Co-delivery of zinc and 5-aminosalicylic acid from alginate/N-succinyl-chitosan blend microspheres for synergistic therapy of colitis

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• 作者：Haogang Duan^a ; ^b ; ^{duanhg13@lzu.edu.cn} ; Shaoyu Lü ; ^a ; ^{lshy@lzu.edu.cn} ; Hongyan Qin^b ; ^{candyqinhy@163.com} ; Chunmei Gao^a ; ^{gaochm@lzu.edu.cn} ; Xiao Bai^a ; ^{baix12@lzu.edu.cn} ; Yuhui Wei^b ; ^{weiyh_001@163.com} ; Xin&rsquo ; an Wu^b ; ^{xinanwu6511@163.com} ; Mingzhu Liu^a ; ^{mzliu@lzu.edu.cn} ; Xinyu Zhang^c ; ^{xzz0004@auburn.edu} ; Zhen Liu^d ; ^{zliu@frostburg.edu}
• 关键词：Alginate ; N-succinyl-chitosan ; Blend microspheres ; Co-delivery ; Colon-specific
• 刊名：International Journal of Pharmaceutics
• 出版年：2017
• 出版时间：10 January 2017
• 年：2017
• 卷：516
• 期：1-2
• 页码：214-224
• 全文大小：3981 K
• 卷排序：516

文摘

The present study developed novel zinc ion cross-linked alginate/N-succinyl-chitosan (NSC) blend microspheres (MS) for co-delivery of zinc and 5-aminosalicylic acid (5-ASA) for synergistic therapy of colitis. Physicochemical characterization of blend MS was assessed using scanning electron microscopy (SEM), Fourier transform infrared (FTIR) spectroscopy, and energy dispersive X-ray spectrometer (EDS). In vitro release studies demonstrated that blend MS has a pH-dependent release property. Both 5-ASA and zinc have lower release in acid medium and higher release in colonic environment. The therapeutic efficacy of zinc cross-linked blend MS was evaluated using induced-colitis rat models, and showed a superior treatment effect in alleviating inflammation of colitis rats. No systemic toxicity was observed after oral administration of blend MS. Therefore, zinc ion cross-linked alginate/N-succinyl-chitosan blend MS appeared to be a good candidate for co-delivery of zinc and 5-ASA to colon, and had great potential application in inflammatory bowel diseases (IBD) treatment.