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Preparation, in vitro and in vivo evaluation of stomach-specific metronidazole-loaded alginate beads as local anti- Helicobacter pylori therapy

Metronidazole (MZ), a common antibacterial drug used in treatment of H. pylori, was prepared in chitosan-treated alginate beads by the ionotropic gelation method. A (3 × 2 × 2) factorially designed experiment was used in which 3 viscosity-imparting polymers namely, methyl cellulose, carbopol 934P an...

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Published in:Journal of controlled release 2007-06, Vol.119 (2), p.207-214
Main Authors: Ishak, Rania A.H., Awad, Gehanne A.S., Mortada, Nahed D., Nour, Samia A.K.
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description Metronidazole (MZ), a common antibacterial drug used in treatment of H. pylori, was prepared in chitosan-treated alginate beads by the ionotropic gelation method. A (3 × 2 × 2) factorially designed experiment was used in which 3 viscosity-imparting polymers namely, methyl cellulose, carbopol 934P and κ-carrageenan, 2 concentrations (0.2 and 0.4% w/v) of chitosan as encapsulating polymer and 2 concentrations (2.5 and 5% w/w) of the low density magnesium stearate as a floating aid were tested. The drug entrapment efficiency (%), the percent of floating beads and the time for 80% of the drug to be released ( T 80%) were the responses evaluated. The bead formula containing 0.5% κ-carrageenan, 0.4% chitosan and 5% magnesium stearate showed immediate buoyancy, optimum drug entrapment efficiency and extended drug release. The histopathological examination of mice stomachs and in vivo H. pylori clearance tests were carried out by orally administering MZ floating alginate beads or MZ suspension, to H. pylori infected mice under fed conditions as a single daily dose for 3 successive days in different doses 5, 10, 15 and 20 mg/kg. The histopathological examination showed that groups receiving MZ in the form of floating alginate beads at doses 10, 15 and 20 mg/kg were better than the corresponding suspension form, regarding eradication of H. pylori infection. The in vivo H. pylori clearance tests showed that MZ floating beads with a dose of 15 mg/kg provided 100% clearance rate whereas the MZ suspension with a dose of 20 mg/kg gave only 33.33%.
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The histopathological examination showed that groups receiving MZ in the form of floating alginate beads at doses 10, 15 and 20 mg/kg were better than the corresponding suspension form, regarding eradication of H. pylori infection. The in vivo H. pylori clearance tests showed that MZ floating beads with a dose of 15 mg/kg provided 100% clearance rate whereas the MZ suspension with a dose of 20 mg/kg gave only 33.33%.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>17412443</pmid><doi>10.1016/j.jconrel.2007.02.012</doi><tpages>8</tpages></addata></record>
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ispartof Journal of controlled release, 2007-06, Vol.119 (2), p.207-214
issn 0168-3659
1873-4995
language eng
recordid cdi_proquest_miscellaneous_70527929
source ScienceDirect Journals
subjects Alginate beads
Alginates - administration & dosage
Alginates - chemical synthesis
Alginates - pharmacokinetics
Animals
Anti-Infective Agents - administration & dosage
Anti-Infective Agents - chemical synthesis
Anti-Infective Agents - pharmacokinetics
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
Biological and medical sciences
Chemistry, Pharmaceutical
Delayed-Action Preparations - administration & dosage
Delayed-Action Preparations - chemical synthesis
Delayed-Action Preparations - pharmacokinetics
Drug Delivery Systems - methods
Drug Evaluation, Preclinical - methods
Floating drug delivery systems (FDDS)
Gastric Mucosa - drug effects
Gastric Mucosa - metabolism
Gastric Mucosa - microbiology
Gastric Mucosa - pathology
General pharmacology
Glucuronic Acid - administration & dosage
Glucuronic Acid - chemical synthesis
Glucuronic Acid - pharmacokinetics
H. pylori clearance
Helicobacter Infections - drug therapy
Helicobacter Infections - metabolism
Helicobacter Infections - pathology
Helicobacter pylori
Helicobacter pylori - drug effects
Helicobacter pylori - isolation & purification
Hexuronic Acids - administration & dosage
Hexuronic Acids - chemical synthesis
Hexuronic Acids - pharmacokinetics
Humans
Local delivery
Male
Medical sciences
Metronidazole
Metronidazole - administration & dosage
Metronidazole - chemical synthesis
Metronidazole - pharmacokinetics
Mice
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Sustained release
title Preparation, in vitro and in vivo evaluation of stomach-specific metronidazole-loaded alginate beads as local anti- Helicobacter pylori therapy
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