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https://www.readbyqxmd.com/read/28092844/enhanced-effect-in-combination-of-curcumin-and-ketoconazole-loaded-methoxy-poly-ethylene-glycol-poly-%C3%AE%C2%B5-caprolactone-micelles
#1
Fangfang Teng, Peizong Deng, Zhimei Song, Feilong Zhou, Runliang Feng
In order to enhance water-solubility and realize controlled release while keeping synergistic effects of ketoconazole and curcumin, drug-loaded methoxy poly (ethylene glycol)-b-poly (ε-caprolactone) micelles were prepared through thin membrane hydration method. Transmission electric microscopy and dynamitic light scattering characterization revealed the formation of ketoconazole- and curcumin-loaded micelles with an average size of 44.70nm and 39.56nm, respectively. The drug-loaded micelles endowed the two drugs' slow controlled release with water-solubility enhanced to 85 and 82000 folds higher than the corresponding raw drugs, respectively...
January 13, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28091671/developing-the-family-of-picolinate-ligands-for-mn-2-complexation
#2
Attila Forgács, Rosa Pujales-Paradela, Martín Regueiro-Figueroa, Laura Valencia, David Esteban-Gómez, Mauro Botta, Carlos Platas-Iglesias
We have reported here a series of ligands containing pentadentate 6,6'-(azanediylbis(methylene))dipicolinic acid units that differ in the substituent present at the amine nitrogen atom (acetate: H3DPAAA; phenyl: H2DPAPhA; dodecyl: H2DPAC12A; 4-hexylphenyl: H2DPAC6PhA). The protonation constants of the hexadentate DPAAA(3-) and pentadentate DPAPhA(2-) ligands and the stability constants of their Mn(2+) complexes were determined using pH-potentiometry (25 °C, 0.15 M NaCl). The mono-hydrated [Mn(DPAAA)](-) complex (log KMnL = 13...
January 16, 2017: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/28089916/stable-curcumin-loaded-polymeric-micellar-formulation-for-enhancing-cellular-uptake-and-cytotoxicity-to-flt3-overexpressing-eol-1-leukemic-cells
#3
Singkome Tima, Songyot Chadarat Anuchapreeda Ampasavate, Cory Berkland, Siriporn Okonogi
The present study aims to develop a stable polymeric micellar formulation of curcumin (CM) with improved solubility and stability, and that is suitable for clinical applications in leukemia patients. CM-loaded polymeric micelles (CM-micelles) were prepared using poloxamers. The chemical structure of the polymers influenced micellar properties. The best formulation of CM-micelles, namely CM-P407, was obtained from poloxamer 407 at drug to polymer ratio of 1:30 and rehydrated with phosphate buffer solution pH 7...
January 12, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28088632/nanosized-complexation-assemblies-housed-inside-reverse-micelles-churn-out-monocytic-delivery-cores-for-bendamustine-hydrochloride
#4
Yuvraj Singh, Anumandla Chandrashekhar, Jaya Gopal Meher, K K Durga Rao Viswanadham, Vivek K Pawar, Kavit Raval, Komal Sharma, Pankaj K Singh, Animesh Kumar, Manish K Chourasia
OBJECTIVE: We explore a plausible method of targeting bendamustine hydrochloride (BM) to circulatory monocytes by exploiting their intrinsic endocytic/phagocytic capability. METHODS: We do so by complexation of sodium alginate and chitosan inside dioctyl sulfo succinate sodium (AOT) reverse micelles to form bendamustine hydrochloride loaded nanoparticles (CANPs). Dynamic light scattering, electrophoretic mobility and UV spectroscopy were used to detail intra-micellar complexation dynamics and to prove that drug was co-captured during interaction of carbohydrate polymers...
January 11, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28087485/stepwise-targeted-drug-delivery-to-liver-cancer-cells-for-enhanced-therapeutic-efficacy-by-galactose-grafted-ultra-ph-sensitive-micelles
#5
Guoqing Yan, Jun Wang, Liefeng Hu, Xin Wang, Guanqing Yang, Shengxiang Fu, Xu Cheng, Panpan Zhang, Rupei Tang
: To promote drug accumulation and cell-killing ability at tumor tissue, we have prepared a stepwise targeted drug delivery system that can remain stealthy and long-circulating in the blood vessels, improve drug retention at extracellular stimuli, enhance cellular uptake through special targeting ligands, and then achieve rapid drug release to improve toxicity to tumor cells at intracellular stimuli. Herein, galactose-grafted, ultra-pH-sensitive drug carriers (POEAd-g-LA-DOX micelles), which could respond to both extracellular and intracellular pH, and combine with galactose-receptors in cell membrane, were constructed by a facile method, therefore achieving: (i) remaining stable at pH 7...
