Center of Eco-material and Green Chemistry, Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences, Lanzhou, PR China.
Drug Dev Ind Pharm. 2010 Sep;36(9):1106-14. doi: 10.3109/03639041003677798.
The aim of this study was to prepare pH-sensitive ofloxacin (OFL)/montmorillonite (MMT)/chitosan (CTS) nanocomposite microspheres that improve the burst release effect of the drug by the solution intercalation technique and emulsification cross-linking techniques.
First, OFL/MMT hybrids were prepared through the solution intercalation technique. Then, OFL/MMT-intercalated OFL/MMT/CTS nanocomposite microspheres were obtained through emulsification cross-linking technology. The intercalated nanocomposite was confirmed by Fourier-transform infrared spectroscopy and X-ray diffraction. Finally, in vitro release of OFL from the microspheres was performed in simulated gastric fluids and simulated intestinal fluids. The effect of MMT content on drug encapsulation efficiency and the drug release of the nanocomposite microspheres were investigated.
The results showed that the release rate of OFL from the nanocomposite microspheres at pH 7.4 was higher than that at pH 1.2. Compared with pure CTS microspheres, the incorporation of certain amount of MMT in the nanocomposite microspheres can enhance the drug encapsulation efficiency and reduce the burst release.
A sustained release particulate system can be obtained by incorporating MMT into the nanocomposite microspheres and can improve the burst release effect of the drug.
本研究旨在制备 pH 敏感的氧氟沙星（OFL）/蒙脱石（MMT）/壳聚糖（CTS）纳米复合微球，通过溶液插层技术和乳化交联技术改善药物的爆发释放效果。
首先，通过溶液插层技术制备 OFL/MMT 杂化物。然后，通过乳化交联技术获得 OFL/MMT 插层-OFL/MMT/CTS 纳米复合微球。通过傅里叶变换红外光谱和 X 射线衍射确认插层纳米复合材料。最后，在模拟胃液和模拟肠液中进行微球中 OFL 的体外释放。考察了 MMT 含量对纳米复合微球药物包封率和药物释放的影响。
结果表明，纳米复合微球在 pH 7.4 时的释放速率高于 pH 1.2 时的释放速率。与纯 CTS 微球相比，纳米复合微球中加入一定量的 MMT 可以提高药物包封率，降低突释。
通过将 MMT 掺入纳米复合微球中，可以获得缓释颗粒系统，从而改善药物的爆发释放效果。
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