Double Target Strategy of Novel Floating Raft System Containing Metronidazole
摘要
This study explores the development of a carboxymethyl alginate-based floating raft system designed to create interpenetrating polymer networks (IPN) with ionic gelation, enhance stomach retention time, and combine temporal and spatial methodologies for the drug release of metronidazole (MTZ). In-situ gels were prepared using varying concentrations of Sodium Alginate (SA), carboxymethyl alginate (CMA), and Hydroxypropyl Methylcellulose K100M (HPMC K100M) as matrix formers, and calcium carbonate as both a crosslinker and gas former. The formulations were comprehensively evaluated across various parameters, such as physicochemical properties, instrumental characterization, drug release, and ex vivo studies. Formulation F9, FRS had a short gelation lag time (14 s), long duration (> 24 h), floating lag time of 16 s, total floating time > 24 h, and raft resilience > 4 h. Drug loading efficiency was 91.08%, and cumulative drug release at the end of 24 h was 72.14%. The optimized batch (F9) was further characterized using FTIR, XRD, DSC, and SEM, which proved drug–polymer compatibility, amorphous nature, thermal stability, and a well-developed porous surface morphology. This supports spatial means targeting the drug to a specific part of organ, means here the stomach. Stomach-specific infections were recovered more efficiently as the release was temporal, as confirmed by a kinetic, microbial, and mucoadhesive study. The results revealed that F9 FRS was retained for more than 24 h and was more effective against stomach infection, E. coli, and S. aureus than commercially available metrogyl® and Gaviscon ® suspensions.
Graphical Abstract