January 10, 2017: Acta Biomaterialia
https://www.readbyqxmd.com/read/28087407/polymeric-micelles-for-ocular-drug-delivery-from-structural-frameworks-to-recent-preclinical-studies
#6
REVIEW
Abhirup Mandal, Rohit Bisht, Ilva D Rupenthal, Ashim K Mitra
Effective intraocular drug delivery poses a major challenge due to the presence of various elimination mechanisms and physiological barriers that result in low ocular bioavailability after topical application. Over the past decades, polymeric micelles have emerged as one of the most promising drug delivery platforms for the management of ocular diseases affecting the anterior (dry eye syndrome) and posterior (age-related macular degeneration, diabetic retinopathy and glaucoma) segments of the eye. Promising preclinical efficacy results from both in-vitro and in-vivo animal studies have led to their steady progression through clinical trials...
January 10, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28087380/polymeric-mixed-micelles-as-nanomedicines-achievements-and-perspectives
#7
REVIEW
Maximiliano Cagel, Fiorella C Tesan, Ezequiel Bernabeu, Maria J Salgueiro, Marcela B Zubillaga, Marcela A Moretton, Diego A Chiappetta
During the past few decades, polymeric micelles have raised special attention as novel nano-sized drug delivery systems for optimizing the treatment and diagnosis of numerous diseases. These nanocarriers exhibit several in vitro and in vivo advantages as well as increased stability and solubility to hydrophobic drugs. An interesting approach for optimizing these properties and overcoming some of their disadvantages is the combination of two or more polymers in order to assemble polymeric mixed micelles. This review article gives an overview on the current state of the art of several mixed micellar formulations as nanocarriers for drugs and imaging probes, evaluating their ongoing status (preclinical or clinical stage), with special emphasis on type of copolymers, physicochemical properties, in vivo progress achieved so far and toxicity profiles...
January 10, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28087376/ir780-loaded-tpgs-tos-micelles-for-breast-cancer-photodynamic-therapy
#8
Cleide Pais-Silva, Duarte de Melo-Diogo, Ilídio J Correia
IR780 iodide is a near-infrared (NIR) dye with a huge potential for cancer imaging and phototherapy. However, its biomedical application is strongly impaired by its lipophilic character. Herein, amphiphilic micelles based on d-α-tocopheryl polyethylene glycol succinate (TPGS) and d-α-tocopheryl succinate (TOS), two vitamin E derivatives with intrinsic anticancer activity, are explored to load IR780. IR780-loaded micelles with suitable sizes are obtained by using specific TPGS and TOS weight feed ratios during micelles formulation and these are able to encapsulate IR780 with high efficiency...
January 11, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28080053/lipid-drug-conjugate-for-enhancing-drug-delivery
#9
Danielle Irby, Chengan Du, Feng Li
Lipid-drug conjugates (LDCs) are drug molecules that have been covalently modified with lipids. The conjugation of lipids to drug molecules increases lipophilicity and also changes other properties of drugs. The conjugates demonstrate several advantages including improved oral bioavailability, improved targeting to the lymphatic system, enhanced tumor targeting, and reduced toxicity. Based on the chemical nature of drugs and lipids, various conjugation strategies and chemical linkers can be utilized to synthesize LDCs...
January 12, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28079955/solubilization-of-membrane-proteins-into-functional-lipid-bilayer-nanodiscs-using-a-diisobutylene-maleic-acid-copolymer
#10
Abraham Olusegun Oluwole, Bartholomäus Danielczak, Annette Meister, Jonathan Oyebamiji Babalola, Carolyn Vargas, Sandro Keller
Once removed from their natural environment, membrane proteins depend on membrane-mimetic systems to retain their native structures and functions. To this end, lipid-bilayer nanodiscs that are bounded by scaffold proteins or amphiphilic polymers such as styrene/maleic acid (SMA) copolymers have been introduced as alternatives to detergent micelles and liposomes for in vitro membrane-protein research. Herein, we show that an alternating diisobutylene/maleic acid (DIBMA) copolymer shows equal performance to SMA in solubilizing phospholipids, stabilizes an integral membrane enzyme in functional bilayer nanodiscs, and extracts proteins of various sizes directly from cellular membranes...
