Design and Optimization of Guar Gum-Carboxymethyl Cellulose-Based Gastro-Retentive Floating Tablets of Levofloxacin through Melt Granulation Technique

Gastroretentive delivery of therapeutics has gained considerable attention from researchers in recent times due to its effectiveness in localizing the delivery system in the stomach. Stomach-specific delivery of antibiotics is essential to eradicate Helicobacter pylori. The aim of the present investigation is to optimize and evaluate the effect of guar gum (GG) and carboxymethyl cellulose (CMC) on sustaining the release of levofloxacin from the formulated gastroretentive floating matrix tablets. Optimization of the formulation was done using Design Expert 13 software Trial Version. Thermoplastic granulation technique was employed using stearic acid for granule preparation. The developed matrix tablets were evaluated through several evaluation techniques. The Fourier transform infrared (FTIR) technique was used to investigate the compatibility between levofloxacin and the used polymers. The pre-compression and post-compression parameters were also evaluated. The FTIR spectra reflected excellent compatibility between the drug and other excipients. The floating lag time was found to decrease with increasing polymer concentration. The total floating duration was reported up to 456 ± 14.4 mins for F6 (10% GG & 15% CMC). The drug release study in 0.1 N HCl buffer showed a gradual decrease in cumulative drug release % with increasing guar gum concentration. The drug release mechanism was found to follow Korsemeyer-Peppas kinetics, and the n value indicated Fickian diffusion of the dissolved drug from the tablet matrix. The obtained results indicated the suitability and effectiveness of the developed floating matrix tablets for gastroretentive and sustained release of levofloxacin.