Revaprazan (REV), a novel reversible Proton Pump Inhibitor (PPI) used to treat peptic ulcers, faces challenges in therapeutic efficacy due to its poor dissolution properties and a short half-life. Solid lipid nanoparticles (SLNs) have emerged as a drug delivery system capable of enhancing dissolution and bioavailability of lipid soluble drugs. Here, we report on the development and optimization of a smart gastro-retentive raft system of REV-loaded SLNs (GRS/REV-SLNs) to enhance drug bioavailability and gastric retention. The optimized REV-SLNs had a particle size of 120 nm, a Polydispersity Index (PDI) of 0.313, a zeta potential of -20.7 mV, and efficient drug incorporation of 88 %. Transmission Electron Microscopy (TEM) affirmed the spherical morphology of these REV-SLNs, while Fourier Transform Infrared Spectroscopy (FTIR) revealed no chemical interactions among components. In-vitro assessment of the final GRS/REV-SLNs demonstrated sustained gelation and buoyancy for over 12 h, which would significantly enhance REV retention and its release within the stomach. Further assessments in rats confirmed successful gel transformation within the stomach, resulting in the improved bioavailability of REV. Thus, the development of GRS/REV-SLNs significantly improved the delivery and bioavailability of REV within the stomach, and offers a potentially improved method of treating peptic ulcers.
Keywords: Gastro-retention; Peptic ulcer; Raft system; Revaprazan; Smart drug delivery; Solid lipid nanoparticles.
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