Program of Petrochemistry and Polymer Science, Chulalongkorn University, Bangkok, Thailand.
Arch Pharm Res. 2010 Jun;33(6):889-99. doi: 10.1007/s12272-010-0612-8. Epub 2010 Jul 6.
This work focused on the development of mucoadhesive and floating chitosan-coated alginate beads as a gastroretensive delivery vehicle for amoxicillin, towards the effective eradication of Helicobacter pylori, a major causative agent of peptic ulcers. Alginate was used as the core bead core polymer and chitosan as the mucoadhesive polymer coating. Amoxicillin-loaded alginate beads coated with 0.5% (w/v) chitosan (ALG/0.5%CHI) exhibited excellent floating ability, high encapsulation efficiency, high drug loading capacity, and a strong in vitro mucoadhesion to the gastric mucosal layer. In vitro, amoxicillin was released faster in simulated gastric fluid (pH 1.2, HCl) than in simulated intestinal fluid (phosphate buffer, pH 7.4). ALG/0.5%CHI could be prepared with a > 90% drug encapsulation efficiency and exhibited more than 90% muco-adhesiveness, 100% floating ability, and achieved sustained release of amoxicillin for over six hours in SGF.
本工作致力于开发具有黏膜黏附性和漂浮性的壳聚糖包被海藻酸钠珠作为阿莫西林的胃滞留给药载体，以有效根除消化性溃疡的主要病原体——幽门螺杆菌。海藻酸钠用作核心珠核聚合物，壳聚糖用作黏膜黏附性聚合物涂层。载阿莫西林的 0.5%（w/v）壳聚糖包被海藻酸钠珠（ALG/0.5%CHI）表现出优异的漂浮能力、高包封效率、高载药量和对胃黏膜层的强体外黏膜黏附性。在体外，阿莫西林在模拟胃液（pH 1.2，HCl）中的释放速度快于模拟肠液（磷酸盐缓冲液，pH 7.4）。ALG/0.5%CHI 可制备出大于 90%的药物包封效率，并表现出超过 90%的黏膜黏附性、100%的漂浮能力，并在 SGF 中实现阿莫西林的持续释放超过六个小时。
