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mixed micelles

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
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
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...
December 2016: British Journal of Nutrition
Yi Cao, Min Liu, Kunchi Zhang, Guangyue Zu, Ye Kuang, Xiaoyan Tong, Dangsheng Xiong, Renjun Pei
There was much interest in the development of nanoscale delivery vehicles based on polymeric micelles to realize the diagnostic and therapeutic applications in biomedicine. Here, with the purpose of constructing a micellar magnetic resonance imaging (MRI) contrast agent (CA) with well biocompatibility and targeting specificity, two types of amphiphilic diblock polymers, mPEG-PG(DOTA(Gd))-b-PCL and FA-PEG-b-PCL, were synthesized to form mixed micelles by coassembly. The nanostructure of the resulting micellar system consisted of poly(caprolactone) (PCL) as core and poly(glycerol) (PG) and poly(ethylene glycol) (PEG) as shell, simultaneously modified with DOTA(Gd) chelates and folic acid (FA), which afforded functions of MRI contrast enhancement and tumor targeting...
January 9, 2017: Biomacromolecules
Miki Fujimori, Kazunori Kadota, Yuichi Tozuka
Transglycosylated stevia (stevia-G) can effectively improve the dissolution and bioavailability of poorly water-soluble drugs. Furthermore, addition of an ionic surfactant to stevia-G solution has been shown to enhance the dissolution effect of stevia-G on flurbiprofen (FP). Herein, four surfactants, namely sodium dodecyl sulfate (SDS); sodium N-dodecanoylsarcosinate (SLAS); sodium monododecyl phosphate (SMP) and lauryltrimethylammonium chloride (LTAC) were screened to investigate their synergistic effect with stevia-G in enhancing the solubility of mefenamic acid (MFA)...
January 2, 2017: Journal of Pharmaceutical Sciences
Mio Tange, Akino Matsumoto, Miyako Yoshida, Honami Kojima, Tamami Haraguchi, Takahiro Uchida
The purpose of the study was to evaluate the adsorption of filgrastim on infusion sets (comprising infusion bag, line and filter) and to compare the adsorption of the original filgrastim preparation with biosimilar preparations using HPLC. The inhibitory effect of polysorbate 80 on this adsorption was also evaluated. Filgrastim was mixed with isotonic sodium chloride solution or 5% (w/v) glucose solution in the infusion fluid. Filgrastim adsorption on infusion sets was observed with all preparations and with both types of infusion solution...
2017: Chemical & Pharmaceutical Bulletin
Zahra Hami, Seyed Mahdi Rezayat, Kambiz Gilani, Mohsen Amini, Mahmoud Ghazi-Khansari
OBJECTIVES: The pH-sensitive doxorubicin (DOX)-conjugated and docetaxel (DTX)-conjugated poly(lactic acid)-poly(ethylene glycol)-folate (PLA-PEG-FOL)-based polymeric micelles were developed and characterized in this study. KEY FINDINGS: The drugs were released from the micelles (particle size, ~185 nm) in a pH-dependent manner. The drug-conjugated PLA-PEG-FOL micelles showed higher cellular uptake than nontargeting ones. Single agent and combination in-vitro cytotoxicity studies were also performed using the two drugs in both free and their micellar forms in SKOV3 human ovarian cancer cells using three different cytotoxicity assays...
February 2017: Journal of Pharmacy and Pharmacology
Gregory M Lanza, John Jenkins, Anne H Schmieder, Aigul Moldobaeva, Grace Cui, Huiying Zhang, Xiaoxia Yang, Qiong Zhong, Jochen Keupp, Ismail Sergin, Krishna S Paranandi, Lindsey Eldridge, John S Allen, Todd Williams, Michael J Scott, Babak Razani, Elizabeth M Wagner
Although angiogenesis is a hallmark feature of asthmatic inflammatory responses, therapeutic anti-angiogenesis interventions have received little attention. Objective: Assess the effectiveness of anti-angiogenic Sn2 lipase-labile prodrugs delivered via αvβ3-micellar nanotherapy to suppress microvascular expansion, bronchial remodeling, and airway hyper-responsiveness in Brown Norway rats exposed to serial house dust mite (HDM) inhalation challenges. Results: Anti-neovascular effectiveness of αvβ3-mixed micelles incorporating docetaxel-prodrug (Dxtl-PD) or fumagillin-prodrug (Fum-PD) were shown to robustly suppress neovascular expansion (p<0...
