QbD-derived development of multilayer cellulose based polymeric coated extended-release gastroretentive effervescent floating pellets of moxifloxacin and its in silico PBPK modeling
Abstract
This study aims to design Moxifloxacin (MFX) 400 mg extended-release gastro-retentive floating pellets using different cellulose derivatives with pyrrolidones and methacrylate co-polymers for effective eradication of H. pylori in stomach. The drug loaded core pellets were prepared by extrusion and spheronization technique using microcrystalline cellulose and crospovidone by central composite design (CCD). The optimized core pellets were coated for three consecutive layers, an inner seal coat of ethyl cellulose (EC) and polyvinylpyrrolidone (PVPK30), an effervescent layer of sodium bicarbonate and hydroxypropyl methylcellulose (HPMC E5) and an outer gas entrapping polymeric membrane of Eudragit RL30D. The optimum concentration of Eudragit RL30D and percent coating weight gain were obtained by CCD to get the targeted buoyancy and percentage drug release. The core and coated formulations were characterized for percentage drug release, surface morphology, chemical interaction, thermal chemical stability, and in vivo imaging. The optimized coated formulation (FCopt) followed zero-order release kinetics and drug release was found ~100 % upto12th hour. The in silico PBPK model was developed to predict the in vivo pharmacokinetic profile. The combined effect of carbohydrate polymers with methacrylate and pyrrolidone based compounds were found promising in designing gastroretentive extended release floating pellets of MFX to target H pylori manifestation.
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