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Preparation of pH- and thermo-sensitive chitosan-PNIPAAm core-shell nanoparticles and evaluation as drug carriers

机译:pH和热敏壳聚糖-PNIPAAm核壳纳米粒子的制备及作为药物载体的评价

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Environmentally sensitive polysaccharide nanoparticles (NPs) were prepared by in situ polymerization of N-isopropylacrylamide (NIPAAm) monomer in the presence of chitosan (CS) micelles. First, CS was found to develop a cationic micelle-like structure in the acetic acid solution when its concentration was increased to above the critical micelle concentration, as evidenced by fluorescence and TEM. When the NIPAAm was polymerized in the CS micelle solution by using potassium persulfate as initiator, the produced PNIPAAm with anionic chain end(s) became hydrophobic, as long as the reaction temperature was above its phase transition temperature; and therefore it would diffuse into the hydrophobic core of the CS micelles, producing CS-PNIPAAm core-shell NPs. Increasing the feeding amount of NIPAAm increased the monomer conversion and therefore the particle size; yet it decreased the surface zeta potential. Moreover, the CS-PNIPAAm NPs were sensitive to both pH value and temperature. For the study of drug release properties, doxycycline hyclate was used as a model drug and loaded into the NPs at pH 4.5 and 25 °C. The result illustrated that these NPs had a continuous drug release behavior up to 1 week, depending on the pH value and temperature. In addition, enzyme or hydrogen peroxide capable of degrading CS shell was added in the solution to facilitate the drug release.
机译:通过在壳聚糖(CS)胶束存在下原位聚合N-异丙基丙烯酰胺(NIPAAm)单体制备对环境敏感的多糖纳米颗粒(NPs)。首先,发现CS的浓度增加到临界胶束浓度以上时,在乙酸溶液中会形成阳离子胶束状结构,如荧光和TEM所示。当使用过硫酸钾作为引发剂使NIPAAm在CS胶束溶液中聚合时,只要反应温度高于其相变温度,生成的带有阴离子链端的PNIPAAm就会变为疏水性。因此它会扩散到CS胶束的疏水核中,产生CS-PNIPAAm核-壳NP。增加NIPAAm的进料量可以提高单体转化率,从而提高粒径。但是它降低了表面ζ电势。此外,CS-PNIPAAm NP对pH值和温度均敏感。为了研究药物的释放特性,使用盐酸多西环素作为模型药物,并在pH 4.5和25°C的条件下将其加载到NP中。结果表明,这些NP在长达1周的时间内具有连续的药物释放行为,具体取决于pH值和温度。另外,将能够降解CS壳的酶或过氧化氢加入溶液中以促进药物释放。

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