Amoxicillin loaded chitosan-alginate polyelectrolyte complex nanoparticles as mucopenetrating delivery system for h. Pylori.
Amoxicillin loaded chitosan-alginate polyelectrolyte complex nanoparticles as mucopenetrating delivery system for h. Pylori.
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DOI：
10.3797/scipharm.1011-05
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发表时间：
2011-07-01
影响因子：
2.5
通讯作者：
Budhiraja, Ramji D
中科院分区：
文献类型：
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作者：
Arora, Saahil;Gupta, Sankalp;Budhiraja, Ramji D
本研究旨在应用纳米粒粘蛋白渗透给药系统彻底根除幽门螺杆菌（H。pylori），定殖到胃粘膜内层深处。大多数现有的药物递送系统由于不适当的粘膜粘附或粘膜渗透而失败，并且迄今为止还没有设计出具有粘附和渗透双重活性的剂型用于治疗H。幽门螺杆菌引起的疾病。在本研究中，新型壳聚糖-海藻酸钠复合物（CS-ALG PEC）阿莫西林纳米粒的设计和优化的各种变量，如pH值和混合比的聚合物，聚合物，药物和表面活性剂的浓度，使用3（3）Box-Behnken设计。在大鼠模型上进行了各种研究，如纳米颗粒的粒径、表面电荷、药物包封百分比、体外粘膜粘附和体内粘膜渗透。优化的FITC标记的CS-ALG PEC纳米颗粒相对于普通壳聚糖纳米颗粒显示出相对较低的体外粘膜粘附，但如在胃粘膜中连续6小时增加的荧光所观察到的，具有优异的粘膜渗透和定位，这在临床上可以帮助根除H.幽门。
The present study has been undertaken to apply the concept of nanoparticulate mucopenetrating drug delivery system for complete eradication of Helicobacter pylori (H. pylori), colonised deep into the gastric mucosal lining. Most of the existing drug delivery systems have failed on account of either improper mucoadhesion or mucopenetration and no dosage form with dual activity of adhesion and penetration has been designed till date for treating H. pylori induced disorders. In the present study, novel chitosan-alginate polyelectrolyte complex (CS-ALG PEC) nanoparticles of amoxicillin have been designed and optimized for various variables such as pH and mixing ratio of polymers, concentrations of polymers, drug and surfactant, using 3(3) Box-Behnken design. Various studies like particle size, surface charge, percent drug entrapment, in-vitro mucoadhesion and in-vivo mucopenetration of nanoparticles on rat models were conducted. The optimised FITC labelled CS-ALG PEC nanoparticles have shown comparative low in-vitro mucoadhesion with respect to plain chitosan nanoparticles, but excellent mucopenetration and localization as observed with increased fluorescence in gastric mucosa continuously over 6 hours, which clinically can help in eradication of H. pylori.