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https://www.readbyqxmd.com/read/28430398/impact-of-acid-reducing-agents-on-the-pharmacokinetics-of-palbociclib-a-weak-base-with-ph-dependent-solubility-with-different-food-intake-conditions
#1
Wan Sun, Karen J Klamerus, Lisa M Yuhas, Sylvester Pawlak, Anna Plotka, Melissa O'Gorman, Leonid Kirkovsky, Maha Kosa, Diane Wang
Palbociclib free base capsule is a weak base drug with highly pH-dependent solubility. In vitro and in vivo studies evaluated the impact of acid-reducing agents on exposure of palbociclib and determined whether the impact, if any, can be mitigated by food. A drug-drug interaction study (study 1) was conducted first under fasted conditions and showed that coadministration of multiple doses of the proton-pump inhibitor rabeprazole substantially reduced palbociclib mean area under the concentration-time curve from time 0 to infinity and maximum observed plasma concentration by 62% and 80%, respectively...
April 21, 2017: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/28429740/micelle-template-synthesis-of-hollow-silica-spheres-for-improving-water-vapor-permeability-of-waterborne-polyurethane-membrane
#2
Yan Bao, Tong Wang, Qiaoling Kang, Chunhua Shi, Jianzhong Ma
Hollow silica spheres (HSS) with special interior spaces, high specific surface area and excellent adsorption and permeability performance were synthesized via micelle-template method using cetyl trimethyl ammonium bromide (CTAB) micelles as soft template and tetraethoxysilane (TEOS) as silica precursor. SEM, TEM, FT-IR, XRD, DLS and BET-BJH were carried out to characterize the morphology and structure of as-obtained samples. The results demonstrated that the samples were amorphous with a hollow structure and huge specific surface area...
April 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28418442/network-analysis-and-percolation-transition-in-hydrogen-bonded-clusters-nitric-acid-and-water-extracted-by-tributyl-phosphate
#3
Michael J Servis, David T Wu, Jenifer C Braley
Extraction of polar molecules by amphiphilic species results in a complex variety of clusters whose topologies and energetics control phase behavior and efficiency of liquid-liquid separations. A computational approach including quantum mechanical vibrational frequency calculations and molecular dynamics simulation with intermolecular network theory is used to provide a robust assessment of extractant and polar solute association through hydrogen bonding in the tributyl phosphate (TBP)/HNO3/H2O/dodecane system for the first time...
April 18, 2017: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/28407531/precise-ratiometric-loading-of-ptx-and-dox-based-on-redox-sensitive-mixed-micelles-for-cancer-therapy
#4
Dujuan Zhao, Jilian Wu, Chuanxiang Li, Huiyuan Zhang, Zhonghao Li, Yuxia Luan
PTX and DOX have different anticancer mechanisms. The combination of the two anticancer drugs could synergically enhance their anticancer effect, but simultaneously accompanied by severe side effects. In the present study, we constructed a mixed micelle system based on redox-sensitive mPEG-SS-PTX and mPEG-SS-DOX conjugate. The drug delivery system has a fixed and high drug loading content of 24.2% (PTX∼14.8% and DOX∼9.4%) with a precise ratio of PTX and DOX to realize the synchronized and controlled release...
April 2, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28402119/impact-of-electrolyte-on-adsorption-at-the-air-water-interface-for-ternary-surfactant-mixtures-above-the-critical-micelle-concentration
#5
Jessica R Liley, Robert K Thomas, Jeffrey Penfold, Ian M Tucker, Jordan T Petkov, Paul Stevenson, John R P Webster
The composition of the air-water adsorbed layer of the ternary surfactant mixture, octaethylene monododecyl ether, C12E8, sodium dodecyl 6-benzenesulfonate, LAS, and sodium dioxyethylene glycol monododecyl sulfate, SLES, and of each of the binary mixtures, with varying amounts of electrolyte, has been studied by neutron reflectivity. The measurements were made above the mixed critical micelle concentration. In the absence of electrolyte adsorption is dominated by the nonionic component C12E8 but addition of electrolyte gradually changes this so that SLES and LAS dominate at higher electrolyte concentrations...
