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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.
Abstract:
This investigation is part of our ongoing effort to develop effective drug delivery systems for the treatment of Helicobacter pylori infection using polycarbonate (PC) floating microspheres as drug carriers. In an effort to augment the anti-H. pylori effect of acetohydroxamic acid (AHA), floating PC microspheres, which have the ability to reside in the gastrointestinal (GI) tract for an extended period, were prepared by emulsion (O/W) solvent evaporation technique. The effect of PC concentration on the morphology, particle size, entrapment efficiency and drug release rate was studied. In-vitro studies confirmed the excellent floating properties of PC microspheres. In-vitro and in-vivo growth inhibition studies were performed on developed system(s) taking isolated cultures of H. pylori and H. pylori-infected Mongolian gerbils, respectively. The drug and PC microspheres both showed anti-H. pylori activity in vivo, but the required dose of AHA was effectively reduced by a factor of 10 in the case of PC microspheres. In conclusion, the floating microspheres more effectively cleared H. pylori from the GI tract than the drug because of the prolonged gastric residence time resulting from the excellent buoyancy of the PC.
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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