Stomach-Specific Controlled Release Gellan Beads of Acid-Soluble Drug Prepared by Ionotropic Gelation Method

Abstract

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.

Biopolímeros: aplicações farmacêutica e biomédica

“…Na área farmacêutica, a crescente utilização da gelana pode ser exemplificada por diversos sistemas de liberação de fármacos descritos na literatura destinados ao tratamento dos mais diversos tipos de patologias, dentre eles estão os hidrogéis 113 , microesferas 112,117 , microcápsulas 118,119 , esferas flutuantes 123 , entre outros. Recentemente, a gelana tem sido estudada para aplicações biomédicas, mais precisamente na medicina regenerativa.…”

Floating-bioadhesive gastroretentiveCaesalpinia pulcherrima-based beads of amoxicillin trihydrate forHelicobacter pylorieradication

“…Helicobacter pylori eradication treatment is not all the time successful and exhibit some injurious with side effects, expenditure of therapy are the major limitations of the therapy. Therefore, distributing drug at the site of infection for an extended period of time, healing a gastric or peptic ulcer, recovering the stability of antibiotics in gastric environment, piercing through gastric mucus layer to act effectively and prevention of repetition are the few approaches to improve the efficacy of antibiotic therapy (Rajinikanth et al, 2008;Narkar et al, 2010;Gattani et al, 2010). Thus, Gastroretentive Drug Delivery System (GRDDS) can be developed to perk up the effectiveness of antibiotic therapy for prolonged gastric residence and probable longer drug release in the ecological niche of the bacterium.…”

Dual drug delivery system for targeting H. pylori in the stomach: preparation and in vitro characterization of amoxicillin-loaded Carbopol® nanospheres

“…Consequently, it is expected that if local delivery of antimicrobial agents from the gastric lumen into the mucus layer can be achieved, the H. pylori eradication rate would be increased. 11 Several formulations have been suggested to help retain amoxicillin in the stomach, including gellan beads, 12 nanocapsules, 13 hydrogel nanoparticles, 14 floating microballoons, 15 and mucoadhesive microspheres, 16 which are able to remain in the gastrointestinal tract for a longer time, and therefore be more effective in H. pylori eradication.…”