FORMULATION AND EVALUATION OF AMOXICILLIN-TRIHYDRATE, METRONIDAZOLE AND FAMOTIDINE LOADED-MUCOADHESIVE GASTRO-RETENTIVE FILMS
Objective: To developed mucoadhesive gastro-retentive films of amoxicillin trihydrate, metronidazole and famotidine by using polymers and plasticizer for eradication of H. pylori infection.
Methods: The mucoadhesive gastro-retentive films of amoxicillin trihydrate, metronidazole and famotidine were prepared using solvent casting method. The optimized gastro-retentive films were characterized by using various parameters such as DSC, drug content uniformity, in vitro drug release, FTIR spectroscopy, SEM and ex-vivo drug permeation studies across the mucous membrane. The prepared mucoadhesive gastro-retentive films were evaluated with in vitro growth inhibition study and in vivo bacterial clearance study.
Results: The FTIR spectra indicated that there was no any interaction between the drugs and polymer. Drugs content was found to be in the range and there was no significant change in the surface morphology of the films after under storage. The bioadhesive property of prepared films exhibited highly bioadhesive property when increased the amount of chitosan and PAA (Polyacrylic Acid) used. We found that CH-PAA IPC (Chitosan-Polyacrylic Acid Inter-polymer Complex) films exhibited greater bioadhesion. The percent of growth inhibition by using each drug such as amoxicillin, metronidazole and famotidine was found to be 51.61%, 46.59% and 34.76%, respectively whereas the combination of drugs were exhibited highest % growth inhibition. The % inhibition was found to be 81.00%. The optimized formulation CH-PAA IPC (C1P2G2) and CH film (C1G2) showed highest growth inhibition of H. pylori bacteria. The growth inhibition was found to be 96.77% and 92.26%, respectively. In vivo Bacterial Clearance Studies showed that the drugs loaded CH-PAA IPC film (C1P2G2) formulation exhibited better clearance from infection than CH film (C1G2) formulation and plain drugs solution at same doses. Drugs loaded CH-PAA IPC film formulation was found to be effective in the treatment of H. pylori infections effectively.
Conclusion: The developed gastro-retentive films of amoxicillin trihydrate, metronidazole and famotidine combination could be used for batter management of mucosal ulcer disease and eradication of H. pylori bacteria.
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