Floating microspheres bearing acetohydroxamic acid for the treatment of Helicobacter pylori

R B Umamaheshwari1, Subheet Jain, Dipankar Bhadra

  • 1Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences, Dr Hari Singh Gour University, Sagar (M.P.) 470 003, India.

Insights

Polycarbonate floating microspheres loaded with acetohydroxamic acid (AHA) offer an effective drug delivery system for Helicobacter pylori infections. These microspheres significantly enhance treatment efficacy and reduce the required AHA dosage due to prolonged gastric residence time.

Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Microbiology

Background:

  • Helicobacter pylori infection is a significant global health concern.
  • Developing effective drug delivery systems is crucial for treating H. pylori.
  • Acetohydroxamic acid (AHA) shows anti-H. pylori activity, but requires optimized delivery.

Purpose of the Study:

  • To develop and evaluate polycarbonate (PC) floating microspheres as a drug delivery system for acetohydroxamic acid (AHA).
  • To enhance the anti-H. pylori efficacy of AHA through improved gastrointestinal (GI) residence time.
  • To investigate the impact of PC concentration on microsphere characteristics and drug release.

Main Methods:

  • Floating PC microspheres were prepared using an emulsion (O/W) solvent evaporation technique.
  • Microsphere properties including morphology, particle size, entrapment efficiency, and drug release were analyzed.
  • In vitro and in vivo studies assessed the anti-H. pylori activity and efficacy of the developed system.

Main Results:

  • PC microspheres demonstrated excellent in vitro floating properties and prolonged GI tract residence.
  • Both AHA and PC microspheres exhibited in vivo anti-H. pylori activity.
  • The required AHA dose was reduced by a factor of 10 when delivered via PC microspheres.

Conclusions:

  • Floating PC microspheres represent a promising drug delivery system for H. pylori infections.
  • The enhanced efficacy is attributed to the prolonged gastric residence time provided by the microspheres' buoyancy.
  • This approach offers a more effective method for clearing H. pylori from the GI tract compared to conventional drug administration.

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