Development and in vivo Evaluation of Gastroretentive Floating Microballoons of Acetohydroxamic Acid for Enhanced Oral Bioavailability
Munija Pancheddula
Vision College of Pharmaceutical Sciences & Research, Boduppal, Hyderabad, India.
Nemuri Mounika
Vision College of Pharmaceutical Sciences & Research, Boduppal, Hyderabad, India.
Upparaboina Srilatha
Vision College of Pharmaceutical Sciences & Research, Boduppal, Hyderabad, India.
Shayeda *
Department of Pharmaceutics, University College of Pharmaceutical Sciences, Kakatiya University, Warangal-506009, India.
*Author to whom correspondence should be addressed.
Abstract
The oral route remains the most preferred and patient-friendly mode of drug administration. Microballoons, a non-effervescent gastroretentive system, are hollow microspheres (<200 µm) composed of polymers or proteins that exhibit excellent buoyancy due to their internal cavity. As multiple-unit systems, they ensure uniform drug distribution, minimise dose dumping, and allow controlled drug release by optimising polymer composition. Acetohydroxamic acid, a urease inhibitor structurally similar to urea, effectively inhibits Helicobacter pylori by penetrating bacterial cells and blocking urease activity, making it suitable for stomach-specific delivery. This study involved the formulation of acetohydroxamic acid floating microballoons, the evaluation of gastric retention by X-ray imaging in rabbits, and bioavailability assessment through pharmacokinetic studies. DSC and FTIR confirmed drug–polymer compatibility. The percentage yield was in the range of 60-90 % for all the formulations. It was found to be less than 70% yield with ethyl cellulose and HPMC K4M, and for the optimised formulation, the yield was around 80 %. The entrapment efficiency was in the range of 60-90 % for all the formulations and was found to be 89.6%for optimized formulation. The percentage buoyancywas in the range of 60-90 % for all the formulations and was found to be 85.5% for optimized formulation. Drug content of all the prepared formulations was found to be within the acceptable range of 90.0 -110.0%. This manuscript is important to the scientific community as it provides a comprehensive and well-validated approach to gastroretentive drug delivery using floating microballoons as a non-effervescent, multiparticulate system. The work offers a reproducible formulation strategy for stomach-specific delivery of urease inhibitors, addressing a critical challenge in the management of Helicobacter pylori infections. Overall, the findings contribute valuable translational insights for the development of advanced oral drug delivery systems with improved clinical efficacy.
Keywords: Acetohydroxamic acid, floating microballoons, solvent evaporation method, gastric residence time, floating, gastroretentive drug delivery systems