April 20, 2017: Langmuir: the ACS Journal of Surfaces and Colloids
https://www.readbyqxmd.com/read/28398739/precipitate-coacervate-transformation-in-polyelectrolyte-mixed-micelle-systems
#6
Fatih Comert, Duy Nguyen, Marguerite Rushanan, Peker Milas, Amy Y Xu, Paul L Dubin
The polycation/anionic-nonionic mixed micelle, poly(diallyldimethylammonium chloride)-sodium dodecyl sulfate/Triton X-100 (PDADMAC-SDS/TX100), is a model polyelectrolyte-colloid system in that the micellar mole fraction of SDS (Y) controls the micelle surface charge density, thus modulating the polyelectrolyte-colloid interaction. The exquisite temperature dependence of this system provides an important additional variable, controlling both liquid-liquid (L-L) and liquid-solid (L-S) phase separation, both of which are driven by the entropy of small ion release...
April 19, 2017: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/28397883/chemical-and-mechanical-modulation-of-polymeric-micelle-assembly
#7
Nicholas E Clay, Joseph J Whittenberg, Jiayu Leong, Vivek Kumar, Jinrong Chen, Insil Choi, Evangelos Liamas, Jeremy M Schieferstein, Jae Hyun Jeong, Dong Hyun Kim, Zhenyu Jason Zhang, Paul J A Kenis, Il Won Kim, Hyunjoon Kong
Recently, polymeric micelles self-assembled from amphiphilic polymers have been studied for various industrial and biomedical applications. This nanoparticle self-assembly typically occurs in a solvent-exchange process. In this process, the quality of the resulting particles is uncontrollably mediated by polymeric solubility and mixing conditions. Here, we hypothesized that improving the solubility of an amphiphilic polymer in an organic solvent via chemical modification while controlling the mixing rate of organic and aqueous phases would enhance control over particle morphology and size...
April 20, 2017: Nanoscale
https://www.readbyqxmd.com/read/28392687/folic-acid-functionalized-drug-delivery-platform-of-resveratrol-based-on-pluronic-127-d-%C3%AE-tocopheryl-polyethylene-glycol-1000-succinate-mixed-micelles
#8
Jifu Hao, Tiantian Tong, Kai Jin, Qiannan Zhuang, Te Han, Yanping Bi, Jianzhu Wang, Xiaodan Wang
A folic acid (FA)-functionalized drug vehicle platform based on Pluronic 127 (P127)/D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) mixed micelles was orchestrated for an effective delivery of the model drug resveratrol in order to address the problem of poor water solubility and rapid metabolism of resveratrol and improve its targeted accumulation at tumor site. The FA-decorated mixed micelles were prepared using thin-film hydration method and optimized by central composite design approach. The micelles were also characterized in terms of size and morphology, drug entrapment efficiency and in vitro release profile...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28372227/lipid-digestion-micelle-formation-and-carotenoid-bioaccessibility-kinetics-influence-of-emulsion-droplet-size
#9
L Salvia-Trujillo, S H E Verkempinck, L Sun, A M Van Loey, T Grauwet, M E Hendrickx
Carotenoid-enriched oil-in-water emulsions with different droplet sizes (small: d43 0.72μm; medium: d43 1.9μm; large: d43 15.1μm) were subjected to simulated gastrointestinal conditions. The kinetics of lipolysis, micelle formation and carotenoid bioaccessibility were monitored during the intestinal phase. The rates of all three processes increased with decreasing droplet size. The large droplet size emulsion contained undigested oil at the end of digestion, whereas an almost complete hydrolysis was observed for the other two emulsions...
August 15, 2017: Food Chemistry
https://www.readbyqxmd.com/read/28358225/improved-solubility-and-oral-bioavailability-ofapigeninvia-soluplus%C3%A2-pluronic-f127binary-mixed-micelles-system
#10
Zhenhai Zhang, Changchang Cui, Fang Wei, Huixia Lv
The aim of this study was to develop a novel mix micelles system composing of two biocompatible copolymers of Soluplus® and Pluronic F127 to improve the solubility, oral bioavailability of insoluble drug apigenin (AP) as model drug. The AP-loaded mixed micelles (AP-M) were prepared by ethanol thin-film hydration method. The formed optimal formulation of AP-M were provided with small size (178.5 nm) and spherical shape at ratio of 4: 1 (Soluplus®: Pluronic F127), as well as increasing solubility of to 5...
