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https://www.readbyqxmd.com/read/28323118/mixed-poly-vinyl-pyrrolidone-based-drug-loaded-nanomicelles-shows-enhanced-efficacy-against-pancreatic-cancer-cell-lines
#1
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 16, 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
#2
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%C3%A2-tpgs-mixed-micelles-for-dioscin-delivery-in-cancer-therapy
#3
Jing Zhao, Youwei Xv, 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...
March 16, 2017: Drug Development and Industrial Pharmacy
https://www.readbyqxmd.com/read/28297991/solvent-free-molecular-level-modeling-of-self-assembling-amphiphiles-in-water
#4
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-the-effects-of-asymmetry-on-the-composition-dependence-of-the-excess-free-energy
#5
Jessica Liley, Robert K Thomas, Jeff Penfold, Ian M Tucker, Jordan T Petkov, Paul Stevenson, John Robert Peter 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 sulphate, SLES, and of each of the binary mixtures, at solution concentrations greater than the mixed critical micelle concentration (CMC) are highly non-ideal. In the ternary mixture the surface adsorption is dominated by the C12E8 and LAS, and there is little SLES at the interface...
March 15, 2017: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/28283189/metal-ions-and-phosphatidylinositol-4-5-bisphosphate-as-interacting-effectors-of-%C3%AE-type-plant-phospholipase-d
#6
Lars Dreßler, Florian Michel, Iris Thondorf, Johanna Mansfeld, Ralph Golbik, Renate Ulbrich-Hofmann
Plant phospholipases D (PLD) are typically characterized by a C2 domain with at least two Ca(2+) binding sites. In vitro, the predominantly expressed α-type PLDs need 20-100 mM CaCl2 for optimum activity, whereas the essential activator of β- or γ-type PLDs, phosphatidylinositol 4,5-bisphosphate (PIP2), plays a secondary role. In the present paper, we have studied the interplay between PIP2 and metal ion activation of the well-known α-type PLD from cabbage (PLDα). With mixed micelles containing phosphatidyl-p-nitrophenol as substrate, PIP2-concentrations in the nanomolar range are able to activate the enzyme in addition to the essential Ca(2+) activation...
March 7, 2017: Phytochemistry
https://www.readbyqxmd.com/read/28275315/adsorption-and-aggregation-activity-of-sodium-dodecyl-sulfate-and-rhamnolipid-mixture
#7
Diana Mańko, Anna Zdziennicka, Bronisław Jańczuk
Measurements of the surface tension, density and viscosity of sodium dodecyl sulfate (SDS) and rhamnolipid (RL) mixtures were carried out in aqueous solution. From the obtained results, composition of mixed surface layer at the water-air interface, mixed micelles, parameter of intermolecular interactions, activity of SDS and RL in the surface layer and micelles, Gibbs standard free energy of adsorption and micellization as well as Gibbs free energy of SDS and RL mixing in the surface layer and micelles were established...
2017: Journal of Surfactants and Detergents
https://www.readbyqxmd.com/read/28267311/model-free-analysis-of-critical-micellar-concentrations-for-detecting-demixing-in-surfactant-mixtures
#8
Erik Frotscher, Jonas Höring, Grégory Durand, Carolyn Vargas, Sandro Keller
Aqueous mixtures of two or more surfactants are often employed for research or industrial purposes because such mixtures offer advantages over single-surfactant systems. This is particularly true for mixtures of fluorocarbon (FC) and hydrocarbon (HC) surfactants, which display a broad range of mutual miscibilities in mixed micelles. Unfortunately, the prediction and even the experimental elucidation of the micellar mixing behavior of surfactant mixtures remain challenging, as evidenced by conflicting results and conclusions derived from diverse, and often complex, mixing models...
March 21, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/28260893/enhancing-the-oral-bioavailability-of-biochanin-a-by-encapsulation-in-mixed-micelles-containing-pluronic-f127-and-plasdone-s630
#9
Xiaoyan Wu, Weihong Ge, Tengfei Shao, Weijun Wu, Jian Hou, Li Cui, Jing Wang, Zhenghai Zhang
Biochanin A (BCA), a natural dietary isoflavone, has been reported to show anticancer activities. However, its low biological availability and poor aqueous solubility limit its usefulness as a chemotherapeutic agent. We developed BCA-loaded micelles with Pluronic F127 and Plasdone S630 (BCA-FS). The optimized, spherical-shaped BCA-FS was obtained at a ratio of 1:1 (F127:S630). The particle size was 25.17±1.2 nm, and the zeta potential was -10.9±0.24 mV. BCA solubility in water increased to 5.0 mg/mL after encapsulation, and the drug-loading efficiency was 5...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28240872/annexin-v-conjugated-mixed-micelles-as-a-potential-drug-delivery-system-for-targeted-thrombolysis
#10
Yang Pan, Xiaoting Ren, Shuang Wang, Xin Li, Xianglin Luo, Zongning Yin
To alleviate the hemorrhagic side effect of thrombolysis therapy, a thrombus targeted drug delivery system based on the specific affinity of Annexin V to phosphatidylserine exposed on the membrane surface of activated platelet was developed. The amphiphilic and biodegradable biomaterial, polycaprolactone-block-poly(2-(dimethylamino)ethyl methacrylate)-block-poly(2-hydroxyethyl methacrylate) (PCL-b-PDMAEMA-b-PHEMA (PCDH)) triblock polymer, was synthesized via ring opening polymerization (ROP) and atom transfer radical polymerization (ATRP) to use as the nanocarriers of thrombolytic drug...
