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https://www.readbyqxmd.com/read/28334044/in-vitro-and-in-vivo-evaluation-of-docetaxel-loaded-stearic-acid-modified-bletilla-striata-polysaccharide-copolymer-micelles
#1
Qingxiang Guan, Guangyuan Zhang, Dandan Sun, Yue Wang, Kun Liu, Miao Wang, Cheng Sun, Zhuo Zhang, Bingjin Li, Jiayin Lv
Bletilla striata polysaccharides (BSPs) have been used in pharmaceutical and biomedical industry, the aim of the present study was to explore a BSPs amphiphilic derivative to overcome its application limit as poorly water-soluble drug carriers due to water-soluble polymers. Stearic acid (SA) was selected as a hydrophobic block to modify B. striata polysaccharides (SA-BSPs). Docetaxel (DTX)-loaded SA-BSPs (DTX-SA-BSPs) copolymer micelles were prepared and characterized. The DTX release percentage in vitro and DTX concentration in vivo was carried out by using high performance liquid chromatography...
2017: PloS One
https://www.readbyqxmd.com/read/28323118/mixed-poly-vinyl-pyrrolidone-based-drug-loaded-nanomicelles-shows-enhanced-efficacy-against-pancreatic-cancer-cell-lines
#2
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/28323102/preparation-of-core-crosslinked-linear-dendritic-copolymer-micelles-with-enhanced-stability-and-their-application-for-drug-solubilisation
#3
Zhengyuan Zhou, Robert T Forbes, Antony D'Emanuele
In this study we explore the preparation of core-crosslinked micelles of linear-dendritic methoxy-poly(ethylene glycol) (MPEG)-co-poly(ester-sulfide) (PES) polymers to improve the stability of such polymeric micelle systems against premature disintegration and drug release. A series of MPEG-PES copolymers were synthesised via stepwise reactions of acetylation and thiol-ene photoreaction. Surface tension measurement showed that the copolymers with ethenyl surface groups could self-associate in dilute aqueous solutions to form micelles...
March 18, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28322164/solubilization-and-enhancement-of-ex-vivo-vaginal-delivery-of-progesterone-using-solid-dispersions-inclusion-complexes-and-micellar-solubilization
#4
Abeer S Hassan, Ghareb M Soliman, Mona M El-Mahdy, Gamal El-Din A El-Gindy
Progesterone (PG), a natural female sex hormone is used clinically in menopausal hormone replacement therapy and to control reproductive functions. Its very limited aqueous solubility of 7 µg/ml results in reduced oral bioavailability and low patient compliance when administered in high doses. The aim of this study was to enhance PG aqueous solubility and vaginal delivery using solid dispersion, inclusion complex and micellar solubilization techniques. PG solid dispersions and inclusion complexes were prepared by solvent evaporation method using different polymers, such as cyclodextrins, polyvinyl pyrrolidone (PVP), poly (ethylene glycol) 6000, Pluronic® F-127 and Pluronic® F-68...
March 20, 2017: Current Drug Delivery
https://www.readbyqxmd.com/read/28322116/expanding-the-potential-of-mri-contrast-agents-through-multifunctional-polymeric-nanocarriers
#5
Ioana Craciun, Gesine Gunkel-Grabole, Andrea Belluati, Cornelia G Palivan, Wolfgang Meier
MRI is a sought-after, noninvasive tool in medical diagnostics, yet the direct application of contrast agents to tissue suffers from several drawbacks. Hosting the contrast agents in polymeric nanocarriers can solve many of these issues while creating additional benefit through exploitation of the intrinsic characteristics of the polymeric carriers. In this report, the versatility is highlighted with recent examples of dendritic and hyperbranched polymers, polymer nanoparticles and micelles, and polymersomes as multifunctional bioresponsive nanocarriers for MRI contrast agents...