March 30, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28353420/antibody-adsorption-on-the-surface-of-water-studied-by-neutron-reflection
#11
Charles Smith, Zongyi Li, Robert Holman, Fang Pan, Richard A Campbell, Mario Campana, Peixun Li, John R P Webster, Steven Bishop, Rojaramani Narwal, Shahid Uddin, Christopher F van der Walle, Jian R Lu
Surface and interfacial adsorption of antibody molecules could cause structural unfolding and desorbed molecules could trigger solution aggregation, resulting in the compromise of physical stability. Although antibody adsorption is important and its relevance to many mechanistic processes has been proposed, few techniques can offer direct structural information about antibody adsorption under different conditions. The main aim of this study was to demonstrate the power of neutron reflection to unravel the amount and structural conformation of the adsorbed antibody layers at the air/water interface with and without surfactant, using a monoclonal antibody 'COE-3' as the model...
April 2017: MAbs
https://www.readbyqxmd.com/read/28351690/tailoring-thermal-treatment-to-form-liprotide-complexes-between-oleic-acid-and-different-proteins
#12
Henrik V Sørensen, Jannik N Pedersen, Jan Skov Pedersen, Daniel Erik Otzen
Liprotides are protein-lipid complexes in which the fatty acids form a micelle-like core surrounded by a shell of partially unfolded protein molecules. These complexes can be formed in different ways. The simplest approach is a thermal treatment where protein and fatty acid are mixed and then incubated at elevated temperatures. Using this approach we here demonstrate that we can monitor liprotide formation in real time using Small-Angle X-ray Scattering (SAXS). Optimal conditions for liprotide formation, i...
March 27, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28347946/a-two-component-micelle-with-emergent-ph-responsiveness-by-mixing-dilauroyl-phosphocholine-and-deoxycholic-acid-and-its-delivery-of-proteins-into-the-cytosol
#13
Noriko Miyamoto, Shota Fujii, Shinichi Mochizuki, Kazuo Sakurai, Naoki Sakaguchi, Kazunori Koiwai
Providing appropriate pH responsiveness for drug delivery nanoparticles is one of the major issues in developing a new generation of delivery systems. This paper reports that, when phosphocholine and a bile acid were mixed, the resultant two-component micelle gained pH responsiveness, while the individual components did not show any such responsiveness. The pH responsiveness was shown to be determined by the chemical structure, especially the positions and chirality of the OH groups, of the bile acid, and the sensitivity was determined by the alkyl chain length of the phosphocholine...
March 14, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28346751/d-fructose-modification-enhanced-internalization-of-mixed-micelles-in-breast-cancer-cells-via-glut5-transporters
#14
Xu Zhou, Xianyan Qin, Tao Gong, Zhi-Rong Zhang, Yao Fu
d-Fructose modified poly(ε-caprolactone)-polyethylene glycol (PCL-PEG-Fru) diblock amphiphile is synthesized via Cu(I)-catalyzed click chemistry, which self-assembles with D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) into PCL-PEG-Fru/TPGS mixed micelles (PPF MM). It has been proven that glucose transporter (GLUT)5 is overexpressed in MCF-7 cells other than L929 cells. In this study, PPF MM exhibit a significantly higher uptake efficiency than fructose-free PCL-PEG-N3 /TPGS mixed micelles in both 2D MCF-7 cells and 3D tumor spheroids...
March 27, 2017: Macromolecular Bioscience
https://www.readbyqxmd.com/read/28331225/cholesterol-attenuates-cytoprotective-effects-of-phosphatidylcholine-against-bile-salts
#15
Yoshito Ikeda, Shin-Ya Morita, Tomohiro Terada
Bile salts have potent detergent properties and damaging effects on cell membranes, leading to liver injury. However, the molecular mechanisms for the protection of hepatocytes against bile salts are not fully understood. In this study, we demonstrated that the cytotoxicity of nine human major bile salts to HepG2 cells and primary human hepatocytes was prevented by phosphatidylcholine (PC). In contrast, cholesterol had no direct cytotoxic effects but suppressed the cytoprotective effects of PC. PC reduced the cell-association of bile salt, which was reversed by cholesterol...