March 13, 2017: Biomacromolecules
https://www.readbyqxmd.com/read/28235448/ir-spectroscopy-analysis-of-pancreatic-lipase-related-protein-2-interaction-with-phospholipids-1-discriminative-recognition-of-mixed-micelles-versus-liposomes
#11
Eduardo Mateos-Diaz, Jean-Claude Bakala N'Goma, Deborah Byrne, Sylvie Robert, Frédéric Carrière, Hélène Gaussier
Guinea pig pancreatic lipase-related protein 2 (GPLRP2) is an interesting model enzyme that can hydrolyze a large set of acylglycerols in vitro but displays however some selectivity depending on the supramolecular structure of substrate and the presence of surfactants like bile salts. We showed that GPLRP2 hydrolyzes 1,2-Dipalmitoyl phosphatidylcholine (DPPC) present in mixed micelles with sodium taurodeoxycholate (NaTDC) but not in multilamellar (MLV) and large unilamellar (LUV) vesicles of DPPC. After characterization of these lipid aggregates by dynamic light scattering (DLS), the discriminative recognition of DPPC in DPPC/NaTDC micelles versus MLV and LUV by an inactive variant (S152G) of GPLRP2 to avoid the effect of substrate hydrolysis was investigated using Fourier transform infrared spectroscopy (FTIR)...
February 21, 2017: Chemistry and Physics of Lipids
https://www.readbyqxmd.com/read/28225285/multiscale-modeling-of-the-effects-of-salt-and-perfume-raw-materials-on-the-rheological-properties-of-commercial-threadlike-micellar-solutions
#12
Xueming Tang, Weizhong Zou, Peter H Koenig, Shawn D McConaughy, Mike R Weaver, David M Eike, Michael J Schmidt, Ronald G Larson
We link micellar structures to their rheological properties for two surfactant body-wash formulations at various concentrations of salts and perfume raw materials (PRMs) using molecular simulations and micellar-scale modeling, as well as traditional surfactant packing arguments. The two body washes, namely, BW-1EO and BW-3EO, are composed of sodium lauryl ethylene glycol ether sulfate (SLEnS, where n is the average number of ethylene glycol repeat units), cocamidopropyl betaine (CAPB), ACCORD (which is a mixture of six PRMs), and NaCl salt...
March 13, 2017: Journal of Physical Chemistry. B
https://www.readbyqxmd.com/read/28224892/construction-and-in-vitro-evaluation-of-enzyme-nanoreactors-based-on-carboxymethyl-chitosan-for-arginine-deprivation-in-cancer-therapy
#13
Tian Zeng, Yi Zhang, Qiongjiao Yan, Zhijun Huang, Ling Zhang, Xiaozhe Yi, Junrong Chen, Guanghua He, Yihua Yin
In this study, a pH-induced morphological transition from micelles to vesicles for an amphiphilic photo cross-linkable biocopolymer (Az-NaCMCS), synthesized by mixing azidobenzaldehyde (Az) and an aqueous solution of carboxymethyl chitosan sodium salt (NaCMCS), was used for encapsulation of l-arginine deiminase (ADI). The aqueous solution of enzyme-loaded vesicles obtained was followed by UV-irradiation to result in shell cross-linked enzyme nanoreactors. The nanoreactors were characterized by TEM and DLS. Its encapsulation efficiency and loading capacity were determined...
April 15, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28223798/transferrin-receptor-targeted-ph-sensitive-micellar-system-for-diminution-of-drug-resistance-and-targetable-delivery-in-multidrug-resistant-breast-cancer
#14
Wei Gao, Guihua Ye, Xiaochuan Duan, Xiaoying Yang, Victor C Yang
The emergence of drug resistance is partially associated with overproduction of transferrin receptor (TfR). To overcome multidrug resistance (MDR) and achieve tumor target delivery, we designed a novel biodegradable pH-sensitive micellar system modified with HAIYPRH, a TfR ligand (7pep). First, the polymers poly(l-histidine)-coupled polyethylene glycol-2000 (PHIS-PEG2000) and 7pep-modified 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-polyethylene glycol-2000 (7pep-DSPE-PEG2000) were synthesized, and the mixed micelles were prepared by blending of PHIS-PEG2000 and 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-polyethylene glycol-2000 (DSPE-PEG2000) or 7pep-DSPE-PEG2000 (7-pep HD micelles)...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28220208/abcb4-missense-mutations-d243a-k435t-g535d-i490t-r545c-and-s978p-significantly-impair-the-lipid-floppase-and-likely-predispose-to-secondary-pathologies-in-the-human-population
#15
Edward J Andress, Michael Nicolaou, Farrell McGeoghan, Kenneth J Linton
Bile salts are natural detergents required to solubilise dietary fat and lipid soluble vitamins. They are synthesised in hepatocytes and secreted into the luminal space of the biliary tree by the bile salt export pump (BSEP), an ATP-binding cassette (ABC) transporter in the canalicular membrane. BSEP deficiency causes cytotoxic accumulation of bile salts in the hepatocyte that results in mild-to-severe forms of cholestasis. The resulting inflammation can also progress to hepatocellular cancer via a novel mechanism involving upregulation of proliferative signalling pathways...
