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The chemical composition and quantitative molar ratios among all components of biodegradable polyphosphoester copolymers of DL ‐lactide and ethylphosphate were determined by a comprehensive set of NMR spectroscopic methods. The polyphosphoester copolymers studied were synthesized using condensation polymerization of oligomeric DL ‐lactide prepolymers and ethyl dichlorophosphate. Conclusive identification of the chemical shift patterns of all functional groups in the copolymers required additional NMR methods such as 31P‐NMR and two‐dimensional 1H–1H COSY NMR, in addition to the synthesis and comparative NMR analysis of model compounds possessing identical phosphoester linkages in the polyphosphoester copolymers. For the polymers synthesized using the bulk polycondensation process, 1H–1H COSY NMR analysis revealed the presence of a small amount of side products that were undetected by 1H‐NMR alone. These side reactions most likely occurred between the pendant ethoxy group of the phosphoesters and the hydrogen chloride gas generated in the bulk polycondensation process. 31P‐NMR spectra of the copolymers revealed a consistent triple‐peak pattern characteristic of phosphoesters linked to a racemic mixture of D,L ‐lactides. These results offered new insight into the side reactions occurring in bulk polymerization of polyphosphoesters and provided a powerful tool of characterizing complex biodegradable polymers. © 2003 Wiley Periodicals, Inc. J Appl Polym Sci 90: 4021–4031, 2003 相似文献
84.
Renner S Ludwig V Boden O Scheffer U Göbel M Schneider G 《Chembiochem : a European journal of chemical biology》2005,6(6):1119-1125
TAR RNA is a potential target for AIDS therapy. Ligand-based virtual screening was performed to retrieve novel scaffolds for RNA-binding molecules capable of inhibiting the Tat-TAR interaction, which is essential for HIV replication. We used a "fuzzy" pharmacophore approach (SQUID) and an alignment-free pharmacophore method (CATS3D) to carry out virtual screening of a vendor database of small molecules and to perform "scaffold-hopping". A small subset of 19 candidate molecules were experimentally tested for TAR RNA binding in a fluorescence resonance energy transfer (FRET) assay. Both methods retrieved molecules that exhibited activities comparable to those of the reference molecules acetylpromazine and chlorpromazine, with the best molecule showing ten times better binding behavior (IC50 = 46 microM). The hits had molecular scaffolds different from those of the reference molecules. 相似文献
85.
A series of pH‐responsive hydrogels were studied as potential drug carriers for the protection of insulin from the acidic environment of the stomach before releasing in the small intestine. Hydrogels based on poly(vinyl alcohol) networks grafted with acrylic acid or methacrylic acid were prepared by a two‐step process. Poly(vinyl alcohol) hydrogels were prepared by gamma ray irradiation (50 kGy) and then followed by grafting either acrylic acid or methacrylic acid onto these poly(vinyl alcohol) hydrogels with subsequent irradiation (5–20 kGy). These graft hydrogels showed pH‐sensitive swelling behavior and were used as carriers for the controlled release of insulin. The in vitro release of insulin was observed for the insulin‐loaded hydrogels in a simulated intestinal fluid (pH 6.8) but not in a simulated gastric fluid (pH 1.2). The release behavior of insulin in vivo in a rat model confirmed the effectiveness of the oral delivery of insulin to control the level of glucose. © 2003 Wiley Periodicals, Inc. J Appl Polym Sci 91: 636–643, 2004 相似文献
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饮用水短缺和水污染问题严重影响着人类和社会的发展。反渗透技术提供了一种高效经济的方法来生产纯水和处理废水,以缓解这个问题。但是,反渗透膜的污染尤其是生物污染严重制约着其高效应用。膜表面改性技术是提升膜抗污染性能的最常用手段,通过多巴胺盐酸盐(DA)在聚酰胺反渗透膜表面自聚,生成超薄聚多巴胺涂层(PDA),进一步利用PDA涂层上的活性基团将聚乙烯亚胺(PEI)接枝到反渗透膜表面,得到稳定持久的PDA-PEI改性反渗透膜。通过对改性膜的XPS测试,亲水性和抗菌性试验,得到以下结论:PDA成功涂层于反渗透膜表面,且PEI成功接枝于PDA涂层表面;PDA-PEI改性增大了膜表面的亲水性,提升了反渗透膜抗污染的能力,使其具有了一定的抗菌能力。 相似文献
88.
William Leobandung Hideki Ichikawa Yoshinobu Fukumori Nicholas A. Peppas 《应用聚合物科学杂志》2003,87(10):1678-1684
Poly(ethylene glycol)‐based nanoparticles have received significant attention in the field of biomedicine. When they are copolymerized with pH‐ or temperature‐sensitive comonomers, their small size allows them to respond very quickly to changes in the environment, including changes in the pH, ionic strength, and temperature. In addition, the high surface‐to‐volume ratio makes them highly functionalized. In this work, nanoparticles composed of temperature‐sensitive poly(N‐isopropylacrylamide), poly(ethylene glycol) 400 dimethacrylate, and poly(ethylene glycol) 1000 methacrylate were prepared by a thermally initiated, free‐radical dispersion polymerization method. The temperature‐responsive behavior of the hydrogel nanoparticles was characterized by the study of their particle size with photon correlation spectroscopy. The size of the nanoparticles varied from 200 to 1100 nm and was a strong function of the temperature of the system, from 5 to 40°C. The thermal, structural, and morphological characteristics were also investigated. © 2002 Wiley Periodicals, Inc. J Appl Polym Sci 87: 1678–1684, 2003 相似文献
89.
By use of a spectrophotometric method the quantity of binding of medicinal compound [succinate of 2,5‐dimethyl‐4‐benzoyl‐oxypiperidine (AK‐29)], over gels of polyacrylic acid, and liberation of medicinal compound (MC) from the gel phase were investigated. It was established that both concentration and pH dependency of AK‐29 sorption over PAA gels pass through a maximum and increase with increasing degree of gel crosslinking. The yield of MC from the gel phase, depending on the conditions, reaches 80% and accelerates at the change of the aqueous phase to a physiological one. © 2005 Wiley Periodicals, Inc. J Appl Polym Sci 96: 1187–1192, 2005 相似文献
90.
The interaction of water‐soluble and crosslinked polyacrylic acid (PAA) with a medicinal compound (MC) of 2,5‐dimethyl‐4‐benzoyl‐oxypiperidine succinate was investigated. By methods of potentiometry, viscosimetry, and equilibrium swelling it was confirmed that the interaction of linear and network PAA with MC proceeds with complex formation. The degree of complex formation depends on the effect of pH, MC concentration, and degree of polyacid crosslinking. © 2005 Wiley Periodicals, Inc. J Appl Polym Sci 96: 1183–1186, 2005 相似文献