bifunctional hexa- and octadentate analogues of the hydroxamate-containing siderophore desferrichrome (DFC) have been synthesized and evaluated as (89)Zr-chelating agents for immunoPET applications. The in vitro and in vivo inertness of these new ligands, Orn3-hx (hexadentate) and Orn-4hx derivatives (octadentate), was compared to the gold standard hexadentate, hydroxamate-containing chelator for (89)Zr desferrioxamine (DFO). Density functional theory was employed to model the geometries of the resulting Zr(IV) complexes and to predict their relative stabilities as follows: Zr(Orn4-hx) > Zr(DFC) > Zr(Orn3-hx)...
July 19, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28719220/egfr-targeted-cationic-polymeric-mixed-micelles-for-co-delivery-of-gemcitabine-and-mir-205-for-treating-advanced-pancreatic-cancer
#15
Goutam Mondal, Saud Almawash, Amit Kumar Chaudhary, Ram I Mahato
Gemcitabine (GEM), a first-line chemotherapy for pancreatic cancer undergoes rapid metabolism and develops chemoresistance after repeated administration. We previously demonstrated that the combination of GEM and miR-205 provides an effective therapeutic strategy to sensitize GEM-resistant pancreatic cancer cells. Since epidermal growth factor receptor (EGFR) is overexpressed in pancreatic cancer cells, in this study, we aimed to deliver mixed micelles containing GEM and miR-205 decorated with EGFR-targeting cetuximab (C225) monoclonal antibody for targeted therapy...
July 18, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28712302/overcoming-the-hydrolytic-lability-of-a-reaction-intermediate-in-production-of-protein-drug-conjugates-conjugation-of-an-acyclic-nucleoside-phosphonate-to-a-model-carrier-protein
#16
Shengsheng Xu, Igor A Kaltashov
Acquired immunodeficiency syndrome (AIDS) remains one of the most serious public health challenges and a significant cause of mortality for certain populations. Despite the large number of antiretrovirals developed in the past two decades, the inability of small molecule therapeutics to target HIV reservoirs directly creates a significant obstacle to their effective utilization. Indeed, achieving the desired therapeutic outcome in the absence of an effective means of targeted delivery must rely on dosage escalation, which frequently causes severe toxicity...
July 17, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28712300/a-continuous-intestinal-absorption-model-based-on-the-convection-diffusion-equation
#17
Swati Nagar, Richard C Korzekwa, Ken Korzekwa
Prediction of the rate and extent of drug absorption upon oral dosing needs models that capture the complexities of both the drug molecule and intestinal physiology. We report here the development of a continuous intestinal absorption model based on the convection-diffusion equation. The model includes explicit enterocyte apical membrane and intracellular lipid radial compartments along the length of the intestine. Physiologic functions along length x are built into the model, and include velocity, diffusion, surface areas, and pH of the intestine...
July 17, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28661152/profiles-and-gender-specifics-of-udp-glucuronosyltransferases-and-sulfotransferases-expressions-in-the-major-metabolic-organs-of-wild-type-and-efflux-transporter-knockout-fvb-mice
#18
Jiamei Chen, Haihui Zheng, Sijing Zeng, Cong Xie, Xiaoyan Li, Tongmeng Yan, Xia Gong, Linlin Lu, Xiaoxiao Qi, Ying Wang, Ming Hu, Lijun Zhu, Zhongqiu Liu
Hepatic and extrahepatic tissues participate in xenobiotic detoxication, carcinogen activation, prodrug processing, and estrogen regulation through UDP-glucuronosyltransferases (UGTs/Ugts) and sulfotransferases (SULTs/Sults). Wild-type (WT) and efflux transporter knockout (KO) FVB mice have been commonly used to perform the studies of pharmacokinetics, metabolism, and toxicity. We employed the developed UHPLC-MS/MS approach to gain systematic insight on gender-specific of Ugts and Sults in major metabolic organs...
July 17, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28708400/contribution-of-mate1-to-renal-secretion-of-the-nmda-receptor-antagonist-memantine
#19
Fabian Müller, Dietmar Weitz, Volker Derdau, Martin Sandvoss, Katharina Mertsch, Jörg König, Martin F Fromm
The weak base memantine is actively secreted into urine, however the underlying mechanisms are insufficiently understood. Potential candidates involved in memantine renal secretion are organic cation transporter 2 (OCT2) and multidrug and toxin extrusion proteins (MATE1, MATE2-K). The aim of this in vitro study was the examination of the interaction of memantine with OCT2 and MATEs. Memantine transporter inhibition and transport were examined in HEK cells expressing human OCT2, MATE1, or MATE2-K. Monolayers of single- (MDCK-OCT2, MDCK-MATE1) and double-transfected MDCK cells (MDCK-OCT2-MATE1) were used for studies on vectorial, basal to apical memantine transport...
July 14, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28704056/a-nano-in-nano-polymer-dendrimer-nanoparticle-based-nanosystem-for-controlled-multidrug-delivery
#20
Zongmin Zhao, Song Lou, Yun Hu, Jie Zhu, Chenming Zhang
Codelivery of multiple chemotherapeutics with different action mechanisms is a promising strategy for cancer treatment. In this study, we developed a novel polymer-dendrimer hybrid nanoparticle-based nanosystem for efficient and controlled codelivery of two model chemotherapeutics, doxorubicin (DOX) and paclitaxel (PTX). The nanosystem was characterized to have a nano-in-nano structure with a size of around 150 nm. The model drugs could feasibly be loaded into the nanosystem ratiometrically with high drug-loading contents by controlling the feeding drug ratios...
July 27, 2017: Molecular Pharmaceutics
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