February 20, 2017: Cellular and Molecular Life Sciences: CMLS
https://www.readbyqxmd.com/read/28216010/uptake-of-benzo-a-pyrene-but-not-of-phenanthrene-is-inhibited-by-fatty-acids-in-intestinal-brush-border-membrane-vesicles-of-rainbow-trout-oncorhynchus-mykiss
#16
Stefan de Gelder, Liselot van Och, Jan Zethof, Thamar N M Pelgrim, Josef D Rasinger, Gert Flik, Marc H G Berntssen, Peter H M Klaren
Partial replacement of fish ingredients with vegetable ingredients has elevated levels of polycyclic aromatic hydrocarbons (PAHs) in Atlantic salmon reared on these feeds. PAH uptake in the intestinal tract is postulated to occur in association with lipid absorption and could well be affected by fatty acid composition. We therefore investigated the effects of a fish oil and vegetable oil fatty acid, eicosapentaenoic acid (EPA; 20:5n-3) and oleic acid (18:1n-9) respectively, on the uptake of benzo[a]pyrene (BaP) and phenanthrene (PHE) across the intestinal brush border membrane in the salmonid species rainbow trout (Oncorhynchus mykiss)...
February 12, 2017: Comparative Biochemistry and Physiology. Toxicology & Pharmacology: CBP
https://www.readbyqxmd.com/read/28212490/vitamin-e-succinate-grafted-chitosan-oligosaccharide-rgd-conjugated-tpgs-mixed-micelles-loaded-with-paclitaxel-for-u87mg-tumor-therapy
#17
Yanzuo Chen, Shu Feng, Wenchao Liu, Zeting Yuan, Peihao Yin, Feng Gao
The poor therapeutic efficacy of hydrophobic chemotherapeutic drugs is an intrinsic limitation to successful chemotherapy. In the present study, a multitask delivery system based on arginine-glycine-aspartic acid peptide (RGD) decorated vitamin E succinate (VES)-grafted-chitosan oligosaccharide (CSO)/RGD-conjugated d-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS-RGD) mixed micelles (VeC/T-RGD MM) was first prepared for targeted delivery of a hydrophobic anticancer drug, paclitaxel (PTX), to improve the efficacy of U87MG tumor therapy...
February 24, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28211226/supramolecularly-engineered-amphiphilic-macromolecules-molecular-interaction-overrules-packing-parameters
#18
Prithankar Pramanik, Debes Ray, Vinod K Aswal, Suhrit Ghosh
We report molecular interaction-driven self-assembly of supramolecularly engineered amphiphilic macromolecules (SEAM) containing a single supramolecular structure-directing unit (SSDU) consisting of an H-bonding group connected to a naphthalene diimide chromophore. Two such SEAMs, P1-50 and P2-50, having the identical chemical structure and hydrophobic/hydrophilic balance, exhibit distinct self-assembled structures (polymersome and cylindrical micelle, respectively) due to a difference in the H-bonding group (hydrazide or amide, respectively) of the single SSDU...
February 17, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28202545/the-basis-for-acyl-specificity-in-the-tafazzin-reaction
#19
Michael Schlame, Yang Xu, Mindong Ren
Tafazzin is a mitochondrial enzyme that transfers fatty acids from phospholipids to lysophospholipids. Mutations in tafazzin cause abnormal molecular species of cardiolipin and the clinical phenotype of Barth syndrome. However, the mechanism by which tafazzin creates acyl specificity has been controversial. We have shown that the lipid phase state can produce acyl specificity in the tafazzin reaction but others have reported that tafazzin itself carries enzymatic specificity. To resolve this issue, we replicated and expanded the controversial experiments, i...
February 15, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28192249/a-glucose-targeted-mixed-micellar-formulation-outperforms-genexol-in-breast-cancer-cells
#20
Marcela A Moretton, Ezequiel Bernabeu, Estefanía Grotz, Lorena Gonzalez, Marcela Zubillaga, Diego A Chiappetta
Breast cancer represents the top cancer among women, accounting 521.000 deaths per year. Development of targeted nanomedicines to breast cancer tissues represents a milestone to reduce chemotherapy side effects. Taking advantage of the over-expression of glucose (Glu) membrane transporters in breast cancer cells, we aim to expand the potential of a paclitaxel (PTX)-loaded mixed micellar formulation based on polyvinyl caprolactam-polyvinylacetate-polyethylene glycol graft copolymer (Soluplus®) and D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) by its surface decoration with Glu moieties...
February 10, 2017: European Journal of Pharmaceutics and Biopharmaceutics
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