Mucoadhesive and floating chitosan-coated alginate beads for the controlled gastric release of amoxicillin.
This work focused on the development of mucoadhesive and floating chitosan-coated alginate beads as a gastroretensive delivery vehicle for amoxicillin, towards the effective eradication of Helicobacter pylori, a major causative agent of peptic ulcers. Alginate was used as the core bead core polymer and chitosan as the mucoadhesive polymer coating. Amoxicillin-loaded alginate beads coated with 0.5% (w/v) chitosan (ALG/0.5%CHI) exhibited excellent floating ability, high encapsulation efficiency, high drug loading capacity, and a strong in vitro mucoadhesion to the gastric mucosal layer. In vitro, amoxicillin was released faster in simulated gastric fluid (pH 1.2, HCl) than in simulated intestinal fluid (phosphate buffer, pH 7.4). ALG/0.5%CHI could be prepared with a > 90% drug encapsulation efficiency and exhibited more than 90% muco-adhesiveness, 100% floating ability, and achieved sustained release of amoxicillin for over six hours in SGF.
Sahasathian
Teerawat
T
Program of Petrochemistry and Polymer Science, Chulalongkorn University, Bangkok, Thailand.
Praphairaksit
Nalena
N
Muangsin
Nongnuj
N
D000268:Adhesiveness; D000464:Alginates / Q000737:chemistry* / Q000648:ultrastructure; D000658:Amoxicillin / Q000008:administration & dosage* / Q000032:analysis; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000032:analysis; D055598:Chemical Phenomena; D048271:Chitosan / Q000737:chemistry*; D003692:Delayed-Action Preparations / Q000008:administration & dosage; D004058:Diffusion; D004339:Drug Compounding; D016503:Drug Delivery Systems; D005753:Gastric Mucosa / Q000378:metabolism* / Q000382:microbiology; D005772:Gastrointestinal Transit; D005780:Gelatin / Q000737:chemistry; D020723:Glucuronic Acid / Q000737:chemistry; D016481:Helicobacter Infections / Q000188:drug therapy; D016480:Helicobacter pylori / Q000187:drug effects; D006603:Hexuronic Acids / Q000737:chemistry; D007419:Intestinal Secretions / Q000737:chemistry; D007700:Kinetics; D008863:Microspheres; D010437:Peptic Ulcer / Q000188:drug therapy / Q000382:microbiology; D014677:Pharmaceutical Vehicles; D013499:Surface Properties
D000464:Alginates; D000900:Anti-Bacterial Agents; D003692:Delayed-Action Preparations; D006603:Hexuronic Acids; D014677:Pharmaceutical Vehicles; D000658:Amoxicillin; D020723:Glucuronic Acid; D005780:Gelatin; D048271:Chitosan