January 12, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28079203/complexation-of-short-ds-rna-dna-oligonucleotides-with-gemini-micelles-a-time-resolved-saxs-and-computational-study
#11
Sara Falsini, Emanuela Di Cola, Martin In, Maria Giordani, Stefano Borocci, Sandra Ristori
Gene therapy is based on nucleic acid delivery to pathogenic cells in order to modulate their gene expression. The most used non viral vectors are lipid-based nanoaggregates, which are safer than viral carriers and have been shown to assemble easily with both DNA and RNA. However, the transfection efficiency of non viral carriers still needs to be improved before intensive practise in clinical trials can be implemented. For this purpose, the in depth characterization of the complexes formed by nucleic acids and their transporters is of great relevance...
January 12, 2017: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/28074953/gastrointestinal-interactions-absorption-splanchnic-metabolism-and-pharmacokinetics-of-orally-ingested-phenolic-compounds
#12
REVIEW
J Abraham Domínguez-Avila, Abraham Wall-Medrano, Gustavo R Velderrain-Rodríguez, C-Y Oliver Chen, Norma Julieta Salazar-López, Maribel Robles-Sánchez, Gustavo A González-Aguilar
The positive health effects of phenolic compounds (PCs) have been extensively reported in the literature. An understanding of their bioaccessibility and bioavailability is essential for the elucidation of their health benefits. Before reaching circulation and exerting bioactions in target tissues, numerous interactions take place before and during digestion with either the plant or host's macromolecules that directly impact the organism and modulate their own bioaccessibility and bioavailability. The present work is focused on the gastrointestinal (GI) interactions that are relevant to the absorption and metabolism of PCs and how these interactions impact their pharmacokinetic profiles...
January 11, 2017: Food & Function
https://www.readbyqxmd.com/read/28073428/formation-of-charge-carriers-in-liquids
#13
Dennis C Prieve, Benjamin A Yezer, Aditya S Khair, Paul J Sides, James W Schneider
After presenting a brief historical overview of the classic contributions of Faraday, Arrhenius, Kohlrausch, Bjerrum, Debye, Hückel and Onsager to understanding the conductivity of true electrolytes in aqueous solutions, we present an in-depth review of the 1933 work of Fuoss & Kraus who explored the effect of the solvent on electrolyte dissociation equilibria in either polar or nonpolar media. Their theory predicts that the equilibrium constant for dissociation decays exponentially with the ratio of the Bjerrum length λB to the ion-pair size a...
November 19, 2016: Advances in Colloid and Interface Science
https://www.readbyqxmd.com/read/28073063/self-assembled-micelles-based-on-chondroitin-sulfate-poly-d-l-lactideco-glycolide-block-copolymers-for-doxorubicin-delivery
#14
Hui Zhang, Jiangkang Xu, Liang Xing, Jianbo Ji, Aihua Yu, Guangxi Zhai
Doxorubicin (DOX) is one of the most common chemotherapeutic agents for the treatment of various cancers, but its clinical usage is limited by dose-dependent cardiotoxicity. We have recently synthesized a series of Chondroitin sulfate/poly (d,l-lactideco-glycolide) block copolymers (Chs-b-PLGA) with different length of hydrophobic block by an end-to-end coupling strategy. The structure of the amphiphilic block copolymers with low critical micelle concentration (∼28mg/L) were confirmed by (1)H NMR. The copolymers could self-assemble into stable micelles in aqueous environment with homogeneous size distribution and negative zeta potential...
December 23, 2016: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/28071889/enzyme-and-redox-dual-triggered-intracellular-release-from-actively-targeted-polymeric-micelles
#15
Lei Zhang, Yi Wang, Xiaobin Zhang, Xiao Wei, Xiang Xiong, Shaobing Zhou
Highly effective delivery of therapeutic agents into target cells using nanocarriers and subsequently rapid intracellular release are of great importance in cancer treatment. Here, we developed an enzyme and redox dual-responsive polymeric micelle with active targeting abilities to achieve rapid intracellular drug release. To overcome both its poor solubility in water and instability in the blood circulation, camptothecin (CPT) was chemically conjugated to monomethyl poly(ethylene glycol) (mPEG) via a redox-responsive linker to form polymeric prodrugs...