2017: Theranostics
Guangda Han, Jin-Tao Wang, Xiaotian Ji, Li Liu, Hanying Zhao
Proteinosomes are a type of protein-based spherical capsules, which have potential applications in drug delivery, cell imaging, gene expression and biocatalysis. In this research, a novel approach to the fabrication of proteinosomes entirely composed of protein molecules based on self-assembly of a supramolecular protein-polymer conjugate, is proposed. A supramolecular protein-polymer conjugate was prepared by mixing βCD-modified bovine serum albumin (BSA) and adamantane-terminated poly(N-isopropylamide) (Ad-PNIPAM) in aqueous solution...
December 30, 2016: Bioconjugate Chemistry
Mei Hu, Jinjie Zhang, Rui Ding, Yao Fu, Tao Gong, Zhirong Zhang
The clinical use of dabigatran etexilate (DABE) is limited by its poor absorption and relatively low bioavailability. Our study aimed to explore the potential of a mixed micelle system composed of Soluplus(®) and D-alpha tocopheryl polyethylene glycol 1000 succinate (TPGS) to improve the oral absorption and bioavailability of DBAE. DBAE was first encapsulated into Soluplus/TPGS mixed micelles by a simple thin film hydration method. The DBAE loaded micelles displayed an average size distribution of around 83...
December 29, 2016: Drug Development and Industrial Pharmacy
Yao Chen, Fulin Qiao, Yaxun Fan, Yuchun Han, Yilin Wang
This work studied the interactions of oppositely charged surfactant mixture of oleyl bis(2-hydroxyethyl) methyl ammonium bromide (OHAB) and sodium dodecyl sulfate (SDS) with 1,2-di-(9Z-octadecenoyl)-sn-glycero-3-phosphocholine (DOPC) vesicles as well as the penetration of the OHAB/SDS mixture through model skin, aimed at understanding the relationship between the ability of different surfactant aggregates in solubilizing phospholipid vesicles and their potential in irritating skin. By changing the molar fraction of OHAB (XOHAB), five kinds of aggregates are constructed: OHAB and SDS separately form cationic and anionic small micelles, while the OHAB/SDS mixtures form cationic and anionic vesicles at XOHAB = 0...
December 25, 2016: Langmuir: the ACS Journal of Surfaces and Colloids
Zhongcheng Ke, Zhenghai Zhang, Hao Wu, Xiaobin Jia, Youjie Wang
In this study, a new type of mixed micelles was developed using Soluplus(®) (SOL) and Pluronic(®) P105 (P105) for the encapsulation of Oridonin (ORN). Oridonin-loaded micelles (ORN-M) were simply prepared using solvent evaporation and characterized for particle size, particle morphology, encapsulation efficiency, and drug loading. In addition, the in vitro drug release behavior of ORN-M was assessed using the widely applied dialysis bag technique. The pharmacokinetic property of ORN was explored in rats after oral administration of ORN-M...
December 22, 2016: International Journal of Pharmaceutics
Juan Zhang, Yingxia Wang, Guiying Xu, Meinqin Lin, Tianyu Fan, Zihao Yang, Zhaoxia Dong
From catanionic fluoro-/hydro-carbon mixtures of fluoroacetic acid (CF3COOH) and tetradecyldimethylaminoxide (C14DMAO) in water, viscoelastic wormlike micelles are successfully constructed which are determined by cryo-TEM measurements. It is found that the formation and rheological behavior of the wormlike micelles are greatly affected by the total concentration and mixing ratio of CF3COOH and C14DMAO as well as temperature. The driving force for the formation of wormlike micelles here is considered to be the electrostatic attractive interaction between the two molecules which is confirmed by (1)H NMR measurements...
January 18, 2017: Soft Matter
Malika Talantikite, Kahina Aoudia, Lazhar Benyahia, Lila Chaal, Christophe Chassenieux, Claude Deslouis, Cédric Gaillard, Boualem Saidani
Self-assembly in aqueous solutions of an amphiphilic comblike polyelectrolyte (80C12) that consists of a polystyrene (PS) backbone onto which quaternary ammonium pendant moieties have been grafted has been investigated by light scattering and cryo-transmission electron microscopy measurements in the presence of KCl and methylviologen dication (MV(2+)) under conditions mimicking those for electrochemical measurements. Polymer chains self-assemble within branched cylindrical micelles that display viscoelastic properties, characterized by a relaxation time of 4 s...
