Characterization of thermosensitive chitosan gels for the sustained delivery of drugs
Characterization of thermosensitive chitosan gels for the sustained delivery of drugs
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DOI：
10.1016/s0378-5173(00)00428-2
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发表时间：
2000-08-10
影响因子：
5.8
通讯作者：
Leroux, JC
中科院分区：
文献类型：
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作者：
Ruel-Gariépy, E;Chenite, A;Leroux, JC
本研究旨在研究在37℃下凝胶化的壳聚糖/甘油磷酸酯（GP）温敏溶液的物理性质，并评估不同模型化合物的体外释放曲线。凝胶化速率取决于温度和壳聚糖的脱乙酰度。含有84%脱乙酰化壳聚糖的溶液在4℃下可储存3个月，粘度无明显变化。模型化合物的体外释放曲线取决于壳聚糖溶液中GP的存在、它们的分子量以及释放介质中溶菌酶的存在。当模型化合物浓度较低时，它们不受其静电荷的影响。在最初的4小时内，释放伴随着凝胶重量的大量损失，这主要归因于水和过量GP的浸出。扫描电子显微镜照片显示，在暴露于连续流动的磷酸盐缓冲盐水24小时后，这些溶液形成具有高度多孔结构的凝胶。这些结果表明，壳聚糖/GP温敏溶液在体温下迅速凝胶化，在4℃下可保持溶胶状态，并能维持大分子的释放。（C）2000 Elsevier Science B.V.保留所有权利。
The aim of this study was to investigate the physical properties of a chitosan/glycerophosphate (GP) thermosensitive solution which gels at 37 degrees C and evaluate the in vitro release profiles of different model compounds. The gelation rate was dependent on the temperature and on the chitosan deacetylation degree. The solution containing 84%-deacetylated chitosan could be stored 3 months at 4 degrees C without apparent change in viscosity. The in vitro release profiles of the model compounds depended on the presence of GP in the chitosan solution, on their molecular weight and on the presence of lysozyme in the release media. They were not affected by the electrostatic charge of the model compound when present at low concentrations. During the first 4 h, the release was accompanied by a substantial loss of the gel weight which was mainly attributed to the leaching of water and excess GP. Scanning electron micrographs revealed that the solutions yield gels with a highly porous structure after 24 h of exposure to a continuous flow of phosphate buffered saline. These results indicate that the chitosan/GP thermosensitive solutions gel rapidly at body temperature, can remain in the sol state at 4 degrees C and can sustain the delivery of macromolecules. (C) 2000 Elsevier Science B.V. All rights reserved.