March 22, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28323118/mixed-poly-vinyl-pyrrolidone-based-drug-loaded-nanomicelles-shows-enhanced-efficacy-against-pancreatic-cancer-cell-lines
#16
Anisha Veeren, Archana Bhaw-Luximon, Debabrata Mukhopadhyay, Dhanjay Jhurry
We report in this paper on the enhanced efficacy of a physical mixture of two single anti-cancer loaded nanomicelles against PANC-1 and BxPC-3. Poly(vinyl pyrrolidone-b-polycaprolactone) (PVP-b-PCL) and poly(vinyl pyrrolidone-b-poly(dioxanone-co-methyl dioxanone)) (PVP-b-P(DX-co-MeDX)) were synthesized and successfully loaded with various anti-cancer drugs - gemcitabine (GEM), doxorubicin.HCl (DOX.HCl), doxorubicin.NH2 (DOX), 5-fluorouracil (5-FU) and paclitaxel (PTX). Spherical micelles of size 160-477 nm were obtained as characterized by DLS while sizes determined by TEM were in the range 140-250 nm...
March 18, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28317731/encapsulation-of-sesamol-in-phosphatidyl-choline-micelles-enhanced-bioavailability-and-anti-inflammatory-activity
#17
P S Yashaswini, Nawneet K Kurrey, Sridevi A Singh
Sesamol, the phenolic degradation product of sesamolin, although recognised for its anti-inflammatory effects, has low bioavailability. In this manuscript, we attempted to improve its bioavailability by encapsulation in mixed phosphatidylcholine micelles. Sesamol could be solubilised and entrapped in phosphatidylcholine mixed micelles (PCS) with 96.8% efficiency (particle size 3.0±0.06nm). Fluorescence spectra of PCS revealed lower relative fluorescence intensity (RFI 112) compared to 'free' sesamol (FS) (RFI 271)...
August 1, 2017: Food Chemistry
https://www.readbyqxmd.com/read/28300426/soluplus-tpgs-mixed-micelles-for-dioscin-delivery-in-cancer-therapy
#18
Jing Zhao, Youwei Xu, Changyuan Wang, Yanfang Ding, Manyu Chen, Yifei Wang, Jinyong Peng, Lei Li, Li Lv
BACKGROUND: Dioscin has shown cytotoxicity against cancer cells, but its poor solubility and stability have limited its clinical application. In this study, we designed mixed micelles composed of TPGS and Soluplus(®) copolymers entrapping the poorly soluble anticancer drug dioscin. METHOD: In order to improve the aqueous solubility and bioactivity of dioscin, TPGS/Soluplus(®) mixed micelles with an optimal ratio were prepared using a thin-film hydration method, and their physicochemical properties were characterized...
April 2, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28297991/solvent-free-molecular-level-modeling-of-self-assembling-amphiphiles-in-water
#19
Somajit Dey, Jayashree Saha
Aggregation mesophases of self-assembling amphiphiles in water are highly important in the context of biology (biomembranes), therapy (liposomes), industry (polymer surfactants), and condensed-matter physics (lyotropic liquid crystals). Besides helping to increase fundamental understanding of collective molecular behavior, simulations of these lyotropic phases are pivotal to technological and medical developments such as smart drug carriers for gene therapy. Implicit-solvent, coarse-grained, low resolution modeling with a simple pair potential is the key to realizing the larger length and time scales associated with such mesoscopic phenomena during a computer simulation...
February 2017: Physical Review. E
https://www.readbyqxmd.com/read/28294613/surface-adsorption-in-ternary-surfactant-mixtures-above-the-critical-micelle-concentration-effects-of-asymmetry-on-the-composition-dependence-of-the-excess-free-energy
#20
Jessica R Liley, Robert K Thomas, Jeffrey Penfold, Ian M Tucker, Jordan T Petkov, Paul Stevenson, John R P Webster
The composition of the adsorbed layer of a ternary surfactant mixture at the air-water interface has been studied by neutron reflectivity. The adsorption of the ternary mixture of octaethylene monododecyl ether (C12E8) sodium dodecyl 6-benzene sulfonate (LAS), and sodium dioxyethylene glycol monododecyl sulfate (SLES), as well as each of the binary mixtures, at solution concentrations greater than the mixed critical micelle concentration is highly nonideal. In the ternary mixture, the surface adsorption is dominated by C12E8 and LAS, and there is little SLES at the interface...
March 28, 2017: Journal of Physical Chemistry. B
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