title: Stomach-specific controlled release gellan beads of acid-soluble drug prepared by ionotropic gelation method.
abstract: The purpose of the present work was the development and evaluation of stomach-specific controlled release mucoadhesive drug delivery system prepared by ionotropic gelation of gellan beads, containing acid-soluble drug amoxicillin trihydrate, using 3(2) factorial design with concentration of gellan gum and quantity of drug as variables. The study showed that beads prepared in alkaline cross-linking medium have higher entrapment efficiency than the acidic cross-linking medium. The entrapment efficiency was in the range of 32% to 46% w/w in acidic medium, which increased up to 60% to 90% w/w in alkaline medium. Batches with lowest, medium, and highest drug entrapment were subjected to chitosan coating to form a polyelectrolyte complex film. As polymer concentration increases, entrapment efficiency and particle size increases. Scanning electron microscopy revealed spherical but rough surface due to leaching of drug in acidic cross-linking solution, dense spherical structure in alkaline cross-linking solution, and rough surface of chitosan-coated beads with minor wrinkles. The in vitro drug release up to 7 h in a controlled manner following the Peppas model (r = 0.9998). In vitro and in vivo mucoadhesivity study showed that beads have good mucoadhesivity and more than 85% beads remained adhered to stomach mucosa of albino rat even after 7 h. In vitro growth inhibition study showed complete eradication of Helicobacter pylori. These results indicate that stomach-specific controlled release mucoadhesive system of amoxicillin gellan beads may be useful in H. pylori treatment.
authors.affiliation: Department of Pharmaceutics, Poona College of Pharmacy, Bharti Vidyapeeth University, Erandwane, Pune, 411038 Maharashtra, India.
authors.forename: Mrunalini
authors.initials: M
authors.lastname: Narkar
authors.forename: Praveen
authors.initials: P
authors.lastname: Sher
authors.forename: Atmaram
authors.initials: A
authors.lastname: Pawar
mesh_terms: D000143:Acids / Q000627:therapeutic use; D000658:Amoxicillin / Q000627:therapeutic use*; D000818:Animals; D048271:Chitosan / Q000737:chemistry / Q000627:therapeutic use; D003692:Delayed-Action Preparations / Q000627:therapeutic use; D004304:Dosage Forms; D016503:Drug Delivery Systems / Q000379:methods; D005079:Excipients / Q000627:therapeutic use; D005260:Female; D016480:Helicobacter pylori / Q000187:drug effects*; D008297:Male; D010316:Particle Size; D011135:Polysaccharides, Bacterial / Q000737:chemistry* / Q000627:therapeutic use; D051381:Rats; D017207:Rats, Sprague-Dawley; D013270:Stomach / Q000187:drug effects*
chemical_list: D000143:Acids; D003692:Delayed-Action Preparations; D004304:Dosage Forms; D005079:Excipients; D011135:Polysaccharides, Bacterial; C048288:gellan gum; D000658:Amoxicillin; D048271:Chitosan