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Facile synthesis of amphiphilic chitosan-g-poly(lactic acid) derivatives and the study of their controlled drug release

机译:两亲性壳聚糖-g-聚乳酸衍生物的简便合成及其药物控制释放的研究

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摘要

We report here a simple and green procedure for the synthesis of amphiphilic chitosan (CS) derivatives with poly(lactic acid) (PLA) side chains, without the use of high pure lactide, high temperatures, or large amounts of organic solvent. The chemical structure and physical properties of these CS derivatives were characterized by Fourier transform infrared spectroscopy, 1H-NMR, thermogravimetric analysis, and X-ray diffraction. The formation and characteristics of polymeric micelles based on these CS derivatives were studied by fluorescence spectroscopy and dynamic light scattering. The critical aggregation concentration in water varied from 0.048 to 0.021 mg/mL, and the mean diameter was in the range 169.8-260.7 nm in aqueous solution at 25°C when the PLA grafting percentage increased from 92 to 132%. Transmission electron microscopy showed that the micelles exhibited a nanospheric morphology within a size range of 60-120 nm. For the resulting micellar aggregates, the drug loading and in vitro drug-release characteristics were studied with indomethacin as the model drug. We found that such micellar aggregates could be potentially used as nanocarriers for drug delivery.
机译:我们在这里报告了一种简单且绿色的过程,无需使用高纯丙交酯,高温或大量有机溶剂,即可合成具有聚乳酸(PLA)侧链的两亲性壳聚糖(CS)衍生物。这些CS衍生物的化学结构和物理性质通过傅里叶变换红外光谱,1 H-NMR,热重分析和X射线衍射来表征。通过荧光光谱和动态光散射研究了基于这些CS衍生物的聚合物胶束的形成和特性。水中的临界聚集浓度在0.048至0.021 mg / mL之间变化,当PLA接枝率从92%增加到132%时,在25°C的水溶液中,平均直径在169.8-260.7 nm范围内。透射电子显微镜显示,胶束在60-120nm的尺寸范围内表现出纳米球形形态。对于所得的胶束聚集体,以吲哚美辛为模型药物研究了载药量和体外释药特性。我们发现这种胶束聚集体可以潜在地用作药物递送的纳米载体。

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