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111.
The hindered monomer, 2,3,4-trimethyl-3-pentyl methacrylate (I), was synthesized for penultimate effect studies. Since it readily homopoiymerized (km111≠ 0) and readily copolymerized with styrene, copolymerizations of I with styrene were carried out at 60°C in benzene with AIBN as initiator. The conversion to copolymer and the copolymer composition were determined by using GLC techniques. Composition-conversion data was analyzed by performing a computerized nonlinear least-squares fitting to the integrated form of the penultimate model equation. The experimental design included the use of optimized M1°/M2° ratios. The penultimate reactivity ratios calculated from these data were r1′ = 0.23, r1′= 0.59, r2 = 0.59, r2′ = 1.34. Thus, when I is the penultimate unit, a terminal styryl radical prefers to add styrene, whereas when styrene is the penultimate unit, terminal styryl radicals prefer to add I. These results constitute the best evidence for a steric penultimate effect yet available in the literature from composition-conversion studies. However, the case is not yet proved. Further studies to strengthen this conclusion are proposed. 相似文献
112.
T. M. Pramod Kumar H. M. Umesh H. G. Shivakumar Valluru Ravi 《高分子科学杂志,A辑:纯化学与应用化学》2013,50(6):583-589
A series of terbutaline sulphate drug incorporated polyvinyl alcohol (PVA) matrix films were produced by the solvent evaporation method. The effect of xanthan gum and plasticizers (propylene glycol and dibutyl phthalate) on the rate and amount of drug diffusion from PVA membrane across the hydrated cellophane membrane has been evaluated, using an open glass diffusion‐tube. The obtained films were clear, smooth and flexible having sufficient mechanical strength. The mechanical performance of the dry PVA films with xanthan gum and plasticizers were also ascertained. Polyvinyl alcohol‐xanthan gum blends showed a high rate of drug release compared to that of polyvinyl alcohol film alone. Among the two plasticizers employed, propylene glycol showed better permeability. Among different formulations studied, the formulation PVA/xanthan gum/propylene glycol (F7) was found to be an optimized composition for efficient transdermal delivery of the model drug, terbutaline sulphate. The mechanism of drug diffusion has been evaluated using the Peppas model. Stability studies carried out on polymer‐drug formulations revealed that the drug is stable at 40°C and 75% RH for a period of 6 weeks. 相似文献
113.
Petruta Flocea Liliana Verestiuc Marcel Popa Valeriu Sunel Adriana Lungu 《高分子科学杂志,A辑:纯化学与应用化学》2013,50(6):616-625
The paper presents the experimental studies regarding synthesis and characterization of hydrogels based on gellan (Gel)/chitosan (CS) and collagen (Col), obtained by crosslinking with glutaraldehyde (GLA). The influence of the polysaccharide content and GLA ratio on the final composition and swelling characteristics was evaluated. Hydrogels swelling analysis, in distilled water and phosphate buffer (PBS, pH 7.2) has shown higher swelling degrees at increased concentration of polysaccharide into hydrogels. In vitro release of pilocarpine has demonstrated the possibility to use gellan-collagen and chitosan-collagen hydrogels as ophthalmic drug delivery matrix. 相似文献
114.
Nikolaus Krall Dr. Jörg Scheuermann Prof. Dario Neri 《Angewandte Chemie (International ed. in English)》2013,52(5):1384-1402
The targeted delivery of potent cytotoxic agents has emerged as a promising strategy for the treatment of cancer and other serious conditions. Traditionally, antibodies against markers of disease have been used as drug‐delivery vehicles. More recently, lower molecular weight ligands have been proposed for the generation of a novel class of targeted cytotoxics with improved properties. Advances in this field crucially rely on efficient methods for the identification and optimization of organic molecules capable of high‐affinity binding and selective recognition of target proteins. The advent of DNA‐encoded chemical libraries allows the construction and screening of compound collections of unprecedented size. In this Review, we survey developments in the field of small ligand‐based targeted cytotoxics and show how innovative library technologies will help develop the drugs of the future. 相似文献
115.