March 21, 2017: Nanomedicine
https://www.readbyqxmd.com/read/28315495/legumain-cleavable-4-arm-poly-ethylene-glycol-doxorubicin-conjugate-for-tumor-specific-delivery-and-release
#6
Huicong Zhou, Huanjiao Sun, Shixian Lv, Dawei Zhang, Xuefei Zhang, Zhaohui Tang, Xuesi Chen
Traditional chemotherapy strategy exists undesirable toxic side-effects to normal tissues due to the low selectively to cancer cells of micromolecule cytotoxic drugs. One considered method to realizing the targeted delivery and increasing the specificity to tumor tissues of the cytotoxic drug is to transporting and discharging it through an environment-sensitive mechanism. In this study, a novel enzyme-sensitive polymer-doxorubicin conjugate was designed to delivery chemotherapeutic drug in a tumor-specific behavior and selectively activated in tumor tissue...
March 14, 2017: Acta Biomaterialia
https://www.readbyqxmd.com/read/28314988/polymeric-micelles-as-mighty-nanocarriers-for-cancer-gene-therapy-a-review
#7
REVIEW
Mahsa Yousefpour Marzbali, Ahmad Yari Khosroushahi
PURPOSE: Gene therapy has shown extensive potential to treat human diseases occurring from the defection of genes like various types of cancers. The cationic polymers, as non-viral gene carriers, offer the ability to engineer carrier systems having customized features that can be adapted to suit any system. Upon polymeric micelle systems' core-shell structure, micelles can create the capacity to load genes/gene-drugs into the different micelle compartments, respectively. METHODS: The search will be managed in Pubmed, Medline, Cochrane library, Embase and Proquest for articles related to polymeric micelle-based gene delivery in order to cancer gene therapy using the accommodative search terms...
March 17, 2017: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/28300411/h2s-releasing-polymer-micelles-for-studying-selective-cell-toxicity
#8
Jeffrey C Foster, Scott C Radzinski, Xianlin Zou, Carla V Finkielstein, John B Matson
We report the preparation of S-aroylthiooxime (SATO) functionalized amphiphilic block copolymer micelles that release hydrogen sulfide (H2S), a gaseous signaling molecule of relevance to various physiological and pathological conditions. The micelles release H2S in response to cysteine with a half-life of 3.3 h, which is substantially slower than a related small molecule SATO. Exogenous administration of H2S impacts growth and proliferation of cancer cells; however, the limited control over H2S generation from inorganic sulfide sources results in conflicting reports...
March 16, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28297991/solvent-free-molecular-level-modeling-of-self-assembling-amphiphiles-in-water
#9
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/28286038/multi-stimuli-responsive-biohybrid-nanoparticles-with-cross-linked-albumin-coronae-self-assembled-by-a-polymer-protein-biodynamer
#10
Lin Wang, Li Liu, Bingyang Dong, Hanying Zhao, Mingming Zhang, Wenjuan Chen, Yanhang Hong
A thermoresponsive polymer-protein biodynamer was prepared via the bioconjugation of an aliphatic aldehyde-functionalized copolymer to hydrazine-modified bovine serum albumin (BSA) through reversible pyridylhydrazone linkages. Sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) and size exclusion chromatography (SEC) results indicated that the pyridylhydrazone linkages cleaved in an intracellular-mimicking acidic milieu, thus leading to the release of BSA. The dynamic character of the protein biodynamer was demonstrated by exchange reactions with aldehyde-containing molecules...
March 8, 2017: Acta Biomaterialia
https://www.readbyqxmd.com/read/28282137/enhanced-performance-of-blended-polymer-excipients-in-delivering-a-hydrophobic-drug-through-the-synergistic-action-of-micelles-and-hpmcas
#11
Ziang Li, Lindsay M Johnson, Ralm G Ricarte, Letitia J Yao, Marc A Hillmyer, Frank S Bates, Timothy P Lodge
Blends of hydroxypropyl methylcellulose acetate succinate (HPMCAS) and dodecyl (C12)-tailed poly(N-isopropylacrylamide) (PNIPAm) were systematically explored as a model system to dispense the active ingredient phenytoin by rapid dissolution, followed by the suppression of drug crystallization for an extended period. Dynamic and static light scattering revealed that C12-PNIPAm polymers, synthesized by reversible addition-fragmentation chain-transfer polymerization, self-assembled into micelles with dodecyl cores in phosphate-buffered saline (PBS, pH 6...
