Key Laboratory of Drug Targeting and Drug Delivery, Ministry of Education, West China School of Pharmacy, Sichuan University, Chengdu, Sichuan, People's Republic of China.
J Mater Sci Mater Med. 2012 Apr;23(4):983-90. doi: 10.1007/s10856-012-4567-9. Epub 2012 Feb 10.
Insufficient gastric mucosa drug concentration and short contact time were the main reason for the lack of eradication efficacy of Helicobacter pylori for peptic ulcer patients. Novel multi-core chitosan microspheres were prepared for stomach-specific delivery of hydrophilic antibiotics for the treatment of peptic ulcer. Chitosan microspheres with multiple Eudragit L100 cores were easily prepared by a new emulsification/coagulation encapsulating method. Swelling behaviors, surface amino groups and mucin absorption ability were investigated and the formulation that showed best mucoadhesive potential was adopted. The multi-core chitosan microspheres exhibited good mucoadhesiveness as well as controlled release manner for incorporated antibiotics in acidic environment. The release rate could be easily modulated with accumulative release ranging from 47.3 to 79.3% in 6 h. Accordingly, the multi-core chitosan microspheres could serve as a satisfactory vehicle for stomach-specific delivery of hydrophilic antibiotics.
胃酸黏膜药物浓度不足和接触时间短是消化性溃疡患者幽门螺杆菌根除疗效差的主要原因。为了治疗消化性溃疡，将新型多芯壳聚糖微球用于亲水性抗生素的胃内靶向传递。通过一种新的乳化/凝聚包埋方法，很容易制备出具有多个 Eudragit L100 核的壳聚糖微球。考察了溶胀行为、表面氨基和粘蛋白吸收能力，并采用表现出最佳粘膜粘附潜力的配方。多芯壳聚糖微球在酸性环境中对包封的抗生素表现出良好的粘膜粘附性和控制释放方式。通过 6 小时内的累积释放，释放率可轻松调节，在 47.3%至 79.3%的范围内。因此，多芯壳聚糖微球可以作为一种理想的亲水性抗生素胃内靶向传递载体。
