Levofloxacin Hemihydrate-Adorned Floating Drug Delivery System to Ameliorate H. Pylori Infection: Formulation Development, Optimization, and Characterization.

Objective

This study focused on developing and characterizing Levofloxacin hemihydrate floating bioadhesive tablets for the treatment of Helicobacter pylori (H. pylori) infection.

Significance

This study demonstrates a promising gastroretentive and bioadhesive drug delivery system that enhances the effectiveness of levofloxacin in the stomach for targeted H. pylori infection treatment.

Methods

Floating bio-adhesive tablets were prepared by direct compression using sodium bicarbonate (NaHCO3) as a gas-generating agent and HPMC K4M/chitosan and carbopol 940P/sodium alginate as release retardants and bio-adhesives. Pre-formulation flow properties were evaluated. Tablets were characterized by physicochemical parameters, bioadhesion on goat stomach mucosa, and FTIR, which confirmed drug-excipient compatibility.

Results

The optimized formulation (FT7) showed a buoyancy lag time of 62.59 ± 6.83 second, a total floating time of more than 12h, a swelling index of 81.89%, and a bioadhesion strength of 28.19 ± 5.12g. The formulation remained physically stable after three months of storage at 40 °C and 75% RH. Drug release followed a non-Fickian diffusion mechanism (n = 0.514) and best fit the Korsmeyer-Peppas model (R2 = 0.989). In vitro and in vivo mucoadhesion studies demonstrated good retention of the tablet in the rabbit stomach for over 12 h. In-vivo barium sulfate X-ray imaging further confirmed that the tablet remained floating in the stomach 12 hours after oral administration.

Conclusion

A matrix-floating bio-adhesive tablet containing levofloxacin hemihydrate was successfully developed to effectively eliminate H. pylori infection.