March 10, 2017: Langmuir: the ACS Journal of Surfaces and Colloids
https://www.readbyqxmd.com/read/28277671/enzyme-cleavable-polymeric-micelles-for-the-intracellular-de-livery-of-pro-apoptotic-peptides
#12
Hanna B Kern, Selvi Srinivasan, Anthony J Convertine, David Hockenbery, Oliver W Press, Patrick S Stayton
Peptides derived from the third Bcl-2 homology domain (BH3) renormalize apoptotic signaling by antagonizing pro-survival Bcl-2 family members. They serve as a model for potential peptide drugs that possess therapeutic activities but are limited by delivery barriers including short circulation half-lives and poor penetration into cells. A diblock polymeric micelle carrier for the BIM BH3 peptide was recently described that demonstrated anti-tumor activity in a B-cell lymphoma xenograft model [Berguig et al., Mol Ther, 2015]...
March 9, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28273121/polymer-micelle-formulation-for-the-proteasome-inhibitor-drug-carfilzomib-anticancer-efficacy-and-pharmacokinetic-studies-in-mice
#13
Ji Eun Park, Se-Eun Chun, Derek Reichel, Jee Sun Min, Su-Chan Lee, Songhee Han, Gongmi Ryoo, Yunseok Oh, Shin-Hyung Park, Heon-Min Ryu, Kyung Bo Kim, Ho-Young Lee, Soo Kyung Bae, Younsoo Bae, Wooin Lee
Carfilzomib (CFZ) is a peptide epoxyketone proteasome inhibitor approved for the treatment of multiple myeloma (MM). Despite the remarkable efficacy of CFZ against MM, the clinical trials in patients with solid cancers yielded rather disappointing results with minimal clinical benefits. Rapid degradation of CFZ in vivo and its poor penetration to tumor sites are considered to be major factors limiting its efficacy against solid cancers. We previously reported that polymer micelles (PMs) composed of biodegradable block copolymers poly(ethylene glycol) (PEG) and poly(caprolactone) (PCL) can improve the metabolic stability of CFZ in vitro...
2017: PloS One
https://www.readbyqxmd.com/read/28267318/modular-synthetic-approach-for-adjusting-the-disassembly-rates-of-enzyme-responsive-polymeric-micelles
#14
Assaf J Harnoy, Marina Buzhor, Einat Tirosh, Rona Shaharabani, Roy Beck, Roey J Amir
Self-assembled nanostructures and their stimuli-responsive degradation have been recently explored to meet the increasing need for advanced biocompatible and biodegradable materials for various biomedical applications. Incorporation of enzymes as triggers that can stimulate the degradation and disassembly of polymeric assemblies may be highly advantageous owing to their high selectivity and natural abundance in all living organisms. One of the key factors to consider when designing enzyme-responsive polymers is the ability to fine-tune the sensitivity of the platform toward its target enzyme in order to control the disassembly rate...
March 21, 2017: Biomacromolecules
https://www.readbyqxmd.com/read/28263559/coordination-driven-syntheses-of-compact-supramolecular-metallacycles-toward-extended-metallo-organic-stacked-supramolecular-assemblies
#15
Christophe Lescop
One important concept associated with supramolecular chemistry is supramolecular self-assembly, which deals with the way discrete individual components interact via intermolecular interactions in order to build, upon their spontaneous association, high order functional assemblies. The accumulation of these very simple and localized noncovalent interactions (such as H-bonding, dipole-dipole, hydrophobic/hydrophilic, van der Waals, π-π, π-CH, etc.) is ubiquitous in the complexity of natural systems (such as DNA, proteins, membranes, micelles, etc...
