Novel chitosan-based solid-lipid nanoparticles to enhance the bio-residence of the miraculous phytochemical "Apocynin".
Apocynin (APO), a specific NADPH oxidase inhibitor, is a bioactive phytochemical that exhibits versatile pharmacological activities. However, its rapid elimination and poor bioavailability represent great challenges to pharmaceutical scientists. Accordingly, novel chitosan-based APO-loaded solid lipid nanoparticles (CS,APO - loaded SLNS) were developed to address such obstacles. A full 24 factorial design of experiment approach was employed to evaluate the individual and combined effect of critical process parameters namely; the amount of glycerol tristearate (GTS, XA) and sucrose mono palmitate (SMP, XB) as well as the concentration of chitosan (CS, XC) and polyvinyl alcohol (PVA, XD), on different critical quality attributes. Full characterization and extensive in vitro-in vivo evaluations of the optimized SLNs formula were conducted. The optimized formula, with core (CS,APO) and shell (PVA), has enhanced oral and intravenous bioavailability in rats as clearly verified when compared with APO solution. Probably, PVA hindered opsonization intravenously and SLNs reduced pre-systemic effect. In conclusion, the novel chitosan-based SLNs system would open new vistas in potentiating the bioavailability and sustaining the effect of APO and other bioactive phytochemicals with comparable properties.
['Aman|Reham Mokhtar|RM|', 'Abu Hashim|Irhan Ibrahim|II|', 'Meshali|Mahasen Mohamed|MM|']
D000098:Acetophenones D000818:Animals D048271:Chitosan D004337:Drug Carriers D065546:Drug Liberation D008297:Male D053758:Nanoparticles D064209:Phytochemicals D011142:Polyvinyl Alcohol D017207:Rats, Sprague-Dawley D013228:Stearates D013395:Sucrose
Apocynin Bioactive phytochemical Bioavailability Solid lipid nanoparticles Factorial design Chitosan