Department of Pharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat-Yai, Songkhla, Thailand.
Drug Dev Ind Pharm. 2011 Apr;37(4):408-18. doi: 10.3109/03639045.2010.518149.
To investigate the muco/bioadhesive properties of chitosan, polyvinylpyrrolidone (PVP), and chitosan/PVP blends and the release of amoxicillin (AMX) contained in AMX-alginate beads coated with these materials.
Chitosan, PVP, and chitosan/PVP blends at various volume ratios were coated onto calcium alginate beads containing AMX. The muco/bioadhesive properties of all materials and the AMX-alginate beads coated with these materials were characterized.
Measurements of their viscosity, texture, and adhesion to HT29 cells demonstrated that chitosan/PVP at a volume ratio of 5/5 had the best muco/bioadhesive properties when compared with chitosan, PVP, and blends of other ratios. Wash-off tests indicated that the mucoadhesive property of the coated AMX-alginate beads was significantly higher than that of the uncoated beads. Diffuse reflectance infrared Fourier transform spectroscopy showed that there were interactions between chitosan-PVP, chitosan-mucin, PVP-mucin, and chitosan/PVP blend-mucin. Scanning electron microscopy revealed that the surfaces of the coated beads were smoother than those of the uncoated beads. All coated AMX-alginate beads were able to provide a controlled release of AMX with Super Case II transport properties, at a pH of 4. This was probably a result of the rapid and extensive swelling of the alginate beads. The more rapid release of AMX at pH 1 was probably because of the rapid dissolution of the drug at this pH.
From the controlled drug release and muco/bioadhesive properties of these coated AMX-alginate beads, we suggest that the alginate-coated beads might be a promising drug delivery system to assist with the eradication of Helicobacter pylori infections.
研究壳聚糖、聚乙烯吡咯烷酮（PVP）和壳聚糖/PVP 混合物的粘膜/生物粘附特性，以及用这些材料涂覆的含阿莫西林（AMX）的藻酸钠珠的 AMX 释放情况。
将壳聚糖、PVP 和不同体积比的壳聚糖/PVP 混合物涂覆到含有 AMX 的藻酸钙珠上。对所有材料的粘膜/生物粘附特性以及用这些材料涂覆的 AMX-藻酸盐珠进行了表征。
通过对它们的粘度、质地和与 HT29 细胞的粘附性的测量，发现当与壳聚糖、PVP 和其他比例的混合物相比时，体积比为 5/5 的壳聚糖/PVP 具有最佳的粘膜/生物粘附特性。冲洗试验表明，涂覆的 AMX-藻酸盐珠的粘膜粘附性明显高于未涂覆的珠。漫反射红外傅里叶变换光谱表明壳聚糖-PVP、壳聚糖-粘蛋白、PVP-粘蛋白和壳聚糖/PVP 混合物-粘蛋白之间存在相互作用。扫描电子显微镜显示，涂覆珠的表面比未涂覆珠的表面更光滑。所有涂覆的 AMX-藻酸盐珠都能够在 pH 值为 4 时提供具有超级案例 II 传输特性的 AMX 控制释放。这可能是由于藻酸盐珠的快速广泛膨胀所致。在 pH 值为 1 时 AMX 更快的释放可能是由于该 pH 值下药物的快速溶解所致。
从这些涂覆的 AMX-藻酸盐珠的控释和粘膜/生物粘附特性来看，我们认为藻酸盐涂覆珠可能是一种有前途的药物递送系统，有助于根除幽门螺杆菌感染。