January 10, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28069810/sensitive-versatile-fluorogenic-transmembrane-peptide-substrates-for-rhomboid-intramembrane-proteases
#16
Anežka Tichá, Stancho Stanchev, Jan Škerle, Jakub Began, Marek Ingr, Kateř Ina Švehlová, Lucie Polovinkin, Martin Růžička, Lucie Bednárová, Romana Hadravová, Edita Poláchová, Petra Rampírová, Jana Březinová, Václav Kašička, Pavel Majer, Kvido Strisovsky
Rhomboid proteases are increasingly being explored as potential drug targets, but their potent and specific inhibitors are not available, and strategies for inhibitor development are hampered by the lack of widely usable and easily modifiable in vitro activity assays. Here we address this bottleneck and report on the development of new fluorogenic transmembrane peptide substrates, which are cleaved by several unrelated rhomboid proteases, can be used both in detergent micelles and in liposomes, and contain red-shifted fluorophores that are suitable for high-throughput screening of compound libraries...
January 9, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28069089/dietary-calcium-impairs-tomato-lycopene-bioavailability-in-healthy-humans
#17
Patrick Borel, C Desmarchelier, U Dumont, C Halimi, D Lairon, D Page, J L Sébédio, C Buisson, C Buffière, D Rémond
Lycopene (LYC) bioavailability is relatively low and highly variable, because of the influence of several factors. Recent in vitro data have suggested that dietary Ca can impair LYC micellarisation, but there is no evidence whether this can lead to decreased LYC absorption efficiency in humans. Our objective was to assess whether a nutritional dose of Ca impairs dietary LYC bioavailability and to study the mechanism(s) involved. First, in a randomised, two-way cross-over study, ten healthy adults consumed either a test meal that provided 19-mg (all-E)-LYC from tomato paste or the same meal plus 500-mg calcium carbonate as a supplement...
January 10, 2017: British Journal of Nutrition
https://www.readbyqxmd.com/read/28068593/visible-light-induced-crosslinking-and-physiological-stabilization-of-diselenide-rich-nanoparticles-for-redox-responsive-drug-release-and-combination-chemotherapy
#18
Shaodong Zhai, Xianglong Hu, Yongjun Hu, Baoyan Wu, Da Xing
Undesired physiological instability of nanocarriers and premature drug leakage during blood circulation result in compromised therapeutic efficacy and severe side effects, which have significantly impeded the development of nanomedicine. Facile crosslinking of drug-loaded nanocarriers while keeping the potency of site-specific degradation and drug release has emerged as a viable strategy to overcome these drawbacks. Additionally, combination therapy has already shown advantages in inhibiting advanced tumors and life extension than single drug therapy...
January 3, 2017: Biomaterials
https://www.readbyqxmd.com/read/28068545/design-preparation-and-characterization-of-ph-responsive-prodrug-micelles-with-hydrolyzable-anhydride-linkages-for-controlled-drug-delivery
#19
Girija Seetharaman, Adarsh R Kallar, Vineeth M Vijayan, Jayabalan Muthu, Shivaram Selvam
We report a new prodrug micelle-based approach in which a model hydrophobic non-steroidal anti-inflammatory drug (NSAID), ibuprofen (Ibu), is tethered to amphiphilic methoxy polyethylene glycol-polypropylene fumarate (mPEG-PPF) diblock copolymer via hydrolytic anhydride linkages for potential controlled release applications of NSAIDs. Synthesized mPEG-PPF-Ibu polymer drug conjugates (PDCs) demonstrated high drug conjugation efficiency (∼90%) and self-assembled to form micellar nanostructures in aqueous medium with critical micelle concentrations ranging between 16 and 30μg/mL...
December 31, 2016: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/28068313/two-dimensional-assemblies-from-crystallizable-homopolymers-with-charged-termini
#20
Xiaoming He, Ming-Siao Hsiao, Charlotte E Boott, Robert L Harniman, Ali Nazemi, Xiaoyu Li, Mitchell A Winnik, Ian Manners
The creation of shaped, uniform and colloidally stable two-dimensional (2D) assemblies by bottom-up methods represents a challenge of widespread current interest for a variety of applications. Herein, we describe the utilization of surface charge to stabilize self-assembled planar structures that are formed from crystallizable polymer precursors by a seeded growth approach. Addition of crystallizable homopolymers with charged end-groups to seeds generated by the sonication of block copolymer micelles with crystalline cores yields uniform platelet micelles with controlled dimensions...
January 9, 2017: Nature Materials
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