Purpose

Floating drug delivery systems present one of the effective strategies to treat gastric disorders including peptic ulcer. To improve the retention of Clarithromycin at the target site of H. pylori induced ulcer, the current study undertakes development of gastro-retentive drug delivery systems based on muco-adhsesion (type I) and floating (type II) properties of the beads.

Method

Two different types of beads were prepared by ionic gelation method. The type-I beads comprised of chitosan and tripolyphosphate (TPP) while the type-II beads contain chitosan and xanthan gum to promote floating properties. The prepared beads were analyzed for size, morphology, circularity, roughness, drug content and association efficiency. The drug release profile of the beads was determined by USP Type II method. The floating capabilities of the beads were confirmed by using floating lag and total floating time. The swelling of the beads was evaluated using water bath at an agitation speed of 100 revolutions per minute. The in-vitro evaluation of muco-adhesion was determined using the fresh chicken eggshell membranes.

Results

The beads ranged in size from 1.9 to 3.0 mm. The size of type-II beads (F3 and F4) was significantly higher than type-I (F1 and F2) beads. The beads of formulations containing higher concentration of polymer (F1 and F2) were more circular while the roughness of type-II beads was significantly higher than type-I (p ≤ 0.05). The association efficiency ranged from 92.67 ± 5.42 to 95.97 ± 2.28% for type-I and type-II beads respectively. The type-I beads have shown sustained drug release in comparison to type-II beads due to compact nature. The type-II beads float within half a minute with total floating time of about 10 h. The type-II beads achieved significantly higher swelling than type-I beads, while the mucoadhesive property of F1 and F2 was significantly higher due to the presence of chitosan.

Conclusion

The study reports two types of beads that can be effectively utilized in H-pylori induced peptic ulcer using improved gastric drug retention via mucoadhesive (type-I) and floating (type-II) characteristics.

Graphical Abstract

中文翻译：

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用于改善克拉霉素胃滞留的粘膜粘附（I 型）和漂浮（II 型）壳聚糖珠

目的

漂浮药物递送系统是治疗包括消化性溃疡在内的胃部疾病的有效策略之一。为了改善克拉霉素在幽门螺杆菌引起的溃疡的靶位点的保留，当前的研究基于微珠的粘膜粘附（I 型）和漂浮（II 型）特性开发胃滞留药物递送系统。

方法

采用离子凝胶法制备了两种不同类型的珠子。I 型珠由壳聚糖和三聚磷酸盐 (TPP) 组成，而 II 型珠包含壳聚糖和黄原胶以提高漂浮性能。分析制备的珠子的尺寸、形态、圆形度、粗糙度、药物含量和缔合效率。珠子的药物释放曲线通过 USP II 型方法测定。通过使用漂浮滞后和总漂浮时间来确认珠子的漂浮能力。使用水浴以每分钟100转的搅拌速度评价珠的溶胀。使用新鲜鸡蛋壳膜测定粘膜粘附力的体外评价。

结果

珠子的尺寸范围为 1.9 至 3.0 毫米。II 型珠（F3 和 F4）的尺寸显着大于 I 型（F1 和 F2）珠。含有较高浓度聚合物的配方（F1和F2）的珠子更圆，而II型珠子的粗糙度显着高于I型（p≤0.05 ）  。I 型和 II 型珠子的结合效率范围分别为 92.67 ± 5.42 至 95.97 ± 2.28%。由于结构紧凑，与 II 型微珠相比，I 型微珠显示出持续的药物释放。II型珠在半分钟内漂浮，总漂浮时间约10小时。II 型微珠比 I 型微珠实现了显着更高的溶胀，而由于壳聚糖的存在，F1 和 F2 的粘膜粘附特性​​显着更高。

结论

该研究报告了两种类型的珠子，它们可以通过粘膜粘附（I 型）和漂浮（II 型）特性改善胃内药物保留，从而有效地用于幽门螺杆菌诱导的消化性溃疡。

图形概要