March 6, 2017: Accounts of Chemical Research
https://www.readbyqxmd.com/read/28260803/reversal-of-paclitaxel-resistance-in-human-ovarian-cancer-cells-with-redox-responsive-micelles-consisting-of-%C3%AE-tocopheryl-succinate-based-polyphosphoester-copolymers
#16
Feng-Qian Chen, Jin-Ming Zhang, Xie-Fan Fang, Hua Yu, Yu-Ling Liu, Hui Li, Yi-Tao Wang, Mei-Wan Chen
P-glycoprotein (P-gp)-mediated multidrug resistance (MDR) is a major obstacle in achieving the therapeutic benefits of paclitaxel (PTX) in the treatment of human ovarian carcinoma. This study is aimed to develop an efficient PTX drug delivery approach to overcome MDR. Redox-responsive micelles consisting of amphiphilic polymers containing disulfide linkages, ie, poly (phosphate ester)-SS-D-α-tocopheryl succinate (POPEA-SS-TOS, PSST) were prepared. PTX-loaded PSST micelles (PTX/PSST-M) designed to display synergistic functions, including reversible inhibition of P-gp, intracellular redox-sensitive release and potent anticancer activities...
March 6, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28258718/micellar-liquid-chromatography-of-terephthalic-acid-impurities
#17
Ashley E Richardson, Shakeela D McPherson, Jennifer M Fasciano, Richard E Pauls, Neil D Danielson
The production of terephthalic acid (TPA) by oxidation of p-xylene is an important industrial process because high purity TPA is required for the synthesis of polyethylene terephthalate, the primary polymer used to make plastic beverage bottles. Few separation methods have been published that aim to separate TPA from eight major aromatic acid impurities. This work describes a "green" micellar liquid chromatography (MLC) method using a C18 column (100×2.1mm, 3.5μm), an acidic 1% sodium dodecyl sulfate (SDS) mobile phase, and a simple step flow rate gradient to separate TPA and eight impurities in less than 20min...
March 31, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28252120/amphiphilic-nanosheet-self-assembly-at-the-water-oil-interface-computer-simulations
#18
Wenjun Xiang, Shuangliang Zhao, Xianyu Song, Shenwen Fang, Fen Wang, Cheng Zhong, Zhaoyang Luo
In this paper, dissipative particle dynamics simulations are performed to study the interfacial and emulsion stabilizing properties of various systems of amphiphilic nanosheets (ANs) self-assembled at the oil/water (O/W) interface. The ANs have a dimensional symmetry structure that encompasses a triangular-plate at the center and two soft comb-like shells constructed with hydrophilic and hydrophobic polymers. As the simulation results show, the AN molecules are highly oriented in interfacial films with their triangular nanosheets parallel to the O/W interface, while their hydrophobic and hydrophilic segments attempt to immerse into the oil phase and aqueous phase, respectively...
March 2, 2017: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/28250648/the-influence-of-pluronic-f68-and-f127-nanocarrier-on-physicochemical-properties-in-vitro-release-and-antiproliferative-activity-of-thymoquinone-drug
#19
Salwa Shaarani, Shahrul Sahul Hamid, Noor Haida Mohd Kaus
BACKGROUND: This study reports on hydrophobic drug thymoquinone (TQ), an active compound found in the volatile oil of Nigella sativa that exhibits anticancer activities. Nanoformulation of this drug could potentially increase its bioavailability to specific target cells. OBJECTIVE: The aim of this study was to formulate TQ into polymer micelle, Pluronic F127 (5.0 wt %) and Pluronic F68 (0.1 wt %), as a drug carrier to enhance its solubility and instability in aqueous media...
January 2017: Pharmacognosy Research
https://www.readbyqxmd.com/read/28244754/1-2-dithiolane-derived-dynamic-covalent-materials-cooperative-self-assembly-and-reversible-cross-linking
#20
Xiangyi Zhang, Robert M Waymouth
The use of dithiolane-containing polymers to construct responsive and dynamic networks is an attractive strategy in material design. Here, we provide a detailed mechanistic study on the self-assembly and gelation behavior of a class of ABA triblock copolymers containing a central poly(ethylene oxide) block and terminal polycarbonate blocks with pendant 1,2-dithiolane functionalities. In aqueous solution, these amphiphilic block copolymers self-assemble into bridged flower micelles at high concentrations. The addition of a thiol initiates the reversible ring-opening polymerizations of dithiolanes in the micellar cores to induce the cross-linking and gelation of the micellar network...
February 28, 2017: Journal of the American Chemical Society
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