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

Abstract

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.

• Authors: Haogang Duan, Shaoyu Lü, Hongyan Qin, Chunmei Gao, Xiao Bai, Yuhui Wei, Xin'an Wu, Mingzhu Liu, Xinyu Zhang, Zhen Liu
• Journal: International journal of pharmaceutics (Int J Pharm) Vol. 516 Issue 1-2 Pg. 214-224 (Jan 10 2017) ISSN: 1873-3476 [Electronic] Netherlands
• PMID: 27851980 (Publication Type: Journal Article)
• Copyright: Copyright © 2016 Elsevier B.V. All rights reserved.

Chemical References

• Alginates
• Anti-Inflammatory Agents, Non-Steroidal
• Drug Carriers
• Drug Combinations
• Hexuronic Acids
• N-succinyl-chitosan
• Mesalamine
• Glucuronic Acid
• Chitosan
• Zinc

Topics

• Administration, Oral
• Alginates (chemistry)
• Animals
• Anti-Inflammatory Agents, Non-Steroidal (administration & dosage, pharmacology)
• Chitosan (chemistry)
• Colitis (drug therapy, pathology)
• Disease Models, Animal
• Drug Carriers (chemistry)
• Drug Combinations
• Drug Delivery Systems
• Drug Liberation
• Drug Synergism
• Glucuronic Acid (chemistry)
• Hexuronic Acids (chemistry)
• Hydrogen-Ion Concentration
• Male
• Mesalamine (administration & dosage, pharmacology)
• Microscopy, Electron, Scanning
• Microspheres
• Rats
• Rats, Wistar
• Spectroscopy, Fourier Transform Infrared
• Zinc (administration & dosage, pharmacology)