January 19, 2017: Journal of Physical Chemistry. B
Rinku Dutta, Virender Kumar, Yang Peng, Ruby E Evande, Jean L Grem, Ram I Mahato
PURPOSES: To determine the pharmacokinetic parameters and biodistribution of GDC-0449 loaded polymeric micelles after systemic administration into common bile duct ligation (CBDL) induced liver fibrotic mice. METHODS: We used GDC-0449 encapsulated methoxy poly (ethylene glycol)-block-poly (2-methyl-2-carboxyl-propylene carbonate)-graft-dodecanol (PEG-PCD) non-targeted polymeric micelles for GDC-0449 delivery to normal and liver fibrotic mice. To maximize GDC-0449 delivery to hepatic stellate cells (HSCs), mixed micelles formulations with 10, 20 and 30% w/w mannose-6-phosphate (M6P)-conjugated micelles were administered to normal and liver fibrotic mice for targeting M6P/IGF-IIR overexpressed on activated HSCs and biodistribution of GDC-0449 was determined at 30 and 120 min post systemic administration...
December 19, 2016: Pharmaceutical Research
Vo Thu An Nguyen, Marie-Claire De Pauw-Gillet, Olivier Sandre, Mario Gauthier
Water-dispersible polyion complex (PIC) micelles were prepared by the self-assembly of an arborescent polystyrene-graft-poly(2-vinylpyridine) copolymer (denoted G0PS-g-P2VP or G1) serving as core and a poly(acrylic acid)-block-poly(2-hydroxyethyl acrylate) (PAA-b-PHEA) double-hydrophilic block copolymer (DHBC) forming a shell. Varying the density of hydrophilic polymer chains in the stabilizing layer provided control over the size and structure of the entities obtained, from large flocculated species to stable isolated PIC micelles with diameters ranging from 42 to 67 nm...
December 20, 2016: Langmuir: the ACS Journal of Surfaces and Colloids
M C di Gregorio, M Gubitosi, L Travaglini, N V Pavel, A Jover, F Meijide, J Vázquez Tato, S Sennato, K Schillén, F Tranchini, S De Santis, G Masci, L Galantini
Supramolecular rearrangements are crucial in determining the response of stimuli sensitive soft matter systems such as those formed by mixtures of oppositely charged amphiphiles. Here mixtures of this kind were prepared by mixing the cationic block copolymer pAMPTMA30-b-pNIPAAM120 and an anionic surfactant obtained by the modification of the bile salt sodium cholate. As pure components, the two compounds presented a thermoresponsive self-assembly at around 30-35 °C; a micelle formation in the case of the copolymer and a transition from fibers to tubes in the case of the bile salt derivative...
January 4, 2017: Physical Chemistry Chemical Physics: PCCP
Diogo Silva Pellosi, Italo Rodrigo Calori, Leonardo Barcelos de Paula, Noboru Hioka, Fabiana Quaglia, Antonio Claudio Tedesco
Nanotechnology development provides new strategies to treat cancer by integration of different treatment modalities in a single multifunctional nanoparticle. In this scenario, we applied the multifunctional Pluronic P123/F127 mixed micelles for Verteporfin-mediated photodynamic therapy in PC3 and MCF-7 cancer cells. Micelles functionalization aimed the targeted delivery by the insertion of biotin moiety on micelle surface and fluorescence image-based through rhodamine-B dye conjugation in the polymer chains...
February 1, 2017: Materials Science & Engineering. C, Materials for Biological Applications
Sanja Novak, Sara Morasi Piperčić, Sandro Makarić, Ines Primožič, Marija Ćurlin, Zoran Štefanić, Darija Domazet Jurašin
Phase transitions in mixtures of imidazolium based ionic liquid ([C12mim]Br) and anionic double tail surfactant, sodium bis(2-ethylhexyl) sulfosuccinate (AOT), were studied using a multitechnique approach. The system was primarily chosen for its expected ability to form a variety of lamellar and nonlamellar liquid crystalline phases which can transform into each other via different mechanisms. Depending on the bulk composition and total surfactant concentration, mixed micelles, coacervates, and lamellar and inverse bicontinuous cubic liquid crystalline phase were observed...
December 15, 2016: Journal of Physical Chemistry. B
Zacharoula Iatridi, Kosmas Vamvakidis, Ioannis Tsougos, Katerina Vassiou, Catherine Dendrinou-Samara, Georgios Bokias
Adequately designed multiresponsive water-soluble graft copolymers were used to serve as a multifunctional polymeric platform for the encapsulation and transfer in aqueous media of hydrophobic magnetic nanoparticles (MNPs). The backbone of the graft copolymers was composed of hydrophilic sodium methacrylate units, hydrophobic dodecyl methacrylate units, and luminescent quinoline-based units, while either the homopolymer poly(N-isopropylacrylamide) or a poly(N,N-dimethylacrylamide-co-N-isopropylacrylamide) copolymer was used as thermosensitive pendent side chains...
December 28, 2016: ACS Applied Materials & Interfaces
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