Dr. Jing Xu Dominica H. C. Wong James D. Byrne Kai Chen Dr. Charles Bowerman Prof. Joseph M. DeSimone 《Angewandte Chemie (International ed. in English)》2013,52(26):6580-6589
Particle replication in nonwetting templates (PRINT) is a continuous, roll‐to‐roll, high‐resolution molding technology which allows the design and synthesis of precisely defined micro‐ and nanoparticles. This technology adapts the lithographic techniques from the microelectronics industry and marries these with the roll‐to‐roll processes from the photographic film industry to enable researchers to have unprecedented control over particle size, shape, chemical composition, cargo, modulus, and surface properties. In addition, PRINT is a GMP‐compliant (GMP=good manufacturing practice) platform amenable for particle fabrication on a large scale. Herein, we describe some of our most recent work involving the PRINT technology for application in the biomedical and material sciences. 相似文献
116.
Wanhua Lei Dr. Guoyu Jiang Dr. Qianxiong Zhou Dr. Yuanjun Hou Prof. Baowen Zhang Prof. Xuexin Cheng Prof. Xuesong Wang 《Chemphyschem》2013,14(5):1003-1008
Nanoscaled coordination polymers based on biologically prevalent ions have potential applications in drug delivery and biomedical imaging. Herein, coordination polymer nanoparticles of anionic porphyrins, including meso‐tetra(4‐carboxyphenyl)‐porphyrin (H2TCPP4?) and meso‐tetra(4‐sulfonatophenyl)‐porphyrin (H2TPPS4?), and alkaline or alkaline earth metal cations, such as K+ and Ca2+, were constructed in aqueous solution in the presence of cucurbit[7]uril (CB7) or cucurbit[8]uril (CB8). UV/Vis absorption and fluorescence spectroscopy, dynamic light scattering (DLS), scanning electron spectroscopy (SEM), and atomic force microscopy (AFM) were applied to explore the assembly and particle formation of porphyrin anions and metal cations mediated by CBn. The particle size depends on the kinds of CBn and metal cations and their concentrations. The uptake of H2TPPS4? particles by tumor cells (A549 cells) was found to be more efficient than H2TPPS4? at 37 °C, showing the application potential of such assembled particles in biology and medicine. 相似文献
117.
Yang Sun Zhipeng Ran Hongyan Tang Yong Li Wenshuang Song Qingguang Ren Wuli Yang Jilie Kong 《中国化学》2013,31(6):787-793
Mesoporous silica nanoparticles (MSN) were coated by pH‐responsive polymer chitosan‐poly (methacrylic acid) (CS‐PMAA). This nano drug delivery system showed good application prospects and the polymer‐coated microspheres were promising site‐specific anticancer drug delivery carriers in biomedical field. A continuous detection of pH‐responsive drug delivery system in cells in situ, utilizing MSN/CS‐PMAA composite microspheres, was proposed. Two kinds of different cell lines, tumor cell line (Hela) and normal somatic cells (293T), were used to investigate the behaviours of the drug loaded system in the cells. Conclusions could be drawn from the fluorescent images obtained by confocal laser scanning microscopy (CLSM), modified drug‐loaded microspheres (MSN/CS‐PMAA) were ingested into cells more easily, the uptake of DOX@FITC‐MSN/CS‐PMAA by HeLa/293T cells were performed at pH 7.4/pH 6.8, DOX was released during the ingestion process, fluorescence intensity decreased with time because of efflux transport and photo‐bleaching. Fluoresence detection by flow cytometry was performed as comparison. The continuous fluorescent observation in situ could be widely used in the pH‐responsive releasing process of drug delivery system in the cells. 相似文献
118.
Peter C. Griffiths Nicolo Mauro Damien M. Murphy Emma Carter Simon C. W. Richardson Paul Dyer Paolo Ferruti 《Macromolecular bioscience》2013,13(5):641-649
A series of nanoparticles is prepared via layer‐by‐layer assembly of oppositely charged, synthetic biocompatible polyamidoamine polymers as potential carriers. Particle size, surface charge and internal chain mobility are quantified as a function of the polymer type and number of layers. The effect of addition of surfactant is examined to simulate the effects of nanoparticle dissolution. The cyctotoxicity of these particles (in epithelia and murine cell lines) are orders of magnitude lower than polyethyleneimine controls. Stable nanoparticles may be prepared from mixtures of strongly, oppositely charged polymers, but less successfully from weakly charged polymers, and, given their acceptable toxicity characteristics, such modularly designed constructs show promise for drug and gene delivery.
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