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Gastric Mucosa Quantitative Polymerase Chain Reaction Analysis for Detecting Helicobacter pylori and Antibiotic Resistance
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Gastric Mucosa Quantitative Polymerase Chain Reaction Analysis for Detecting Helicobacter pylori and Antibiotic Resistance

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Development of gastroretentive metronidazole floating raft system for targeting Helicobacter pylori

Nancy Abdel Hamid Abou Youssef1, Abeer Ahmed Kassem2, Magda Abd Elsamea El-Massik1

  • 1Department of Pharmaceutics, Faculty of Pharmacy and Drug Manufacturing, Pharos University in Alexandria, Egypt.

International Journal of Pharmaceutics
|April 7, 2015
PubMed

Insights

This study developed a novel floating raft system (FRS) for metronidazole (Mz) to extend drug release and gastric residence time. The optimized alginate-based FRS demonstrated excellent buoyancy, sustained release, and stability for effective Helicobacter pylori eradication.

Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Polymer Science

Background:

  • Gastric residence time significantly impacts oral drug efficacy.
  • Developing sustained-release formulations for gastric targeting remains a challenge.
  • Metronidazole (Mz) is a key antibiotic for treating H. pylori infections.

Purpose of the Study:

  • To develop and evaluate an ion-sensitive in situ gel-forming floating raft system (FRS) for prolonged gastric residence and sustained release of metronidazole (Mz).
  • To investigate the impact of different polymers (alginate and gellan gum) and lipid excipients on FRS performance.
  • To assess the suitability of the optimized FRS for gastric targeting in H. pylori eradication.

Main Methods:

  • Formulation of FRS using sodium alginate or gellan gum with calcium carbonate and sodium citrate.
  • Incorporation of lipids (glyceryl monostearate, Precirol®, Compritol®) into gellan gum-based FRS.
  • Evaluation of FRS properties including buoyancy, gelation capacity, viscosity, and drug release kinetics.
  • Stability testing of the selected optimized formulation.

Main Results:

  • Alginate-based FRS (Alg4%C2%) showed rapid gelation (3s), prolonged buoyancy (>24h), and sustained metronidazole release (MDT 6h).
  • Gellan gum-based FRS achieved gastroretention but lacked sufficient gelation capacity.
  • Incorporation of glyceryl monostearate (Mz:GMS 1:1) improved gelation and maintained sustained release and stability.
  • Optimized FRS demonstrated excellent potential for gastric targeting.

Conclusions:

  • Alginate-based floating raft systems are effective for prolonging gastric residence time and achieving sustained metronidazole release.
  • The optimized FRS formulation exhibits favorable characteristics for enhanced therapeutic efficacy against H. pylori.
  • This novel FRS represents a promising approach for gastric drug delivery and H. pylori eradication therapy.
Keywords:
Compritol(®)Gelation capacityGellan gumGlyceryl mono stearatePrecirol(®)Sodium alginate

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