Levofloxacin hemihydrate-adorned floating drug delivery system to ameliorate H. pylori infection: formulation development, optimization, and characterization
Abstract
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 940 P/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 s, a total floating time of more than 12 h, a swelling index of 81.89%, and a bioadhesion strength of 28.19 ± 5.12 g. 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 h after oral administration.…
Read the paper
Related studies
- Ferulic acid regulates the AKT/GSK-3β/CRMP-2 signaling pathway in a middle cerebral artery occlusion animal model
- Novel Pharmacokinetic/Pharmacodynamic Parameters Quantify the Exposure–Effect Relationship of Levofloxacin against Fluoroquinolone-Resistant Escherichia coli
- Photochemical behavior of levofloxacin
- Correlation Between Dissolution Profiles of Salt-Form Drugs in Biorelevant Bicarbonate Buffer and Oral Drug Absorption: Importance of Dose/ Fluid Volume Ratio
- Evaluation of the synergistic potential and mechanisms of action for de novo designed cationic antimicrobial peptides
- Synthesis of [11C]levofloxacin
Go deeper in Evidence Hub
Evidence Hub adds a study data sheet (design, sample size, evidence level, key numbers), an AI summary and a chat grounded in the paper's text.